Настройки

Укажите год
-

Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

Подробнее
-

Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год
Применить Всего найдено 1449. Отображено 100.
22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Автор: Akihiro Morinaka, Ken Chikauchi, Mizuyo Ida, Takao Abe, Toshiaki Kudo, Yukiko Hiraiwa
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

Подробнее
Номер записи: 1
08-11-2012 дата публикации

Novel processes for the preparation of cyclopropyl-amide derivatives

Номер: US20120283433A1
Автор: Chennagiri R. Pandit, David C. Palmer, Mayra B. Reyes, Neelakandha S. Mani, Sergio Cesco-Cancian, TONG XIAO
Принадлежит: Individual

The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.

Подробнее
Номер записи: 2
21-03-2013 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

Номер: US20130072491A1
Автор: Eto Yuzuru, KITAHARA Yoshiro, Yasuda Reiko
Принадлежит: AJINOMOTO CO., INC.

An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula). 7. The method according to claim 6 , comprising administering 2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid claim 6 , 2-amino-3-{[(3-chloro-4-methyl-5-sulfophenyl)carbamothioyl]amino}propanoic acid claim 6 , or 2-amino-3-{[(3-chloro-2-methyl-5-sulfophenyl)carbamoyl]amino}propanoic acid as an active component. This application is a continuation of International Patent Application No. PCT/JP2011/055124, filed on Mar. 4, 2011, and claims priority to Japanese Patent Application No. 2010-048310, filed on Mar. 4, 2010, and Japanese Patent Application No. 2010-086548, filed on Apr. 2, 2010, all of which are incorporated herein by reference in their entireties.The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a prophylactic or therapeutic agent for diabetes or obesity, which comprises an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active component.Energy metabolism in the body is controlled by insulin produced by pancreatic beta-cells. Insulin plays an important role in controlling the blood sugar level by affecting and promoting the peripheral tissues or cells to take up sugar from the blood. However, insulin sensitivity of the cells is reduced by continuous intake of high caloric diet, an increase in the blood sugar level as well as oversecretion of insulin proceed at the same time. As a result, pancreatic beta-cells are worn out and thus become ...

Подробнее
Номер записи: 3
20-06-2013 дата публикации

PHENYLAMIDINES HAVING A HIGH FUNGICIDAL ACTIVITY AND USE THEREOF

Номер: US20130157851A1
Автор: Badaracco Christian, BRAVINI Paolo, Elmini Alexia, FILIPPINI Lucio, Gusmeroli Marilena, PELLACINI Franco, VAZZOLA Matteo Santino
Принадлежит: ISAGRO S.P.A.

New phenylamidines are described, having general formula (I): 4. Fungicidal compositions comprising one or more compounds having formula (I) claim 1 , according to claim 1 , a solvent and/or a solid or liquid diluent claim 1 , optionally a surfactant.5. The compositions according to claim 4 , also comprising active principles compatible with the compounds having general formula (I) claim 4 , selected from fungicides other than the compounds having general formula (I) claim 4 , phytoregulators claim 4 , antibiotics claim 4 , herbicides claim 4 , insecticides claim 4 , fertilizers and/or mixtures thereof claim 4 , antifreeze agents claim 4 , adhesion agents.6. The compositions according to claim 4 , wherein the concentration of compounds having general formula (I) ranges from 1 to 90% by weight with respect to the total weight of the composition claim 4 , preferably from 5 to 50% by weight with respect to the total weight of the composition.8. Use of the compounds according to claim 2 , for the control of phytopatogenic fungi in agricultural crops.9. Use of the compositions according to for the control of phytopatogenic fungi in agricultural crops.10PucciniaUstilagoTilletiaUromycesPhakopsoraRhizoctoniaErysipheSphaerothecaPodosphaeraUncinulaHelminthosporiumRhynchosporiumPyrenophoraMoniliniaSclerotiniaSeptoriaMycosphaerellaVenturiaBotrytisAlternariaFusariumCercosporaCercosporella herpotrichoides, ColletotrichumPyricularia oryzae, SclerotiumPhytophtoraPythiumPlasmopara viticola, PeronosporaPseudoperonospora cubensis, Bremia lactucae.. Use according to claim 7 , for the control of phytopatogenic fungi belonging to the group of Basidiomycetes claim 7 , Ascomycetes claim 7 , Deuteromycetes or imperfect fungi claim 7 , Oomycetes: spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. (spp.) claim 7 , ...

Подробнее
Номер записи: 4
20-06-2013 дата публикации

Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis

Номер: US20130158022A1
Автор: He Kunlun, Hu Guoliang, Li Ruijun, Li Song, Li Wei, Li Xin, Liu Chunlei, Liu Juan, Long Long, TANG JIE, WANG JIE, Wang Lili, Xiao Junhai, Zheng Zhibing, Zhong Wu
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having any one of the following structures claim 1 , or their isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (2E)-3-(2-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(2) (2E)-3-(3-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(3) (2E)-3-(2-thienyl)-N-[1-(4-tolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(4) (2E)-3-(2-thienyl)-N-[1-(2-methoxyanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(5) (2E)-3-(2-thienyl)-N-(1-benzylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(6) (2E)-3-(2-thienyl)-N-(1-cyclohexylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(7) (2E)-3-(2-thienyl)-N-[1-isopropylaminothioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(8) (2E)-3-(2-thienyl)-N-[1-(2-fluoroanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(9) (2E)-3-(2-thienyl)-N-[1-(3-isopropoxypropylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(10) (2E)-3-(2-thienyl)-N-[1-(2-methoxyformylanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(11) (2E)-3-(2-thienyl)-N-(1-cycloheptylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(12) (2E)-3-(2-thienyl)-N-[1-(1-morpholinyl)thioformylamino-2,2,2- ...

Подробнее
Номер записи: 5
04-07-2013 дата публикации

PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH

Номер: US20130172560A1
Автор: Stranne Robert
Принадлежит: AstraZeneca AB

Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition. 3. The process of claim 2 , wherein said base is sodium hydroxide.4. The process of claim 2 , wherein said peroxide is hydrogen peroxide.5. The process of claim 2 , wherein said acidic solution is an aqueous solution of sodium hydrogen sulfate.7. The process of claim 6 , wherein X is Br.8. The process of claim 6 , wherein said metal is zinc.9. The process of claim 6 , wherein said metal cyanide is zinc-(II)-cyanide.10. The process of claim 6 , wherein said catalyst is bis(tri-t-butylphosphine)palladium(0).15. The process of claim 14 , wherein said activating agent is 1 claim 14 ,1′-carbonyldiimidazole.19. The process of claim 18 , wherein the activating agent is a mixture of 1-hydroxybenzotriazole and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride.21. The process of claim 16 , wherein said acid is hydrochloric acid.23. The process of claim 17 , wherein said reducing agent is sodium triacetoxy borohydride. Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.The histamine H3 receptor is of current interest in developing new medicaments. The H3 receptor is a presynaptic autoreceptor located both in the central and peripheral nervous systems, the skin, and in organs, such as, for example, the lung, the intestine, probably the spleen, and the gastrointestinal tract. Recent evidence suggests the H3 receptor has intrinsic ...

Подробнее
Номер записи: 6
25-07-2013 дата публикации

BIS-FATTY ACID CONJUGATES AND THEIR USES

Номер: US20130190327A1
Автор: Bemis Jean E., Jirousek Michael R., Milne Jill C., Vu Chi B.
Принадлежит: CATABASIS PHARMACEUTICALS INC

The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate. 1. A molecular conjugate , directly or indirectly covalently linked wherein the linker comprises at least one amide , comprising two or more fatty acids selected from the group consisting of omega-3 fatty acids , fatty acids that are metabolized in vivo to omega-3 fatty acids , and lipoic acid , with the proviso that the molecular conjugate is not (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethylamino]-ethyl}-amide (A); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethylamino]-ethyl}-amide (B); (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethoxy]-ethyl}-amide (C); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethoxy]-ethyl}-amide (D); or (S)-2 ,6-Bis-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-hexanoic acid (E).2. The molecular conjugate of claim 1 , wherein the fatty acid is selected from the group consisting of all-cis-7 claim 1 ,10 claim 1 ,13-hexadecatrienoic acid claim 1 , α-linolenic acid claim 1 , stearidonic acid claim 1 , eicosatrienoic acid claim 1 , eicosatetraenoic acid claim 1 , eicosapentaenoic acid (EPA) claim 1 , docosapentaenoic acid claim 1 , docosahexaenoic acid (DHA) claim 1 , tetracosapentaenoic acid claim 1 , tetracosahexaenoic acid and lipoic acid.3. The molecular conjugate of claim 2 , wherein the fatty acid is selected from ...

Подробнее
Номер записи: 7
29-08-2013 дата публикации

BENZAMIDE DERIVATIVE WITH ANTICANCER ACTIVITY AND PREPARATION METHOD AND USE THEREOF

Номер: US20130225810A1
Автор: Bai Hua, Gong Yongxiang, Liu Lifei, Liu Xiaoyu, Zhao Xuyang, Zhong Jinqing, Zhou Qixian, Zhu Qifeng
Принадлежит: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description. 2. The compound according to claim 1 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 1 , substituted or unsubstituted (C-C)alkyl claim 1 , —CORor —COR claim 1 , and Rand Rcan also cyclize to form a substituted or unsubstituted 4- claim 1 , 5- claim 1 , or 6-membered ring claim 1 , wherein Ris a substituted or unsubstituted (C-C)alkyl claim 1 , a substituted or unsubstituted (C-C)alkenyl claim 1 , a substituted or unsubstituted (C-C)alkynyl claim 1 , a substituted or unsubstituted (C-C)cycloalkyl claim 1 , and a substituted or unsubstituted aryl; Ris a substituted or unsubstituted (C-C)alkyl claim 1 , a substituted or unsubstituted (C-C)alkenyl claim 1 , a substituted or unsubstituted (C-C)alkynyl claim 1 , and a substituted or unsubstituted (C-C)cycloalkyl.3. The compound according to claim 2 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 2 , substituted or unsubstituted (C-C)alkyl claim 2 , —CORor —COR claim 2 , and Rand Rcan also cyclize to form a substituted or unsubstituted 4- claim 2 , 5- claim 2 , or 6-membered ring claim 2 , wherein Ris a substituted or unsubstituted (C-C)alkyl claim 2 , a substituted or unsubstituted (C-C)cycloalkyl claim 2 , a substituted or unsubstituted aryl; Ris a substituted or unsubstituted (C-C)alkyl claim 2 , a substituted or unsubstituted (C-C)cycloalkyl.4. The compound according to claim 3 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 3 , methyl claim 3 , ethyl claim 3 , and propyl.5. The compound according to claim 3 , wherein Rand Rcan also cyclize to form a substituted or unsubstituted 5- or 6-membered ring which may contain one or more ...

Подробнее
Номер записи: 8
05-09-2013 дата публикации

Novel Intermediate for Preparing Tapentadol or Analogues Thereof

Номер: US20130231478A1
Автор: LI DEGANG, LI XIAOXIANG, XU ZIAO, ZHAO YUANHAI
Принадлежит:

The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production. 2. The compound according to claim 1 , wherein Ris selected from Cl claim 1 , methyl claim 1 , OH claim 1 , NHor methoxy.3. The compound according to claim 1 , characterized in that Y is selected from OR claim 1 , wherein Ris selected from methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl.4. The compound according to claim 1 , characterized in that Y is selected from NRR claim 1 , wherein R claim 1 , Rand N form substituted or unsubstituted saturated nitrogen-containing heteorcyclyl containing oxygen or not jointly.5. The compound according to claim 4 , wherein R claim 4 , Rand N form tetrahydropyrrole ring claim 4 , piperidine ring claim 4 , 4-methylpiperidine ring claim 4 , morpholine ring claim 4 , methylpiperazine ring or 4-hydroxypiperidine jointly.6. The compound according to claim 1 , selected from the following compounds:valeryl 2-methyl-3-(3-methoxyphenyl)chloride;methyl 2-methyl-3-(3-methoxyphenyl)sulfovalerate;methyl 2-methyl-3-(3-hydroxyphenyl) ulfovalerate;2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-methoxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-diethyl-2-methyl-3-(3-methoxyphenyl)valeramide;3-(3-methoxyphenyl)-2-methyl-1-(piperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-(4-methylpiperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-(morpholin-1-yl)pentan- ...

Подробнее
Номер записи: 9
05-09-2013 дата публикации

ARYLOXYUREA COMPOUND AND PEST CONTROL AGENT

Номер: US20130231479A1
Автор: Furukawa Hironori, HANAI Daisuke, Nakamura Takehiko, Tamai Tetsuo
Принадлежит:

The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein Rto Reach independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof. 3. A pest control agent claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.4. An acaricide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.5. A fungicide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.6. A pest control agent claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.7. An acaricide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.8. A fungicide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient. The present invention relates to a novel pest control agent. More specifically, the present invention relates to an aryloxyurea compound, which is superior in acaricidal activity and/or fungicidal activity, superior in properties and safety, and which can be industrially and advantageously synthesized, and an acaricide and/or fungicide including the aryloxyurea compound as an active ingredient.Priority is claimed on Japanese Patent Application No. 2010-229617, filed Oct. 12, 2010, the content of which is incorporated herein by reference.Compounds represented by formulas (A) to (E), which are structurally relevant to the compound of the present invention, are disclosed in Patent documents 1 to 5.In the formula, Rrepresents a C1-6 alkyl group.Rrepresents a hydrogen ...

Подробнее
Номер записи: 10
12-09-2013 дата публикации

ALKYLAMINE DERIVATIVE

Номер: US20130237702A1
Автор: Okamatsu Toru, Sugiki Masayuki, Taniguchi Shinya, YANO Tetsuo
Принадлежит: AJINOMOTO CO., INC.

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi. 3. A pharmaceutical agent comprising the compound or a pharmaceutically acceptable salt thereof according to or as an active ingredient.6. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for a disease that is ameliorated through CaSR activation.7. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for hyperparathyroidism.8. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for diarrhea.9. The pharmaceutical agent according to claim 3 , which is a prophylactic or therapeutic agent for peptic ulcer.10. Seasonings comprising the compound according to either one of and or an edible salt thereof as an active ingredient.11. A kokumi-imparting agent comprising the compound according to either one of and or an edible salt thereof as an active ingredient. The present invention relates to an alkylamine derivative or a salt thereof, and a pharmaceutical agent comprising the same. More particularly, the present invention relates to a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation, a prophylactic or therapeutic agent for hyperparathyroidism, diarrhea and peptic ulcer, and seasonings and an agent for imparting kokumi, which have an alkylamine derivative or a pharmaceutically acceptable salt thereof as an active ingredient.The calcium receptor, also called the calcium sensing receptor (also referred to as “CaSR”), was cloned from bovine thyroid in 1993 as G-protein ...

Подробнее
Номер записи: 11
19-09-2013 дата публикации

CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES

Номер: US20130244962A1
Автор: BEAULIEU Christian, ISABEL Elise, MELLON Christopher
Принадлежит: Merck Frosst Canada Ltd.

Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. 121.-. (canceled)23. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.24. A pharmaceutical composition of further comprising another agent selected from the group consisting of: nifurtimox claim 23 , benznidazole claim 23 , allopurinol claim 23 , terbinafine claim 23 , lovastatin claim 23 , ketoconazole claim 23 , itraconazole claim 23 , posaconazole claim 23 , miltefosine claim 23 , ilmofosine claim 23 , pamidronate claim 23 , alendronate claim 23 , risedronate claim 23 , chloroquine claim 23 , proguanil claim 23 , mefloquine claim 23 , quinine claim 23 , pyrimethamine-sulphadoxine claim 23 , doxocycline claim 23 , berberine claim 23 , halofantrine claim 23 , primaquine claim 23 , atovaquone claim 23 , pyrimethamine-dapsone claim 23 , artemisinin claim 23 , quinhaosu claim 23 , meglumine antimonite claim 23 , sodium stibogluconate claim 23 , amphotericin B claim 23 , praziquantel claim 23 , oxamniquine claim 23 , pentamidine claim 23 , melarsoprol claim 23 , suramin and eflornithine and the pharmaceutically acceptable salts and mixtures thereof.25. A method of treating a patient having a parasitic disease comprising administering to the patent in need thereof a composition comprising a compound of claim 22 , wherein the parasitic disease is selected from the group consisting of toxoplasmosis claim 22 , malaria claim 22 , ...

Подробнее
Номер записи: 12
19-09-2013 дата публикации

HETEROARYL-SUBSTITUTED UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE

Номер: US20130245022A1
Автор: Breitenbucher J. Guy, Chambers Alison L., Hawryluk Natalie A., Jones William M., Keith John M., Merit Jeffrey E., Sierestad Mark J., Tichenor Mark S., Timmons Amy K.
Принадлежит: Janssen Pharmaceutica NV

Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). 2. A chemical entity as in claim 1 , wherein Aris isoxazolo[5 claim 1 ,4-c]pyridin-3-yl claim 1 , isoxazolo[4 claim 1 ,5-c]pyridin-3-yl claim 1 , imidazo[1 claim 1 ,2-b]pyridazin-3-yl claim 1 , 1H-pyrrolo[2 claim 1 ,3-b]pyridin-5-yl claim 1 , imidazo[1 claim 1 ,2-a]pyridin-5-yl claim 1 , 6-[1 claim 1 ,2 claim 1 ,3]triazol-2-yl-pyridin-3-yl claim 1 , 5-methyl-[1 claim 1 ,3 claim 1 ,4]oxadiazol-2-yl claim 1 , imidazo[1 claim 1 ,2-a]pyrimidin-5-yl claim 1 , 4-[1 claim 1 ,2 claim 1 ,3]triazol-1-yl-phenyl claim 1 , 4-[1 claim 1 ,2 claim 1 ,3]triazol-2-yl-phenyl claim 1 , 2-phenyl-pyrimidin-5-yl claim 1 , isoxazolo[4 claim 1 ,5-b]pyridin-3-yl claim 1 , 1 claim 1 ,3-dimethyl-1H-pyrazolo[3 claim 1 ,4-b]pyridin-5-yl claim 1 , benzooxazol-6-yl claim 1 , or 2-methyl-2H-indazol-4-yl.3. A chemical entity as in claim 1 , wherein Aris isoxazolo[5 claim 1 ,4-c]pyridin-3-yl claim 1 , isoxazolo[4 claim 1 ,5-c]pyridin-3-yl claim 1 , isoxazolo[4 claim 1 ,5-b]pyridin-3-yl claim 1 , imidazo[1 claim 1 ,2-b]pyridin-8-yl claim 1 , imidazo[1 claim 1 ,2-a]pyridin-7-yl claim 1 , imidazo[1 claim 1 ,2-a]pyridin-5-yl claim 1 , imidazo[1 claim 1 ,2-a]pyrimidin-7-yl claim 1 , imidazo[1 claim 1 ,2-a]pyrimidin-5-yl claim 1 , imidazo[1 claim 1 ,2-c]pyrimidin-7-yl.45.-. (canceled)6. A chemical entity as in claim 1 , wherein Aris phenyl claim 1 , substituted with one or two Rmoieties.7. A chemical entity as in claim 6 , wherein each Rmoiety is independently selected from the group consisting of: chloro claim 6 , fluoro claim 6 , ...

Подробнее
Номер записи: 13
03-10-2013 дата публикации

Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof

Номер: US20130261121A1
Автор: Shi Qian, SHIH Charles C.Y., Su Ching-Yuan, Wang Hui-Kang
Принадлежит:

The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof. 2. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is an androgen receptor associated medical condition that is induced claim 1 , caused or mediated by a normal or abnormal androgen receptor.3. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is inflammation.4. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is acne.5. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is alopecia.6. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is hirsutism.7. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is a wound.8. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated ...

Подробнее
Номер записи: 14
03-10-2013 дата публикации

CALCIUM-SENSING RECEPTOR-ACTIVE COMPOUNDS

Номер: US20130261132A1
Автор: BlÆher Lars Kristian Albert, Vedsø Per
Принадлежит: LEO PHARMA A/S

Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds. 3. A compound according to claim 1 , wherein Ar represents phenyl or naphthyl claim 1 , optionally substituted with one or two claim 1 , same or different substituents selected from halogen or Calkoxy.4. A compound according to claim 3 , wherein phenyl is substituted with one or two claim 3 , same or different substituents selected from chloro claim 3 , fluoro or methoxy.5. A compound according to claim 4 , wherein Ar represents 4-fluoro-3-methoxy or 3-chlorophenyl.6. A compound according to claim 1 , wherein Ar represents naphthyl.7. A compound according to claim 1 , wherein Rrepresents Calkenyl claim 1 , hydroxyCalkyl claim 1 , hydroxyCalkylaminoCalkyl claim 1 , Calkyl sulfonyl amino Calkyl claim 1 , aminosulfonylCalkyl claim 1 , aminocarbonylCalkyl claim 1 , or Cheterocycloalkyl comprising 1-2 hetero atoms selected from N claim 1 , O and S.8. A compound according to claim 7 , wherein Rrepresents hydroxyCalkylaminoCalkyl claim 7 , Calkyl sulfonylaminoCalkyl claim 7 , amino sulfonylCalkyl claim 7 , amino carbonyl Calkyl claim 7 , or Cheterocycloalkyl comprising 1-2 hetero atoms selected from N and O.9. A compound according to claim 1 , wherein Rrepresents hydrogen.10. A compound according claim 1 , wherein Rand Rtogether with the nitrogen to which they are attached form a 6 membered Cheterocycloalkyl comprising one or two nitrogen atom(s) claim 1 , said heterocyclic ring being optionally substituted with oxo claim 1 , —S(O)NH claim 1 , Calkylcarbonyl claim 1 , or hydroxyCalkyl.11. A compound according to claim 10 , wherein the heterocyclic ring is selected from the group consisting of piperazinyl or piperidyl claim 10 , ...

Подробнее
Номер записи: 15
10-10-2013 дата публикации

N,N+hu 1 +l SUBSTITUTED PIPERAZINES HAVING COMBINED ANTIAGGREGANT, ANTICOAGULANT AND VASODILATORY ACTIVITY, AND METHOD FOR PRODUCING SAME

Номер: US20130267707A1
Автор: Petrishchev Nikolay Nikolaevich, Poplavskaya Yuliya Vyacheslavovna, Veselkina Olga Sergejevna, Viktorov Nikolay Borisovich
Принадлежит: ZAKRYTOE AKTSIONERNOE OBSCHSHESTVO "VERTEX"

The invention relates to derivatives of N,N′-substituted piperazines of the general formula (I): 6. The method for synthesis of N claim 3 ,N′-substituted piperazines of claim 3 , wherein said carboxamidating agents are represented by: 1H-pyrazole-1-carboxamidine claim 3 , or dicyandiamide claim 3 , or salts thereof.7. The method for synthesis of N claim 3 ,N′-substituted piperazines of claim 3 , wherein said bases are represented by: alkaline metal hydroxides claim 3 , or carbonates claim 3 , or organic bases thereof.83. The method for synthesis of N claim 3 ,N′-substituted piperazines of claim claim 3 , wherein said organic solvents are represented by one of the following: lower aliphatic alcohols claim 3 , acetonitrile claim 3 , tetrahydrofurane claim 3 , dimethylformamide claim 3 , dimethylsulfoxide claim 3 , dichloromethane claim 3 , or mixtures thereof.13. The method for synthesis of said compounds of N claim 10 ,N′-substituted piperazines according to claim 10 , wherein said organic solvents are represented by one of the following: lower aliphatic alcohols claim 10 , acetonitrile claim 10 , tetrahydrofurane claim 10 , dimethylformamide claim 10 , dimethylsulfoxide claim 10 , dichloromethane claim 10 , chloroform claim 10 , or mixtures thereof used.14. The method for synthesis of said compounds of N claim 10 ,N′-substituted piperazines according to claim 10 , wherein said halogenalkylsulfonic acids or salts thereof are represented by: 2-bromoethanesulfonic acid claim 10 , 2-hydroxy-3-chloropropanesulfonic acid claim 10 , or sodium salts thereof.15. The method for synthesis of said compounds of N claim 10 ,N′-substituted piperazines according to claim 10 , wherein said bases are represented by: ammonia claim 10 , sodium hydroxide claim 10 , or potassium hydroxide claim 10 , or sodium carbonate claim 10 , or sodium hydrocarbonate claim 10 , or potassium carbonate claim 10 , or potassium hydrocarbonate.16. The compounds according to claim 1 , wherein said low ...

Подробнее
Номер записи: 16
10-10-2013 дата публикации

Aromatic ketone synthesis with amide reagents and related reactions

Номер: US20130267712A1
Автор: Douglas A. Klumpp, Erum K. Raja
Принадлежит: Northern Illinois University

A method of preparing an aryl carbonyl or aryl thiocarbonyl compound, comprises reacting an N-(nitroaryl)-amide or N-(nitroaryl)-thioamide with an aromatic ring, with a superacid catalyst, to produce the aryl carbonyl or aryl thiocarbonyl compound. The superacid is present in an amount of at most 8 equivalents in proportion to the N-(nitroaryl)-amide or N-(nitroaryl)-thioamide. A method of preparing aryl amide or aryl thioamide, comprises reacting an N-(nitroaryl)-carbamide or N-(nitroaryl)-thiocarbamide with an aromatic ring, with a superacid catalyst, to produce the aryl amide or aryl thioamide.

Подробнее
Номер записи: 17
17-10-2013 дата публикации

FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20130274240A1
Автор: Ito Hirotsugu, Kobayashi Satoru, Morita Toru, Motomura Takahisa, Nagamori Hironobu, Shinkai Hisashi, Suzawa Koichi
Принадлежит:

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: 217.-. (canceled)18. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.1923.-. (canceled)24. A method of inhibiting PDHK in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.25. A method of inhibiting PDHK2 in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.26. A method of decreasing the blood glucose level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.27. A method of decreasing lactate level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.28. A method for the treatment or prophylaxis of diabetes claim 1 , diabetic complications claim 1 , insulin resistance syndrome claim 1 , metabolic syndrome claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , atherosclerosis claim 1 , ...

Подробнее
Номер записи: 18
31-10-2013 дата публикации

(4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES

Номер: US20130289043A1
Автор: Cumming John, Faull Alan, Waterson David
Принадлежит: AstraZeneca AB

The present invention relates to compounds of formula (I) 1. 4-[(2R)-4-tert-butylpiperazine-2-carbonyl]-N-(4-chloro-3-fluorophenyl)piperazine-1-carboxamide as a base or a pharmaceutically acceptable salt thereof.2. 4-[(2R)-4-tert-butylpiperazine-2-carbonyl]-N-(4-chloro-3-fluorophenyl)piperazine-1-carboxamide.3. (canceled)4. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable excipients claim 1 , carriers or diluents.57-. (canceled)8. A method comprising treating pain in a warm-blooded animal by administering to said animal in need of such treatment a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.9. A method comprising treating pain in a warm-blooded animal by administering to said animal in need of such treatment a pharmaceutical composition according to .10. The method according to or claim 4 , wherein said pain is neuropathic pain.1112-. (canceled)13. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 2 , and at least one pharmaceutically acceptable excipient claim 2 , carrier claim 2 , or diluent.14. A method comprising treating pain in a warm-blooded animal by administering to said animal in need of such treatment a therapeutically effective amount of a compound according to .15. A method comprising treating pain in a warm-blooded animal by administering to said animal in need of such treatment a pharmaceutical composition according to .16. The method according to or claim 13 , wherein said pain is neuropathic pain. The present invention relates to pharmaceutical compositions, which comprise compounds that act via antagonism of the CCR2b receptor for which MCP-1 is one of the known ligands and so may be used to treat inflammatory disease and/or neuropathic pain, which is mediated ...

Подробнее
Номер записи: 19
05-12-2013 дата публикации

Method of use of pharmaceutical formulations for the treatment of apicomplexan diseases in animals

Номер: US20130324555A1
Автор: Fomovska Alina, McLeod Rima, Mui Ernest, Welsh William, Wood Richard Delarey
Принадлежит:

The present invention is directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a salicylanilide or salicylanilide derivative, disclosed herein, alone or in combination with one or more other active or excipient pharmaceutical substances. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein. The present invention is further directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a combination of salicylanilides or salicylanilide derivatives, disclosed herein, further comprised of one or more active or excipient pharmaceutical substances. 1. The method of use of one or more compound of Formula I to prevent or treat a disorder caused wholly or in part by one or more apicomplexan parasite, wherein said method comprises contacting an animal in need of said prevention or treatment with an effective amount said compound, wherein said compound has the structure{'sub': 1', '6, 'R═H, SH, or OR;'}{'sub': 2', '3', '3', '2', '3', '2', '2', '3', '3', '2, 'Rand Rare selected from fused phenyl, H, lower alkyl, I, Br, Cl, F, CF, CHCF, CHPh, CH═CH, C≡CH, OCH, OCF, Ph, OPh, and NO;'}{'sub': 4', '3', '2', '3', '2', '2', '3', '3', '2, 'Ris selected from the group consisting of H, lower alkyl, I, Br, Cl, F, CF, CHCF, CHPh, CH═CH, C≡CH, C≡N, OCH, OCF, Ph, OPh, and NO;'}{'sub': '5', 'Ris H, lower alkyl, or phenyl;'}{'sub': 6', '3', '2', '3', '3', '2', '3', '3', '2', '6', '4', '2', '6', '4', '6', '4', '2', '3', '2', '2', '3', '2', '3', '2', '3', '2', '2', '3', '2, 'Ris selected from the group consisting of H, COCH, COCHCH, COCH(CH), COC(CH), COPh, ...

Подробнее
Номер записи: 20
12-12-2013 дата публикации

CYCLOALKYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF

Номер: US20130331392A1
Автор: Hurd Alexander R., Taylor Clarke B., Toogood Peter L., Van Huis Chad A.
Принадлежит:

The invention provides cycloalkyl guanidine compounds that inhibit FF-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer. 2. The compound of claim 1 , wherein A is cycloalkylene claim 1 , that in addition to R claim 1 , is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , cycloalkyl claim 1 , —N(R)COR claim 1 , —N(R)C(O)R claim 1 , —N(R)(R) claim 1 , —OR claim 1 , and —C(O)R.3. (canceled)4. The compound of claim 1 , wherein A is cyclobutylene claim 1 , cyclopentylene claim 1 , or cyclohexylene claim 1 , each of which is claim 1 , in addition to R claim 1 , optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , hydroxyl claim 1 , and —N(R)(R).5. The compound of claim 1 , wherein A is cyclohexylene.6. The compound of claim 1 , wherein Rrepresents independently for each occurrence halogen claim 1 , haloalkyl claim 1 , alkyl claim 1 , or C-Calkoxy.7. The compound of claim 1 , wherein Rrepresents independently for each occurrence chloro claim 1 , fluoro claim 1 , or trifluoromethyl.8. The compound of claim 1 , wherein Ris hydrogen.9. (canceled)10. The compound of claim 1 , wherein Ris —N(R)COR claim 1 , —N(R)C(O)R claim 1 , —N(R)C(O)N(R)(R) claim 1 , —N(R)SOR claim 1 , or —N(R)(R).11. The compound of claim 1 , wherein Ris —N(R)COR.12. The compound of claim 1 , wherein Ris —N(R)C(O)R.1316-. (canceled)17. The compound of claim 1 , wherein Ris aryl or aralkyl claim 1 , each of which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , haloalkyl claim 1 , alkyl claim 1 , cycloalkyl claim 1 , and C-Calkoxy.18. The compound of claim 1 , wherein Ris phenyl optionally substituted ...

Подробнее
Номер записи: 21
12-12-2013 дата публикации

PIPERAZINYL AND PIPERIDINYL UREAS AS MODULATORS OF FATTY ACID AMIDE HYDROLASE

Номер: US20130331396A1
Автор: Apodaca Richard, Breitenbucher J. Guy, Pattabiraman Kanaka, Seierstad mark, Xiao Wei
Принадлежит: Janssen Pharmaceutica NV

Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis). 126.-. (canceled)28. A method according to claim 27 , wherein said compound is selected from the group consisting of:4-naphthalen-2-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-quinolin-2-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-benzo[b]thiophen-2-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-(3,4-dibromo-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(1-methyl-1H-indol-2-ylmethyl)-piperazine-1-carboxylic acid phenylamide;4-quinolin-3-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-(4-iodo-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(3-benzyloxy-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(5-bromo-2-hydroxy-3-methoxy-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(4-bromo-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(3-phenoxy-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(3-bromo-4-fluoro-benzyl)piperazine-1-carboxylic acid phenylamide;4-indan-5-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-benzo[b]thiophen-3-ylmethyl-piperazine-1-carboxylic acid phenylamide;4-(4-isopropyl-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(4-ethyl-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(5-bromo-2-hydroxy-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(2,3-dihydro-benzo[1,4]dioxin-6-ylmethyl)-piperazine-1-carboxylic acid phenylamide;4-(4-methoxy-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(3-vinyl-benzyl)-piperazine-1-carboxylic acid phenylamide;4-(2,3-dihydro-benzofuran-5-ylmethyl)-piperazine-1-carboxylic acid phenylamide;4-(3-methoxy-benzyl)-piperazine-1- ...

Подробнее
Номер записи: 22
19-12-2013 дата публикации

Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof

Номер: US20130338160A1
Автор: Shi Qian, SHIH Charles, Wang Hui-Kang
Принадлежит:

The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof. 2. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is an androgen receptor associated medical condition that is induced claim 1 , caused or mediated by a normal or abnormal androgen receptor.3. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is inflammation.4. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is acne.5. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is alopecia.6. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is hirsutism.7. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is a wound.8. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated ...

Подробнее
Номер записи: 23
02-01-2014 дата публикации

Substituted Aromatic Sulfur Compounds and Methods of Their Use

Номер: US20140005175A1
Автор: DORSEY Bruce D., Kuwada Scott K., Theroff Jay P., ZIFICSAK Craig A.
Принадлежит:

Compounds of formula II are described: 2. The compound of claim 1 , wherein A is at the 4-position of the phenyl ring.4. The compound of claim 1 , wherein Rand Rare each —CH.5. The compound of claim 3 , wherein Ris —OH.6. The compound of claim 3 , wherein Ris substituted or unsubstituted heterocycloalkyl.7. The compound of claim 3 , wherein Ris —NRR.8. The compound of claim 7 , wherein Ris H.9. The compound of claim 8 , wherein Ris substituted or unsubstituted alkyl.10. The compound of claim 8 , wherein Ris substituted or unsubstituted aryl.11. The compound of claim 8 , wherein Ris substituted or unsubstituted aralkyl.12. The compound of claim 8 , wherein Ris substituted or unsubstituted heteroaryl.13. The compound of claim 8 , wherein Ris substituted or unsubstituted heteroaralkyl.14. The compound of claim 8 , wherein Ris substituted or unsubstituted cycloalkyl.15. The compound of claim 8 , wherein Ris substituted or unsubstituted heterocycloalkyl.16. The compound of claim 8 , wherein Ris substituted or unsubstituted alkyene oxide.17. The compound of claim 8 , wherein Ris —NHCOcycloalkyl.18. The compound of claim 8 , wherein Rand R claim 8 , together with the atoms through which they are attached claim 8 , form a substituted or unsubstituted heterocycloalkyl ring.19. The compound of claim 3 , wherein Ris —CH.20. The compound of claim 19 , wherein Ris substituted or unsubstituted alkyl.21. The compound of claim 19 , wherein Ris substituted or unsubstituted aryl.22. The compound of claim 19 , wherein Ris substituted or unsubstituted aralkyl.23. The compound of claim 19 , wherein Ris substituted or unsubstituted heteroaryl.24. The compound of claim 19 , wherein Ris substituted or unsubstituted heteroaralkyl.25. The compound of claim 19 , wherein Ris substituted or unsubstituted cycloalkyl.26. The compound of claim 19 , wherein Ris substituted or unsubstituted heterocycloalkyl.27. The compound of claim 19 , wherein Ris substituted or unsubstituted alkyene oxide.28. The ...

Подробнее
Номер записи: 24
06-02-2014 дата публикации

HETEROCYCLIC COMPOUNDS AS CCR2B ANTAGONISTS

Номер: US20140038978A1
Автор: Bower Justin Fairfield, Poyser Jeffrey Philip, Turner Paul, Waterson David, Winter Jon
Принадлежит: AstraZeneca AB

Compounds of formula (I) 126-. (canceled)28. The method according to wherein Ris t-butyl.30. The method according to wherein P is phenyl substituted by 1 or 2 substituents independently selected from chlorine claim 29 , fluorine claim 29 , bromine claim 29 , methyl claim 29 , ethyl claim 29 , cyano claim 29 , trifluoromethyl claim 29 , methoxy claim 29 , trifluoromethoxy claim 29 , phenyl claim 29 , phenoxy claim 29 , benzoxy claim 29 , thiomethyl claim 29 , thioethyl claim 29 , trifluoromethylthio claim 29 , methoxycarbonyl claim 29 , ethoxycarbonyl claim 29 , and NO.31. The method according to wherein P is phenyl substituted by 1 or 2 substituents independently selected from chlorine and fluorine.32. The method according to wherein the compound of Formula I has 2R stereochemistry.33. The method of claim 27 , wherein said compound is selected from:N-(4-Chlorophenyl)-4-{[(2R)-4-ethylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;N-(3-Chlorophenyl)-4-{[(2R)-4-ethylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;N-(3,4-Dichlorophenyl)-4-{[(2R)-4-ethylpiperazin-2-yl]carbonyl}piperazine-1-carboxamideN-(3,4-dichlorophenyl)-4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;4-[(2R)(4-Cyclopropylpiperazin-2-yl)carbonyl]-N-(3,4-dichlorophenyl)piperazine-1-carboxamide;N-(3,4-Dichlorophenyl)-4-{[(2R)-4-(2-phenylethyl)piperazin-2-yl]carbonyl}piperazine-1-carboxamide;N-(3,4-Dichlorophenyl)-4-{[(2R)-4-methylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;N-(3-chlorophenyl)-4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}-N-[4-(trifluoromethyl)phenyl]piperazine-1-carboxamide;N-[4-chloro-3-(trifluoromethyl)phenyl]-4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}-N-[3-(trifluoromethyl)phenyl]piperazine-1-carboxamide;N-(4-chlorophenyl)-4-{[(2R)-4-isopropylpiperazin-2-yl]carbonyl}piperazine-1-carboxamide;N-(3-chloro-4-fluorophenyl)-4 ...

Подробнее
Номер записи: 25
20-02-2014 дата публикации

HETEROCYCLIC COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS

Номер: US20140051857A1
Автор: Hirokawa Yutaka, Ishiwata Norihisa, Iwamoto Shunsuke, Miyaji Katsuaki, Nakamura Takanori, OWADA Shingo, YANAGIHARA Kazufumi
Принадлежит: Nissan Chemical Industries Limited

A compound represented by the formula (1): 1. A compound represented by the formula (1){'sup': 4', '4', '5', '5', '5', '5', '6', '7', '6', '7', '6', '7', '26', '27', '26', '27', '8', '8, 'sub': 2-6', '2-6', '1-10', '2-6', '2-6', '1-10', '2-6', '2-6', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-6', '1-6', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2', '1-10', '2-6', '2-6', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-6', '1-6', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '1-10', '2-6', '2-6', '1-10', '1-10', '2-10', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-6', '1-6', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2', 'm1', '2', 'm2', '1-10', '2-14', '1-10', '2-14', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-6', '1-6', '2-14', '2-14', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14, 'claim-text': [{'sup': 9', '9, 'sub': 1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '2-6', '2-6', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '1-10', '2-14', '2-14', '2-14', '2-14', '1-6', '1-6', '2-14', '2-14', '1-10', '1-10', '2-6', ' ...

Подробнее
Номер записи: 26
27-02-2014 дата публикации

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

Номер: US20140057892A1
Автор: Boyer Angelique Sun, Evdokimov Artem G., Greis Kenneth D., Kawamoto Richard Masaru, Warshakoon Namal C., Wu Shengde
Принадлежит: Akebia Therapeutics, Inc.

The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD) heart failure, ischemia, and anemia. 132-. (canceled) This application is a Continuation Application of U.S. application Ser. No. 11/821,936, filed Jun. 26, 2007, which claims the benefit of Provisional Application Ser. No. 60/816,522 filed on Jun. 26, 2006, and the entire disclosures of Provisional Application Ser. No. 60/816,522 and U.S. application Ser. No. 11/821,936 are incorporated herein by reference in its entirely.The present disclosure relates, in some aspects, to HIF-1α prolyl hydroxylase inhibitor compounds and pharmaceutically acceptable salts thereof, compositions comprising the HIF-1α prolyl hydroxylase inhibitor compounds, and to methods for treating or controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.HIF-1α under normal healthy conditions wherein the cells have a sufficient supply of oxygen is readily converted to a degraded form by one of several prolyl hydroxylase enzymes, infer alia, EGLIN. When cells undergo hypoxia, this enzymatic transformation is slow or entirely stopped and HIF-1α begins to build up in the cell. When this build up of HIF-1α occurs, this protein combines with another factor, HIF-1β which together form an active transcription factor complex. This transcription factor then activates several biological pathways which are present as a response to and a means for alleviating the body's state of hypoxia. These responses include, inter alia, angiogenic, erythropoietic (EPO), glucose metabolism, and matrix alteration responses.In patients where there is a need for stimulating one or more of these responses, for example, in patients in need of increased tissue oxygen due to peripheral vascular ...

Подробнее
Номер записи: 27
27-02-2014 дата публикации

PHARMACEUTICAL COMPOSITION FOR TREATING ALZHEIMER'S DISEASE

Номер: US20140058097A1
Автор: Haraguchi Hidekazu, Hori Akihiro, Itoh Naohiro, Kanda Yasuhiko, Kato Akira, Kobayashi Naotake, Kooriyama Yuuji, Sakaguchi Gaku, Suzuki Shinji, UEDA Kazuo, Yasui Ken, Yukimasa Akira
Принадлежит: Shionogi & Co., Ltd.

A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): 221-. (canceled) The present invention relates to a pharmaceutical composition which has reducing effect to produce amyloid β protein and is useful as an agent for treating disease induced by production, secretion and/or deposition of amyloid β protein, especially Alzheimer's disease.In the brain of Alzheimer's patient, the peptide composed of about 40 amino acids residue as is called amyloid β protein, that accumulates to form insoluble specks (senile specks) outside nerve cells is widely observed. It is concerned that this senile specks kill nerve cells to cause Alzheimer's disease. The therapeutic agents for Alzheimer's disease, such as decomposition agents of amyloid β protein and amyloid β vaccine, are under investigation.Secretase is an enzyme which cleaves amyloid 3 precursor protein (APP) in cell and produce amyloid 13 protein. The enzyme which controls the production of N terminus of amyloid β protein is called as BACE 1 (beta-site APP-cleaving enzyme 1, β-secretase). It is thought that inhibition of this enzyme leads to reduction of producing amyloid β protein and that the therapeutic agent for Alzheimer's disease will be created by the inhibition.Patent Literature 1 describes the compounds which are similar to those of the compounds contained in the pharmaceutical composition of the present invention, and the compounds have NO synthase enzyme inhibitory activity and are useful for dementia.Patent Literature 2 to 10 describes the compounds which are known as BACE 1 inhibitor, however, have different structures from the compounds contained in the pharmaceutical composition of the present invention.The present invention provides pharmaceutical compositions which have reducing effects to produce amyloid β protein, especially BACE 1 inhibitory activity, and which are useful as an agent for treating disease induced by production, secretion ...

Подробнее
Номер записи: 28
13-03-2014 дата публикации

BRADYKININ B1 ANTAGONISTS

Номер: US20140073627A1
Автор: Hallett David James, MADDEN James, PARKES Alastair, RAOOF Ali, WANG Xiaolu
Принадлежит: EVOTEC AG

The invention relates to compounds of formula (I) 2. The compound of claim 1 , wherein X is phenyl claim 1 , or thiophene claim 1 , and wherein X is substituted with Rand is optionally substituted with one or more R claim 1 , which are the same or different.3. The compound of claim 1 , wherein two adjacent Rare joined together with the atoms to which they are attached to form benzo and wherein benzo is optionally substituted with one or more R claim 1 , which are the same or different.4. The compound of claim 1 , wherein X is substituted in 2-position relative to the sulfonamide group in formula (I) with Rand is optionally substituted with one or more R claim 1 , which are the same or different.5. The compound of claim 1 , wherein R claim 1 , R claim 1 , Rare independently selected from the group consisting of CH claim 1 , CF claim 1 , CHCH claim 1 , CHOH claim 1 , OCH claim 1 , Cl claim 1 , Br claim 1 , and phenyl.6. The compound of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , phenyl claim 1 , or cyclopropylmethyl.7. The compound of claim 1 , wherein R claim 1 , Rare independently selected from the group consisting of H claim 1 , and methyl.9. The compound of claim 1 , wherein Ris H; or CH.10. The compound of claim 1 , wherein R claim 1 , Rare joined to form a ring selected from the group consisting of piperidine; piperazine; morpholine; 2 claim 1 ,8-diazaspiro[4.5]decane; pyrrolidine; and diazepane claim 1 , wherein the ring is optionally substituted with one or more R claim 1 , which are the same or different.11. The compound of claim 1 , wherein Ris CH-T claim 1 , CH—CH(CH)-T claim 1 , or CH—CH-T.12. The compound of claim 1 , wherein Tis phenyl; or pyridine.13. The compound of claim 1 , wherein R claim 1 , Rare independently selected from the group consisting of CN claim 1 , C(O)N(RR) claim 1 , C(NR)N(RR) claim 1 , C(NR)N(R)OR claim 1 , N(RR) claim 1 , N(R)C(O)N(RR) claim 1 , C(O)R claim 1 ...

Подробнее
Номер записи: 29
13-03-2014 дата публикации

QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES

Номер: US20140073642A1
Автор: Embrechts Werner, Jonckers Tim Hugo Maria, Last Stefaan Julien, McGowan David, Pieters Serge Maria Aloysius, Raboisson Pierre Jean-Marie Bernard
Принадлежит: JANSSEN R&D IRELAND

This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved. 2. A compound of formula (I) according to wherein Ris butyl claim 1 , pentyl or 2-pentyl and wherein R claim 1 , R claim 1 , Rand Rare as specified above.3. A compound of formula (I) according to wherein Ris Calkyl substituted with a hydroxyl claim 1 , and wherein R claim 1 , R claim 1 , Rand Rare as specified above.5. A compound of formula (I) according to wherein Ris preferably hydrogen or fluorine and R claim 1 , R claim 1 , R claim 1 , and Rare as described above.6. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof and one or more pharmaceutically acceptable excipients claim 1 , diluents or carriers.7. (canceled)8. A method for the treatment of a subject having a disorder in which the modulation of TLR7 and/or TLR8 is involved claim 1 , said method comprising administration of a compound or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof claim 1 , or a pharmaceutical composition according to to the subject.9. A compound of having a structure shown in Table 1 claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate or polymorph thereof. This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.The present invention relates to the use of quinazoline derivatives in the treatment of viral infections, immune or inflammatory disorders, whereby the modulation, or agonism, of toll-like-receptors (TLRs) is involved. Toll-Like Receptors are primary transmembrane proteins characterized by an extracellular leucine rich domain and a cytoplasmic extension that contains a conserved region. The innate immune system can recognize pathogen-associated molecular patterns via these ...

Подробнее
Номер записи: 30
20-03-2014 дата публикации

VEGFR3 INHIBITORS

Номер: US20140080798A1
Автор: Camerino Michelle Ang, Choi Neil, Foitzik Richard Charles, Ganame Danny, Harvey Andrew John, Hemley Catherine Fae, Holmes Ian Peter, Kersten Wilhelmus Johannes Antonius, Lessene Romina, Lunniss Gillian Elizabeth, Morrow Benjamin Joseph, Stupple Paul Anthony
Принадлежит: Cancer Therapeutics CRC Pty Limited

This invention relates to compounds of the formula (I): 3. A compound according to claim 1 , wherein A is an optionally substituted 6 membered heteroaryl group.4. A compound according to claim 3 , wherein A is optionally substituted pyridyl.7. A compound according to claim 1 , wherein A is an optionally substituted 5 membered heteroaryl group.8. A compound according to claim 7 , wherein A is optionally substituted pyrazolyl.11. A compound according to claim 1 , where no Rsubstituents are present on A.12. A compound according to claim 1 , where Ris methyl.13. A compound according to claim 1 , where a single Rsubstituent is present.18. A compound according to claim 14 , where no Rsubstituents are present on A.19. A compound according to claim 14 , where Ris methyl.20. A compound according to claim 14 , where a single Rsubstituent is present.2126-. (canceled)29. A compound according to claim 1 , wherein Ris H.30. A compound according to claim 29 , wherein Ris methyl.31. A compound according to claim 29 , wherein Ris CF.3336-. (canceled)37. A compound according to claim 1 , wherein Ris a substituted 6 membered heteroaryl group claim 1 , where the heteroaryl ring system contains 1 or 2 N heteroatoms.3945-. (canceled)52. A compound selected from compounds 1 to 42 as described herein.54. A pharmaceutical agent comprising a compound or an isomer claim 1 , salt claim 1 , solvate or prodrug thereof according to .55. A composition comprising a compound or an isomer claim 1 , salt claim 1 , solvate or prodrug thereof according to claim 1 , and a pharmaceutically acceptable carrier or diluent.56. (canceled)57. A method for treating a disease ameliorated by the inhibition of VEGFR3 comprising administering an effective amount of an isomer claim 1 , salt claim 1 , solvate or prodrug thereof according to to a subject in need thereof.58. A method for treating cancer comprising administering an effective amount of a compound or an isomer claim 1 , salt claim 1 , solvate or prodrug ...

Подробнее
Номер записи: 31
20-03-2014 дата публикации

Inhibitors of Histone Deacetylase

Номер: US20140080802A1
Автор: Haggarty Stephen, Holson Edward, Tsai Li-Huei, Wagner Florence Fevrier, Weiwer Michel, ZHANG YAN-LING
Принадлежит:

The present invention relates to compounds of formula (I): 10. A pharmaceutical composition comprising an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof and a pharmaceutical carrier claim 1 , diluent claim 1 , or excipient.11. A method of treating claim 1 , alleviating claim 1 , and/or preventing a condition in a subject comprising administering to the subject in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate or prodrug thereof.12. The method of claim 11 , wherein the condition is selected from a neurological disorder claim 11 , memory loss or impairment claim 11 , cognitive function disorder or impairment claim 11 , extinction learning disorder claim 11 , fungal disease or infection claim 11 , inflammatory disease claim 11 , hematological disease claim 11 , and neoplastic disease.13. The method of claim 11 , wherein the condition is selected from:a cognitive function disorder or impairment associated with Alzheimer's disease, Huntington's disease, seizure induced memory loss, schizophrenia, Rubinstein Taybi syndrome, Rett Syndrome, Fragile X, Lewy body dementia, vascular dementia, ADHD, dyslexia, bipolar disorder and social, cognitive and learning disorders associated with autism, traumatic head injury, or attention deficit disorder, anxiety disorder, conditioned fear response, panic disorder, obsessive compulsive disorder, posttraumatic stress disorder, phobia, social anxiety disorder, substance dependence recovery or Age Associated Memory Impairment (AAMI), or Age Related Cognitive Decline (ARCD);a hematological disease selected from acute myeloid leukemia, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia;a cancer; andan extinction learning disorder selected from a fear extinction deficit and post-traumatic ...

Подробнее
Номер записи: 32
20-03-2014 дата публикации

STRUCTURE-GUIDED IDENTIFICATION OF BINDING INTERACTIONS OF HUMAN LAMININ RECEPTOR PRECURSOR WITH LAMININ AND IDENTIFICATION OF COMPOUNDS THAT AFFECT BINDING

Номер: US20140080824A1
Автор: DiGiacomo Vincent, Jamieson Kelly, Meruelo Daniel
Принадлежит: New York University

The present invention pertains to compounds which interfere with the binding of laminin to the laminin receptor (LamR). Such compounds are useful for treating diseases such as cancer, Alzheimer's Disease, and certain viral and bacterial infections. 1. A pharmaceutical formulation for treating a mammal suffering from a disease mediated by the laminin receptor (LamR) comprising an agent selected from N-dibenzo[a ,c]phenazin-11-yl-4-morpholinecarbothioamide) , and N-(2-hydroxyethyl)dibenzo[a ,c]phenazine-11-carboxamide. and a pharmaceutically acceptable carrier or diluent.2. The pharmaceutical formulation of wherein said disease is selected from a tumor claim 1 , Alzheimer's disease claim 1 , and prion disease.3. A method for treating a mammal suffering from a tumor comprising administering to a mammal in need of such treatment an amount of an agent selected from N-(2-hydroxyethyl)dibenzo[a claim 1 ,c]phenazine-11-carboxamide and N-dibenzo[a claim 1 ,c]phenazin-11-yl-4-morpholinecarbothioamide). effective to treat said tumor and a pharmaceutically acceptable carrier or diluent.4. The method of wherein said agent is administered systemically.5. The method of wherein said agent is administered parenterally.6. The method of wherein said mammal is a human.7. The method of wherein said tumor expresses greater levels of LamR than normal cells of the same lineage.8. A method for reducing metastatic growth of a tumor in a mammal comprising administering to a mammal harboring a tumor and in need of such treatment an amount of an agent selected from N-(2-hydroxyethyl)dibenzo[a claim 3 ,c]phenazine-11-carboxamide and N-dibenzo[a claim 3 ,c]phenazin-11-yl-4-morpholinecarbothioamide). effective to reduce metastatic growth of said tumor in said mammal and a pharmaceutically acceptable carrier or diluent.9. The method of wherein said agent is administered systemically.10. The method of wherein said compound is administered parenterally.11. The method of wherein said mammal is a human ...

Подробнее
Номер записи: 33
20-03-2014 дата публикации

IRE-1alpha INHIBITORS

Номер: US20140080832A1
Автор: Flynn Gary A., LONERGAN David Gregory, PALLAI Peter V., PATTERSON John Bruce, ZENG Qingping
Принадлежит: MANNKIND CORPORATION

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies. 2. The compound of claim 1 , wherein the compound is represented by structural formula (E).3. The compound of claim 1 , wherein the compound is represented by structural formula (X).8. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound of or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable carrier.9. A method of inhibiting IRE-1α activity claim 1 , comprising administering to a subject a compound of or a pharmaceutically acceptable salt of the compound.10. The method of claim 1 , wherein the compound is a compound of .11. The method of claim 1 , wherein the compound is a compound of .12. The method of claim 1 , wherein the compound is a compound of .13. The method of claim 1 , wherein the compound is a compound of .14. The method of claim 1 , wherein the compound is a compound of15. The method of claim 1 , wherein the compound is a compound of .16. The method of wherein cells of the subject have an activated unfolded protein response.17. The method of claim 9 , wherein the subject has cancer.18. The method of claim 17 , wherein the cancer is myeloma.19. The method of claim 9 , further comprising administering to the subject an agent that induces or up-regulates IRE-1α expression.20. The method of claim 9 , further comprising administering to the subject a biotherapeutic agent claim 9 , a chemotherapeutic agent claim 9 , radiation claim 9 , or a proteasome inhibitor. This application is a division of Ser. No. 12/941,530 filed on Nov. 8, 2010, which is a continuation of Ser. No. 12/135,571 filed on Jun. 9, 2008, now U.S. Pat. No. 7,858,666, which claims the benefit of Ser. No. 60/942,743 filed Jun. 8, 2007. ...

Подробнее
Номер записи: 34
07-01-2016 дата публикации

NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN

Номер: US20160002188A1
Автор: Bair Kenneth W., JR. David R., Lancia, LI Hongbin, Loch James
Принадлежит:

The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: 6. The compound of claim 2 , wherein A and B are 0.10. The compound of claim 2 , wherein Aris a substituted or unsubstituted 5-6 membered monocyclic aryl or heteroaryl.11. The compound of claim 10 , wherein Aris a substituted or unsubstituted 5 membered monocyclic aryl or heteroaryl and said heteroaryl has 1 or 2 heteroatoms which are independently S or N.13. The compound of claim 10 , wherein Aris a substituted or unsubstituted 6 membered monocyclic aryl or heteroaryl and said heteroaryl has 1 or 2 heteroatoms which are N.18. The compound of claim 2 , wherein Aris a substituted or unsubstituted 9 membered 6 claim 2 ,5-bicyclic heteroaryl and said heteroaryl has 1 claim 2 , 2 claim 2 , or 3 heteroatoms which are independently O claim 2 , S or N.20. The compound of claim 2 , wherein Ris a substituted or unsubstituted monocyclic or bicyclic 5-10 membered aryl or heteroaryl.21. The compound of claim 20 , wherein Ris a substituted or unsubstituted monocylic 6 membered aryl.23. The compound of claim 20 , wherein Ris a substituted or unsubstituted bicyclic 8-10 membered aryl or 8-10 membered heteroaryl.24. The compound of claim 23 , wherein Ris a substituted or unsubstituted 8 membered 5 claim 23 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 23 , 2 claim 23 , 3 claim 23 , or 4 heteroatoms and said heteroatoms are independently O claim 23 , S claim 23 , or N.26. The compound of claim 20 , wherein Ris a substituted or unsubstituted 9 membered 6 claim 20 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 20 , 2 claim 20 , 3 claim 20 , or 4 heteroatoms and said heteroatoms are independently O claim 20 , S claim 20 , or N.28. The compound of claim 20 , wherein Ris a substituted or unsubstituted 10 membered 6 claim 20 ,6 bicyclic aryl or heteroaryl and said heteroaryl has 1 claim ...

Подробнее
Номер записи: 35
04-01-2018 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

Номер: US20180002277A1
Автор: Anderson Eric, Jiang Xin, Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 1257-. (canceled)259264-. (canceled)266. The method of claim 265 , wherein Ris hydrogen.267. The method of claim 265 , wherein Ris alkylor substituted alkyl.268. The method of claim 265 , wherein Ris alkylsulfonyl claim 265 , arylsulfonyl claim 265 , aralkylsulfonyl claim 265 , heteroarylsulfonyl claim 265 , heteroaralkylsulfonyl claim 265 , or a substituted version of any of these groups.269. The method of claim 265 , wherein Ris acylor substituted acyl.270. The method of claim 269 , wherein Ris substituted acyl.272. The method of claim 271 , wherein Ris hydrogen.273. The method of claim 271 , wherein Ris alkylor substituted alkyl.274. The method of claim 271 , wherein Ris alkylsulfonyl claim 271 , arylsulfonyl claim 271 , aralkylsulfonyl claim 271 , heteroarylsulfonyl claim 271 , heteroaralkylsulfonyl claim 271 , or a substituted version of any of these groups.275. The method of claim 271 , wherein Ris acylor substituted acyl.276. The method of claim 271 , wherein Ris substituted acyl.278. The method of claim 277 , wherein the acylation agent is an acyl halide or an anhydride.279. The method of claim 277 , wherein the acylation agent is an acyl halide.280. The method of claim 277 , wherein the acylation agent is an acyl chloride.281. The method of claim 258 , wherein the modification is conducted in a medium comprising a solvent.282. The method of claim 281 , wherein the solvent is benzene or dichloromethane.283. The method of claim 258 , wherein the modification is conducted in the presence of a base.284. The method of claim 283 , wherein the base is NEt. The present application is a continuation of U.S. patent application Ser. No. 14/753,297, filed Jun. 29, 2015, now U.S. Pat. No. 9,670,147, which is a continuation of U.S. patent application Ser. No. 13/861,208, filed Apr. 11, 2013, now U.S. Pat. No. 9,102,681, which is a continuation of U.S. patent application ...

Подробнее
Номер записи: 36
02-01-2020 дата публикации

Novel Raft Agents and their Use in the Development of Polyvinylpyrrolidone Grafted Nanoparticles

Номер: US20200002447A1
Автор: Benicewicz Brian, Wang Lei
Принадлежит:

Nanoparticles having a plurality of PVP chains covalently bonded to a surface of the nanoparticle are provided, along with their methods of formation and the RAFT agents for the polymerization of the PVP chains. RAFT agents are generally provided, along with their methods of formation and use. Methods are also generally provided for grafting a PVP polymer onto a nanoparticle. In one embodiment, the method includes polymerizing a plurality of monomers in the presence of a RAFT agent to form a polymeric chain covalently bonded to the nanoparticle. 120-. (canceled)22. The method of claim 21 , wherein Ror Ris H.23. The method of claim 21 , wherein Ror Ris CN claim 21 , NO claim 21 , SOH claim 21 , or a halogen.24. The method of claim 23 , wherein Ror Ris a nitrile group.25. The method of claim 21 , wherein n or m is 2.26. The method of claim 21 , wherein Ror Ris ORwith Rbeing a Cto Calkyl group.27. The method of claim 21 , wherein Ror Ris a hydroxyl group.28. The method of claim 21 , wherein Ror Ris a thioazoline group. The present application claims priority to U.S. Provisional Patent Application Ser. No. 62/027,510, filed on Jul. 22, 2014, the disclosure of which is incorporated by reference herein.Polymer grafted nanoparticles are very appealing composite materials ascribed to their broad applications in coatings, biomedical field and chemosensors. In addition, the properties of the composites can be tailored by choosing different substrate nanoparticles and polymer shells. The graft density and chain lengths of the surface attached polymers are able to greatly affect the dispersion and the final properties of the nanoparticles. Thus, controlling the growth of polymer on surfaces is extremely significant.Poly(vinyl pyrrolidone) (PVP), a very important water soluble polymer, has been widely applied in biomedical area and cosmetic industry due to its nontoxic and nonionic characteristics, and its biocompatibility. It is particularly attractive in the drug delivery ...

Подробнее
Номер записи: 37
20-01-2022 дата публикации

PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS

Номер: US20220016046A1
Автор: BEAN Bruce P., Woolf Clifford J.
Принадлежит:

The invention provides compounds, compositions, methods, and kits for the treatment or neurogenic inflammation. 1. A method for treating neurogenic inflammation in a patient , said method comprising administering to said patient a therapeutically effective amount of a compound that is capable of (i) entering a nociceptor through a channel-forming receptor present in said nociceptor when said receptor is activated and (ii) inhibiting a voltage-gated ion channel present in said nociceptor , wherein said compound does not substantially inhibit said channel when applied to the extracellular face of said channel and when said receptor is not activated.2. The method of claim 1 , wherein said compound inhibits voltage-gated sodium channels.3. The method of claim 2 , wherein said compound is QX-314 claim 2 , N-methyl-procaine claim 2 , QX-222 claim 2 , N-octyl-guanidine claim 2 , 9-aminoacridine claim 2 , pancuronium claim 2 , or another low molecular weight claim 2 , charged molecule that inhibits voltage-gated sodium channels when present inside of said nociceptor.4. The method of claim 1 , wherein said compound is a quarternary amine derivative or other charged derivative of a compound selected from the group consisting of riluzole claim 1 , mexilitine claim 1 , phenytoin claim 1 , carbamazepine claim 1 , procaine claim 1 , tocainide claim 1 , prilocaine claim 1 , articaine claim 1 , bupivicaine claim 1 , mepivicine claim 1 , diisopyramide claim 1 , bencyclane claim 1 , quinidine claim 1 , bretylium claim 1 , lifarizine claim 1 , lamotrigine claim 1 , flunarizine claim 1 , and fluspirilene.5. The method of claim 1 , wherein said compound inhibits calcium channels.6. The method of claim 5 , wherein said compound is selected fromD-890, CERM 11888, N-methyl-verapamil, N-methylgallopamil, N-methyl-devapamil, and dodecyltrimethylammonium;a quaternary amine derivative of verapamil, gallopamil, devapamil, diltiazem, fendiline, mibefradil, or farnesyl amine;a compound according ...

Подробнее
Номер записи: 38
12-01-2017 дата публикации

Polymerizable compound, polymer, polymerizable composition, film, and half mirror for displaying projection image

Номер: US20170009138A1
Автор: Daisuke Hayashi, Hiroshi Matsuyama, Masaru Yoshikawa, Shunya Katoh, Yuki Nakazawa
Принадлежит: Fujifilm Corp

The present invention provides a polymerizable compound denoted by Formula (I): in the formula, Z 1 and Z 2 represent an arylene group, and the like, m represents 1 or 2, n represents an integer of 0 or 1, and when m is 2, n is 0, L 1 , L 2 , L 3 , and L 4 each independently represent a linking group such as —C(═O)O— and —OC(═O)—, T 3 represents -Sp 4 -R 4 , X represents —O—, and the like, r represents 1 to 4, Sp 1 , Sp 2 , Sp 3 , Sp 4 , and Sp 5 each independently represent a single bond or a linking group, R 1 and R 2 each independently represent a polymerizable group, and R 3 , R 4 , and R 5 each independently represent a hydrogen atom, a polymerizable group, or the like; a polymerizable composition containing the polymerizable compound described above; a film formed of the polymerizable composition described above; and a half mirror for displaying a projection image including the film described above.

Подробнее
Номер записи: 39
14-01-2016 дата публикации

PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF TO MODULATE LIPID METABOLISM

Номер: US20160009748A1
Автор: Cale Jacqueline, Cupp Jeanne Ann, Emal Cory, Lawrence Daniel A., Li Shih-Hon, Su Enming Joe, Warnock Mark
Принадлежит:

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. 139.-. (canceled)44. A method of increasing circulating high density lipoprotein (HDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to increase HDL.45. A method of decreasing circulating very low density lipoprotein (VLDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to decrease VLDL.46. The method of claim 44 , wherein the subject is human.47. The method of claim 44 , wherein the PAI-1 inhibitor decreases PAI-1 binding to apolipoprotein E (ApoE) claim 44 , apolipoprotein A (ApoA) claim 44 , and/or VLDL.48. (canceled)49. (canceled)50. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of vitronectin.51. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of urokinase type plasminogen activator (uPA).52. A method of modulating cholesterol and/or lipid uptake comprising the step of administering a PAI-1 inhibitor compound according to in an amount effective to modulate cholesterol and/or lipid uptake.53. A method of modulating cholesterol and/or lipid clearance comprising the step of administering a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to inhibit very low density lipoprotein (VLDL) or apolipoprotein E (ApoE) or apolipoprotein A (ApoA) binding to VLDL-R and modulate cholesterol and/or lipid clearance.54. A method of modulating cholesterol and/or lipid clearance ...

Подробнее
Номер записи: 40
14-01-2016 дата публикации

FUNCTIONALISED ANTIFOULING COMPOUNDS AND USE THEREOF

Номер: US20160009926A1
Автор: Burkett Brendan Adrian, Chai Christina Li Lin, Dickinson Gary Howard, Hong Han, Lee Serina Siew Chen, Rittschof Daniel, Teo Serena Lay Ming
Принадлежит:

The present invention relates to derivatives of α, α-disubstituted amide compounds which comprise a substituted aryl at the a carbon such that the substituent provides a means for attachment or incorporation of the compound to or in a polymer. The provision of such a substituent on the aryl has surprisingly been found not only to permit attachment to or incorporation n a polymer but also retention of useful antifouling activity. In embodiments, the substituent is selected from hydroxyl, ethers, esters, carboxyls, alkylsilyls and alkenyls. Experiments demonstrate that antifouling activity can be as good or better as the corresponding unsubstituted compound and that polymers functionalised so as to include or be formed from the substituted compound can be used to reduce settlement. 3. A compound according to claim 2 , wherein in respect of option (i) each of Rand Ris H; and in respect of option (ii) each of Rand Ris Me.5. A compound according to any one of to claim 2 , wherein Ris Calkyl or Calkyl.7. A compound according to any one of to claim 2 , wherein claim 2 , if present claim 2 , each R' is independently optionally substituted Cto Calkylene claim 2 , and wherein claim 2 , if present claim 2 , each Ris independently selected from optionally substituted Cto Calkyl and Cto Calkenyl and Cto Calkylsilyl-Cto Calkylene.9. A compound according to claim 8 , wherein at least two of claim 8 , R claim 8 , R claim 8 , Rand Rare H.10. A compound according to claim 8 , wherein at least three of R claim 8 , R claim 8 , R claim 8 , Rand Rare H.11. A compound according to claim 1 , wherein the compound is selected from compounds 15.1 claim 1 , 15.2 claim 1 , 15.3 claim 1 , 15.4 claim 1 , 15.5 claim 1 , 15.6 claim 1 , 15.7 claim 1 , 16.1 claim 1 , 16.2 claim 1 , 16.3 claim 1 , 16.4 claim 1 , 16.5 claim 1 , 16.6 claim 1 , 16.7 claim 1 , 16.8 claim 1 , 16.9 claim 1 , 16.10 claim 1 , 16.11 claim 1 , 17.1 claim 1 , 17.2 claim 1 , 17.3 claim 1 , 17.4 claim 1 , 17.5 claim 1 , 17.6 claim ...

Подробнее
Номер записи: 41
03-02-2022 дата публикации

HYDROXAMIC ACID DERIVATIVE, METHOD FOR PRODUCING SAME AND USE THEREOF

Номер: US20220033369A1
Автор: Du Xiaonan, Wang Juxian, Wang Minghua, WANG Yucheng, You Xuefu, Zhang Guoning, ZHU Mei
Принадлежит:

The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield. 115.-. (canceled)20. The method according to claim 18 , wherein claim 18 , the molar ratio of the Dess-Martin periodinane to the compound of Formula (II) is 1.0 to 1.2.21. The method according to claim 19 , wherein claim 19 , the molar ratio of the Dess-Martin periodinane to the compound of Formula (II) is 1.0 to 1.2.22. The method according to claim 18 , wherein claim 18 , the oxidation reaction is conducted at room temperature for 2 to 8 hours.23. The method according to claim 20 , wherein claim 20 , the oxidation reaction is conducted at room temperature for 2 to 8 hours.24. The method according to claim 18 , wherein claim 18 , the molar ratio of the compound of Formula (III)/triphenylphosphine/carbon tetrabromide is 1:(3.8-4.2):(1.8-2.2).25. The method according to claim 18 , wherein claim 18 , the Corey-Fuchs reaction is conducted at a temperature of −20 to −78° C.26. The method according to claim 24 , wherein claim 24 , the Corey-Fuchs reaction is conducted at a temperature of −20 to −78° C.27. The method according to claim 18 , wherein claim 18 , the molar ratio of the compound of Formula (IV)/tris(dibenzylideneacetone)dipalladium/the compound of Formula (a)/triethylamine is 1:(0.02-0.04):(1.8-2.2):(2.8-3.2).28. The method according to claim 18 , wherein claim 18 , the ...

Подробнее
Номер записи: 42
21-01-2016 дата публикации

THROMBOXANE RECEPTOR ANTAGONISTS

Номер: US20160016900A1
Автор: "OConnor Barry", Guiry Patrick, Kinsella B. Therese, Reid Helen
Принадлежит:

The invention generally relates to compounds that function as TP antagonists for treating thrombosis and other cardiovascular, renal, or pulmonary diseases. In some embodiments, the invention provides a compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating thrombosis by administering an antithrombotic compound that preferentially binds to a thromboxane receptor, has preferential binding for either TPalpha (TPα) or TPbeta (TPβ) receptor subtype.

Подробнее
Номер записи: 43
16-01-2020 дата публикации

ADAMANTANE DERIVATIVES FOR THE TREATMENT OF FILOVIRUS INFECTION

Номер: US20200017514A1
Автор: Brown Eric, Gantla Vidyasagar, Henkel Gregory, McCormack Kenneth, Plewe Michael, Sokolova Nadezda
Принадлежит:

Compounds of structural Formula I were developed for the treatment of infections by filoviruses including Ebolavirus and Marburgvirus, wherein, R, R, R, X and Y are defined in the specification. 119-. (canceled)21. The compound of claim 20 , wherein:{'sup': 4', '5, 'X is C-A-D and Y is CRR.'}23. The compound of claim 22 , wherein:{'sup': 2', '11a', '11b', '12, 'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10', '1', '10', '2', 'n, 'Ris selected from hydrogen, (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl, (Cto C) alkoxy, —(CH)C(O)N(RR), and —C(O)R, wherein'}{'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10', '1', '10, 'sup': '13', 'each of the said (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl, and (Cto C) alkoxy is optionally substituted with at least one Rgroup;'}{'sup': '3', 'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10, 'Ris selected from hydrogen, (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, and (Cto C) cycloalkenyl, wherein'}{'sub': 1', '10', '1', '10', '1', '10', '6', '10', '5', '10, 'sup': '13', 'each of the said (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl is optionally substituted with at least one Rgroup.'}24. The compound of claim 23 , wherein:{'sup': '3', 'Ris hydrogen.'}31. The method of claim 30 , wherein the infection is associated with filovirus selected from the group consisting of Ebolavirus and Marburgvirus.32. The method of claim 31 , where the filovirus is Ebolavirus.33. The method of claim 31 , including administering a therapeutic amount of a therapeutic agent selected from the group consisting of Ribavirin claim 31 , viral RNA-dependent-RNA polymeras inhibitors including favipiravir claim 31 , Triazavirin claim 31 , Remdesivir (GS-5734) claim 31 , monoclonal antibody therapies including claim 31 , ZMapp claim 31 , REGN3470-3471-3479 claim 31 , mAb 114 ...

Подробнее
Номер записи: 44
28-01-2016 дата публикации

INHIBITING NEUROTRANSMITTER REUPTAKE

Номер: US20160024044A1
Автор: Carlier Paul, Fauq Abdul H., Monceaux Christopher J., Richelson Elliott
Принадлежит:

This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided. Specifically gamma-amino alcohol derivatives that inhibit the reuptake of neurotransmitters such as dopamine, serotonin, epinephrine or norepinephrine are provided as therapeutic agents for the treatment of depression or anxiety in a mammalian subject. 17-. (canceled)9. The compound of claim 8 , wherein Ris optionally substituted with one or two substituents.11. The compound of claim 10 , wherein at least two of R claim 10 , R claim 10 , R claim 10 , R claim 10 , and Rare hydrogen.12. The compound of claim 11 , wherein the remaining R claim 11 , R claim 11 , R claim 11 , R claim 11 , and Rare independently selected from ethyl claim 11 , chloro claim 11 , and bromo.13. The compound of claim 10 , wherein R claim 10 , R claim 10 , and Rare hydrogen; and Rand Rare independently selected from ethyl claim 10 , chloro claim 10 , and bromo.15. The compound of claim 14 , wherein each of Rand Ris not hydrogen.17. The compound of claim 16 , wherein Ris selected from hydrogen claim 16 , lower alkyl claim 16 , halo claim 16 , hydroxyl claim 16 , lower alkoxy claim 16 , methylsulfanyl claim 16 , and methsulfonyl; and Ris selected from hydrogen claim 16 , lower alkyl claim 16 , halo claim 16 , dimethylamino claim 16 , methylsulfanyl claim 16 , and 1 claim 16 ,1 claim 16 ,1-trifluoromethanesulfonamide.1826-. (canceled) This application claims the benefit of U.S. Provisional Application Ser. No. 61/783,122, filed Mar. 14, 2013. The disclosure of the prior application is considered part of (and is incorporated by reference in) the disclosure of this application.1. Technical FieldThis document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake.2. Background InformationNeuronal signals are ...

Подробнее
Номер записи: 45
28-01-2016 дата публикации

NOVEL RAFT AGENTS AND THEIR USE IN THE DEVELOPMENT OF POLYVINYLPYRROLIDONE GRAFTED NANOPARTICLES

Номер: US20160024234A1
Автор: BENICEWICZ BRIAN C., Wang Lei
Принадлежит:

Nanoparticles having a plurality of PVP chains covalently bonded to a surface of the nanoparticle are provided, along with their methods of formation and the RAFT agents for the polymerization of the PVP chains. RAFT agents are generally provided, along with their methods of formation and use. Methods are also generally provided for grafting a PVP polymer onto a nanoparticle. In one embodiment, the method includes: polymerizing a plurality of monomers in the presence of a RAFT agent to form a polymeric chain covalently bonded to the nanoparticle. 2. The RAFT agent of claim 1 , wherein Ris H.3. The RAFT agent of claim 1 , wherein Ris a nitrile group.4. The RAFT agent of claim 1 , wherein n is 2.5. The RAFT agent of claim 1 , wherein Ris a hydroxyl group.7. The RAFT agent of claim 1 , wherein Ris a thioazoline group.9. The RAFT agent of claim 1 , wherein the nitrogen containing heterocyclic aromatic organic group is substituted with an organic group.10. The RAFT agent of claim 1 , wherein the nitrogen containing heterocyclic aromatic organic group is unsubstituted.12. The RAFT agent of claim 11 , wherein Ris H claim 11 , and wherein Ris a nitrile group.13. The RAFT agent of claim 11 , wherein n is 2.14. The RAFT agent of claim 11 , wherein Ris a hydroxyl group.16. The RAFT agent of claim 11 , wherein Ris a thioazoline group.18. The RAFT agent of claim 11 , wherein the nitrogen containing heterocyclic aromatic organic group is substituted with an organic group.19. The RAFT agent of claim 11 , wherein the nitrogen containing heterocyclic aromatic organic group is unsubstituted.21. A nanoparticle claim 11 , comprising:a plurality of PVP chains covalently bonded to a surface of the nanoparticle.22. The nanoparticle of claim 21 , further comprising:an antimicrobial agent non-covalently attached to the PVP chains. The present application claims priority to U.S. Provisional Patent Application Ser. No. 62/027,510 titled “Novel RAFT Agents and Their Use in the Development of ...

Подробнее
Номер записи: 46
01-02-2018 дата публикации

DRUG COMBINATIONS COMPRISING A DGAT INHIBITOR AND A PPAR-AGONIST

Номер: US20180028660A1
Автор: Hrupka Brian Joel, LINDERS Joannes Theodorus Maria, Roevens Peter Walter Maria
Принадлежит:

The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. 6. The combination according to wherein the DGAT inhibitor is selected from:4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]hydroxyacetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;4-[4-[[2,6-dichloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;4-[4-[[2,6-dichloro-4-[[4-(methylsulfonyl)-1-piperazinyl]methyl]phenyl]acetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;4-[4-[[4-[(4-acetyl-1-piperazinyl)methyl]-2,6-dichlorophenyl]acetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;4-[4-[[2,6-dichloro-4-[(4-ethyl-1-piperazinyl)methyl]phenyl]acetyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)phenyl]-benzamide;including any stereochemically isomeric form thereof;a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof.7. The combination according to wherein the DGAT inhibitor is selected from:N4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]phenyl]-4-methoxy-benzeneacetamide;4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]-N-[[3-(1-pyrrolidinyl)phenyl]methyl]-benzamide;4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]hydroxyacetyl]-1-piperazinyl]-N-[[3-(1-pyrrolidinyl)phenyl]methyl]-benzamide;4-[4-[[2,6-dichloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]-N-[(3,5-dimethoxyphenyl)methyl]-benzamide;4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]acetyl]-1-piperazinyl]-N-[(3,5-dimethoxyphenyl)methyl]-benzamide;4-[4-[[2-chloro-4-(1-pyrrolidinylmethyl)phenyl]hydroxyacetyl]-1-piperazinyl]-N-[(3 ...

Подробнее
Номер записи: 47
29-01-2015 дата публикации

PHTHALANILATE COMPOUNDS AND METHODS OF USE

Номер: US20150031663A1
Автор: Chang Mayland, Hesek Dusan, Mobashery Shahriar
Принадлежит: University of Notre Dame du Lac

The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo. 2. The compound of wherein:{'sub': '2', 'W is absent, oxygen, —CH—, or carbonyl;'}Y is oxygen or sulfur;Z is carbon or nitrogen;{'sub': '1', 'Ris —CO2H, —CS2H, —CO2Na, or —COSH;'}{'sub': '2', 'Ris hydrogen, fluorine, chlorine, bromine, or nitro;'}{'sub': 3', '4, 'Rand Rare each independently hydrogen, fluorine, chlorine, bromine, or methyl;'}{'sub': '5', 'Ris hydrogen, fluorine, chlorine, or bromine;'}{'sub': 6', '7, 'Ris hydrogen or methyl; Ris hydrogen or chlorine;'}{'sub': '8', 'Ris absent, hydrogen, or oxygen;'}{'sub': 9', '2', '7', '3', '2', '9', '3', '2', '15', '3', '2', '3', '3', '2', '2', '2', '2', '2', '2', '3', '3, 'Ris hydrogen, chlorine, —(CH)CH, —(CH)CH, —(CH)CH, —O(CH)CH, —CHCH(OH)CHOCH(cyclopropyl); or —CHCH(OH)CHO(CH)CH;'}{'sub': 10', '2, 'Ris hydrogen, cyano, chlorine, trifluoromethyl, —CHOH, or methyl;'}{'sub': 10', '11, 'R, R, and the atoms in between form a fused 3-hydroxyphenyl; and'}{'sub': '11', 'Ris hydrogen.'}3. The compound of wherein Y is oxygen claim 1 , Z is carbon claim 1 , and Ris hydrogen.4. The compound of wherein Ris —COH or —CONa.5. The compound of wherein Ris hydrogen claim 1 , fluoro claim 1 , chloro claim 1 , bromo claim 1 , or nitro.6. The compound of wherein R claim 1 , R claim 1 , and Rare halo.7. The compound of wherein R claim 1 , R claim 1 , and Rare hydrogen.8. The compound of wherein Rand Rare each hydrogen.9. The compound of wherein —WRis —O(C-C) ...

Подробнее
Номер записи: 48
04-02-2021 дата публикации

PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS

Номер: US20210030695A1
Автор: BEAN Bruce P., Woolf Clifford J.
Принадлежит:

The invention provides compounds, compositions, methods, and kits for the treatment of neurogenic inflammation. 146-. (canceled)48. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient.49. A method of treating a neurogenic inflammatory disorder in a human patient claim 47 , the method comprising administering a therapeutically effective amount of the compound of to the patient.50. The method of claim 49 , wherein the neurogenic inflammatory disorder is selected from asthma claim 49 , rhinitis claim 49 , conjunctivitis claim 49 , arthritis claim 49 , colitis claim 49 , contact dermatitis claim 49 , pancreatitis claim 49 , chronic cough claim 49 , diabetes claim 49 , rheumatic disease claim 49 , eczema claim 49 , cystitis claim 49 , gastritis claim 49 , urethritis claim 49 , migraine headache claim 49 , psoriasis claim 49 , sinusitis claim 49 , chronic rhinosinusitis claim 49 , traumatic brain injury claim 49 , sepsis claim 49 , polymicrobial sepsis claim 49 , tendinopathy claim 49 , chronic urticaria claim 49 , rosacea claim 49 , sunburn claim 49 , inhaled tear gases claim 49 , acute lung injury claim 49 , inhalation of irritants claim 49 , inhalation of pollutants claim 49 , and exposure to chemical warfare agents.51. A kit comprising the compound of and instructions for administering the compound to a patient to treat neurogenic inflammation.53. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient.54. A method of treating a neurogenic inflammatory disorder in a human patient claim 52 , the method comprising administering a therapeutically effective amount of the compound of to the patient.55. The method of claim 54 , wherein the neurogenic inflammatory disorder is selected from asthma claim 54 , rhinitis claim 54 , conjunctivitis claim 54 , arthritis claim 54 , colitis claim 54 , contact dermatitis claim 54 , pancreatitis claim 54 , chronic cough claim 54 , diabetes claim ...

Подробнее
Номер записи: 49
11-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160037778A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butomethyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

Подробнее
Номер записи: 50
08-02-2018 дата публикации

ETHYLENEDIAMINETETRAACETIC ACID BIS(AMIDE) DERIVATIVES AND THEIR RESPECTIVE COMPLEXES WITH MN(II) ION FOR USE AS MRI CONTRAST AGENT

Номер: US20180036436A1
Автор: BARANYAI Zsolt, GARDA Zoltán, GHIANI Simona, KÁLMÁN Ferenc Krisztián, KRUSPER László, MAIOCCHI Alessandro, TIRCSÓ Gyula, TOTH Imre
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to novel substituted ethylenediaminetetraacetic acid bisamide derivatives, their complexes with Mn(II) ion and the use thereof as contrast agents for Magnetic Resonance Imaging (MRI) analysis. 2. The compound according to claim 1 , wherein n is 2.3. The compound according to claim 1 , wherein Rand Rare alkyl groups and only one of them is substituted by the carboxyl group.4. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 5 membered unsubstituted aromatic ring.5. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6-7 membered unsubstituted saturated ring.6. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6 membered saturated ring substituted by one hydroxyl and one additional moiety selected from the group consisting of methyl claim 1 , hydroxymethyl claim 1 , cyclopentylmethylene claim 1 , and cyclohexylmethylene.7. The compound according to claim 6 , wherein the methyl or hydroxymethyl moiety is at an ortho position and the hydroxyl moiety is at a meta position.8. The compound according to claim 6 , wherein the methyl or hydroxymethyl moiety is at a meta position and the hydroxyl moiety is at the other meta position or at the para position.9. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 5-6 membered saturated ring substituted by a carboxyl moiety.10. The compound according to claim 9 , wherein the carboxyl is at a meta or the para position.11. The compound according to claim 1 , wherein Rand R claim 1 , taken together with the adjacent N atom claim 1 , form a 6 membered saturated ring substituted by an aminocarbonyl moiety which is in turn substituted at the aminocarbonyl nitrogen by bis(hydroxymethyl)methyl [—CH(CHOH)] claim 1 , 2 claim 1 ,3 claim 1 ,4 claim ...

Подробнее
Номер записи: 51
11-02-2016 дата публикации

LSD1-SELECTIVE INHIBITOR HAVING LYSINE STRUCTURE

Номер: US20160039748A1
Автор: ITOH Yukihiro, KAWAHARA Masahiro, Miyata Naoki, Mizukami Tamio, OGASAWARA Daisuke, SASAKI Ryuzo, SUZUKI Takayoshi, TAKAORI Akifumi
Принадлежит:

Provided is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: 4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is any one of the following compounds:2-(N-benzenecarbonyl)amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-(N-tert-butoxycarbonyl)amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-methylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-tert-butylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-chlorobenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-fluorobenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-trifluoromethylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-{3-[(2-amino)ethylcarbamoyl]benzenecarbonylamino}-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[3-(piperazine-1-carbonyl)benzenecarbonylamino}-6-(trans-2-phenylcyclopropan-1-amino)-N-benzylhexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(4-methylbenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(4-fluorobenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(4-phenylbenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(4-tert-butylbenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(3-methylbenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(3-fluorobenzyl)hexanamide;2-[N-(4-phenylbenzenecarbonyl)]amino-6-(trans-2-phenylcyclopropan-1-amino)-N-(3- ...

Подробнее
Номер записи: 52
24-02-2022 дата публикации

AMINE-BORANES AS BIFUNCTIONAL REAGENTS FOR DIRECT AMIDATION OF CARBOXYLIC ACIDS

Номер: US20220055983A1
Автор: Hamann Henry J., Ramachandran Padinjaremadhom V.
Принадлежит: PURDUE RESEARCH FOUNDATION

The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide RCONRR. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(RCO)—B—NHRR]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated. 1. A process for direct activation and subsequent amidation of an aliphatic or an aromatic carboxylic acid to manufacture an amide RCONRR , comprising the steps of{'sup': 1', '2', '1', '2', '1', '2', '1', '2, 'sub': '3', 'a. preparing an amine-borane RRNH—NHfrom an amine RRNH; wherein Rand Rare, independently, hydrogen, an alkyl, or an aryl, wherein said alkyl or aryl are optionally substituted and said Rand Rare not both an aryl or a hydrogen at the same time;'}{'sup': 3', '3, 'b. preparing a carboxylic acid RCOOH, wherein Ris an alkyl or an aryl, each of which is optionally substituted;'}c. dissolving one equivalent of said amine-borane and about three equivalents of said carboxylic acid in xylenes or a compatible solvent to afford a reaction mixture;d. first heating said reaction mixture to about 90-100° C. for about 1 hour, then raising the temperature to about 150° C. for about 12 hours; and{'sup': 3', '1', '2', '3, 'e. resolving said reaction mixture to afford said amide RCONRRtogether with recovered excess carboxylic acid RCOOH.'}2. The process according to claim 1 , wherein said optionally substituted alkyl or aryl may comprises one or more heteroatoms selected from the group consisting of B claim 1 , N claim 1 , O claim 1 , S claim 1 , Se claim 1 , Cl claim 1 , Br claim 1 , F claim 1 , I claim 1 , Si claim 1 , As claim 1 , Te claim ...

Подробнее
Номер записи: 53
18-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160044919A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butometyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

Подробнее
Номер записи: 54
18-02-2016 дата публикации

N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES

Номер: US20160046570A1
Автор: BROOKFIELD Frederick Arthur, COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Sutton Art, Toscano John P.
Принадлежит:

The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. 2. The compound of claim 1 , wherein L is —SO—.3. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or more substituents independently selected from W.4. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or two substituents independently selected from W.5. The compound of claim 1 , wherein Y is phenyl and said phenyl is unsubstituted or substituted with one or more substituents independently selected from W.6. The compound of claim 1 , wherein W is halo or —SO.7. The compound of claim 1 , wherein W is chloro claim 1 , bromo or —SO.8. The compound of claim 1 , wherein R is alkyl or phenyl claim 1 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more halos.9. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more substituents independently selected from W.10. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more halos.11. The compound of claim 9 , wherein R is alkyl or phenyl claim 9 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more substituents independently selected from halo claim 9 , nitro claim 9 , alkylsulfonyl and trihalomethyl.12. The compound of claim 1 , wherein the ...

Подробнее
Номер записи: 55
16-02-2017 дата публикации

Novel Prodrugs And Methods Of Use Thereof

Номер: US20170044191A1
Автор: Ackerley David Francis, ASHOORZADEH AMIR, Copp Janine Naomi, Guise Christopher Paul, Mowday Alexandra Marie, PATTERSON ADAM VORN, Smaill Jeffrey Bruce, Williams Elsie May
Принадлежит:

The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds. 115-. (canceled)17. A compound of formula (I) according to claim 16 ,whereinW represents Br or I,{'sub': '2', 'X represents Br or OSOMe,'}R is methyl or ethyl, and{'sub': '1', 'Rrepresents a methyl, ethyl, propyl or isopropyl group.'}18. A compound of formula (I) as claimed in claim 16 , being a pharmaceutically acceptable salt of said compound claim 16 , wherein said salt is a methanesulfonate salt.20. A compound of formula (Ih) according to claim 19 , wherein X represents OSOMe.25. A compound of formula (Ii) according to claim 24 , wherein Rrepresents methyl or ethyl.27. A compound of formula (I) according to claim 16 , wherein the compound is selected from the group consisting of:2-(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-N-methyl-2-nitrobenzamido)ethyl dihydrogen phosphate,3-(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-N-methyl-2-nitrobenzamido)propyl dihydrogen phosphate,5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-N-(2-hydroxyethyl)-N-methyl-2-nitrobenzamide,5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-N-(3-hydroxypropyl)-N-methyl-2-nitrobenzamide,(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl) (4-methylpiperazin-1-yl)methanone,(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl) (4-ethylpiperazin-1-yl)methanone,(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl) (4-isopropylpiperazin-1-yl)methanone,(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl) (4-methylpiperazin-1-yl)methanone,(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl) (4-ethylpiperazin-1-yl)methanone,(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl) (4-isopropylpiperazin-1-yl ...

Подробнее
Номер записи: 56
13-02-2020 дата публикации

FATTY ACID ACETYLATED SALICYLATES AND THEIR USES

Номер: US20200046738A1
Автор: Bemis Jean E., Jirousek Michael R., Milne Jill C., Smith Jesse J.
Принадлежит:

The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative. 2. The method of claim 1 , wherein Wis NH.5. The method of claim 1 , wherein Q is Z.7. The method of claim 1 , wherein Q is Z and Z is H.8. The method of claim 1 , wherein two of n claim 1 , o claim 1 , p claim 1 , and q are each 1.12. The method of claim 11 , wherein Wis NH.15. The method of claim 11 , wherein Q is Z.16. (canceled)17. The method of claim 11 , wherein Q is Z and Z is H.18. The method of claim 11 , wherein two of n claim 11 , o claim 11 , p claim 11 , and q are each 1.2230-. (canceled) This application is a continuation of U.S. patent application Ser. No. 15/839,346, filed Dec. 12, 2017, which is a continuation of U.S. patent application Ser. No. 15/283,995, filed Oct. 3, 2016, which is a continuation of U.S. patent application Ser. No. 14/251,247, filed Apr. 11, 2014, now U.S. Pat. No. 9,458,094, which is a continuation of U.S. patent application Ser. No. 13/427,650, filed Mar. 22, 2012, now U.S. Pat. No. 8,735,379, which is a divisional of U.S. patent application Ser. No. 12/499,779 filed Jul. 8, 2009, now U.S. Pat. No. 8,173,831, which claims priority to and the benefit of U.S. Provisional Application No. 61/148,658, filed Jan. 30, 2009, U.S. Provisional Application No. 61/104,363, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,364, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,366, filed Oct. 10, 2008, and U.S. Provisional Application No. 61/078,983, filed Jul. 8, 2008. The entire disclosures of those applications are relied on and incorporated into this application by reference.The invention relates to Fatty Acid Acetylated Salicylate Derivatives, Fatty Acid Acetylated Diflunisal Derivatives ...

Подробнее
Номер записи: 57
25-02-2016 дата публикации

Novel Intermediate Used for Preparing Tapentadol or Analogues Thereof

Номер: US20160052866A1
Автор: LI DEGANG, LI XIAOXIANG, XU ZIAO, ZHAO YUANHAI
Принадлежит:

The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production. 2. The compound according to claim 1 , wherein Ris selected from Cl claim 1 , methyl claim 1 , OH hydroxy claim 1 , NHamino or methoxy.3. The compound according to claim 1 , characterized in that Y is selected from OR claim 1 , wherein Ris selected from methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl.4. The compound according to claim 1 , characterized in that Y is selected from NRR claim 1 , wherein R claim 1 , Rand N form substituted or unsubstituted saturated nitrogen-containing heteorcyclyl containing oxygen or not jointly.5. The compound according to claim 4 , wherein R claim 4 , Rand N form tetrahydropyrrole ring claim 4 , piperidine ring claim 4 , 4-methylpiperidine ring claim 4 , morpholine ring claim 4 , methylpiperazine ring or 4-hydroxypiperidine jointly.6. The compound according to claim 1 , selected from the following compounds:valeryl 2-methyl-3-(3-methoxyphenyl)chloride;methyl 2-methyl-3-(3-methoxyphenyl)sulfovalerate;methyl 2-methyl-3-(3-hydroxyphenyl)sulfovalerate;2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-methoxyphenyl)sulfovaleramide;N,N-dimethyl-2-methyl-3-(3-hydroxyphenyl)sulfovaleramide;N,N-diethyl-2-methyl-3-(3-methoxyphenyl)valeramide;3-(3-methoxyphenyl)-2-methyl-1-(piperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-(4-methylpiperidin-1-yl)pentan-1-one;3-(3-methoxyphenyl)-2-methyl-1-( ...

Подробнее
Номер записи: 58
12-03-2015 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20150072984A1
Автор: Qian Xiangping
Принадлежит:

Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. 2. At least one chemical entity of wherein Ris chosen from hydrogen claim 1 , optionally substituted alkyl claim 1 , optionally substituted cycloalkyl claim 1 , and optionally substituted heterocycloalkyl.3. At least one chemical entity of wherein Ris chosen from optionally substituted alkyl claim 1 , optionally substituted cycloalkyl claim 1 , and optionally substituted heterocycloalkyl.4. At least one chemical entity of wherein Rand Rare independently chosen from optionally substituted alkyl.5. At least one chemical entity of wherein Rand Rare joined together to form an optionally substituted 4- to 8-membered heterocycloalkyl ring.6. At least one chemical entity of wherein Rand Rare joined together to form an optionally substituted pyrrolidin-1-yl claim 5 , morpholin-1-yl claim 5 , piperidin-1-yl claim 5 , piperazin-1-yl claim 5 , 1 claim 5 ,4-diazepan-1-yl claim 5 , and 1 claim 5 ,4-diazocan-1-yl.7. At least one chemical entity of any one of to wherein Ris chosen from hydrogen claim 5 , optionally substituted alkyl claim 5 , optionally substituted cycloalkyl claim 5 , optionally substituted heterocycloalkyl claim 5 , optionally substituted aryl claim 5 , optionally substituted heteroaryl claim 5 , optionally substituted aminocarbonyl claim 5 , and optionally substituted phosphato.8. At least one chemical entity of wherein Ris chosen from hydrogen claim 7 , optionally substituted lower alkyl claim 7 , and optionally substituted aminocarbonyl.9. At least one chemical entity of wherein Ris hydrogen.10. At least one chemical entity of wherein Ris optionally substituted lower alkyl.11. At least one chemical entity of wherein Ris methyl.12. At least one chemical entity of wherein Ris lower alkyl substituted with hydroxyl or amino.13. At least one chemical entity of wherein Ris optionally substituted aminocarbonyl.14. At least one chemical ...

Подробнее
Номер записи: 59
24-03-2022 дата публикации

High-throughput method to rapidly add chemical moieties to a small molecule library

Номер: US20220089537A1
Автор: Angela N. Koehler, Brice CURTIN, Catherine HENRY, Chia-Fu Chang, Christina Woo, Jasmin KRUELL, Sebastian POMPLUN
Принадлежит: Harvard College, Massachusetts Institute of Technology

Organic compounds for target identification, drug discovery, chemical library production, high-throughput screening, fluorophore conjugation, chemiluminescent compound conjugation, creation of proximity induced modulators (e.g., protein degraders)/chimeric molecules, or a combination thereof are described. The compounds can contain small molecule moieties for identification of their potential targets; an isocyanate, photoactivatable groups; chemical moieties for enrichment and detection of target-small molecule moiety interactions; proximity induced modulator element; fluorophores; chemiluminescent groups; or combinations thereof.

Подробнее
Номер записи: 60
07-03-2019 дата публикации

Octahydroanthracene Compound, Preparation Method and Application Thereof

Номер: US20190071393A1
Автор: BAO Xuefei, CHEN Guoliang, FANG Wuhong, GAO Jinheng, REN Fulong, YUAN Chunling, ZHANG Daiming, ZHENG Zhonghui, ZHOU Linbo, ZOU Libo
Принадлежит:

An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound. 2. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , whereinthe Linker is a substituted/unsubstituted phenyl group, pyridine, furan, pyrrole, thiazole or thiophene; wherein a substituent of the substituted phenyl group, pyridine, furan, pyrrole, thiazole or thiophene is a C1-C6 alkyl group or a C1-C6 alkoxy group.3. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , wherein the nitrogen-free structural fragment is C1-C10 alkyl group.5. The octahydroanthracene compound and the pharmaceutically acceptable salts of the octahydroanthracene compound of claim 1 , wherein X is hydrogen claim 1 , methyl or ethyl.6. An octahydroanthracene compound and pharmaceutically acceptable salts of the octahydroanthracene compound claim 1 , selecting from:4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] methyl benzoate;4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzoic acid;N-hydroxy-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N-(2-aminophenyl)-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4 5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N[2-(N,N-diethylamino)]ethyl-4-[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5,6,7,8-octahydro-9-anthryl) carbamoyl] benzamide;N-(2-amino) ethyl -4[(1,1,4,4,5,5,8,8-octamethyl-1,2,3,4,5 ...

Подробнее
Номер записи: 61
07-03-2019 дата публикации

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

Номер: US20190071395A1
Автор: CHOI YongSeok, GOO Ja-Il, HAN Hyo-Kyung, Kim Jae-Hong, KWON Jinsun, LEE Kyeong, WEI Jun Dong
Принадлежит:

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases. 3. The method of claim 1 , wherein the compound represented by Formula 1 is selected from the group consisting of:tert-butyl 4-(4-(3-(N-phenylpentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-phenyl-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-methylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-ethylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isopropylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(2-hydroxyethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-cyclohexylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclohexylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isobutylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-phenyl-N-(3-(4-(4-(prop-2-ynyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-cyanopiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;tert-butyl 4-(4-(3-(N-(3-fluorophenyl)pentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-(3-fluorophenyl)-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-fluorophenyl)-N-( ...

Подробнее
Номер записи: 62
15-03-2018 дата публикации

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Номер: US20180072997A1
Автор: Belema Makonen, Bender John A., Beno Brett R., Fridell Robert A., Lopez Omar D., Meanwell Nicholas A., Nguyen Van N., Thangathirupathy Srinivasan, Wang Alan Xiangdong, Wang Gan, Yang Zhong
Принадлежит:

Compounds of Formulas I-VI, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth. Formula I is exemplified below: 2. The compound of wherein A is a bond.4. The compound of wherein A is selected from C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , aryl claim 1 , C-Ccycloalkyl claim 1 , C-Cbicycloalkyl claim 1 , —CO— claim 1 , —CS— claim 1 , —C(═N—CN)— claim 1 , heterocyclyl claim 1 , nitrogen claim 1 , sulfur claim 1 , oxygen claim 1 , —O—(C-Calkyl)-O— claim 1 , —N(R)CON(R)— claim 1 , and ferrocene.5. The compound of wherein at least one of X and Xare a bond.8. The compound as claimed in claim 7 , wherein A is selected from C-Calkyl claim 7 , C-Calkenyl claim 7 , aryl with 1 to 2 rings claim 7 , C-Ccycloalkyl claim 7 , —CO— claim 7 , heterocyclyl with 1 to 2 rings claim 7 , nitrogen claim 7 , sulfur claim 7 , oxygen claim 7 , —O—(C-Calkyl)-O— claim 7 , —N(R)CON(R)— claim 7 , and ferrocene;{'sup': 1', 'y', 'xa', 'xa', 'xa', 'xa, 'sub': 1', '4', '2', '3', '1', '2', '1', '2', '1', '2', '1', '4', '1', '4', '2', '2', '2', '1', '4', '2', '2', '2', '2, 'each Ris independently selected from hydrogen, C-Calkyl, C-Calkenyl, C-Calkoxy, aryl, carboxylic acid, cyano, halogen, C-Chaloalkyl, C-Chaloalkoxy, heterocyclyl, hydroxy, C-Chydroxyalkyl, —CO—(C-Calkyl), CO(R), —CON(R), —NHCON(R), —SO—(C-Calkyl), —SO—N(R), —SO-heterocyclyl, and —N(R);'}p is from 0 to 4;{'sup': 4', '4, 'sub': 1', '3', '1', '2, 'each Ris independently selected from hydrogen, C-Calkyl, aryl(C-Calkyl), hydroxyl, or halogen with the option for two “R”s on the same or adjacent carbon(s) to form a ring; and'}n is from 0 to 2.9. The compound as claimed in claim 8 , wherein A is selected from C-Calkyl claim 8 , C-Calkenyl claim 8 , aryl with 1 to 2 rings claim 8 , C-Ccycloalkyl claim 8 , —CO— claim 8 , heterocyclyl with 1 to 2 rings claim 8 , nitrogen claim 8 , oxygen claim 8 , —O—(C-Calkyl)-O— claim 8 , ...

Подробнее
Номер записи: 63
19-03-2015 дата публикации

Compounds, Compositions, and Methods For Modulating Ferroptosis and Treating Excitotoxic Disorders

Номер: US20150079035A1
Автор: Brent R. Stockwell, Rachid Skouta, Scott J. Dixon
Принадлежит: Columbia University of New York

The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

Подробнее
Номер записи: 64
12-06-2014 дата публикации

ENZYME INHIBITORS

Номер: US20140163042A1
Автор: Baker Kenneth William John, Davidson Alan Hornsby, Davies Stephen John, Donald Alastair David Graham, Drummond Alan Hastings, Mazzei Francesca Ann, Moffat David Festus Charles, Patel Sanjay Ratilal
Принадлежит: Chroma Therapeutics Ltd.

Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein Ris a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; Ris the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O), —S(═O)—, —C(═O)O—, —C(O)NR—, —C(═S)—NR, —C(═NH)NRor —S(═O)NR— wherein Ris hydrogen or optionally substituted C-Calkyl; Lis a divalent radical of formula -(Alk)(Q)(Alk)- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X-Q- or -Q-X— wherein Xis —O—, S— or NR— wherein Ris hydrogen or optionally substituted C-Calkyl, and Qis an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, Alkand Alkindependently represent optionally substituted divalent C-Ccycloalkyl radicals, or optionally substituted straight or branched, C-Calkylene, C-Calkenylene, or C-Calkynylene radicals which may optionally contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR—) link wherein Ris hydrogen or optionally substituted C-Calkyl; Xrepresents a bond; —C(═O); or —S(═O)—; —NRC(═O)—, —C(═O)NR—, —NRC(═O)NR—, —NRS(═O)—, or —S(═O)NR— wherein Rand Rare independently hydrogen or optionally substituted C-Calkyl; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals RRNH—Y-L-X-[CH]— and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONIIOII, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the ...

Подробнее
Номер записи: 65
21-03-2019 дата публикации

PHARMACOLOGICALLY ACTIVE COMPOUNDS

Номер: US20190084993A1
Автор: "ONeill Paul M.", BERRY Neil, Leuwer Martin, Pidathala Chandrakala
Принадлежит: THE UNIVERSITY OF LIVERPOOL

The present invention relates to compounds of formula I shown below: 2. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen claim 1 , fluoro or methyl; or Rand Rare linked such that together they form a 4 or 5 membered carbocyclic or heterocyclic ring.3. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare all hydrogen; or Rand Rare linked such that together they form a 4 or 5 membered heterocyclic ring.4. A compound according to claim 1 , wherein one or two of R claim 1 , R claim 1 , Rand Ris a substituent other than hydrogen.5. A compound according to claim 1 , wherein Rand Rare hydrogen and one of Rand Ris fluoro.618-. (canceled)19. A compound according to claim 1 , which is selected from any one of the following:(3-fluoroazetidin-1-yl)(4-hydroxy-3,5-diisopropylphenyl) methanone; and(4-Hydroxy-3,5-diisopropylphenyl)(2-oxa-6-azaspiro[3.3]heptan-6-yl)methanone;or a pharmaceutically acceptable salt or solvate thereof.20. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in admixture with a pharmaceutically acceptable diluent or carrier.2123-. (canceled)24. A method of treating chronic pain or inducing anaesthesia in a patient in need of such treatment claim 1 , said method comprising administering to said patient a therapeutically effective amount of a compound according to .26. A pharmaceutical composition comprising a compound according to claim 19 , or a pharmaceutically acceptable salt thereof claim 19 , in admixture with a pharmaceutically acceptable diluent or carrier.27. A method of treating chronic pain or inducing anaesthesia in a patient in need of such treatment claim 19 , said method comprising administering to said patient a therapeutically effective amount of a compound according to . This application is a continuation of U.S. application Ser. No. 15/587,068, filed May 4, 2017, which is ...

Подробнее
Номер записи: 66
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171308A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

Подробнее
Номер записи: 67
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171313A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

Подробнее
Номер записи: 68
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171314A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

Подробнее
Номер записи: 69
14-04-2016 дата публикации

METHODS AND COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS AND VIRAL INFECTIONS

Номер: US20160102051A1
Автор: Kinsella B. Therese, Reid Helen
Принадлежит:

The invention generally relates to methods and compounds for treating proliferative disorders, viral infections, or both. In some embodiments, the invention provides an anticancer or antiviral compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating a proliferative disorder or a viral infection including administering an anticancer or antiviral compound that binds to a thromboxane receptor, has preferential binding for either TPalpha (TPα) or TPbeta (TPβ) receptor subtype. 6. (canceled)10. An anticancer compound that specifically binds to a thromboxane receptor and has preferential binding for either TP-alpha or TP-beta receptor subtype.11. The anticancer compound of further comprising:a substituted nitro phenoxy phenyl;a sulfonylurea; andan alkyl group, wherein the alkyl group is selected from the list consisting of: an isopropyl group, a pentyl group, a tert-butyl group, and a cyclohexyl group.12. A method of treating cancer comprising administering an anticancer compound claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein the anticancer compound or the salt thereof binds preferentially to a thromboxane receptor and has preferential binding for either TP-alpha or TP-beta receptor subtype.13. The method of wherein the cancer is one selected from the list consisting of non-Hodgkin's lymphoma claim 12 , colorectal claim 12 , prostate claim 12 , ovary claim 12 , breast claim 12 , pancreatic claim 12 , bladder claim 12 , colon claim 12 , and ovarian cancer.14. The method of wherein the anticancer compound comprises:a substituted nitro phenoxy phenyl;a sulfonylurea; andan alkyl group, wherein the alkyl group is selected from the list consisting of: an isopropyl group, a pentyl group, a tert-butyl group, and a cyclohexyl group.20. (canceled)2446-. (canceled) This application claims priority to, and the benefit of, U.S. Provisional Application Nos. 61 ...

Подробнее
Номер записи: 70
26-06-2014 дата публикации

METHODS FOR TREATING COGNITIVE DISORDERS USING 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS

Номер: US20140179925A1
Автор: Donello John E., Luhrs Lauren M., Schweighoffer Fabien J.
Принадлежит: ALLERGAN, INC.

Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 2. The use of claim 1 , wherein the sum of the integers m claim 1 , n and q is 3.3. The use of claim 2 , wherein one of the W claim 2 , X and Y groups is N.4. The use of claim 3 , wherein Rand Rtogether with the atoms to which they are attached jointly form a carbocyclic or a heterocyclic ring.5. The use of claim 2 , wherein none of the W claim 2 , X and Y groups is a heteroatom.6. The use of wherein Rand Rtogether with the atoms to which they are attached jointly form a carbocyclic or a heterocyclic ring.7. The use of claim 1 , wherein the sum of the integers m claim 1 , n and q is 2 and at least one of W claim 1 , X and Y is a heteroatom.8. The use of claim 7 , wherein only one of W claim 7 , X and Y represents a heteroatom.9. The use of claim 7 , wherein two of the W claim 7 , X and Y groups each represent an independently selected heteroatom.10. The use of claim 1 , wherein Ris H.11. The use of claim 10 , wherein both Rgroups are H.12. The use of claim 10 , wherein one Rgroup is H and the other Rgroup is CO—Ror alkyl of 1 to 20 carbons.13. The use of claim 10 , wherein Ris independently selected from H and alkyl of 1 to 10 carbons.14. The use of claim 1 , wherein Ris CO—R.15. The use of claim 1 , wherein Rand Rtogether with the nitrogen form a 4 claim 1 , 5 claim 1 , 6 or 7 membered ring.16. The use of claim 15 , wherein Rand Rtogether with the nitrogen form a 5 membered ring.17. The use of claim 15 , wherein Rand Rtogether with the nitrogen form a 6 membered ring.18. The use of claim 1 , wherein both Rand Rare hydrogen.20. The use of claim 19 , wherein Ris H.21. The use of claim 19 , wherein both Rgroups are H.22. The use of claim 19 , wherein both Rand Rare hydrogen.24. The use of claim 23 , wherein Ris H.25. The use of claim 23 , wherein both Rgroups are H.29. The use of claim 28 , wherein the sum of the integers m claim 28 , n and q is 3 ...

Подробнее
Номер записи: 71
03-07-2014 дата публикации

ANTI-AMYLOID COMPOUNDS AND METHODS

Номер: US20140187556A1
Автор: Banfield Scott C., BARDEN Christopher J., Reed Mark A., YADAV Arun
Принадлежит: Treventis Corporation

Anti-amyloid compounds are provided along with methods of use thereof. 2. The compound of in which the compound is according to Formula Ia.3. The compound of in which the compound is according to Formula Ib.4. The compound of in which the compound is according to Formula Ic.5. The compound of in which the compound is according to Formula Id.6. The compound of in which the compound is according to Formula Ie.7. The compound of in which the compound is according to Formula If.8. The compound of in which E is carbon.9. The compound of in which E is nitrogen.10. The compound of in which Ris nitro and Ris selected from the group consisting of ethanol-1-yl claim 3 , methanol claim 3 , 2 claim 3 ,2 claim 3 ,2-trifluoro-1-hydroxyethanol-1-yl claim 3 , and 2 claim 3 ,2 claim 3 ,2-trifluoroethanol-1-yl.11. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethanol.12. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethane-1 claim 10 ,1-diol.13. The compound of in which Ris nitro and Ris C-linked tetrazole.14. The compound of in which Ris nitro.15. The compound of in which Ris selected from the group consisting of sulfonamide claim 14 , alkylamide claim 14 , dialkylamide claim 14 , benzyl alkylamide claim 14 , N-pyrrolidinamide claim 14 , (N′-methanonylpiperazine)amide claim 14 , (N′-methylpiperazine)amide claim 14 , morphilinamide claim 14 , and piperidineamide.16. The compound of claim 1 , wherein compound inhibits the aggregation of an amyloidogenic protein.17. The compound of for use in the preparation of a pharmaceutically effective dosage form the treatment of amyloid diseases.18. The compound of claim 16 , wherein said amyloid disease is selected from the group consisting of Alzheimer's disease claim 16 , Parkinson's disease claim 16 , Huntington's disease claim 16 , and prion diseases.19. A ...

Подробнее
Номер записи: 72
10-07-2014 дата публикации

PYRUVATE KINASE ACTIVATORS FOR USE IN THERAPY

Номер: US20140194402A1
Автор: Su Shin-San M.
Принадлежит: AGIOS PHARMACEUTICALS, INC

Described herein are methods for using compounds that activate pyruvate kinase. 2. The method of claim 1 , wherein the compound is added directly to whole blood or packed cells extracorporeally.3. The method of claim 1 , wherein the pharmaceutical composition is administered to a subject in need thereof.4. A method for regulating 2 claim 1 ,3-diphosphoglycerate levels in blood in need thereof comprising contacting blood an effective amount of (1) a compound of formula I or a pharmaceutically acceptable salt thereof; (2) a composition comprising a compound of formula I or a salt thereof claim 1 , and a carrier or (3) a pharmaceutically acceptable composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier; wherein formula I is as defined in .5. A method for treating hereditary non-spherocytic hemolytic anemia comprising administering to a subject in need thereof a therapeutically effective amount of an effective amount of (1) a compound of formula II or a pharmaceutically acceptable salt thereof; or (2) a pharmaceutically acceptable composition comprising a compound of formula II or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier; wherein formula II is as defined in .6. A method for treating sickle cell anemia comprising administering to a subject in need thereof a therapeutically effective amount of an effective amount of (1) a compound of formula I or a pharmaceutically acceptable salt thereof; or (2) a pharmaceutically acceptable composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier; wherein formula I is as defined in .8. The method of claim 7 , wherein h is 1 and g is 1.9. The method of claim 8 , wherein W claim 8 , X claim 8 , Y and Z are CH.10. The method of claim 9 , wherein D is NRand Dis a bond.11. The method of claim 10 , wherein Ris H ...

Подробнее
Номер записи: 73
09-06-2022 дата публикации

PREPARING METHOD OF COMPOUNDS INCLUDING AMIDE GROUP FROM TERTIARY AMINE

Номер: US20220177416A1
Автор: Lee Hyoyoung, LEE Seungeun, VASIMALLA Suresh
Принадлежит:

Provided is a preparing method of an amide directly from a tertiary amine by using a reduced titanium dioxide (Blue TiO), which is formed by mixing a titanium dioxide having an anatase phase and a rutile phase with a reducing agent and selectively reducing any one of the anatase phase and the rutile phase, as a photocatalyst. 1. A preparing method of a compound including an amide group , comprising:{'sub': '2', 'a process of forming a reduced titanium dioxide which is formed by mixing a titanium dioxide (TiO) having an anatase phase and a rutile phase with a reducing agent and selectively reducing any one of the anatase phase and the rutile phase; and'}a process of preparing a compound including an amide group by reacting a tertiary amine in the presence of the reduced titanium dioxide.2. The preparing method of a compound including an amide group according to claim 1 , wherein the process of preparing a compound including an amide group by reacting a tertiary amine in the presence of the reduced titanium dioxide includes a process of reacting the tertiary amine with a compound including an aldehyde group.3. The preparing method of a compound including an amide group according to claim 1 , wherein the process of preparing a compound including an amide group by reacting a tertiary amine in the presence of the reduced titanium dioxide includes a process of irradiating light and performing a reaction using the reduced titanium dioxide as a photocatalyst.4. The preparing method of a compound including an amide group according to claim 1 , wherein the process of preparing a compound including an amide group by reacting a tertiary amine in the presence of the reduced titanium dioxide includes a process of adding an electron acceptor.5. The preparing method of a compound including an amide group according to claim 4 , wherein the electron acceptor includes hydrogen peroxide (HO) claim 4 , tert-Butyl hydroperoxide (TBHP) claim 4 , dioxane claim 4 , ammonium persulfate ((NH) ...

Подробнее
Номер записи: 74
27-04-2017 дата публикации

NOVEL ORGANOSELENIUM COMPOUNDS, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL USES THEREOF IN PARTICULAR AS ANTITUMOR AGENTS

Номер: US20170114011A1
Автор: Erdelmeier Irene, LEBEL Rémi, MOUTET Marc, YADAN Jean-Claude
Принадлежит:

The invention relates to a selenium compound. Said selenium compound has formula (I), where R=alkyl; R=H, RC(=0), ROC(=0), a-aminoacyl, CHSeCHCHCH(NH)C(=0), CHSeCHCHCH(OH)C(=0); X=OH, OR, NH, NRR, α-amino acid, CHSeCHCHCH(COOH)NH—, CHSeCHCHCH(COOH)0-; R=alkyl; R=alkyl, aryl; R=H, alkyl, aryl; Rand Rwhich can together form a 5- or 6-membered cycloalkyl radical which can comprise a heteroatom; provided that when X=NH-terbutyl, R≠C(=0)CH. Said compound can be used as a pharmaceutical substance, in particular as an antitumour substance. 2. The selenium compound according to claim 1 , wherein Rrepresents a methyl claim 1 , ethyl claim 1 , allyl group.3. The selenium compound according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , α-aminoacyls claim 1 , R(C═O) claim 1 , RO(C═O) claim 1 , CHSeCHCHCH(OH)C(═O).4. The selenium compound according to claim 1 , wherein X is selected from the group OH claim 1 , α-amino acid claim 1 , CHSeCHCHCH(COOH)NH— claim 1 , CHSeCHCHCH(COOH)O—.5. The selenium compound according to claim 1 , wherein Rrepresents a methyl claim 1 , ethyl claim 1 , allyl group; Rrepresents R(C═O) claim 1 , RO(C═O) claim 1 , and X represents OH or OR.6. The selenium compound according to claim 1 , wherein the pharmaceutically acceptable acids are selected from the mineral acids such as hydrochloric claim 1 , hydrobromic claim 1 , hydroiodic claim 1 , sulfuric claim 1 , tartaric claim 1 , phosphoric acids; or selected from the organic acids such as formic claim 1 , acetic claim 1 , trifluoroacetic claim 1 , propionic claim 1 , benzoic claim 1 , maleic claim 1 , fumaric claim 1 , succinic claim 1 , citric claim 1 , oxalic claim 1 , glyoxylic claim 1 , aspartic acids claim 1 , alkanesulfonic acids such as methanesulfonic claim 1 , trifluoromethanesulfonic claim 1 , ethanesulfonic claim 1 , arylsulfonic acids such as benzene- and paratoluenesulfonic acids.7. The selenium compound according to claim 1 , wherein the pharmaceutically ...

Подробнее
Номер записи: 75
13-05-2021 дата публикации

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

Номер: US20210137901A1
Автор: Boyer Angelique Sun, Evdokimov Artem G., Greis Kenneth D., Kawamoto Richard Masaru, Warshakoon Namal C., Wu Shengde
Принадлежит:

The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. 132.-. (canceled)36. The process of claim 33 , wherein the catalyst is [1 claim 33 ,1′-bis (diphenylphosphino)ferrocine]dichloro palladium(II).37. The process of claim 33 , wherein the reaction is conducted in the presence of a base that is KPO.38. The process of claim 34 , wherein the coupling reagents in step (c) are 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 1-hydroxybenzotriazole (HOBt).39. The process of claim 34 , wherein the catalyst in step (d) is Pd/C.42. The process of claim 40 , wherein the catalyst in step (a) is [1 claim 40 ,1-bis (diphenylphosphino)ferrocine]dichloro palladium(II).43. The process of claim 40 , wherein the reaction in step (a) is conducted in the presence of a base that is KPO.44. The process of claim 40 , wherein the coupling reagents in step (c) are 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 1-hydroxybenzotriazole (HOBt). This application is a Continuation Application of Ser. No. 14/854,080, filed Sep. 15, 2015, now U.S. Pat. No. 9,598,370, which is a Continuation Application of U.S. application Ser. No. 14/568,200, filed on Dec. 12, 2014, which is a Continuation Application of U.S. application Ser. No. 14/062,011, filed Oct. 24, 2013, now U.S. Pat. No. 8,940,773, which is a Divisional Application of U.S. application Ser. No. 13/681,876, filed on Nov. 20, 2012, now U.S. Pat. No. 8,598,210, which is a Continuation of U.S. application Ser. No. 12/860,073, filed on Aug. 20, 2010, now U.S. Pat. No. 8,343,952, which is a Continuation Application of U.S. application Ser. No. 11/821,936, filed Jun. 26, 2007, now U.S. Pat. No. 7,811,595, which claims the benefit of Provisional Application Ser. No. 60/816,522 filed ...

Подробнее
Номер записи: 76
07-05-2015 дата публикации

PROCESS FOR PREPARATION OF N,N-DI SUBSTITUTED CARBOXAMIDES

Номер: US20150126734A1
Автор: Ganesan Kumaran, Rao Ambati Narasimha, Vijayaraghavan Rajagopalan
Принадлежит: DIRECTOR GENERAL, DEFENCE RESEARCH & DEVELOPMENT ORGNISATION

The present disclosure relates to a single pot process for preparation of a N,N-di substituted carboxamide compounds of formula (I), said process comprising: reacting a carboxylic acid with a di-substituted carbamoyl chloride in presence of an organic tertiary base to obtain the N,N-di substituted carboxamide compounds of formula (I). 2. The process as claimed in claim 1 , wherein the carboxylic acid is an aromatic or an aliphatic carboxylic acid selected from the group consisting of phenyl acetic acid claim 1 , 3-methyl benzoic acid claim 1 , benzoic acid claim 1 , morpholine 4-carboxylic acid claim 1 , nicotinic acid claim 1 , propionic acid claim 1 , butanoic acid claim 1 , pentanoic acid claim 1 , octanoic acid claim 1 , hexadecanoic acid claim 1 , or octadecanoic acid.3. The process as claimed in claim 1 , wherein the di-substituted carbomyl chloride is sleeted from the group consisting of N claim 1 ,N-dimethyl carbamoyl chloride claim 1 , N claim 1 ,N-diethyl carbomyl chloride claim 1 , N claim 1 ,N-dibutyl carbomyl chloride claim 1 , N-methyl-N-ethyl carbomyl chloride claim 1 , and N-propyl-N-ethyl carbomyl chloride.4. The process as claimed in claim 1 , wherein the organic tertiary base is selected from the group consisting of triethylamine claim 1 , tributylamine claim 1 , 1-methyl imidazole claim 1 , pyridine claim 1 , piperidine claim 1 , N-methyl pyrrolidine claim 1 , N-methyl pyrrole claim 1 , N-methyl piperidine and 4-methyl morpholine.5. The process a claimed in claim 1 , said process comprising:reacting phenyl acetic acid with N,N-diethyl carbamoyl chloride in presence of 1-methylimidazole for a time period in the range of 25 to 35 minutes, and at a temperature in the range of 10° C. to 50° C. to obtain N,N-diethyl-2-phenyl acetamide.6. The process a claimed in claim 1 , said process comprising:reacting 3-methyl benzoic acid with N,N-diethyl carbamoyl chloride in presence of triethylamine for a time period in the range of 15 to 25 minutes, and at a ...

Подробнее
Номер записи: 77
25-04-2019 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

Номер: US20190119202A1
Автор: Anderson Eric, Jiang Xin, Visnick Melean
Принадлежит:

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 1264-. (canceled)267. The method of claim 266 , wherein Ris hydrogen.268. The method of claim 266 , wherein Ris alkylor substituted alkyl.269. The method of claim 266 , wherein Ris arylor substituted aryl.270. The method of claim 266 , wherein Ris alkylor substituted alkyl.271. The method of claim 266 , where Rand Rare taken together and are -alkanediyl- or substituted —alkanediyl-.272. The method of claim 266 , where Rand Rare taken together and are —N═CHCH═CH—.274. The method of claim 273 , wherein Ris hydrogen.275. The method of claim 273 , wherein Ris alkylor substituted alkyl.276. The method of claim 273 , wherein Ris arylor substituted aryl.277. The method of claim 273 , wherein Ris alkylor substituted alkyl.278. The method of claim 273 , where Rand Rare taken together and are -alkanediyl- or substituted —alkanediyl-.279. The method of claim 273 , where Rand Rare taken together and are —N═CHCH═CH—.281. The method of claim 265 , wherein the modification is conducted in the absence of a solvent (i.e. neat).282. The method of claim 265 , wherein the modification is conducted in a medium comprising a solvent.283. The method of claim 282 , wherein the solvent is tetrahydrofuran claim 282 , benzene claim 282 , or dichloromethane.284. The method of claim 265 , wherein the modification is conducted in the presence of a base.285. The method of claim 284 , wherein the base is NEtor NaH. The present application is a continuation of U.S. patent application Ser. No. 15/615,393, filed Jun. 6, 2017, which is a continuation of U.S. patent application Ser. No. 14/753,297, filed Jun. 29, 2015, now U.S. Pat. No. 9,670,147, which is a continuation of U.S. patent spplication Ser. No. 13/861,208, filed Apr. 11, 2013, now U.S. Pat. No. 9,102,681, which is a continuation of U.S. patent application Ser. No. 13/356,455, filed on Jan. 23, 2012, now U.S. Pat. No. 8,440,854, which is a ...

Подробнее
Номер записи: 78
17-05-2018 дата публикации

QUINONE COMPOUNDS FOR TREATING APE1 MEDIATED DISEASES

Номер: US20180133175A1
Автор: KELLEY Mark R., Wikel James H.
Принадлежит:

The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases. 129.-. (canceled)31. The compound of claim 30 , wherein R is methyl.32. The compound of claim 30 , wherein R is methoxy.33. The compound of claim 30 , wherein each Ris methyl or ethyl.34. The compound of claim 30 , wherein at least one Ris hydrogen.35. The compound of claim 30 , wherein at least one Ris alkyl.36. The compound of claim 30 , wherein one Ris alkyl claim 30 , and one Ris hydrogen.37. The compound of claim 30 , wherein Y is NROR.38. The compound of claim 30 , wherein Y is N(R).39. The compound of claim 30 , wherein both Rare methyl.40. The compound of claim 30 , wherein Ris C-Calkyl.41. The compound of claim 30 , wherein Ris Calkyl.42. The compound of claim 30 , wherein Ris n-nonyl.43. The compound of claim 30 , wherein Ris C-Calkyl.44. The compound of claim 30 , wherein Ris C-Calkyl.45. The compound of claim 30 , wherein Ris C-Calkyl.46. The compound of claim 30 , wherein Ris methyl.47. A pharmaceutical composition comprising one or more compounds of .48. The composition of claim 47 , further comprising one or more carriers claim 47 , or excipients claim 47 , or a combination thereof.49. A unit dose or unit dosage form composition comprising one or more compounds of for treating a disease responsive to Ape1 inhibition. This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 61/490,141, filed May 26, 2011, which is expressly incorporated by reference herein.The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.Apurinic/apyrimidic ...

Подробнее
Номер записи: 79
17-05-2018 дата публикации

MAGL INHIBITORS

Номер: US20180134674A1
Автор: Buzard Daniel J., GRICE Cheryl A., SHAGHAFI Michael B.
Принадлежит:

Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein Ris —OR.3. The compound of claim 2 , or a pharmaceutically acceptable salt or solvate thereof claim 2 , wherein Ris —(CRR)—R.4. The compound of claim 3 , or a pharmaceutically acceptable salt or solvate thereof claim 3 , wherein m is 1 claim 3 , 2 claim 3 , or 3.5. The compound of claim 4 , or a pharmaceutically acceptable salt or solvate thereof claim 4 , wherein each Rand Ris each independently selected from H and Calkyl claim 4 , or Rand R claim 4 , together with the carbon to which they are attached claim 4 , form a Ccycloalkyl ring.6. The compound of claim 5 , or a pharmaceutically acceptable salt or solvate thereof claim 5 , wherein Ris —C(O)OR.7. The compound of claim 6 , or a pharmaceutically acceptable salt or solvate thereof claim 6 , wherein Ris H.8. The compound of claim 6 , or a pharmaceutically acceptable salt or solvate thereof claim 6 , wherein Ris Calkyl.9. The compound of claim 5 , or a pharmaceutically acceptable salt or solvate thereof claim 5 , wherein Ris —C(O)R.10. The compound of claim 9 , or a pharmaceutically acceptable salt or solvate thereof claim 9 , wherein Ris —NHSOR.11. The compound of claim 10 , or a pharmaceutically acceptable salt or solvate thereof claim 10 , wherein Ris Calkyl.12. The compound of claim 10 , or a pharmaceutically acceptable salt or solvate thereof claim 10 , wherein Ris Ccycloalkyl.13. The compound of claim 7 , or a pharmaceutically acceptable salt or solvate thereof claim 7 , wherein each Ris independently selected from Calkyl claim 7 , halogen claim 7 , and Chaloalkyl.14. The compound of claim 13 , or a pharmaceutically acceptable salt or solvate ...

Подробнее
Номер записи: 80
07-08-2014 дата публикации

Factor ixa inhibitors

Номер: US20140219989A1
Автор: Claire Lankin, Craig Boyle, Samuel Chackalamannil, William Greenlee
Принадлежит: Individual

The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.

Подробнее
Номер записи: 81
08-09-2022 дата публикации

High purity 2-naphthylacetonitrile and method for producing same

Номер: US20220281806A1
Автор: Daiki OKADO, Hirotsugu TANIIKE, Masaki NAGAHAMA
Принадлежит: API Corp

The present invention provides high purity 2-naphthylacetonitrile with fewer impurities that is useful as a starting material or intermediate for the synthesis of various pharmaceutical products, agricultural chemicals, and chemical products, and a production method thereof. A high purity 2-naphthylacetonitrile having an HPLC purity of 2-naphthylacetonitrile of not less than 95 area %, and containing naphthalene compounds represented by the formulas (a)-(j) at a content of a predetermined area % or below. A method for producing high purity 2-naphthylacetonitrile, including the following step 1 and step 2: step 1: a step of subjecting 2′-acetonaphthone to a Willgerodt reaction in the presence of an additive where necessary, and hydrolyzing the obtained amide compound to give 2-naphthylacetic acid; step 2: a step of reacting the 2-naphthylacetic acid obtained in step 1, a halogenating agent and sulfamide in the presence of a catalyst as necessary in an organic solvent to give 2-naphthylacetonitrile.

Подробнее
Номер записи: 82
09-05-2019 дата публикации

COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS

Номер: US20190135782A1
Автор: Dixon Scott J., Skouta Rachid, Stockwell Brent R.
Принадлежит:

The present invention provides, inter alia, a compound having the structure: 131-. (canceled)33. The method according to claim 32 , wherein the neurodegenerative disease is selected from the group consisting of Alzheimer's claim 32 , Parkinson's claim 32 , Amyotrophic lateral sclerosis claim 32 , Friedreich's ataxia claim 32 , Multiple sclerosis claim 32 , Huntington's Disease claim 32 , Transmissible spongiform encephalopathy claim 32 , Charcot-Marie-Tooth disease claim 32 , Dementia with Lewy bodies claim 32 , Corticobasal degeneration claim 32 , Progressive supranuclear palsy claim 32 , and Hereditary spastic paraparesis.34. The method according to further comprising co-administering to the subject an effective amount of one or more compositions selected from the group consisting of Donepezil (Aricept) claim 32 , Rivastigmine (Exelon) claim 32 , Galantamine (Razadyne) claim 32 , Tacrine (Cognex) claim 32 , Memantine (Namenda) claim 32 , Vitamin E claim 32 , CERE-110: Adeno-Associated Virus Delivery of NGF (Ceregene) claim 32 , LY450139 (Eli Lilly) claim 32 , Exenatide claim 32 , Varenicline (Pfizer) claim 32 , PF-04360365 (Pfizer) claim 32 , Resveratrol claim 32 , Carbidopa/levodopa immediate-release (Sinemet) claim 32 , Carbidopa/levodopa oral disintegrating (Parcopa) claim 32 , Carbidopa/levodopa/Entacapone (Stalevo) claim 32 , Ropinirole (Requip) claim 32 , Pramipexole (Mirapex) claim 32 , Rotigotine (Neupro) claim 32 , Apomorphine (Apokyn) claim 32 , Selegiline (I-deprenyl claim 32 , Eldepryl) claim 32 , Rasagiline (Azilect) claim 32 , Zydis selegiline HCL Oral disintegrating (Zelapar) claim 32 , Entacapone (Comtan) claim 32 , Tolcapone (Tasmar) claim 32 , Amantadine (Symmetrel) claim 32 , Trihexyphenidyl (formerly Artane) claim 32 , Benztropine (Cogentin) claim 32 , IPX066 (Impax Laboratories Inc.) claim 32 , ioflupane 1231 (DATSCAN®) claim 32 , safinamide (EMD Serono) claim 32 , Pioglitazone claim 32 , riluzole (Rilutek) claim 32 , Lithium carbonate claim ...

Подробнее
Номер записи: 83
10-06-2021 дата публикации

FATTY ACID ACETYLATED SALICYLATES AND THEIR USES

Номер: US20210169905A1
Автор: Bemis Jean E., Jirousek Michael R., Milne Jill C., Smith Jesse J.
Принадлежит:

The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative. 2. The method of claim 1 , wherein Wis NH.5. The method of claim 1 , wherein Q is Z.7. The method of claim 1 , wherein Q is Z and Z is H.8. The method of claim 1 , wherein two of n claim 1 , o claim 1 , p claim 1 , and q are each 1.12. The method of claim 11 , wherein Wis NH.15. The method of claim 11 , wherein Q is Z.16. (canceled)17. The method of claim 11 , wherein Q is Z and Z is H.18. The method of claim 11 , wherein two of n claim 11 , o claim 11 , p claim 11 , and q are each 1.2230-. (canceled) This application is a continuation of U.S. patent application Ser. No. 16/353,575 filed Mar. 14, 2019, which is a continuation of U.S. patent application Ser. No. 15/839,346, filed Dec. 12, 2017, which is a continuation of U.S. patent application Ser. No. 15/283,995, filed Oct. 3, 2016, which is a continuation of U.S. patent application Ser. No. 14/251,247, filed Apr. 11, 2014, now U.S. Pat. No. 9,458,094, which is a continuation of U.S. patent application Ser. No. 13/427,650, filed Mar. 22, 2012, now U.S. Pat. No. 8,735,379, which is a divisional of U.S. patent application Ser. No. 12/499,779 filed Jul. 8, 2009, now U.S. Pat. No. 8,173,831, which claims priority to and the benefit of U.S. Provisional Application No. 61/148,658, filed Jan. 30, 2009, U.S. Provisional Application No. 61/104,363, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,364, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,366, filed Oct. 10, 2008, and U.S. Provisional Application No. 61/078,983, filed Jul. 8, 2008. The entire disclosures of those applications are relied on and incorporated into this application by reference.The invention relates ...

Подробнее
Номер записи: 84
26-05-2016 дата публикации

PRODRUGS OF PHENOLIC TRPV1 AGONISTS

Номер: US20160145225A1
Автор: DONOVAN John F., Husfeld Craig
Принадлежит:

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity. 2. (canceled)3. (canceled)4. The compound of claim 1 , wherein Ris hydrogen and Ris H or substituted or unsubstituted alkyl.5. The compound of claim 4 , wherein X is —N(R)—.6. The compound of claim 5 , wherein Rand Rgroups on adjacent atoms claim 5 , together with the atoms to which they are attached claim 5 , form a substituted or unsubstituted heterocycloalkyl group.7. The compound of claim 6 , wherein the heterocycloalkyl group is a substituted or unsubstituted pyrrolidine ring claim 6 , substituted or unsubstituted piperidine ring claim 6 , or substituted or unsubstituted piperazine ring.1018.-. (canceled)20. (canceled) This application claims benefit of U.S. Provisional Application No. 62/084,515, filed on Nov. 25, 2014, which is herein incorporated by reference in its entirety.Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate the transient receptor potential vanilloid 1 receptor (TRPV1) activity.In one aspect, described herein is a compound having the structure of Formula (I):wherein:Y is a phenolic TRPV1 agonist, wherein the hydrogen atom of the phenolic hydroxyl group is replaced by a covalent bond to —C(O)—X—(C(R)(R))—Z;X is —C(R)(R)—, —O—, —N(R)— or —S—;n is an integer from 1 to 10;Z is —NRRor —COH;Ris hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, and each Rand Ris each independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted acyl, or Rand Rtogether with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl group, or two Ror Rgroups on adjacent carbon atoms, together with the carbon atoms to which ...

Подробнее
Номер записи: 85
28-05-2015 дата публикации

INDANYLOXYPHENYLCYCLOPROPANECARBOXYLIC ACIDS

Номер: US20150148347A1
Автор: HAMPRECHT Dieter, LINGARD Iain
Принадлежит:

A compound of formula I, 2. The compound according to claim 1 , wherein:{'sup': '1', 'claim-text': a phenyl ring, a tetrazolyl ring,', 'a 5-membered heteroaromatic ring containing 1 —NH— or —O— group,', 'a 5-membered heteroaromatic ring containing 1 —NH— or —O— group and additionally 1 or 2=N— atoms,', [{'sup': '1a', 'wherein the phenyl ring, tetrazolyl ring, and 5- or 6-membered heteroaromatic ring are optionally substituted at a carbon atom with one group R, and'}, {'sup': '1b', 'wherein the phenyl ring, tetrazolyl ring, 5- or 6-membered heteroaromatic ring are optionally additionally substituted at carbon atoms with 1 to 3 groups independently selected from R, and'}, {'sup': 'M', 'wherein the H-atom in one or more NH groups present in the tetrazolyl ring, 5- or 6-membered heteroaromatic ring optionally is replaced by R;'}], 'a 6-membered heteroaromatic ring containing 1, 2, or 3=N— atoms,'}], 'Ris selected from the group consisting of'}{'sub': 2', '2, 'X is —O—, >S═O, >S(═O), or —CH—;'}m is 1 or 2;n is 0 or 1;{'sup': 1a', 'N', 'M', 'M, 'sub': 1-4', '2-4', '2-4', '3-6', '3-6', '1-4', '1-4', '1-4', '2', '1-4', '1-6', '3-6', '3-6', '1-4', '1-4', '2', '1-3, 'claim-text': [{'sub': 2', '4-6', '2, 'sup': 'N', 'wherein a —CH— member within a C-cycloalkyl- group or sub-group within the groups thereof is optionally replaced by —NR—, —O—, or —S(O)—, or'}, {'sub': 2', '2', '2', '5-6', '2', '2, 'sup': M', 'M, 'wherein a >CH—CH— member or a —CH—CH— member within a C-cycloalkyl-group or sub-group within the groups thereof is optionally replaced by >N—C(O)—, >N—S(O)—, —N(R)—C(O)—, or —N(R)—S(O)—, and'}, {'sub': 1-3', '1-3', '1-3', '1-4', '1-4', '2', '1-4', '1-4', '2, 'wherein each alkyl and cycloalkyl group and each alkyl and cycloalkyl sub-group within the groups thereof is optionally substituted with HO—, HO—C-alkyl-, C-alkyl-oxy, C-alkyloxy-O-alkyl-, C-alkyl-sulfonyl, HN—C(O)—, C-alkyl-NH—C(O)—, or (C-alkyl)N—C(O)—, and/or optionally substituted with 1 to 3 F atoms;'}], 'Ris ...

Подробнее
Номер записи: 86
10-06-2021 дата публикации

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

Номер: US20210171521A1
Автор: Eric Brown, Gregory Henkel, Kenneth McCormack, Michael Bruno Plewe, Nadezda V. Sokolova, Vidyasagar Reddy Gantla
Принадлежит: Arisan Therapeutics Inc

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections.X is selected from the group consisting of O and H;R1 is selected from (C6 to C10) aryl and (C2 to C9) heteroaryl, andR2 is selected from (C1 to C10) alkyl, (C1 to C10) alkenyl, (C1 to C10) alkynyl, (C3 to C10) cycloalkyl, and (C5 to C10) cycloalkenyl, andNR3aR3b is defined in the specification.These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

Подробнее
Номер записи: 87
09-05-2019 дата публикации

NOVEL COMPOUND, PHOTOCURABLE COMPOSITION, CURED PRODUCT OF SAME, PRINTING INK, AND PRINTED MATTER SURING THE PRINTING INK

Номер: US20190137872A1
Автор: Miyamoto Masanori, Wakahara Keisuke, YAMADA Tomokazu
Принадлежит: DIC CORPORATION

A novel compound is used as a novel photopolymerization initiator, the novel compound having a molecular structure represented by general formula 1 below 5. A photopolymerization initiator comprising the novel compound according to .6. A photocurable composition comprising the photopolymerization initiator according to and a photocurable compound as essential components.7. A cured product produced by curing the photocurable composition according to .8. A photocurable printing ink comprising the photocurable composition according to . The present invention relates to a novel compound useful as a photopolymerization initiator, a photocurable composition containing the photopolymerization initiator, a cured product thereof, a photocurable printing ink containing the photopolymerization initiator, and a printed matter using the printing ink.In general, a photocuring system has been widely used from the viewpoint of high production efficiency, lower cost of curing energy, and VOC reduction. In particular, an ultraviolet curing system becomes a mainstream because it has lower equipment introduction cost and smaller installation area than other photocuring systems.Unlike a reactive monomer which is fixed as a high molecular weight material in a cured film after curing, a photopolymerization initiator used as an essential component in the ultraviolet curing system remains as the photopolymerization initiator or a decomposed product thereof in a cured product. Most of the photopolymerization initiators currently distributed are low-molecular-weight compounds, and thus the remaining photopolymerization initiators or decomposed products thereof also have a low molecular weight. This has been a cause for an odor or the like.Further, it has recently been pointed out that the residues may migrate to the side of a material in contact with the cured product, and in particular, residues of an ultraviolet curable ink used for a printed matter for food packaging may migrate to the ...

Подробнее
Номер записи: 88
04-06-2015 дата публикации

Hepatitis B Antiviral Agents

Номер: US20150152073A1
Автор: Flores Osvaldo A., Hartman George D.
Принадлежит:

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention. 146-. (canceled)48. The compound of claim 47 , or a pharmaceutically acceptable salt thereof;whereinring B is a monocyclic aryl ring;{'sup': 2', '5', '8', '8', '8', '9', '8, 'sub': m', 'm', '2', 'm', '2', 'm', 'm', '2', '1', '6', '1', '6, 'Rand Rare independently selected at each occurrence from the group consisting of halo, -(L)-OR, -(L)-N(R), -(L)-C(═O)N(R), -(L)-C(═O)R, -(L)COR, —C-Calkyl, and —C-Cheteroalkyl;'}{'sup': '4', 'Ris H;'}{'sup': 6', '2', '6', '2, 'sub': 1', '6', '2', '10, 'each Ris independently selected from the group consisting of C-Calkyl, and wherein the alkyl group is optionally substituted with 0-5 substituents selected from R, or the Rgroups attached to the same N atom are taken together with the N atom to which they are attached to form an optionally substituted C-Cheterocycloalkyl ring, wherein the ring optionally comprises a moiety selected from 0, and wherein the heterocycloalkyl ring is optionally substituted with 0-5 substituents selected from R;'}{'sup': '8', 'sub': 1', '6, 'each Ris independently, at each occurrence, H, C-Calkyl;'}{'sup': '9', 'sub': 3', '10, 'Ris C-Ccycloalkyl or aryl;'}each occurrence of x and y is independently selected from the group consisting of 0, 1, 2, 3 and 4;and,each occurrence of m is independently 0.49. The compound of claim 47 , or a pharmaceutically acceptable salt thereof;whereinring B is a monocyclic aryl ring;{'sup': 2', '5', '8, 'sub': m', '1', '6, 'Rand Rare independently selected at each occurrence from the group consisting of halo, -(L)-OR, and —C-Calkyl;'}{'sup': '4', 'Ris H;'}{'sup': 6', '2', '6', '2, 'sub': 1', '6', '2', '10, 'each Ris independently selected from the group consisting of C-Calkyl, and wherein the alkyl group is optionally substituted ...

Подробнее
Номер записи: 89
02-06-2016 дата публикации

SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT

Номер: US20160151375A1
Автор: BRAVO Yalda, Chen Austin, Clark Ryan C., Jacintho Jason, Pedram Bijan, Stock Nicholas
Принадлежит:

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris morpholinyl.4. A composition comprising a compound according to claim 1 , or a salt claim 1 , solvate claim 1 , or N-oxide thereof claim 1 , further comprising at least one pharmaceutically acceptable carrier.5. A method of treating an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound according to .6. The method of claim 5 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of an HBV vaccine claim 5 , HBV polymerase inhibitor claim 5 , interferon claim 5 , pegylated interferon claim 5 , viral entry inhibitor claim 5 , viral maturation inhibitor claim 5 , BAY 41-4109 claim 5 , reverse transcriptase inhibitor claim 5 , a TLR-agonist claim 5 , AT-61 ((E)-N-(1-chloro-3-oxo-1-phenyl-3-(piperidin-1-yl)prop-1-en-2-yl)benzamide) claim 5 , and AT-130 ((E)-N-(1-bromo-1-(2-methoxyphenyl)-3-oxo-3-(piperidin-1-yl)prop-1-en-2-yl)-4-nitrobenzamide) claim 5 , and a combination thereof.7. The method of claim 6 , wherein the pegylated interferon is pegylated interferon alpha (IFN-α) claim 6 , pegylated interferon lambda (IFN-λ) claim 6 , or pegylated interferon gamma (IFN-γ).8. The method of claim 6 , wherein the reverse transcriptase inhibitor is at least one of Zidovudine claim 6 , Didanosine claim 6 , Zalcitabine claim 6 , ddA claim 6 , Stavudine claim 6 , Lamivudine claim 6 , Abacavir claim 6 , Emtricitabine claim 6 , Entecavir claim 6 , Apricitabine claim 6 , Atevirapine claim 6 , ribavirin claim 6 , acyclovir claim 6 , famciclovir claim 6 , valacyclovir claim 6 , ...

Подробнее
Номер записи: 90
02-06-2016 дата публикации

MALEIC ACID DERIVATIVE, PRODUCTION METHOD FOR SAME, AND ANTI-CANCER COMPOSITION COMPRISING SAME

Номер: US20160152607A1
Автор: Kim Dae Gyu, KIM Sunghoon, Kwon Nam Hoon, Lee Sunkyung, Song Jong Hwan
Принадлежит:

A maleic acid derivative represented by Chemical Formula 1 below or a pharmaceutically acceptable salt thereof: 2. The maleic acid derivative or the pharmaceutically acceptable salt thereof of claim 1 , wherein the maleic acid derivative represented by Chemical Formula 1 is at least one selected from the group consisting of:(Z)-4-oxo-4-(pyridin-2-ylamino)but-2-enoic acid;(Z)-4-[(4-methylpyridin-2-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-oxo-4-(pyridin-3-ylamino)but-2-enoic acid;(Z)-4-[(4,6-dimethylpyridin-2-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-[(5-chloropyridin-2-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-[(6-bromopyridin-3-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-[(5-methyl-1,3,4-thiadiazol-2-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-oxo-4-[(thiophen-2-ylmethyl)amino]but-2-enoic acid;(Z)-4-[(3-cyanothiophen-2-yl)amino]-4-oxobut-2-enoic acid;(Z)-4-(isoxazol-3-ylamino)-4-oxobut-2-enoic acid;ethyl (Z)-4-[(3,4-dimethylphenyl)amino]-4-oxobut-2-enoate;(Z)-4-oxo-4-(piperidin-1-yl)-N-(m-tolyl)but-2-enamide;(Z)—N-(3,5-dimethylphenyl)-4-oxo-4-(piperidin-1-yl)but-2-enamide;(Z)—N-(4-methylpyridin-2-yl)-4-oxo-4-(piperidin-1-yl)but-2-enamide;(Z)-4-oxo-4-(piperidin-1-yl)-N-(pyridin-2-yl)but-2-enamide;(Z)-4-oxo-4-(piperidin-1-yl)-N-(pyridin-3-yl)but-2-enamide;(Z)—N-(4,6-dimethylpyridin-2-yl)-4-oxo-4-(piperidin-1-yl)but-2-enamide;(Z)-4-morpholino-4-oxo-N-(m-tolyl)but-2-enamide;(Z)—N-(3,5-dimethylphenyl)-4-morpholino-4-oxobut-2-enamide;(Z)—N-(4-methylpyridin-2-yl)-4-morpholino-4-oxobut-2-enamide;(Z)-4-oxo-4-(pyrrolidin-1-yl)-N-(m-tolyl)but-2-enamide;(Z)—N-(3,5-dimethylphenyl)-4-oxo-4-(pyrrolidine-1-yl)but-2-enamide;(Z)—N-(4-methylpyridin-2-yl)-4-oxo-4-(pyrrolidine-1-yl)but-2-enamide;(Z)—N-(pyridin-2-yl)-4-oxo-4-(pyrrolidine-1-yl)but-2-enamide;(Z)—N-(4-bromophenyl)-4-oxo-4-(piperidin-1-yl)but-2-enamide;(Z)—N-(4-chlorophenyl)-4-oxo-4-(piperidin-1-yl)but-2-enamide;(Z)—N-(4-bromophenyl)-4-morpholino-4-oxobut-2-enamide;(Z)—N-(5-chloropyridin-2-yl)-4-(piperidin-1-yl)-4-oxobut-2-enamide;(Z)—N-(6- ...

Подробнее
Номер записи: 91
31-05-2018 дата публикации

Novel Prodrugs And Methods Of Use Thereof

Номер: US20180148463A1
Автор: Ackerley David Francis, ASHOORZADEH AMIR, Copp Janine Naomi, Guise Christopher Paul, Mowday Alexandra Marie, PATTERSON ADAM VORN, Smaill Jeffrey Bruce, Williams Elsie May
Принадлежит:

The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds. 4. The method according to claim 1 , wherein the compound is selected from the group consisting of:(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl)(4-methylpiperazin-1-yl)methanone (compound 22),(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl)(4-ethylpiperazin-1-yl)methanone (compound 23),(5-(bis(2-bromoethyl)amino)-4-(methylsulfonyl)-2-nitrophenyl)(4-isopropylpiperazin-1-yl)methanone (compound 24), (5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl)(4-methylpiperazin-1-yl)methanone (compound (25),(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl)(4-ethylpiperazin-1-yl)methanone (compound 26),(5-(bis(2-bromoethyl)amino)-4-(ethylsulfonyl)-2-nitrophenyl)(4-isopropylpiperazin-1-yl)methanone (compound 27).2-((2-bromoethyl)(5-(4-methylpiperazine-1-carbonyl)-2-(methylsulfonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 310),2-((2-bromoethyl)(5-(4-ethylpiperazine-1-carbonyl)-2-(methylsulfonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 311),2-((2-bromoethyl)(5-(4-isopropylpiperazine-1-carbonyl)-2-(methylsulfonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 312),2-((2-bromoethyl)(2-ethylsulfonyl)-5-(4-methylpiperazine-1-carbonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 313),2-((2-bromoethyl)(5-(4-ethylpiperazine-1-carbonyl)-2-(ethylsulfonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 314), and2-((2-bromoethyl)(2-ethylsulfonyl)-5-(4-isopropylpiperazine-1-carbonyl)-4-nitrophenyl)amino)ethyl methanesulfonate (compound 315).5. The method according to claim 1 , wherein the compound is a pharmaceutically acceptable salt of said ...

Подробнее
Номер записи: 92
21-08-2014 дата публикации

N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES

Номер: US20140235636A1
Автор: BROOKFIELD Frederick Arthur, COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Sutton Art, Toscano John P.
Принадлежит:

The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. 2. The compound of claim 1 , wherein L is —SO—.3. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or more substituents independently selected from W.4. The compound of claim 1 , wherein Y is aryl and said aryl is unsubstituted or substituted with one or two substituents independently selected from W.5. The compound of claim 1 , wherein Y is phenyl and said phenyl is unsubstituted or substituted with one or more substituents independently selected from W.6. The compound of claim 1 , wherein W is halo or —SO.7. The compound of claim 1 , wherein W is chloro claim 1 , bromo or —SO.8. The compound of claim claim 1 , wherein R is alkyl or phenyl claim 1 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more halos.9. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more substituents independently selected from W.10. The compound of claim 2 , wherein Y is alkyl and said alkyl is unsubstituted or substituted with one or more halos.11. The compound of claim 9 , wherein R is alkyl or phenyl claim 9 , wherein said alkyl and phenyl are unsubstituted or substituted with one or more substituents independently selected from halo claim 9 , nitro claim 9 , alkylsulfonyl and trihalomethyl.12. The compound of claim 1 , wherein the ...

Подробнее
Номер записи: 93
01-06-2017 дата публикации

COMPOUND, ACTIVE ENERGY RAY CURABLE COMPOSITION, CURED ARTICLE THEREOF, PRINTING INK, AND INKJET RECORDING INK

Номер: US20170152391A1
Автор: Kondou Akihiro, Miyamoto Masanori, Tanimoto Youichi, YAMADA Tomokazu, Yamamoto Sei, Yogo Azusa
Принадлежит: DIC CORPORATION

A compound obtained through Michael addition reaction of an α-aminoacetophenone skeleton-containing compound (I) represented by the following general formula (1) and a reactive compound (II) having a function as a Michael acceptor is used as a photopolymerization initiator. In the general formula (1), Rrepresents an aliphatic group, Rto Reach independently represent an aliphatic group, etc., Rto Reach independently represent a hydrogen atom, Xrepresents a single bond or a C1-6 alkylene group, Xrepresents a carbonyl group, Yand Yrepresent a group represented by the following general formula (2). However, when Yand Yboth have a structure represented by the general formula (2), Xin at least one of them is —NH—. In the general formula (2), Xand Xeach independently represent a linear or branched alkylene group having 2 to 6 carbon atoms, Xrepresents a single bond, —O— or —NH—. 2. The compound according to claim 1 , wherein the reactive compound (II) having a function as a Michael acceptor is a polyfunctional (meth)acrylate compound.3. The compound according to claim 1 , wherein (the number of the Michael addition donor function-having groups in the α-aminoacetophenone skeleton-containing compound (I) having a function as a Michael addition donor)/(the number of the Michael acceptor function-having groups in the reactive compound) is within a range of 1/20 to 1/2.7. A compound having polymerization initiation performance claim 5 , which is obtained through reaction of the compound (A) of and a compound (B) capable of reacting with the compound (A).8. The compound according to claim 7 , wherein the compound (B) having a functional group reactive with the amino group in the compound or a functional group reactive with the structural moiety represented by:{'br': None, 'sub': '2', '—X—Z,'}in the general formula (1′) is a hydroxyl group-containing (meth)acrylate compound.9. A photopolymerization initiator comprising the compound of .10. An active energy ray curable composition ...

Подробнее
Номер записи: 94
23-05-2019 дата публикации

Novel Prodrugs And Methods Of Use Thereof

Номер: US20190153002A1
Автор: Ackerley David Francis, ASHOORZADEH AMIR, Copp Janine Naomi, Guise Christopher Paul, Mowday Alexandra Marie, PATTERSON ADAM VORN, Smaill Jeffrey Bruce, Williams Elsie May
Принадлежит:

The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds. 120-. (canceled)22. A compound of formula I as claimed in claim 21 , wherein W is bromine or iodine.23. A compound of formula I as claimed in claim 21 , wherein X is bromine or OSOMe.24. A compound of formula I as claimed in claim 21 , wherein Ris hydrogen claim 21 , methyl or ethyl.25. A compound of formula I as claimed in claim 21 , wherein n represents 2 or 3.26. The compound of claim 21 , wherein the pharmaceutically acceptable salt of the compound is a methanesulfonate salt.28. A compound of formula I as claimed in represented by the formula (Ib) wherein Y represents SOMe.30. A compound of formula (Ib) as claimed in selected from:5-(bis(2-bromoethyl)amino)-N-(2-(dimethylamino)ethyl)-4-(methylsulfonyl)-2-nitrobenzamide (compound 36),5-(bis(2-bromoethyl)amino)-N-(2-(dimethylamino)ethyl)-N-methyl-4-(methylsulfonyl)-2-nitrobenzamide (compound 37),5-(bis(2-bromoethyl)amino)-N-(3-(dimethylamino)propyl)-4-(methylsulfonyl)-2-nitrobenzamide (compound 38),5-(bis(2-bromoethyl)amino)-N-(3-(dimethylamino)propyl)-N-methyl-4-(methylsulfonyl)-2-nitrobenzamide (compound 39),5-(bis(2-bromoethyl)amino)-N-(2-(dimethylamino)ethyl)-4-(ethylsulfonyl)-2-nitrobenzamide (compound 48),5-(bis(2-bromoethyl)amino)-N-(2-(dimethylamino)ethyl)-4-(ethylsulfonyl)-N-methyl-2-nitrobenzamide (compound 49),5-(bis(2-bromoethyl)amino)-N-(3-(dimethylamino)propyl)-4-(ethylsulfonyl)-2-nitrobenzamide (compound 50), and5-(bis(2-bromoethyl)amino)-N-(3-(dimethylamino)propyl)-4-(ethylsulfonyl)-N-methyl-2-nitrobenzamide (compound 51).31. A compound of formula I as claimed in wherein X is OSOMe.32. A compound of formula I as claimed in selected from:2-((2- ...

Подробнее
Номер записи: 95
28-08-2014 дата публикации

SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF

Номер: US20140243334A1
Автор: Calderwood Emily F., England Dylan B., Gould Alexandra E., Harrison Sean J., Ma Liting
Принадлежит: Millennium Pharmaceuticals, Inc.

This invention provides compounds of formula (I): 2. The compound of claim 1 , wherein G is —R claim 1 , —V—R claim 1 , —V-L-R claim 1 , -L-V—R claim 1 , or -L-R.3. The compound of claim 2 , wherein:{'sup': 2a', '1, 'Ris R;'}{'sup': '2b', 'Ris G;'}{'sup': 2c', '1, 'Ris R; and'}{'sup': '2d', 'sub': '1', 'Ris R.'}4. The compound of claim 2 , wherein:{'sup': 2a', '1, 'Ris R;'}{'sup': 2b', '1, 'Ris R;'}{'sup': '2c', 'Ris G; and'}{'sup': 2d', '1, 'Ris R.'}5. The compound of claim 2 , wherein:{'sub': 1', '1, 'sup': 3', '3', '3, 'G is —V—R, -L-R, or —R;'}{'sub': 1', '2', '2', '2, 'Lis —CH— or —CHCH—; and'}{'sub': 1', '2, 'sup': 4a', '4a', '4a', '4a', '4a', '4a', '4a, 'Vis —N(R)—, —N(R)—C(O)—, —C(O)—N(R)—, —N(R)—SO—, —O—, —N(R)—C(O)—O—, or —N(R)—C(O)—N(R)—.'}6. The compound of claim 2 , wherein:{'sup': '1a', 'each occurrence of Ris independently hydrogen, fluoro, trifluoromethyl, or methyl;'}{'sup': '1b', 'each occurrence of Ris hydrogen;'}{'sup': '1c', 'Ris hydrogen, hydroxy, fluoro, trifluoromethyl, or methyl;'}{'sup': '1', 'each occurrence of Ris independently hydrogen, chloro, fluoro, cyano, hydroxy, methoxy, ethoxy, trifluoromethyl, methyl, or ethyl.'}7. The compound of claim 2 , wherein:{'sup': 3', '5dd, 'each substitutable carbon chain atom in Ris unsubstituted or substituted with 1-2 occurrences of R;'}{'sup': 3', '5', '5aa, 'sub': '2', 'each substitutable saturated ring carbon atom in Ris unsubstituted or substituted with ═O, ═C(R), or —R;'}{'sup': 3', '5a, 'each substitutable unsaturated ring carbon atom in Ris unsubstituted or is substituted with —R;'}{'sup': 3', '9b, 'claim-text': [{'sup': 5a', '5', '5', '5', '5', '6', '6', '6', '4', '4', '4', '6', '4', '4', '4', '6', '4', '6', '4', '4', '6', '4', '4', '5a, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '1-6, 'each Ris independently halogen, —NO, —CN, —C(R)═C(R), —C≡C—R, —OR, —SR, —S(O)R, —SOR, —SON(R), —N(R), —NRC(O)R, —NRC(O)N(R), —NRCOR, —OC(O)N(R), —C(O)R, —C(O)N(R), —N(R)SOR, —N(R) ...

Подробнее
Номер записи: 96
24-06-2021 дата публикации

Method for treating a patient having cancer

Номер: US20210188765A1
Автор: Abdelsattar M. Omar, Azizah M. Malebari, Dhaval Shah, Farid Ahmed, Maan T. Khayat, Martin K. Safo, Moustafa E. El-Araby
Принадлежит: KING ABDULAZIZ UNIVERSITY

Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.

Подробнее
Номер записи: 97
15-06-2017 дата публикации

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Номер: US20170166541A1
Автор: Salituro Francesco G., Saunders Jeffrey O.
Принадлежит:

Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. 2. The compound of claim 1 , wherein B and Bare taken together with the carbon atoms to which they are attached to form a carbonyl group.3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein D is a bond and Dis NR.5. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein D is a bond and Dis NR.6. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris hydrogen.7. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris heteroaralkyl substituted with 0-3 occurrences of R.8. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein A is phenyl substituted with 1 or 2 occurrences of R.9. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —ORand Ris alkyl.10. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris —ORand Ris alkyl.11. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris alkyl.12. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris alkyl.17. A method of treating a cancer characterized as having an IDH mutation claim 1 , the method comprising administering to a subject a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.18. A method of treating a cancer characterized as having an IDH mutation claim 4 , the method comprising administering to a subject a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.19. The method of claim 17 , wherein the IDH1 mutation is IDH1 R132X.20. The method of claim 18 , wherein the IDH1 mutation is IDH1 R132X. This continuation application claims priority from U.S. Ser. No. 13/492,159, filed Jun. 8, 2012, which is a continuation of International Patent Application PCT/US2010/059778, ...

Подробнее
Номер записи: 98
11-09-2014 дата публикации

LYSINE DEMETHYLASE INHIBITORS FOR DISEASES AND DISORDERS ASSOCIATED WITH FLAVIVIRIDAE

Номер: US20140256742A1
Автор: BAKER Jonathan A., Fyfe Matthew Collin Thor
Принадлежит:

The invention relates to methods and compositions for the treatment or prevention of Flaviviridae infections. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing Flaviviridae infections, including hepatitis C virus infections.

Подробнее
Номер записи: 99
18-09-2014 дата публикации

SULFONYL SEMICARBAZIDES, SEMICARBAZIDES AND UREAS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS FOR TREATING HEMORRHAGIC FEVER VIRUSES, INCLUDING INFECTIONS ASSOCIATED WITH ARENAVIRUSES

Номер: US20140275037A1
Автор: Bailey Thomas R., DENG Yijun, Laquerre Sylvie, Nitz Theodore J., Zhang Yanming
Принадлежит: Siga Technologies, Inc.

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 134-. (canceled)38. A pharmaceutical composition of claim 35 , wherein n is 0 or 1.39. A pharmaceutical composition of claim 35 , wherein n is 0.40. A pharmaceutical composition of claim 35 , wherein m is 1 and p is 1.41. A pharmaceutical composition of claim 35 , wherein m is 0 and p is 0.44. A pharmaceutical composition of claim 35 , wherein the compound of formula I is selected from the group consisting of:N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[4-(phenyl)-phenylsulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[4-(2-methyl-2-propyl)-phenylsulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[7-(4-methyl-3,4-dihydro-2H-benzo[1,4]oxazinyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[5-(1-dimethylamino-naphthyl) sulfonyl]hydrazine-1-carboxamide; N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(2,4,6-trimethylphenyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(3-chloro-6-methoxyphenyl) sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(3,6-dimethoxyphenyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(4-(4-[1,2,3]thiadiazolyl) phenyl)sulfonyl ...

Подробнее
Номер записи: 100