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 5092. Отображено 100.
16-02-2012 дата публикации

Substituted acylguanidine derivatives (as amended)

Номер: US20120041036A1
Автор: Isao Kinoyama, Takehiro Miyazaki, Takuya Washio, Yohei Koganemaru
Принадлежит: Astellas Pharma Inc

An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT 5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT 5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.

Подробнее
Номер записи: 1
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Автор: Hiroki Fukudome, Hiroshi Moritani, Takahiro Nigawara, Takeshi Hanazawa, Tomoaki Kawano, Yasuhiro Yonetoku
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

Подробнее
Номер записи: 2
10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Автор: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

Подробнее
Номер записи: 3
07-06-2012 дата публикации

Biphenylacetamide derivative

Номер: US20120142771A1
Автор: Nana Yajima, Seiji Iwama, Tomoyuki Tanaka
Принадлежит: Sumitomo Dainippon Pharma Co Ltd

The present invention provides a compound of formula (I) or a salt thereof, wherein R 1 , R 2 and R 3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 4 and R 5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C 1-6 alkyl, C 1-6 alkoxy substituted with fluorine atom, and others; R 6 and R 7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R 8 and R 9 are independently selected from the group consisting of hydrogen atom, C 1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

Подробнее
Номер записи: 4
21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Автор: Haiqing Yuan, John E. Donello, Michael E. Garst, Richard I. Beard, Veena Viswanath, Xiaoxia Liu
Принадлежит: Allergan Inc

The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Подробнее
Номер записи: 5
28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Автор: Daniel D. Long, Lan Jiang, Michael R. Leadbetter, Sabine Axt, Sean G. Trapp
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Подробнее
Номер записи: 6
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Joerg Kley, Martin Fleck, Niklas Heine, Thorsten Lehmann-Lintz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Подробнее
Номер записи: 7
06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Автор: Andrew F. Kolodziej, Michael H. Cardone, Xiang Y. Yu
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

Подробнее
Номер записи: 8
18-10-2012 дата публикации

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

Номер: US20120264736A1
Автор: Chad E. Bennett, Chad E. Knutson, David J. Cole, Dmitri A. Pissarnitski, Duane A. Burnett, Haiqun Tang, Hongmei Li, Hubert B. Josien, Jing Su, John W. Clader, Li Qiang, Mark D. Mcbriar, Martin S. Domalski, Mary Ann Caplen, Murali Rajagopalan, Ruo Xu, Thavalakulamgara K. Sasikumar, Theodros Asberom, Thomas A. Bara, Wen-Lian Wu, Zhiqiang Zhao
Принадлежит: Schering Corp

This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Подробнее
Номер записи: 9
02-05-2013 дата публикации

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

Номер: US20130109866A1
Автор: Beard Richard L., Donello John E., Duong Tien T., Garst Michael E., Viswanath Veena
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:a is 1 and b is 0.3. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': 5', '14, 'sub': 'n', 'Ris —S(O)R.'}4. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'sub': '3', 'Ris —CF.'}5) A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'Ris halogen.'}6. A compound according to claim 1 , wherein:a is 1 and b is 0;{'sup': 1', '11', '12', '13, 'sub': '1-8', 'Ris optionally substituted Calkyl, —NRRor —OR;'}{'sup': '2', 'sub': '1-8', 'Ris optionally substituted Calkyl;'}{'sup': 3', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 4', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 5', '14, 'sub': 3', 'n, 'Ris halogen, —CFor —S(O)R;'}n is 0, 1 or 2;{'sup': 6', '15', '13', '11', '−12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 7', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': '8', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '6-10, 'Ris hydrogen, optionally substituted Calkyl or optionally substituted Caryl;'}{'sup': '10', 'sub': '1-8', 'Ris hydrogen or optionally substituted C;'}{'sup': '11', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '12', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '13', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '14', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl; ...

Подробнее
Номер записи: 10
09-05-2013 дата публикации

BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

Номер: US20130116227A1
Автор: Hasegawa Futoshi, Hori Seiji, Katayama Seiji, Suzuki Kuniko
Принадлежит: DAINIPPON SUMITOMO PHARMA CO., LTD.

Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; Ris a substitutable aminosulfonyl group, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable Calkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R, Rand Rare each independently hydrogen atoms, etc.; Ris a halogen atom, a cyano group, etc.; Rand Rare each independently a hydrogen atom, etc.; and m is an integer such as 0.) 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is a group of formula (a).3. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —NHCO—.4. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CONH—.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris [{'sub': '1-6', 'claim-text': [{'sub': '1-6', '(i) amino (in which the amino may be optionally substituted with the same or different 1 to 2 Calkyl),'}, {'sub': '1-6', '(ii) Calkoxy, or'}, '(iii) 4- to 7-membered cyclic amino),, '(a) Calkyl (in which the group may be optionally substituted with'}, {'sub': '1-6', '(b) Calkylcarbonyl,'}, '(c) aminocarbonyl, and', {'sub': '2', '(d) —C(═NH)—NH),'}], '1: aminosulfonyl group (in which the amino may be optionally substituted with the same or different 1 to 2 groups selected from the group consisting of'}{'sub': '1-6', '2: Calkylsulfonyl group, or'}{'sub': '1-6', '3: Calkylsulfonylamino group, or a pharmaceutically acceptable salt thereof.'}6. The compound of claim 5 , wherein Ris aminosulfonyl group claim 5 , or a pharmaceutically acceptable salt thereof.7. The compound of claim ...

Подробнее
Номер записи: 11
04-07-2013 дата публикации

SULFUR-CONTAINING COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF

Номер: US20130172355A1
Автор: CHAO Chih-Hua, SHEU Jyh-Horng, WEN Zhi-Hong
Принадлежит: NATIONAL SUN YAT-SEN UNIVERSITY

The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds. 2. The method according to claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and unsubstituted phenyl.6. The method according to claim 5 , wherein Ris selected from the group consisting of methyl claim 5 , ethyl claim 5 , and unsubstituted phenyl.9. The method according to claim 5 , wherein the disease is selected from the group consisting of inflammation claim 5 , atherosclerosis claim 5 , neuropathic pain claim 5 , inflammatory neointimal proliferation claim 5 , arthritis claim 5 , multiple sclerosis claim 5 , inflammatory pain claim 5 , and spinal cord injury.10. The method according to claim 5 , wherein the compound is administered by injection. This application is a Divisional of the pending U.S. patent application Ser. No. 12/172,633 filed on Jul. 14, 2008, all of which is hereby incorporated by reference in its entirety.Although incorporated by reference in its entirety, no arguments or disclaimers made in the parent application apply to this divisional application. Any disclaimer that may have occurred during the prosecution of the above-referenced application(s) is hereby expressly rescinded. Consequently, the Patent Office is asked to review the new set of claims in view of the entire prior art of record and any search that the Office deems appropriate.1. Field of the InventionThe invention relates to a novel sulfur-containing compound. Said sulfur-containing compound has ability to inhibit the function of inducible nitric oxide synthase (iNOS) and/or ...

Подробнее
Номер записи: 12
11-07-2013 дата публикации

SULFOXIDE-BASED SURFACTANTS

Номер: US20130178540A1
Автор: Arhancet Graciela, Embse Richard Vonder, Grady Brian, Harwell Jeff, Long Scott, Yu Guangzhe
Принадлежит:

The present invention provides sulfoxide compounds comprising hydrophobic ester or amide moieties such that the compounds have surfactant properties. Also provided are methods for using the sulfoxide compounds or mixtures of the sulfoxide compounds in a variety of applications. 2. The compound of claim 1 , wherein Ris alkyl; Ris alkyl claim 1 , acyl claim 1 , (CHCHO)H claim 1 , (CHCH(CH)O)H claim 1 , or a combination of (CHCHO)H and (CHCH(CH)O)H; p is an integer of 2 or greater; and Ris Cto Calkyl.3. The compound of claim 2 , wherein n is 2; Ris methyl; Ris NHor NHR; and Ris Cto Calkyl.5. The compound of claim 4 , wherein Ris alkyl; Ris hydrogen claim 4 , alkyl claim 4 , acyl claim 4 , (CHCHO)H claim 4 , (CHCH(CH)O)H claim 4 , or a combination of (CHCHO)H and (CHCH(CH)O)H; p is an integer of 2 or greater; and Ris Cto Calkyl.6. The compound of claim 5 , wherein n is 2; Ris methyl; and Ris Cto Calkyl.7. The compound of claim 1 , wherein the compound has a critical micelle concentration (CMC) in water at 25° C. and atmospheric pressure.8. The compound of claim 1 , wherein the compound is used in commercial or residential laundry products claim 1 , industrial or household cleaning products claim 1 , floor polishing products claim 1 , personal care or cosmetic products claim 1 , textile processing claim 1 , metal processing claim 1 , paper processing claim 1 , agricultural applications claim 1 , latex production claim 1 , paper de-inking claim 1 , or crude oil drilling applications.10. The compound of claim 9 , wherein Ris alkyl; Ris hydrogen claim 9 , alkyl claim 9 , acyl claim 9 , (CHCHO)H claim 9 , (CHCH(CH)O)H claim 9 , or a combination of (CHCHO)H and (CHCH(CH)O)H; p is an integer of 2 or greater; and Ris Cto Calkyl.11. The compound of claim 10 , wherein n is 2 claim 10 , k is 1 claim 10 , 2 claim 10 , 3 claim 10 , or 4; Ris methyl; Ris hydrogen; Ris Cto Calkyl; and W and X are oxygen.12. The compound of claim 9 , wherein the compound has a critical micelle ...

Подробнее
Номер записи: 13
25-07-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130190338A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris H, halogen or Calkyl; and'}{'sup': '8', 'Ris H or CN.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methyl propionate, methyl-2-benzoic acid, methyl-2-methylbenzoate, methyl-3-methylphenylacetamide, methyl-3-methylphenylsulfonamide, methyl acetic acid, methyl-2-methylphenylcarboxylate or propionic acid;'}{'sup': '5', 'sub': '2', 'Ris —S(O)—, S or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '7', 'Ris chlorine, ...

Подробнее
Номер записи: 14
29-08-2013 дата публикации

SUBSTITUTED NAPHTHYLACETIC ACIDS

Номер: US20130225588A1
Автор: Firooznia Fariborz, LIN Tai-An, Mertz Eric, SIDDURI Achyutharao, So Sung-Sau, Tilley Jefferson Wright
Принадлежит: Hoffmann-La Roche Inc.

The invention is concerned with the compounds of formula (I): 2. The compound according to claim 1 , wherein X is —SO— or —SONH—.3. The compound according to claim 1 , wherein X is —NHSO— claim 1 , —NHC(O)— or —NHC(O)NH—.4. The compound according to claim 1 , wherein X is —SO—.5. The compound according to claim 1 , wherein Y is CH.6. The compound according to claim 1 , wherein Ris F or Cl.7. The compound according to claim 1 , wherein Ris F.8. The compound according to claim 1 , wherein Ris:{'sub': 2', '3, 'claim-text': unsubstituted heteroaryl,', 'unsubstituted cycloalkyl, or', 'unsubstituted heterocycloalkyl., 'phenyl, unsubstituted or mono- or bi-substituted independently with lower alkyl, halogen, alkoxy, —SO-lower alkyl, haloalkyl or —OCF,'}9. The compound according to claim 1 , wherein Ris:{'sub': '2', 'claim-text': {'sub': '2', 'N(lower alkyl), said lower alkyl independently being unsubstituted or substituted with unsubstituted phenyl or phenyl substituted with methoxy.'}, 'lower alkyl, unsubstituted or substituted with hydroxy, unsubstituted phenyl or phenyl substituted with halogen, —SO-lower alkyl or alkoxy, or'}10. The compound according to claim 1 , wherein Ris phenyl claim 1 , unsubstituted or mono- or bi-substituted independently with lower alkyl claim 1 , halogen claim 1 , alkoxy claim 1 , —SO-lower alkyl claim 1 , haloalkyl or —OCF.11. The compound according to claim 1 , wherein Ris methyl.12. The compound according to claim 1 , wherein X is —SO—; Y is C; and Ris phenyl claim 1 , unsubstituted or mono- or bi-substituted independently with lower alkyl claim 1 , halogen claim 1 , alkoxy claim 1 , —SO-lower alkyl claim 1 , haloalkyl or —OCF.13. The compound according to claim 1 , wherein Ris phenyl claim 1 , unsubstituted or mono- or bi-substituted independently with methyl claim 1 , chlorine claim 1 , fluorine claim 1 , —CF claim 1 , —OCFor —OCH.14. The compound according to claim 1 , wherein Ris pyrrolidinyl claim 1 , piperidinyl claim 1 , —N(CHCH) ...

Подробнее
Номер записи: 15
05-12-2013 дата публикации

Indanyloxyphenylcyclopropanecarboxylic acids

Номер: US20130324514A1
Автор: Dieter Hamprecht, Iain Lingard, Sara Frattini, Stefan Peters
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Подробнее
Номер записи: 16
12-12-2013 дата публикации

Lipids for therapeutic agent delivery formulations

Номер: US20130330401A1
Автор: John A. Gaudette, Joseph E. Payne, Jun Zhang, Lei Yu, Mohammad Ahmadian, Neda SAFARZADEH, Priya Karmali, Richard P. Witte, Victor Knopov, Violetta Akopian, Wenbin Ying, Zheng Hou
Принадлежит: Nitto Denko Corp

The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.

Подробнее
Номер записи: 17
16-01-2014 дата публикации

Sulfonamides as hib protease inhibitors

Номер: US20140018326A1
Автор: Daniel J. Mckay, Marie-Eve Lebrun, Oscar M. Moradei, Sheldon Crane, Vouy Linh Truong
Принадлежит: Merck Canada Inc

Compounds of Formula I are disclosed: wherein L, A, R 1 , R 2 , R 3A , R 3B , R 4A , R 4B , R 5 , R 6 and R 7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Подробнее
Номер записи: 18
30-01-2014 дата публикации

Iminopropene compound and use thereof

Номер: US20140031376A1
Автор: Atsushi Iwata, Shigeyuki Itoh
Принадлежит: Sumitomo Chemical Co Ltd

The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Подробнее
Номер записи: 19
06-02-2014 дата публикации

4-Biphenyl-substituted pyrazolidin-3,5-dione derivatives

Номер: US20140039215A1
Автор: ARNOLD Christian, Auler Thomas, BRETSCHNEIDER Thomas, Feucht Dieter, FISCHER Reiner, Gesing Ernst Rudolf F., Hills Martin Jeffrey, KEHNE Heinz, Kuck Karl-Heinz, Lösel Peter, MALSAM Olga
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) 124-. (canceled)27. A compound of the formula (XIX) according to claim 25 , wherein the reagent is dicyclohexylcarbodiimide or toluenesulphonyl chloride. This application is a Continuation of application Ser. No. 13/347,931, filed Jan. 11, 2012, now pending, which is a Division of application Ser. No. 10/567,788, §371(c) date: Feb. 16, 2007, now U.S. Pat. No. 8,119,556, which is U.S. National Phase of International Application No. PCT/EP2004/008638, filed Aug. 2, 2004, which claims the benefit of German Appl. No. DE 10337497.3, filed Aug. 14, 2003. The entirety of each of these applications is incorporated by reference herein.The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to novel selective herbicidal active compound combinations comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives and at least one crop plant compatibility-improving compound, which combinations can be used with particularly good results for the selective control of weeds in various crops of useful plants.4-Arylpyrazolidine-3,5-dione derivatives having herbicidal, acaricidal and insecticidal properties are described in EP-A-508 126, WO 92/16 150, WO 96/721 652, WO 99/43 649, WO 99/47 525, WO 99/48 869, WO 99/55 673, WO 01/17 351, WO 01/17 352, WO 01/17 353, WO 01/17 972, WO 01/17 973, WO 03/062 244, WO 03/028 446. Also known are 4-arylpyrazolidines, which have been described to have fungicidal properties (WO 96/36 229, WO 96/36 615, WO 96/36 616, WO 96/36 633).However, in particular at low application rates and concentrations, the activity and the activity spectrum of these compounds are not always entirely satisfactory. Furthermore, the plant compatibility of ...

Подробнее
Номер записи: 20
27-02-2014 дата публикации

ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES

Номер: US20140058125A1
Автор: Christiansen Elisabeth, ULVEN Trond
Принадлежит: Syddansk Universitet

There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels. 2. The compound of claim 1 , wherein X is —C(RR)—.3. The compound of claim 1 , wherein R claim 1 , Rand Rare independently selected from hydrogen and (C-C)alkyl.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of wherein Rand Rare hydrogen.6. The compound of claim 1 , wherein Ris hydrogen.7. The compound of claim 1 , wherein n is 1 and Ar is selected from the group consisting of an optionally substituted phenyl claim 1 , 2-pyridyl claim 1 , 3-pyridyl claim 1 , 4-pyridyl claim 1 , 2-thienyl claim 1 , 3-thienyl claim 1 , 2-thiazolyl claim 1 , 4-thiazolyl claim 1 , 5-thiazolyl claim 1 , 4-thiazolyl claim 1 , 2-furyl claim 1 , 3-furyl claim 1 , 2-oxazolyl claim 1 , 4-oxazolyl claim 1 , 5-oxazolyl claim 1 , 3-pyrrolyl claim 1 , 1-pyrrazolyl claim 1 , 2-pyrrazolyl claim 1 , 3-pyrrazolyl claim 1 , 2-pyrimidyl claim 1 , 4-pyrimidyl claim 1 , 5-pyrimidyl claim 1 , 4-triazolyl claim 1 , 5-tetrazolyl claim 1 , 2-naphthyl claim 1 , 3-naphthyl claim 1 , 2-quinolyl claim 1 , 3-quinolyl claim 1 , 4-quinolyl claim 1 , 5-quinolyl claim 1 , 6-quinolyl claim 1 , 7-quinolyl claim 1 , 8-quinolyl claim 1 , 2-benzothiazolyl claim 1 , 4-benzothiazolyl claim 1 , 5-benzothiazolyl claim 1 , 6-benzothiazolyl claim 1 , 7-benzothiazolyl claim 1 , 1-indolyl claim 1 , 2-indolyl claim 1 , 3-indolyl claim 1 , 4-indolyl claim 1 , 5-indolyl claim 1 , 6-indolyl and 7-indolyl.8. The compound of claim 1 , wherein n is 1 and Ar is phenyl.9. The compound of claim 1 , wherein n is 1 and Ar is 4-pyridyl.10. The compound of ...

Подробнее
Номер записи: 21
06-03-2014 дата публикации

Bis(Trifluoromethanesulfonyl)Ethyl-Bearing Compound and Acid Catalyst, and Method for Preparing Same

Номер: US20140066659A1
Автор: Hikaru Yanai, Takeo Taguchi
Принадлежит: Central Glass Co Ltd

A bis(trifluoromethanesulfonyl)ethyl group-bearing compound represented by the following formula [1], [2] or [3]

Подробнее
Номер записи: 22
07-01-2016 дата публикации

USE OF ACYLSULFONAMIDES FOR IMPROVING PLANT YIELD

Номер: US20160000084A1
Автор: Bickers Udo, Hacker Erwin, Hills Martin Jeffrey, LEHR Stefan, RUIZ-SANTAELLA MORENO Juan Pedro, Schmidt Mathias, TRABOLD Klaus
Принадлежит:

Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, 2. Compound A as claimed in claim 1 , wherein Compound (A) is selected from compounds of formula (I) or salts thereof claim 1 ,whereinX is CH;{'sup': 1', '5', '6, 'Ris —NH—CO—NRR,'}{'sup': 2', '2', '2', '2, 'sub': n', '1', '2', '1', '2', '1', '2', '1', '2', '1', '2', '1', '2', '1', '2, '(R)is a radical Rif n is 1 or represents n radicals Rattached to different carbon ring atoms of the basic ring if n is more than 1, wherein each Rindependently of one another is halogen, (C-C)haloalkyl, (C-C)haloalkoxy, nitro, (C-C)alkyl, (C-C)alkoxy, (C-C)alkylsulfonyl, [(C-C)alkoxyl]carbonyl or [(C-C)alkyl]carbonyl,'}{'sup': '3', 'Ris hydrogen'}{'sup': 4', '4', '4', '4, 'sub': m', '1', '2', '1', '2', '1', '2', '3', '6', '1', '2', '1', '2', '1', '2, '(R)is a radical Rif m is 1 or represents m radicals Rattached to different carbon ring atoms of the basic ring if m and is more than 1, wherein each Rindependently of one another is halogen, nitro, (C-C)alkyl, (C-C)haloalkyl, (C-C)haloalkoxy, (C-C)cycloalkyl, (C-C)alkoxy, cyano, [(C-C)alkoxyl]carbonyl or [(C-C)alkyl]carbonyl;'}{'sup': '5', 'sub': 1', '2, 'Ris hydrogen, or (C-C)alkyl,'}{'sup': '6', 'sub': 1', '2, 'Ris hydrogen, or (C-C)alkyl,'}n is 0, 1, or 2, optionally 0, or 1, optionally 0m is 0, 1, or 2, optionally 1 or 2, optionally 13. The Compound A as claimed in claim 1 , wherein Compound (A) is N-(2-methoxybenzoy0-4-[(methylaminocarbonyl)amino]benzenesulfonamide (=Compound (A1)).4. The Compound A as claimed in claim 1 , which is capable of increasing grain yield of crop plants selected from group consisting of cereals claim 1 , canola claim 1 , soybean and cotton crops.5. The Compound A as claimed in claim 1 , which is capable of increasing gluten content of seed kernels of crop plants selected from group ...

Подробнее
Номер записи: 23
04-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180000087A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.4. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , CH claim 1 , CF claim 1 , and OCF.5. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.6. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare H.7. A molecule according to claim 1 , wherein Ris Cl.8. A molecule according to claim 1 , wherein Ris Cl.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.11. A molecule according to claim 1 , wherein Ris selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , morpholinyl claim 1 , oxetanyl claim 1 , pyranyl claim 1 , tetrahydrothiophenyl claim 1 , thietanyl claim 1 , thietanyl-oxide claim 1 , and thietanyl-dioxide claim 1 ,{'sub': 3', '3', '3, 'wherein each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, ...

Подробнее
Номер записи: 24
07-01-2016 дата публикации

NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES

Номер: US20160002157A1
Автор: Xu Lina, Yu Chongxi
Принадлежит:

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate. 2. A pharmaceutical composition comprising a high penetration prodrug according to ; a compound comprising a structure selected from the group consisting of Structure NSAID-1 claim 1 , Structure NSAID-2 claim 1 , Structure NSAID-3 claim 1 , Structure NSAID-4 claim 1 , Structure NSAID-5 claim 1 , Structure NSAID-6 claim 1 , Structure NSAID-7 claim 1 , Structure NSAID-8 claim 1 , Structure NSAID-9 claim 1 , Structure NSAID-10 claim 1 , Structure NSAID-11 claim 1 , Structure NSAID-12 claim 1 , and Structure NSAID-13; an aromatic-L-amino-acid decarboxylase inhibitor selected from the group consisting of carbidopa claim 1 , benserazide claim 1 , difluromethyldopa claim 1 , and α-methyldopa; a catechol-O-methyl transferase inhibitor selected from the group consisting of entacapone and tolcapone; and a pharmaceutically acceptable carrier.3. The pharmaceutical composition according to claim 2 , the pharmaceutically acceptable carrier being selected from the group consisting of alcohol claim 2 , acetone claim 2 , ester claim 2 , cellulose claim 2 , mannitol claim 2 , croscarmellose sodium claim 2 , vegetable oil claim 2 , ...

Подробнее
Номер записи: 25
02-01-2020 дата публикации

BIARYL COMPOUND, PREPARATION METHOD AND USE THEREOF

Номер: US20200002280A1
Автор: Huang Yafei, Qiu Ruomeng, Tang Ting, Wang Yonghui
Принадлежит:

The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases. 2. The compound of Formula (I) or (II) or the pharmaceutically acceptable salt thereof according to claim 1 , wherein:{'sub': 1', '2', '3', '3', '5', '3', '6', '3', '6', '9', '10', '1', '2', '3', '2', '6', '3', '7', '1', '2', '3', '2', '6, 'claim-text': {'sub': 9', '10', '1', '6', '3', '6', '3', '8', '9', '10, 'wherein, R, Rare each independently selected from a group consisting of hydrogen, C-Calkyl, C-Ccycloalkyl and C-Cheterocycloalkyl, or Rand Rform a cyclic group having four to seven ring members together with the nitrogen atom to which they attach; the cyclic group contains or does not contain a second heteroatom selected from oxygen as a ring member.'}, 'R, Rand Rare each independently selected from a group consisting of hydrogen, C-Calkyl, C-Ccycloalkyl, C-Cheterocycloalkyl containing one oxygen atom, and —NRR, or any two of R, Rand Rform C-Calkyl alkenyl or C-Ccycloalkyl alkenyl, or R, Rand Rform C-Calkyl alkynyl;'}3. The compound of Formula (I) or (II) or the pharmaceutically acceptable salt thereof according to claim 2 , wherein Ris selected from a group consisting of C-Calkyl claim 2 , C-Ccycloalkyl claim 2 , C-Coxoheterocycloalkyl claim 2 , phenyl substituted with one or more R; pyridyl substituted with one or more R; pyrimidinyl substituted with one or more R; pyridone substituted with one or more R claim 2 , pyrazolyl substituted with one or more R claim 2 , pyrrolyl substituted with one ...

Подробнее
Номер записи: 26
05-01-2017 дата публикации

ANIONIC SURFACTANTS

Номер: US20170002295A1
Автор: Arhancet Graciela B., Grady Brian, Harwell Jeff, Long Scott A., Yu Guangzhe
Принадлежит: Board of Regents of the University of Oklahoma

Sulfur-containing compounds comprising hydrophobic ester moieties and carboxylate moieties, wherein the compounds have surfactant properties, compositions comprising the compounds, and methods of using the compounds or compositions for cleaning purposes. 2. The compound of claim 1 , wherein Y is hydrogen claim 1 , Ris C-Calkyl claim 1 , Ris C-Calkyl or C-Calkenyl claim 1 , k is from 1 to 10 claim 1 , and n is from 1 to 3.3. The compound of claim 2 , wherein Y is an alkali metal claim 2 , Ris methyl claim 2 , Z is sulfur or sulfoxide claim 2 , and n is 2.4. The compound of claim 1 , wherein Y is a cation other than hydrogen claim 1 , Ris C-Calkyl claim 1 , Ris C-Calkyl or C-Calkenyl claim 1 , k is from 1 to 10 claim 1 , and n is from 1 to 3.5. The compound of claim 4 , wherein Y is an alkali metal claim 4 , Ris methyl claim 4 , Z is sulfur or sulfoxide claim 4 , and n is 2.6. The compound of claim 4 , wherein the compound has surfactant properties.7. The compound of claim 4 , wherein the compound has a critical micelle concentration (CMC) in water at room temperature and atmospheric pressure.8. The compound of claim 4 , wherein the compound is used as a cleaning agent in health and personal care products or cosmetic products; a detergent or emulsifying agent in household or industrial laundry products or cleaning products; a surfactant claim 4 , emulsifying agent claim 4 , or lubricant in pet or livestock feed or feed ingredients; a wetting agent in agricultural applications claim 4 , textile industry applications claim 4 , or construction applications; a foaming agent in ore mining operations claim 4 , drilling operations claim 4 , waste treatment applications claim 4 , or fire-fighting applications; an emulsifying agent in petroleum production claim 4 , oil cleanup procedures claim 4 , mining operations claim 4 , and other industries; a demulsifying agent in chemical process industry; or a surfactant in oil recovery claim 4 , oil drilling or crude oil refining ...

Подробнее
Номер записи: 27
11-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180007911A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.4. A molecule according to claim 1 , wherein Ris F or Cl.5. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H.6. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.7. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.8. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHOCHCH claim 1 , CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHCHCH claim 1 , CHCHCHCHCHCH claim 1 , CHCH(CH) claim 1 , CHcyclopropyl claim 1 , CHCHcyclopropyl claim 1 , CHcyclobutyl claim 1 , CHphenyl claim 1 , CHCHphenyl claim 1 , CHC═CH claim 1 , CHC═CH claim 1 , CHCF claim 1 , CHCHF claim 1 , CHCHCF claim 1 , CHCFCF claim 1 , CHCHCHCF claim 1 , CHCHCFCF claim 1 , CHCFCFCF claim 1 , CHCHCHCHF claim 1 , CHCHSCH ...

Подробнее
Номер записи: 28
14-01-2016 дата публикации

PHARMACEUTICAL USES OF SULFUR-CONTAINING COMPOUND

Номер: US20160009642A1
Автор: CHEN Chih-Yi, CHEN SHUO-CHUEH, CHIEN YI-CHUNG, HUANG CHIUNG-YAO, Pan Chun-Hsu, SHEU Jyh-Horng, Wu Chieh-Hsi
Принадлежит:

The invention relates to uses of the sulfur-containing compound in inhibiting activities of a factor related to cancer metastasis and/or growth. Preferably, the invention relates to uses of the sulfur-containing compound in inhibiting lung cancer metastasis and/or growth. 19-. (canceled)11. (canceled)12. (canceled)13. (canceled)14. The method according to claim 10 , wherein the lung cancer is non-small cell lung carcinoma.15. The method according to claim 10 , wherein the lung cancer is Lewis lung carcinoma.16. The method according to claim 10 , wherein the compound is administered by injection. 1. Field of the InventionThe invention relates to uses of a sulfur-containing compound. Said sulfur-containing compound has ability to inhibit activities of a factor related to cancer metastasis and/or growth and to inhibit lung cancer metastasis and/or growth.2. Description of the Related ArtNon-small cell lung cancer (NSCLC) is one of the main causes of cancer death, and its incidence is increasing. Surgery, radiotherapy, and chemotherapy are the major treatment methods to reduce lung cancer mortality (Saba, N. F.; Khuri, F. R. Chemoprevention strategies for patients with lung cancer in the context of screening. 2005, 7, 92-99), however, these treatments have harmful side effects on normal healthy cells in the human body. Therefore, it is important to discover new agents to treat lung cancer safely without affecting the body's healthy cells. The deregulation of signaling pathways such as PI3K/Akt is often implicated in the pathogenesis of NSCLC (Li, C. M.; Narayanan, R.; Lu, Y.; Hurh, E.; Coss, C. C.; Barrett, C. M.; Miller, D. D.; Dalton, J. T. 2-Arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways in cancer cells: 5′-AMP-activated protein kinase (AMPK)/mTOR and PI3K/Akt/mTOR pathways. 2010, 37, 1023-1030). Thus, the need for the accelerated development of effective NSCLC therapies is critical. At present, the design of new therapeutic strategies ...

Подробнее
Номер записи: 29
14-01-2016 дата публикации

POTENT AND SELECTIVE INHIBITORS OF MONOAMINE TRANSPORTERS; METHOD OF MAKING; AND USE THEREOF

Номер: US20160009644A1
Автор: Cao Jianjing, Newman Amy Hauck, OKUNOLA-BAKARE OLUYOMI M
Принадлежит: THE UNITED STATES OF AMERICA, AS REPRESENTED BY TH SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICE

Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds. 2. A compound or salt of in which each of Rand Rindependently is an optionally substituted C-Caryl group.3. A compound or salt of in which Y is S or S(O).4. A compound or salt of any one of in which Z is O or 2H.5. A compound or salt of any one of wherein the substitution on Rand Rare independently chosen from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , C-Calkyl claim 1 , —COOH claim 1 , —CHO claim 1 , —CONH claim 1 , C-Calkoxy claim 1 , C-Calkanoyl claim 1 , mono- or di-C-Calkylamino claim 1 , C-Chaloalkyl claim 1 , or C-Chaloalkoxy.6. A compound or salt of any one of wherein when Rand Rtogether with the adjacent nitrogen atom form a substituted heterocycloalkyl or substituted mono- or bicyclic heteroaryl claim 1 , each substitution is independently chosen from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , C-Calkyl claim 1 , —COOH claim 1 , —CHO claim 1 , —CONH claim 1 , C-Calkoxy claim 1 , C-Calkanoyl claim 1 , mono- or di-C-Calkylamino claim 1 , C-Chaloalkyl claim 1 , or C-Chaloalkoxy.9. A compound or salt of in whichY is S or S(O);Z is 2H; and{'sub': '3', 'Ris ethyl, propyl, butyl, allyl, cyclopropylmethyl, 2-arylethyl, 3-arylpropyl, or 4-arylbutyl.'}11. A compound or salt of in which each of Rand Rindependently is an optionally substituted C-Caryl group;Y is S or ...

Подробнее
Номер записи: 30
09-01-2020 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20200009103A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jamo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, which is ...

Подробнее
Номер записи: 31
08-01-2015 дата публикации

TRITERPENOIDS AND COMPOSITIONS CONTAINING THE SAME

Номер: US20150011627A1
Автор: Fu Liangfeng, Gribble Gordon W., LIBY Karen T., SPORN Michael B.
Принадлежит: Trustees of Dartmouth College

The present invention provides triterpenoids produced from natural compounds such as oleanolic acid, ursolic acid, betulinic acid, and hederagenin. 6. A pharmaceutical composition comprising the compound of , , , or in admixture with a pharmaceutically acceptable carrier. This patent application is a continuation of U.S. patent application Ser. No. 13/466,456 filed May 8, 2012, which is herein incorporated by reference in its entirety.One of the major needs in cancer prevention is the development of effective and safe new agents for chemoprevention. In particular, there is a need for chemopreventative agents targeted at mechanisms known to be involved in the process of carcinogenesis. In recent years, there has been a resurgence of interest in the study of mechanisms of inflammation that relate to carcinogenesis and in the use of such mechanisms as the basis for development of new chemopreventative agents.The concept that inflammation and carcinogenesis are related phenomena has been the subject of many studies that have attempted to link these two processes in a mechanistic fashion (Sporn & Roberts (1986) 78:329-332; Ohshima & Bartsch (1994) 305:253-264). The enzymes that mediate the constitutive synthesis of nitric oxide and prostaglandins from arginine and arachidonate, respectively, have relative little significance for either inflammation or carcinogenesis. In contrast, inducible nitric oxide synthase (iNOS) and inducible cycloxygenase (COX-2) both have critical roles in the response of tissues to injury or infectious agents (Moncada, et al. (1991) 43:109-142; Nathan & Xie (1994) 78:915-918; Siebert & Masferrer (1994) 4(1):17-23; Tamir & Tannebaum (1996) 1288:F31-F36). These inducible enzymes are essential components of the inflammatory process, the ultimate repair of injury, and carcinogenesis. While physiological activity of iNOS and COX-2 may provide a definite benefit to the organism, aberrant or excessive expression of either iNOS or COX-2 has been ...

Подробнее
Номер записи: 32
10-01-2019 дата публикации

Novel Compounds

Номер: US20190010135A1
Автор: Ebere F. IGBOKO, Feng Ren, Hongfu Lu, Lindong Zhu, Paul Bryan Wren, Ting Yang, Weichun Chen, Xichen Lin, Zhongmiao Xu
Принадлежит: GlaxoSmithKline Intellectual Property Development Ltd

The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

Подробнее
Номер записи: 33
17-01-2019 дата публикации

Selective androgen receptor degrader (sard) ligands and methods of use thereof

Номер: US20190015387A1
Автор: Dong-Jin Hwang, Duane D. Miller, Ramesh Narayanan, Thamarai Ponnusamy, Yali He
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Подробнее
Номер записи: 34
21-01-2021 дата публикации

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO

Номер: US20210015098A1
Автор: Eckelbarger Joseph D., Heemstra Ronald J., Hunter Ricky, JR. Ronald, Martin Timothy P., Ross, Trullinger Tony K., Walsh Martin J.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 3. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , SF claim 1 , and CF.4. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , SF claim 1 , and CF.5. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , SF claim 1 , and CF.6. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , SF claim 1 , and CF.7. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , SF claim 1 , and CF.8. A molecule according to wherein at least one of R claim 1 , R claim 1 , and R claim 1 , is SF.9. A molecule according to wherein Ris Cl.10. A molecule according to wherein Ris Cl.11. A molecule according to wherein Rand Rare not the same substituent.12. A molecule according to wherein Qis O.13. A molecule according to wherein Qis O.14. A molecule according to wherein Ris H.15. A molecule according to wherein Ris H.16. A molecule according to wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , CH claim 1 , and CF.17. A molecule according to wherein Ris selected from the group consisting of F claim 1 , Cl claim 1 , CH claim 1 , and OCH.18. A molecule according to wherein Ris ...

Подробнее
Номер записи: 35
16-01-2020 дата публикации

S1PR2 ANTAGONISTS AND USES THEREFOR

Номер: US20200017494A1
Автор: McMaster Christopher, Simms Gordon
Принадлежит:

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-2-cyano-1-(2,6-dichloropyridin-4-yl)-3-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein:{'sub': 1', '12', '12, 'Gis CRand Ris H; and,'}{'sub': 'd', 'Ris H.'}3. The compound of claim 2 , selected from the group consisting of:(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-methylguanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-ethyl-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-propylguanidine;(E)-1-butyl-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-isopropyl-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine;(E)-1-benzyl-2-cyano-3-(2,6-dichloropyridin-4-yl)-1-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine; and,a diastereomer of the foregoing, wherein the cyano group is in the (Z) form; or the pharmaceutically acceptable salt of any of the foregoing.4. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein:{'sub': 1', '12', '12, 'Gis CRand Ris H; and,'}{'sub': 'c', 'Ris H.'}5. The compound of claim 4 , selected from the group consisting of:(Z)-2-cyano-1-(2,6-dichloropyridin-4-yl)-3-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)-1-methylguanidine;(Z)-2-cyano-1-(2,6-dichloropyridin-4 ...

Подробнее
Номер записи: 36
25-01-2018 дата публикации

COMPOUND CONTAINING INDOLEACETIC ACID CORE STRUCTURE AND USE THEREOF

Номер: US20180022700A1
Автор: RAN Ruiqiong
Принадлежит:

Disclosed are a compound as shown by the following formula 1, and a pharmaceutically acceptable salt, an ester, a hydrate and an organic solvate thereof. In the formula (1), the groups Rto Rare independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, C-Calkyl, C-Calkoxy, carbonyl, hydroxyl, amino, azido, carboxyl and C-Calkylsulfinyl, respectively; and X is a carbon or nitrogen atom; Y is selected from the following groups: a single bond, C-Calkylene, C-Carylene and C-Cheteroarylene; and n is an integer from 5 to 20. Also provided in the present invention are a pharmaceutical composition containing the compound, and use thereof in the field of tumor therapy. 2. The compound according to claim 1 , characterized in that the groups Rto Rare each independently selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , C-Calkyl claim 1 , C-Calkoxy claim 1 , carbonyl and hydroxyl; Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , bromine claim 1 , iodine claim 1 , azido and C-Calkylsulfinyl; Rto Rare each independently selected from hydrogen claim 1 , C-Calkyl and C-Calkoxy; R claim 1 , R claim 1 , Rto Rare each independently selected from hydrogen claim 1 , C-Calkyl claim 1 , C-Calkoxy and amino; X is a carbon atom or a nitrogen atom; Y is selected from the group consisting of single bond claim 1 , C-Calkylene claim 1 , C-Carylene and C-Cheteroarylene; and n is an integer of 5 to 20 claim 1 , preferably n=10.4. A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) the compound according to , or a pharmaceutically acceptable salt, ester, hydrate, organic solvate, prodrug, metabolic intermediate, and metabolite thereof;'}(ii) optionally one or more of pharmaceutically acceptable fillers, carriers and diluents; and(iii) optionally pharmaceutically active component different from the component (i).5. ...

Подробнее
Номер записи: 37
10-02-2022 дата публикации

HEAT-SENSITIVE RECORDING MATERIAL

Номер: US20220041923A1
Автор: HORN Michael, Stalling Timo
Принадлежит:

Described are colour developers of formula (I) Ar—SO—NH—CH—SO—CH—NH—CO—NH—Ar(I), a heat-sensitive recording material, comprising a carrier substrate and also a heat-sensitive, colour-forming layer comprising at least one colour former and at least one phenol-free colour developer, the at least one colour developer being the compound of formula (I), and a method for producing this heat-sensitive recording material. 1. A compound of formula (I) ,{'br': None, 'sup': 1', '2, 'sub': 2', '6', '4', '2', '6', '4, 'Ar—SO—NH—CH—SO—CH—NH—CO—NH—Ar\u2003\u2003(I),'}{'sup': 1', '2, 'wherein Arand Arare an unsubstituted or substituted phenyl group; and'}{'sup': 1', '2, 'sub': 2', '6', '4', '2', '6', '4, 'wherein the Ar—SO—NH group and the Ar—NH—CO—NH group are arranged in the 4 and 4′ position or in the 3 and 3′ position, to the —CH—SO—CHgroup.'}2. The compound according to claim 1 , wherein Aris a phenyl group.3. The compound according to claim 1 , wherein Aris a phenyl group.4. The compound according to claim 1 , wherein Aris substituted with at least one C-Calkyl group claim 1 , an alkenyl group claim 1 , an alkynyl group claim 1 , a benzyl group claim 1 , a formyl group claim 1 , a CN group claim 1 , a halogen group claim 1 , an NOgroup claim 1 , an RO group claim 1 , an R—CO group claim 1 , an ROC group claim 1 , an R—OCO group claim 1 , an R—SOO group claim 1 , an R—O—SOgroup claim 1 , an R—SO—NH group claim 1 , an R—NH—SOgroup claim 1 , an R—NH—CO group or an R—CO—NH group claim 1 , wherein R is a C-Calkyl group claim 1 , an alkenyl group claim 1 , an alkynyl group claim 1 , a phenyl group claim 1 , a tolyl group claim 1 , or a benzyl group.5. The compound according to claim 1 , wherein Aris a phenyl group substituted once.6. The compound according to claim 1 , wherein Aris substituted with at least one C-Calkyl group claim 1 , an alkenyl group claim 1 , an alkynyl group claim 1 , a benzyl group claim 1 , a formyl group claim 1 , a CN group claim 1 , a halogen group claim 1 ...

Подробнее
Номер записи: 38
02-02-2017 дата публикации

Substituted Aromatic Sulfur Compounds and Methods of Their Use

Номер: US20170029367A1
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: 39
17-02-2022 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20220047540A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jarmo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, Which is ...

Подробнее
Номер записи: 40
31-01-2019 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20190029990A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jarmo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, which is ...

Подробнее
Номер записи: 41
11-02-2016 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20160037779A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

Подробнее
Номер записи: 42
08-02-2018 дата публикации

BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA

Номер: US20180036296A1
Автор: GOLDMAN Erick A., HUANG Wenrong, Li Wenhao, Scarborough Robert M., Song Yonghong, Wang Lingyan, Zhang Penglie, Zhu Bing-Yan, ZUCKETT Jingmei
Принадлежит:

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. 172.-. (canceled)74. The method of claim 73 , wherein the salt is the maleate salt.75. The method of claim 73 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.76. The method of claim 75 , wherein the pharmaceutical composition is in capsule form.78. The method of claim 77 , wherein the salt is the maleate salt.79. The method of claim 77 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.80. The method of claim 79 , wherein the pharmaceutical composition is in capsule form.82. The method of claim 81 , wherein the salt is the maleate salt.83. The method of claim 81 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.84. The method of claim 83 , wherein the pharmaceutical composition is in capsule form. This invention relates to novel compounds which are potent and highly selective inhibitors of isolated factor Xa or when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, fIXa) or the fibrinolytic cascades (e.g. plasminogen activators, plasmin). In another aspect, the present invention relates to novel monoamidino-containing compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions thereof which are useful as potent and specific inhibitors of blood ...

Подробнее
Номер записи: 43
24-02-2022 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20220055977A1
Автор: HEMEON Ivan William, SAFINA Brian, SUTHERLIN Daniel
Принадлежит:

The invention provides a method of treating a disease or condition in a mammal by administering a compound having the general formula I: 5. The method of claim 1 , wherein ring “B” is selected from the group consisting of cyclobutyl claim 1 , cyclopentyl claim 1 , and cyclohexyl.14. The method of claim 1 , wherein wherein n is 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5.15. The method of claim 1 , wherein ring “A” is a 6-15 membered carbocycle claim 1 , a 6-10 membered aryl claim 1 , or a 4-6 membered heterocycle.18. The method of claim 1 , wherein Xis absent; Xis —O—; m is 1; and -(L)- is an optionally substituted Calkylene.19. The method of claim 1 , wherein wherein:ring “A” is a 6-15 membered carbocycle, a 6-10 membered aryl, or a 4-6 membered heterocycle;{'sup': '1', 'Xis absent;'}{'sup': '2', 'Xis —O—;'}m is 1; and{'sub': '1-4', '-(L)- is an optionally substituted Calkylene.'} This application is a divisional of U.S. application Ser. No. 16/685,335, filed 15 Nov. 2019, which is a continuation of U.S. application Ser. No. 15/896,970, filed 14 Feb. 2018, now abandoned, which is a continuation of International Application No. PCT/US2016/048477, filed 24 Aug. 2016, which claims the benefit of U.S. Provisional Application No. 62/210,891, filed 27 Aug. 2015. The entire content of the applications referenced above are hereby incorporated by reference.The present invention relates to organic compounds useful for therapy in a mammal, and in particular to inhibitors of sodium channel (e.g., NaV1.7) that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the modulation of sodium channels.Voltage-gated sodium channels are transmembrane proteins that initiate action potentials in nerve, muscle and other electrically excitable cells, and are a necessary component of normal sensation, emotions, thoughts and movements (Catterall, W. A., Nature (2001), Vol. 409, pp. 988-990). These channels ...

Подробнее
Номер записи: 44
06-02-2020 дата публикации

PRODRUGS OF GAMMA-HYDROXYBUTYRIC ACID, COMPOSITIONS AND USES THEREOF

Номер: US20200039917A1
Автор: Xiang Jia-Ning, Xu Xuesong, Zhang Xuan
Принадлежит:

The present disclosure discloses prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof. 2. The composition of claim 1 , wherein the composition is a solid.3. The composition of claim 1 , wherein the composition further comprises a solvent for dissolving or dispersing the compound.4. The composition of claim 3 , wherein the solvent comprises water.5. The composition of claim 1 , wherein the composition is in a liquid dosage form.6. The composition of claim 1 , wherein the composition further comprises a flavoring agent claim 1 , sucrose claim 1 , lactose claim 1 , cellulose sugar claim 1 , mannitol claim 1 , maltitol claim 1 , dextran claim 1 , sorbitol claim 1 , starch claim 1 , agar claim 1 , alginates claim 1 , chitins claim 1 , chitosans claim 1 , pectins claim 1 , tragacanth gum claim 1 , gum arabic claim 1 , gelatins claim 1 , collagens claim 1 , casein claim 1 , albumin claim 1 , synthetic or semi-synthetic polymers or glycerides claim 1 , methyl cellulose claim 1 , hydroxypropylmethyl-cellulose claim 1 , or polyvinylpyrrolidone.7. The composition of claim 1 , wherein the composition further comprises a polymeric excipient.8. The composition of claim 1 , wherein the composition comprises a tablet claim 1 , a caplet claim 1 , a capsule claim 1 , a gel cap claim 1 , granules claim 1 , a pill claim 1 , a powder claim 1 , a lozenge claim 1 , a sachet claim 1 , a cachet claim 1 , a suspension claim 1 , an emulsion claim 1 , a solution claim 1 , a slurry claim 1 , or a syrup.9. The composition of claim 1 , wherein the composition is formulated in a unit dosage form.10. The composition of claim 9 , wherein the unit dosage form has a weight from 0.5 grams to 30 grams.11. The composition of claim 10 , wherein the composition is in a liquid dosage form.12. The composition of claim 11 , further comprising a pH adjusting agent selected from sodium hydroxide claim 11 , hydrochloric acid claim 11 , or malic acid.13. The composition of claim 1 , ...

Подробнее
Номер записи: 45
15-02-2018 дата публикации

KINASE INHIBITORS

Номер: US20180044288A1
Автор: BAKER Thomas Matthew, Fyfe Matthew Colin Thor, HARBOTTLE Gareth William, Hasimbegovic Vedran, Meghani Premji, RIGBY Aaron, SAMBROOK-SMITH Colin, THOM Stephen Malcolm
Принадлежит:

There are provided compounds of formula I, 3. A compound as claimed in claim 1 , wherein Rrepresents H claim 1 , halo claim 1 , Calkyl or Calkoxy claim 1 , which latter two groups are optionally substituted by one or more fluoro atoms.4. A compound as claimed in claim 1 , wherein Rrepresents H claim 1 , halo claim 1 , cyano claim 1 , —NRR claim 1 , C(O)OR claim 1 , —C(O)NRR claim 1 , —S(O)NRR claim 1 , —NRC(O)R claim 1 , —NRS(O)R claim 1 , —NRC(O)OR claim 1 , Het claim 1 , —NRS(O)NRR claim 1 , —CHOH or —CHCN.5. A compound as claimed in claim 1 , wherein Rrepresents Hetor Rand Rindependently represent H or Calkyl claim 1 , or Rand Rtogether represent Cn-alkylene optionally interrupted between C2 and C3 by —O— or —N(R)— claim 1 , wherein Rrepresents H or Calkyl.6. A compound as claimed in claim 1 , wherein{'sup': Y', '2, 'Rrepresents H, benzyl or Hetoptionally substituted by one or more substituents selected from the group consisting of methyl, halo, hydroxy and methoxy,'}{'sup': Y', 'Y1, 'sub': 1-4', '3-6', '2', '1-2', '1-2', '2', '1-2, 'or Rand Rindependently represent Calkyl, Ccycloalkyl or phenyl, which latter three groups are optionally substituted by one or more substituents selected from the group consisting of methyl, halo, hydroxy, methoxy, NH, N(H)—Calkyl, N(Calkyl), C(O)OH and C(O)O—(Calkyl),'}{'sup': X', 'Y', 'X2', 'X2, 'sub': 4-5', '1-2, 'or Rand Rtogether represent Cn-alkylene optionally interrupted between C2 and C3 by —O— or —N(R)—, wherein Rrepresents H or Calkyl.'}7. A compound of formula I claim 1 , la or Ib as claimed in claim 1 , wherein Rand Rindependently represent H or halo.8. A compound as claimed in claim 1 , wherein:{'sup': 1D', '2, 'sub': 3-7', '1-2', '2', '3-5', '1-2', '1-2, 'Rrepresents trimethylsilyl, Calkyl, C(Calkyl)-C≡CH, Ccycloalkyl, phenyl or Het, which latter three groups are optionally substituted by one or more substituents selected from the group consisting of Calkyl, halo and Calkoxy; and'}{'sup': '2', 'Hetrepresents a 5- or 6- ...

Подробнее
Номер записи: 46
03-03-2022 дата публикации

Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases

Номер: US20220064157A1
Автор: Chongxi Yu, Lina Xu
Принадлежит: Techfields Pharma Co Ltd

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Подробнее
Номер записи: 47
25-02-2021 дата публикации

Immunomodulator compounds

Номер: US20210052514A1
Автор: Christopher Lange, Darren J. Mcmurtrie, JU Yang, Penglie Zhang, Rajinder Singh, Sreenivas Punna, Viengkham Malathong
Принадлежит: Chemocentryx Inc

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Подробнее
Номер записи: 48
25-02-2016 дата публикации

Novel compounds

Номер: US20160052898A1
Автор: Andrea Hagebarth, Anja Richter, Daniel Basting, Dirk Schneider, Eckhard Bender, Florian Puehler, Franziska SIEGEL, Kai Thede, Ludwig Zorn, Manfred Möwes, Ningshu Liu, Philip Lienau, Stefan Golz, Ursula MÖNNING, William Johnston Scott
Принадлежит: Bayer Pharma AG

The present invention relates to substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disorder, as a sole agent or in combination with other active ingredients.

Подробнее
Номер записи: 49
25-02-2021 дата публикации

Novel thyromimetics

Номер: US20210053917A1
Автор: Bradley Backes, Thomas von Geldern
Принадлежит: Autobahn Therapeutics Inc

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.

Подробнее
Номер записи: 50
23-02-2017 дата публикации

Sulfur derivatives as chemokine receptor modulators

Номер: US20170050925A9
Автор: Haiqing Yuan, John E. Donello, Michael E. Garst, Richard L. Beard, Veena Viswanath, Xiaoxia Liu
Принадлежит: Allergan Inc

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Подробнее
Номер записи: 51
23-02-2017 дата публикации

Benzamide Compounds and Related Methods of Use

Номер: US20170050926A1
Автор: Kazantsev Aleksey G., Khanfar Mohammad, Silverman Richard B., Wang Hua
Принадлежит:

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease. 3. The compound of wherein Ris selected from phenyl claim 2 , 2- claim 2 , 3- claim 2 , and 5-pyridinyl claim 2 , 2-pyrimidinyl claim 2 , 3-pyridazinyl claim 2 , 2-thiazolyl claim 2 , methylene-2-thiazolyl claim 2 , 2-oxadiazolyl claim 2 , 5-isoxazolyl claim 2 , 2-nicotintate and 2-nicotinamide moieties; and Ris selected from phenyl and 2-pyridinyl moieties.4. The compound of wherein a least one of Rand Ris substituted claim 3 , said substituents independently selected from halo claim 3 , cyano claim 3 , C-Calkyl claim 3 , substituted alkyl claim 3 , alkoxy claim 3 , methylsulfinyl claim 3 , hydroxy claim 3 , methylsulfonyl claim 3 , amino claim 3 , alkylamino claim 3 , dialkylamino claim 3 , aceto claim 3 , acetamido claim 3 , nitro claim 3 , aminoalkyl claim 3 , methylthio and 1-hydroxyethyl substituents and combinations thereof.6. The compound of wherein Y is alkyl-substituted methylene and Z is O claim 5 , said alkylene moiety providing a chiral center.7. The compound of wherein said methylene substituent is methyl claim 6 , said compound selected from the (R) and (S) enantiomers.9. The compound of wherein Z is selected from amino claim 8 , alkylamino claim 8 , thio claim 8 , sulfinyl and sulfonyl moieties. This application is a continuation of and claims priority to and the benefit of application Ser. No. 14/139,763 filed on Dec. 23, 2013 and issued as U.S. Pat. No. 9,371,277 on Jun. 21, 2016, which claimed priority to and the benefit of application Ser. No. 61/745,056 filed Dec. 21, 2012—each of which is incorporated herein by reference in its entirety.This invention was made with government support under grant number NS066912 awarded by the National Institutes of Health. The government has certain rights in the invention.Huntington's disease (HD) is an autosomal dominant inherited ...

Подробнее
Номер записи: 52
26-02-2015 дата публикации

Selective androgen receptor modulators

Номер: US20150057452A1
Автор: James David Rozzell, Raymond Mccague
Принадлежит: CATYLIX Inc

Compounds having therapeutic potential as androgen receptor modulators, and methods of making such compounds, are provided. The compounds are structurally related to bicalutamide but bear at least one difluoromethyl or C 2 to C 5 perfluoroalkyl group instead of a trifluoromethyl group.

Подробнее
Номер записи: 53
03-03-2016 дата публикации

COMPOSITION CONTAINING A DIBENZOYLMETHANE SCREENING AGENT AND A HYDROPHILIC OR WATER-SOLUBLE MEROCYANIN UV-SCREENING AGENT; PROCESS FOR PHOTOSTABILIZING THE DIBENZOYLMETHANE SCREENING AGENT

Номер: US20160058682A1
Автор: Muller Benoit, Richard Herve
Принадлежит:

The present invention relates to a cosmetic composition containing a combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II) below: 2. The process according to claim 1 , in which the compounds of formula (I) are chosen from those for which the following conditions are satisfied:{'sub': 1', '1', '8, 'Rdenotes hydrogen; a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms,'}{'sub': 2', '1', '8', '5', '6, 'Rdenotes a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms or a C-Ccycloalkyl radical,'}{'sub': 3', '5', '5, 'Rdenotes a group —COOR, —CN or —CONHR,'}{'sub': 4', '6', '6', '2', '6, 'Rdenotes a group —COOR, —CONHRor —SOR,'}{'sub': 5', '1', '12, 'Rdenotes a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms,'}n is equal to 1 or 2;{'sub': 1', '2', '5', '6, 'claim-text': either an alkylsulfonate radical in its acid or salified form', 'or one or two hydroxyl radicals., 'with at least one or two of the radicals R, R, R, Rcontaining'}5. The process according to claim 1 , in which the compounds of formula (II) are chosen from those for which the following conditions are satisfied:{'sub': 1', '1', '10, 'Rdenotes hydrogen; a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms,'}{'sub': 2', '1', '10', '5', '6, 'Rdenotes a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms; a C-Ccycloalkyl,'}{'sub': 3', '5, 'Rdenotes a group —COORor CN,'}{'sub': 4', '6', '2', '6, 'Rdenotes a group —COORor —SOR,'}{'sub': 5', '1', '12, 'Rdenotes a linear or branched C-Calkyl radical optionally containing from 1 to 3 oxygen atoms,'}{'sub': 2', '3', '3, 'Z is —(CH)— which may or may not be substituted with two groups CH,'}n is equal to 1 or 2;{'sub': 1', '2 ...

Подробнее
Номер записи: 54
10-03-2022 дата публикации

CRYSTALLINE PHARMACEUTICAL AND METHODS OF PREPARATION AND USE THEREOF

Номер: US20220073500A1
Автор: Burnier John, Gadek Thomas, NAUD Frederic
Принадлежит: NOVARTIS PHARMACEUTICALS CORPORATION

Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. 167-. (canceled)69. The method of claim 68 , wherein said compound has a purity of greater than about 98 percent.70. The method of claim 68 , wherein said compound comprises at least about 95 percent of an S-enantiomer.71. The method of claim 68 , wherein said compound is a sodium salt.72. The method of claim 68 , wherein the subject suffers from diabetic retinopathy.73. The method of claim 68 , wherein the subject suffers from diabetic macular edema. This application is a continuation of U.S. application Ser. No. 13/289,172 filed Nov. 4, 2011, which is a continuation of U.S. application Ser. No. 12/386,361 filed on Apr. 15, 2009, issued as U.S. Pat. No. 8,080,562 on Dec. 20, 2011, which claims the benefit of U.S. Provisional Application No. 61/045,142, filed Apr. 15, 2008, which applications are incorporated herein by reference.Cross reference is made to co-pending applications U.S. application Ser. No. 12/288,330, filed on Oct. 17, 2008; U.S. Ser. No. 12/386,359, filed on Apr. 15, 2009; U.S. Ser. No. 12/386,363, filed on Apr. 15, 2009; and U.S. Ser. No. 12/386,347, filed on Apr. 15, 2009, which are hereby incorporated by reference in their entirety.The compound of Formula I:has been found to be an effective inhibitor of Lymphocyte Function-Associated Antigen-1 (LFA-1) interactions with the family of Intercellular Adhesion Molecules (ICAM), and has desirable pharmacokinetic properties, including rapid systemic clearance. Improved forms, including crystalline forms, and their uses in treatment of disorders mediated by the interaction of LFA-1 and ICAM are described herein. Novel polymorphs of the compound of Formula I which may afford improved purity, stability, bioavailability and other ...

Подробнее
Номер записи: 55
02-03-2017 дата публикации

N-ARYLAMIDINE-SUBSTITUTED TRIFLUOROETHYL SULFIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES

Номер: US20170057914A1
Автор: ALIG Bernd, Becker Angela, CEREZO-GALVEZ SILVIA, FISCHER Reiner, Goergens Ulrich, Gomibuchi Takuya, HAHN Julia Johanna, ILG Kerstin, ITO Masahito, KOEHLER Adeline, Moradi Wahed Ahmed, Schwarz Hans-Georg, Shibuya Katsuhiko, Shimojo Eiichi, VOERSTE Arnd, Yamazaki Daiei
Принадлежит:

The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) This application is a divisional application of U.S. application Ser. No. 14/366,715 (filed Jun. 19, 2014), which is a §371 National Stage Application of PCT/EP2012/075269 (filed Dec. 12, 2012), which claims priority to EP 11194855.0 (filed Dec. 21, 2011), the contents of each of which are incorporated herein by reference.Field of the InventionThe present invention relates to novel N-arylamidine-substituted trifluoroethyl sulfide derivatives, to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.Description of Related ArtVarious substituted N-arylamidines and their insecticidal and acaricidal action have already been described in the literature in WO 2007/131680.On application, the active compounds already known from the publications mentioned above have disadvantages, be it that they may have no or else only insufficient insecticidal and/or acaricidal activity against animal pests, in particular at relatively low application rates.Accordingly, it is an object of the present invention to provide corresponding N-arylamidine-substituted trifluoroethyl sulfide derivatives which can be employed as insecticides and/or acaricides with satisfactory insecticidal and/or acaricidal activity against animal pests, in particular at relatively low application rates, with high selectivity and improved compatibility in crops of useful plants.The present invention now provides novel compounds of the formula (I)in whichIf appropriate, the compounds of the formula (I) may be present in various polymorphic forms or as mixtures of different polymorphic forms. Both the pure polymorphs and the polymorph mixtures are provided by the invention and can be used according to the invention.The compounds of the formula (I) optionally comprise diastereomers or enantiomers and also rotamers, tautomers and ...

Подробнее
Номер записи: 56
09-03-2017 дата публикации

CYCLIC COMPOUNDS

Номер: US20170066737A1
Автор: Katoh Taisuke, Kitamoto Naomi, KOBAYASHI Toshitake, NARA Hiroshi, NEGORO Nobuyuki, Saitoh Morihisa, Tanaka Takahiro, WADA Yasufumi, Yamasaki Masashi
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of inflammatory disease and/or central nervous system disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: 2. The compound or salt of claim 1 , wherein Ring A is cyclopentene or cyclohexene.3. The compound or salt of claim 1 , wherein Ring B is a benzene ring optionally substituted by 1 to 3 substituent(s) selected from a halogen atom and a Calkyl group.4. The compound or salt of claim 1 , wherein as to Rand R claim 1 , (1) Rand Rare both hydrogen atoms claim 1 , or (2) one of Rand Ris a hydrogen atom claim 1 , and the other is a hydroxy group claim 1 , or Rand Rmay bond together to form a 3- to 8-membered monocyclic non-aromatic heterocycle optionally substituted by 1 to 3 Calkyl group(s) optionally substituted by 1 to 3 substituent(s) selected from a hydroxy group and a Calkoxy group.5. The compound or salt of claim 1 , wherein W is CHor O.6. The compound or salt of claim 1 , wherein Ris a Calkoxy group optionally substituted by 1 to 3 Ccycloalkyl group(s) optionally substituted by 1 to 3 Calkyl group(s).7. The compound or salt of claim 1 , whereinRing A is cyclopentene or cyclohexene;{'sub': '1-6', 'Ring B is a benzene ring optionally substituted by 1 to 3 substituent(s) selected from a halogen atom and a Calkyl group;'}{'sup': 1', '2', '1', '2', '1', '2', '1', '2, 'sub': 1-6', '1-6, 'as to Rand R, (1) Rand Rare both hydrogen atoms, or (2) one of Rand Ris a hydrogen atom, and the other is a hydroxy group, or Rand Rmay bond together to form a 3- to 8-membered monocyclic non-aromatic heterocycle, which is optionally substituted by 1 to 3 Calkyl group(s) optionally substituted by 1 to 3 substituent( ...

Подробнее
Номер записи: 57
17-03-2016 дата публикации

Lipids for Therapeutic Agent Delivery Formulations

Номер: US20160074514A1
Автор: Ahmadian Mohammad, Akopian Violetta, Gaudette John A., Hou Zheng, Karmali Priya, Knopov Victor, Payne Joseph E., Safarzadeh Neda, Witte Richard P., Ying Wenbin, Yu Lei, ZHANG JUN
Принадлежит:

The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes. 2. The compound of claim 1 , wherein n and m are 1 or 2.3. The compound of claim 1 , wherein X is absent.4. The compound of claim 3 , wherein L is Calkylene.6. The compound of claim 1 , wherein X is —CH—.7. The compound of claim 6 , wherein L is —S—Calylene.8. The compound of claim 7 , wherein L is —S—CH— or —S—CH—CH—.9. The compound of claim 6 , wherein L is —S(O)—Calylene.10. The compound of claim 9 , wherein L is —S(O)—CH—CH—.11. The compound of claim 6 , wherein L is —O—Calkylene.12. The compound of claim 11 , wherein L is —O—CH—CH— or —O—CH—CH—CH—.13. The compound of claim 6 , wherein L is —O—C(O)—Calylene.14. The compound of claim 13 , wherein L is —O—C(O)—CH—CH—CH—.15. The compound of claim 1 , wherein X is S or O.16. The compound of claim 15 , wherein L is Calkylene.17. The compound of claim 16 , wherein L is —CH—CH—.18. The compound of claim 1 , wherein Rand Rare each Calkyl.19. The compound of claim 18 , wherein Rand Rare each Calkyl.20. The compound of claim 1 , wherein Rand Rare each Calkenyl.21. The compound of claim 20 , wherein Rand Rare each Calkenyl.22. The compound of claim 21 , wherein Rand Rare each oleyl or linoleyl.23. A composition comprising a cationic lipid and an ionizable cationic lipid in a lipid nanoparticle comprising a bilayer of lipid molecules.24. A composition comprising a compound of in a lipid nanoparticle comprising a bilayer of lipid molecules.25. The composition of claim 24 , wherein the compound is 5 to 50 mol % of the lipid molecules.26. The composition of claim 24 , further comprising a cationic lipid.28. The composition of claim 26 , wherein the cationic lipid is 5 to 40 mol % of the lipid molecules.29. The composition of claim 26 , wherein the molar ratio of the ionizable lipid and the cationic lipid is about 5:35 to about 35:5. This application is a divisional of U.S. patent application No. 13/913,918 ...

Подробнее
Номер записи: 58
24-03-2016 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20160083342A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит:

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 210.-. (canceled)11. A compound according to claim 1 , selected from:4-chloro-N-[5-chloro-2-(methylsulfinyl)phenyl]-3-methylbenzenesulfonamide;N-[5-chloro-2-(methylsulfinyl)phenyl]-3-nitro-4-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(methylthio)phenyl]-2-fluorobenzenesulfonamide;4-chloro-N-[5-chloro-2-(ethylthio)phenyl]-3-(trifluoromethyl)benzenesulfonamide;tert-Butyl {6-[({2-[(1-benzofuran-2-ylsulfonyl)amino]-4-chlorophenyl}thio)methyl]pyridin-2-yl}carbamate;3-{[4-chloro-2-({[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl}amino)phenyl]sulfonyl}-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(2,4-difluorophenyl)sulfonyl]amino}phenyl)thio]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(2,4-difluorophenyl)sulfonyl]amino}phenyl)sulfinyl]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(2,4-difluorophenyl)sulfonyl]amino}phenyl)sulfonyl]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(4-chloro-2-fluorophenyl)sulfonyl]amino}phenyl)thio]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(4-chloro-2-fluorophenyl)sulfonyl]amino}phenyl)sulfinyl]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(4-chloro-2-fluorophenyl)sulfonyl]amino}phenyl)sulfonyl]-N,N-dimethylpropanamide;4-chloro-N-[5-chloro-2-(methylthio)phenyl]-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(isopropylthio)phenyl]-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-{5-chloro-2-[(2-hydroxyethyl)thio]phenyl}-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(isopropylsulfinyl)phenyl]-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-{5-chloro-2-[(pyridin-2-ylmethyl)thio]phenyl}-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-{5-chloro-2-[(pyridin-3-ylmethyl)thio]phenyl}-3-(trifluoromethyl)benzenesulfonamide;2-{[4-chloro-2-({[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl}amino)phenyl]thio}-N,N-dimethylacetamide;2-{[ ...

Подробнее
Номер записи: 59
12-06-2014 дата публикации

FLUORINATED AROMATIC BIS(ACYL)-CONTAINING COMPOUNDS AND POLYESTERS PREPARED THEREFROM

Номер: US20140163250A1
Автор: Moore George G.I., Wang Lei, Yang Yu
Принадлежит: 3M INNOVATIVE PROPERTIES COMPANY

A fluorinated bis(acyl-containing compound and a fluorinated polyester formed from the fluorinated diacyl are described. More particularly, the fluorinated diacyl has an aromatic ring bonded to two acyl groups plus at least one third group that contains a perfluoroalkylsulfonamido group. The fluorinated polyesters formed from the fluorinated diacyl-containing compound can be used to provide a low energy surface with a relatively low refractive index compared to many other polyesters. 1. A compound of Formula (II){'br': None, 'sub': 2', 'y', '2y', 'y', '2y, 'sup': 3', '1, 'Rf—SO—N(R)—(CH)—Ar—(CH)-Q\u2003\u2003(II)'} Rf is a perfluoroalkyl;', {'sup': '3', 'Ris an alkyl;'}, {'sup': '1', 'Aris a phenylene or diphenylene;'}, 'y is an integer in the range of 1 to 20; and', {'sub': '2', 'sup': 4', '4, 'Q is selected from a halo or group of formula —OSO—Rwhere Ris an alkyl, perfluoroalkyl, aryl, or aryl substituted with an alkyl.'}], 'wherein'}7. A method of preparing a monosubstituted-arylene compound of Formula (XV):{'br': None, 'sup': 1', '2', '2, 'sub': 2', '2, 'Rf-L-CH—Ar—CH—W\u2003\u2003(XV)'} [{'sup': '2', 'Aris a phenylene or diphenylene;'}, {'sup': '1', 'Rfis a perfluoroalkyl with optional O or N within the chain;'}, {'sup': 2', '6, 'sub': 2', '2', '2', '4', '2', '4', '2, 'Lis selected from —O—, —SO—, —CH—O—, —CH—O—, —CH—S—, and —SO—N(R)—;'}, {'sup': '6', 'Ris a C1-C4 alkyl; and'}, 'W is a leaving group;, 'wherein [{'sup': 1', '2, 'a compound of Formula (XVI) Rf-L-H,'}, {'sub': 2', '2, 'sup': '2', 'a compound of Formula (XVII) W—CH—Ar—CH—W, and'}, 'an organic solvent,, 'the method comprising combining a base with components comprisingover a period of time effective to form the monosubstituted-arylene compound of Formula (XV).8. The method of wherein the base is more basic than sodium carbonate.9. The method of wherein the base is an organic base.10. The method of wherein the organic base is selected from 1 claim 9 ,8-diazabicyclo[5.4.0]undec-7-ene claim 9 , 1 claim ...

Подробнее
Номер записи: 60
25-03-2021 дата публикации

IONIC LIQUID CONTAINING DIVALENT CATION AND MONOVALENT ANION AND LUBRICANT COMPOSITION COMPRISING SAME

Номер: US20210087490A1
Автор: HWANG Sun Ae, Shim Yu Na, Shin Sang Hye, Song Ha Na
Принадлежит:

Disclosed are an ionic liquid, having wear resistance maintained at low temperatures and containing a divalent cation including at least one of bis(ammonium) and bis(phosphonium) and a monovalent anion including at least one of sulfonate and phosphate, and a lubricant composition including the ionic liquid. 1. An ionic liquid , comprising:a divalent cation comprising at least one of bis(ammonium) and bis(phosphonium); anda monovalent anion comprising at least one of sulfonate and phosphate.3. The ionic liquid of claim 2 , wherein in Chemical Formula 1 claim 2 , Rand Rare each independently (C1-C20)alkyl claim 2 , (C2-C20)alkenyl claim 2 , (C2-C20)alkynyl claim 2 , (C3-C7)cycloalkyl claim 2 , (C5-C20)heteroalkyl claim 2 , (C6-C20)aryl claim 2 , (C6-C20)ar(C1-C10)alkyl claim 2 , (C1-C10)alkoxy claim 2 , (C6-C20)aryloxy claim 2 , (C1-C10)alkoxycarbonyl(C1-C20)alkyl claim 2 , or (C1-C20)alkylcarbonyl.4. The ionic liquid of claim 2 , wherein in Chemical Formula 1 claim 2 , Rand Rare each independently (C1-C8)alkyl claim 2 , and Ris (CH) claim 2 , where 1≤n≤12.6. The ionic liquid of claim 5 , wherein in Chemical Formula 2 claim 5 , Rand Rare each independently (C1-C20)alkyl claim 5 , (C2-C20)alkenyl claim 5 , (C2-C20)alkynyl claim 5 , (C3-C7)cycloalkyl claim 5 , (C5-C20)heteroalkyl claim 5 , (C6-C20)aryl claim 5 , (C6-C20)ar(C1-C10)alkyl claim 5 , (C1-C10)alkoxy claim 5 , (C6-C20)aryloxy claim 5 , (C1-C10)alkoxycarbonyl(C1-C20)alkyl claim 5 , or (C1-C20)alkylcarbonyl.7. The ionic liquid of claim 5 , wherein in Chemical Formula 2 claim 5 , Rand Rare each independently (C1-C8)alkyl claim 5 , and Ris (CH) claim 5 , where 1≤n≤12.10. The ionic liquid of claim 9 , wherein in Chemical Formula 6 claim 9 , Rand Rare each independently (C1-C20)alkyl claim 9 , (C2-C20)alkenyl claim 9 , (C2-C20)alkynyl claim 9 , (C3-C7)cycloalkyl claim 9 , (C5-C20)heteroalkyl claim 9 , (C6-C20)aryl claim 9 , (C6-C20)ar(C1-C10)alkyl claim 9 , (C1-C10)alkoxy claim 9 , (C6-C20)aryloxy claim 9 , (C1-C10) ...

Подробнее
Номер записи: 61
29-03-2018 дата публикации

EBNA1 INHIBITORS AND THEIR METHOD OF USE

Номер: US20180086699A1
Автор: Lieberman Paul M., McDonnell Mark E., Messick Troy E., Reitz Allen B., Smith Garry R., Velvadapu Venkata, Zhang Yan
Принадлежит:

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection. 4. The method of claim 1 , wherein the compound is at least one selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-7-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[2-( ...

Подробнее
Номер записи: 62
21-03-2019 дата публикации

HEPATITIS B ANTIVIRAL AGENTS

Номер: US20190084994A1
Автор: Cao Hui, Gao Xuri, Jin Meizhong, Kass Jorden, Li Wei, Or Yat Sun, Peng Xiaowen, Qiu Yao-Ling
Принадлежит:

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: 11. A pharmaceutical composition claim 1 , comprising a compound or a combination of compounds according to claim 1 , in combination with a pharmaceutically acceptable carrier or excipient.12. A method of treating or preventing an HBV infection in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of a compound or a combination of compounds according to .13. The method of claim 12 , further comprising administering to the subject at least one additional therapeutic agent selected from the group consisting of HBV polymerase inhibitors claim 12 , interferon claim 12 , viral entry inhibitors claim 12 , viral maturation inhibitors claim 12 , capsid assembly or core protein inhibitors or modulators claim 12 , reverse transcriptase inhibitors claim 12 , TLR-agonists claim 12 , inducers of cellular viral RNA sensor claim 12 , therapeutic vaccines claim 12 , RNA interence (RNAi) or small interfering RNA (siRNA) and combinations thereof.14. The method of claim 13 , wherein the compound and the at least one additional therapeutic agent are co-formulated.15. The method of claim 13 , wherein the at least one additional therapeutic agent is administered at a lower dose and/or frequency than that which is therapeutically effective when said agent is administered alone. This application is a divisional of U.S. application Ser. No. 15/450,125, filed on Mar. 6, 2017, which claims the benefit of U.S. Provisional Application No. 62/304,671, filed on Mar. 7, 2016, and 62/337,675, filed on May 17, 2016. The entire teachings of the above applications are incorporated herein by reference.The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function ...

Подробнее
Номер записи: 63
30-03-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170088507A1
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: 64
02-04-2015 дата публикации

COMPOUNDS AND METHODS FOR TREATING MALARIA

Номер: US20150094294A1
Автор: Costanzo Michael J., Freeman Katie, Greenbaum Doron, KAVASH ROBERT W., Pan Wenxi, Scott Richard W., Xu Yongjiang, YOUNG Trevor
Принадлежит:

The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a species, comprising administering to said mammal or contacting said species with, an effective amount of a pyrimidin--dicarboxylic acid amide derivative. 1144-. (canceled)146. A pharmaceutical composition comprising a compound of claim 145 , or a pharmaceutically acceptable salt thereof claim 145 , and a pharmaceutically acceptable carrier.148. The method of wherein the malaria is chloroquine-sensitive or chloroquine-resistant. The present disclosure was supported by funds from the U.S. Government (NIH/NIAID Grant No. 1R44AI090762-01) and the U.S. Government may therefore have certain rights in the disclosure.The present disclosure is directed, in part, to compounds, and pharmaceutically acceptable salts thereof, and compositions thereof for treating a mammal having malaria, or killing or inhibiting the growth of a species.World-wide, 41% of the population live in areas where malaria is transmitted, such as parts of Africa, Asia, Middle East, Central and South America, Hispaniola, and Oceania. Each year between 350 and 500 million cases of malaria occur worldwide, and over one million people die, most of them young children in sub-Saharan Africa. In areas of Africa with high malaria transmission, an estimated 990,000 people died of malaria in 1995. In 2002, malaria was the fourth cause of death in children in developing countries. In addition, malaria caused 10.7% of all children's deaths in developing countries.Antimicrobial peptides (AMPs) represent a component of the innate immune system that provides resistance to a variety of pathogenic bacteria. AMPs have provided new leads for developing antibiotics, because they play a central role in the innate ...

Подробнее
Номер записи: 65
19-03-2020 дата публикации

LIPIDS FOR THERAPEUTIC AGENT DELIVERY FORMULATIONS

Номер: US20200085957A1
Автор: Ahmadian Mohammad, Akopian Violetta, Gaudette John A., Hou Zheng, Karmali Priya, Knopov Victor, Payne Joseph E., Safarzadeh Neda, Witte Richard P., Ying Wenbin, Yu Lei, ZHANG JUN
Принадлежит:

The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes. 2. The compound of claim 1 , wherein n and m are 1 or 2.3. The compound of claim 2 , wherein X is absent.4. The compound of claim 3 , wherein L is —OCalkylene- or —OC(O)Calkylene-.5. The compound of claim 1 , wherein X is —CH—.6. The compound of claim 5 , wherein L is —OCalkylene-.7. The compound of claim 5 , wherein L is —OCHCH— or —OCHCHCH—.8. The compound of claim 5 , wherein L is —OC(O)Calkylene—.9. The compound of claim 5 , wherein L is —OC(O)CHCHCH—.10. The compound of claim 2 , wherein X is 0.11. The compound of claim 2 , wherein Rand Rare each Calkyl-.12. The compound of claim 12 , wherein Rand Rare each Calkyl-.13. A pharmaceutical composition comprising the compound of .14. The pharmaceutical composition of comprising a therapeutically effective amount of RNA.16. A pharmaceutical composition comprising the compound of .17. The pharmaceutical composition of comprising a therapeutically effective amount of RNA.19. A pharmaceutical composition comprising the compound of .20. The pharmaceutical composition of comprising a therapeutically effective amount of RNA.22. A pharmaceutical composition comprising the compound of .23. The pharmaceutical composition of comprising a therapeutically effective amount of RNA. This application is a continuation of U.S. patent application Ser. No. 14/872,951 filed on Oct. 1, 2015, which is a divisional of U.S. patent application Ser. No. 13/913,918 filed on Jun. 10, 2013, now U.S. Pat. No. 9,308,267, which claims the benefit of U.S. Provisional patent application No. 61/657,480 filed Jun. 8, 2012, which are herein incorporated by reference in their entirety.The description is directed to ionizable lipids for enhancing the delivery of therapeutic agents.A number of techniques are available for delivering a therapeutic agent, for example, siRNA, nucleic acids, etc., into a cell. These techniques include viral and ...

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

Inhibitors of Mycobacterium Tuberculosis Malate Synthase, Methods of Making and Uses Thereof

Номер: US20140171444A1
Автор: FREUNDLICH Joel S., Gawandi Vijay, Ioerger Thomas R., Kriger Inna V., Sacchettini James C.
Принадлежит: The Texas A&M University System

The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided. 2. The substituted diketo acid compound of claim 1 , wherein Ris a 2- or 3-thienyl or (3-methyl)-2-thienyl substituted with Rat C5 claim 1 , wherein Ris one or more of Rat C2 claim 1 , Rat C3 claim 1 , Rat C4 claim 1 , Rat C5 claim 1 , or Rat C6 claim 1 , phenoxyphenyl claim 1 , or 2-thienyl.3. The substituted diketo acid compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , R claim 2 , and Rindependently are H claim 2 , OH claim 2 , NO claim 2 , Calkyl claim 2 , Calkoxy claim 2 , O(Calkyl)O(Calkyl) claim 2 , Br claim 2 , F claim 2 , Cl claim 2 , I claim 2 , Ph claim 2 , PhBr claim 2 , PhF claim 2 , PhCH claim 2 , PhOCH claim 2 , Ph(CH) claim 2 , CF claim 2 , CHSO claim 2 , imidazolyl claim 2 , or wherein Rand Rtogether are benzothienyl claim 2 ,4. The substituted diketo acid compound of claim 3 , wherein one or more of R claim 3 , R claim 3 , R claim 3 , Ror Ris independently methoxy claim 3 , Br claim 3 , F claim 3 , Cl claim 3 , I claim 3 , or methyl and Ris OH or ...

Подробнее
Номер записи: 67
19-03-2020 дата публикации

Therapeutic compounds and methods of use thereof

Номер: US20200087239A1
Автор: Brian Salvatore SAFINA, Daniel Sutherlin, Ivan William Hemeon
Принадлежит: Genentech Inc, Xenon Pharmaceuticals Inc

and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Подробнее
Номер записи: 68
28-03-2019 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20190090488A1
Автор: Baum Erich W., Benko Zoltan L., CHOY Nakyen, Crouse Gary D., Daeuble, DeKorver Kyle A., Demeter David A., Eckelbarger Joseph D., GRAY KAITLYN, Heemstra Ronald J., Hunter Ricky, JR. Ronald, Knueppel Daniel I., Li Fangzheng, Martin Timothy P., Nissen Jeffrey, Olson Monica B., Riener Michelle, Ross, Sparks Thomas C., SR. John F., Trullinger Tony K., Vednor Peter, Wessels Frank J., Yap Maurice C.
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A process to control a pest claim 1 , said process comprising claim 1 , applying to a locus claim 1 , a pesticidally effective amount of a molecule according to . This Application is a continuation of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/679,415, which was filed Aug. 17, 2017, and which is now allowed; Ser. No. 15/679,415 is a divisional of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/092,650, which was filed Apr. 7, 2016, and is now U.S. Pat. No. 9,781,935; Ser. No. 15/092,650 claims the benefit of, and priority from, U.S. provisional application Ser. Nos. 62/148,809; 62/148814; 62/148818; 62/148824; 62/148830; and 62/148,837; all of which were filed on Apr. 17, 2015. The entire contents of all of the above-identified applications are hereby incorporated by reference into this Application.This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides.“Many of the most dangerous human diseases are transmitted by insect vectors” (Rivero et al.). “Historically, malaria, dengue, yellow ...

Подробнее
Номер записи: 69
05-04-2018 дата публикации

POTENT AND SELECTIVE INHIBITORS OF MONOAMINE TRANSPORTERS; METHOD OF MAKING; AND USE THEREOF

Номер: US20180093947A1
Автор: Cao Jianjing, Newman Amy Hauck, Okunola-Bakare Oluyomi M.
Принадлежит:

Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds. 2. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris 3-phenylpropyl, —CHCH(OH)CH, or —CHCH(OH)CHPh;'}{'sub': '3', 'each instance of X is located at the para or meta position and is fluoro, methyl, or CF;'}Y is S or S(O); andZ is O or 2H.3. The method of claim 1 , wherein a sulfoxide fragment has an (R)-configuration.4. The method of claim 1 , wherein a sulfoxide fragment has an (S)-configuration.5. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris —CHCH(OH)CHor —CHCH(OH)CHPh wherein the carbon substituted with —OH is racemic, in the R configuration, or in the S configuration;'}{'sub': '3', 'each instance of X is located at the para or meta position and is fluoro, methyl, or CF;'}Y is S or S(O); andZ is 2H.6. The method of claim 5 , wherein a sulfoxide fragment has an (R)-configuration or an (S)-configuration.7. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris —CHCH(OH)CHor —CHCH(OH)CHPh wherein the carbon substituted with —OH is racemic, in the R configuration, or in the S configuration;'}each instance of X is located at the para or meta position and is fluoro;Y is S or S(O); andZ is 2H.8. The method of claim 7 , wherein a sulfoxide fragment has an (R)-configuration or an (S)-configuration.9. The method of claim 1 , wherein the compound or salt thereof is formulated as a pharmaceutical ...

Подробнее
Номер записи: 70
28-03-2019 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20190092729A1
Автор: Balog James Aaron, BECK Hilary Plake, Guo Weiwei, JAEN Juan Carlos, OSIPOV Maksim, POWERS Jay Patrick, REILLY Maureen Kay, SHUNATONA Hunter Paul, WALKER James Ross, Williams David K., ZIBINSKY Mikhail
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 422-. (canceled)2538-. (canceled)39. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.40. A method of treating a disease claim 1 , disorder or condition claim 1 , mediated at least in part by IDO claim 1 , comprising administering an effective amount of a compound of to a subject in need thereof.41. The method of claim 40 , wherein said compound is administered concurrently with radiation treatment claim 40 , subsequent to radiation treatment claim 40 , or prior to radiation treatment.42. (canceled)43. (canceled)44. The method of claim 40 , wherein said compound is administered in an amount effective to reverse or stop the progression of IDO-mediated immunosuppression.45. The method of claim 40 , wherein said disease claim 40 , disorder or condition is cancer.46. The method of claim 45 , wherein said cancer is a cancer of the prostate claim 45 , colon claim 45 , rectum claim 45 , pancreas claim 45 , cervix claim 45 , stomach claim 45 , endometrium claim 45 , brain claim 45 , liver claim 45 , bladder claim 45 , ovary claim 45 , testis claim 45 , head claim 45 , neck claim 45 , skin (including melanoma and basal carcinoma) claim 45 , mesothelial lining claim 45 , white blood cell (including lymphoma and leukemia) claim 45 , esophagus claim 45 , breast claim 45 , muscle claim 45 , connective tissue claim 45 , lung (including small-cell lung carcinoma and non-small-cell carcinoma) claim 45 , adrenal gland claim 45 , thyroid claim 45 , kidney claim 45 , or bone; or is glioblastoma claim 45 , mesothelioma claim 45 , renal cell ...

Подробнее
Номер записи: 71
16-04-2015 дата публикации

Cyclopentylacrylamide derivative

Номер: US20150105581A1
Автор: Masanori Takadoi, Masanori Yamamoto, Yasumichi Fukuda, Yoshikazu Asahina
Принадлежит: Kyorin Pharmaceutical Co Ltd, Teijin Pharma Ltd

A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R 1 and R 2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C 1 to C 6 alkyl group, a C 1 to C 6 alkoxy group, a C 1 to C 6 alkylsulfanyl group, a C 1 to C 6 alkylsulfinyl group, a C 1 to C 6 alkylsulfonyl group, or a C 1 to C 6 alkoxy-C 1 to C 6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).

Подробнее
Номер записи: 72
03-07-2014 дата публикации

1,3,4-TRISUBSTITUTED BENZENES

Номер: US20140187786A1
Автор: Chesworth Richard, Shapiro Gideon
Принадлежит: EnVivo Pharmaceuticals, Inc.

Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of γ-secretase. The compounds are expected to reduce the level of Aβ42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of Aβ42 and/or the formation of Aβ plaques. 294-. (canceled) This application is a continuation of U.S. application Ser. No. 12/678,175, filed on Oct. 29, 2010, which is the National Stage of International Application No. PCT/US2008/076408, filed Sep. 15, 2008, which claims priority to and U.S. Provisional Patent Application Ser. No. 60/972,299, filed on Sep. 14, 2007. The contents of these applications are hereby incorporated by reference in their entireties.Alzheimer's disease (AD) is the most prevalent form of dementia. It is a neurodegenerative disorder that is associated (though not exclusively) with aging. The disorder is clinically characterized by a progressive loss of memory, cognition, reasoning and judgment that leads to an extreme mental deterioration and ultimately death. The disorder is pathologically characterized by the deposition of extracellular plaques and the presence of neurofibrillary tangles. These plaques are considered to play an important role in the pathogenesis of the disease.These plaques mainly comprise of fibrillar aggregates of (β-amyloid peptide (Aβ), which are products of the amyloid precursor protein (APP), a 695 amino-acid protein. APP is initially processed by β-secretase forming a secreted peptide and a membrane bound C99 fragment. The C99 fragment is subsequently processed by the proteolytic activity of γ-secretase. Multiple sites of proteolysis on the C99 fragment lead to the production of a range of smaller peptides (Aβ 37-42 amino acids). N-terminal truncations can also be found e.g. Aβ (4-42) for convenience Aβ40 and Aβ42 as used herein incorporates these N-terminal truncated peptides. Upon secretion, the Aβ peptides initially form soluble ...

Подробнее
Номер записи: 73
10-07-2014 дата публикации

N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS

Номер: US20140194416A1
Автор: BROOKFIELD Frederick Arthur, Cohen Andrew D., COURTNEY Stephen Martin, FROST Lisa Marie, KALISH Vincent Jacob, Toscano John P.
Принадлежит:

The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives. 2. The compound of claim 1 , wherein Ris H.3. The compound of claim 1 , wherein x and y are both 1.4. The compound of claim 1 , wherein the compound is of the formula (I).5. The compound of wherein the compound is of the formula (I) and at least one of Rand Ris other than H.6. The compound of claim 4 , wherein the compound is of the formula (I) and at least one of Rand Ris an electron withdrawing group.7. The compound of claim 4 , wherein the compound is of the formula (I) and at least one of R claim 4 , R claim 4 , R claim 4 , Rand Ris carboxyl claim 4 , —COO-alkyl claim 4 , —C(O)NH claim 4 , —C(O)NRRwhere Ris hydrogen and Ris alkyl claim 4 , —C(O)NRRwhere Rand Rare independently alkyl claim 4 , —C(O)NRRwhere Rand Rare taken together with the nitrogen to which they are attached to form a heterocyclic or substituted heterocyclic ring claim 4 , —SONH claim 4 , —SONR-alkyl where R is hydrogen claim 4 , —SONR-alkyl where R is alkyl claim 4 , —SONR claim 4 , where the two R groups are taken together with the nitrogen to which they are attached to form a heterocyclic or substituted heterocyclic ring.8. The compound of claim 1 , wherein the compound is of the formula (II).9. The compound of claim 1 , wherein the compound is of the formula (III).10. A method of modulating the in vivo nitroxyl levels in an individual in need thereof claim 1 , the method comprising administering to the individual an N-hydroxysulfonamide of or ...

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

Difluoromethyl-nicotinic-indanyl carboxamides

Номер: US20170114031A1
Автор: AHRENS HARTMUT, Dietrich Hansjoerg, Doerner-Rieping Simon, GATZWEILER ELMAR, Heinemann Ines, ROSINGER CHRISTOPHER HUGH, SCHMUTZLER Dirk, Tiebes Joerg, WALDRAFF CHRISTIAN
Принадлежит:

Herbicidally active N-(1-methyltetrazol-5-yl)benzoic acid amides N-(1-Methyltetrazol-5-yl)benzamides of the general formula (I) are described as herbicides. 2. An N-(1-methyltetrazol-5-yl)benzamide as claimed in claim 1 , whereinX is methyl, ethyl or cyclopropyl,Z is methyl, ethyl, n-propyl or isopropyl,R is methyl, ethyl, cyclopropyl, cyclopropylmethyl or methoxyethyl,n is 1 or 2.3. A herbicidal composition comprising a herbicidally active content of at least one compound of the formula (I) or salt as claimed in either .4. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.5. A method of controlling one or more unwanted plants claim 1 , comprising applying an effective amount of at least one compound of the formula (I) or salt as claimed in or a herbicidal composition thereof to the plants or to a site of unwanted vegetation.6. A product comprising a compound of formula (I) or salt as claimed in or a herbicidal composition thereof for controlling unwanted plants.7. The product as claimed in claim 6 , wherein the compound of formula (I) or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.8. The product as claimed in claim 7 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2012/028579 A1 describes N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and their use as herbicides. The active ingredients described therein do not always exhibit sufficient activity against harmful plants and/or some do not have sufficient compatibility with some important crop plants such as cereal species, corn and rice.It is an object of the present invention to provide alternative herbicidally active ingredients. This object is achieved by the N-(1-methyltetrazol-5-yl)benzamides of the invention that ...

Подробнее
Номер записи: 75
09-04-2020 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20200109110A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Liu Xiaoxia, Viswanath Veena, Yuan Haiqing
Принадлежит:

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 115.-. (canceled)17. The method according to claim 16 , wherein:{'sup': '5', 'Ris —S—.'}18. The method according to claim 16 , wherein:{'sup': '5', 'Ris —S(O)—.'}19. The method according to claim 16 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}20. The method according to claim 16 , wherein the compound is selected from the group consisting of:3,4-dichloro-N-[5-chloro-2-(methylthio)phenyl]benzenesulfonamide;3,4-dichloro-N-[5-chloro-2-(methylsulfinyl)phenyl]benzenesulfonamide;4-chloro-N-[5-chloro-2-(methylsulfinyl)phenyl]-3-methylbenzenesulfonamide;N-[5-chloro-2-(methylsulfinyl)phenyl]-3-nitro-4-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(methylthio)phenyl]-2-fluorobenzenesulfonamide;4-chloro-N-{5-chloro-2-[(1H-imidazol-4-ylmethyl)sulfonyl]phenyl}-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(methylsulfinyl)phenyl]-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(ethylthio)phenyl]-3-(trifluoromethyl)benzenesulfonamide;4-chloro-N-[5-chloro-2-(ethylsulfinyl)phenyl]-3-(trifluoromethyl)benzenesulfonamide;tert-butyl {6-[({2-[(1-benzofuran-2-ylsulfonyl)amino]-4-chlorophenyl}thio)methyl]pyridin-2-yl}carbamate;tert-butyl {6-[({2-[(1-benzofuran-2-ylsulfonyl)amino]-4-chlorophenyl}sulfonyl)methyl]pyridin-2-yl}carbamate;tert-butyl 3-[({2-[(1-benzofuran-2-ylsulfonyl)amino]-4-chlorophenyl}thio)methyl]-1H-pyrazole-1-carboxylate;3-{[4-chloro-2-({[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl}amino)phenyl]sulfinyl}-N,N-dimethylpropanamide;3-{[4-chloro-2-({[4-chloro-3-(trifluoromethyl)phenyl]sulfonyl}amino)phenyl]sulfonyl}-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(2,4-difluorophenyl)sulfonyl]amino}phenyl)thio]-N,N-dimethylpropanamide;3-[(4-chloro-2-{[(2,4-difluorophenyl)sulfonyl]amino}phenyl)sulfinyl]-N,N-dimethylpropanamide;3-[(4-chloro-2 ...

Подробнее
Номер записи: 76
05-05-2016 дата публикации

FLUOROSURFACTANTS IN PESTICIDES

Номер: US20160122297A1
Автор: Jonschker Gerhard, Pahnke Joerg, Schellenberger Steffen
Принадлежит: Merck Patent GmBH

The present invention relates to the use of fluorinated surfactants of formula (I) in pesticides. 2. A Method according to claim 1 , which comprises applying the formulation by spraying in the cultivation of crop or ornamental plants.3. Method according to claim 1 , characterised in that the compounds of the formula (I) improve the efficacy of the pesticide and/or crop-protection agent and/or act as dispersant claim 1 , emulsion stabiliser and/or foam inhibitor.9. A formulation according to claim 6 , characterised in that it further comprises at least one compound of the formula (VI){'br': None, 'sub': m', 'n, '(RF-(spacer))M\u2003\u2003(VI)'}whereRF is a fluorine-containing group,spacer is a single bond or an organic functional carbon chain,n is ≧1,m=0-1 andM is an anionic, cationic, amphoteric or non-ionic group.10. A formulation according to claim 9 , characterised in that the group (RF(spacer))- in the compounds of the formula (VI) is equal to CF— claim 9 , CF—CHCH— claim 9 , CF—OCFCF— claim 9 , CF—OCH— claim 9 , CF—C(O)NH(CH)N═ claim 9 , CF—SONH(CH)N═ claim 9 , CFCCl(CFCl)—CF— or CFCHCHSi(CH)— claim 9 , where n′=4-12 claim 9 , and M is equal to —OPOO claim 9 , —COO claim 9 , —SO claim 9 , —OSO claim 9 , —OP(O)(O)O— or —OP(O)O claim 9 , preferably with H claim 9 , Na claim 9 , K claim 9 , Li or NH as counterion.11. A formulation according to claim 7 , characterised in that it comprises at least one compound of the formula (III) and at least one compound of the formula (VI){'br': None, 'sub': m', 'n, '(RF-(spacer))M\u2003\u2003(VI)'}whereRF is a fluorine-containing group,spacer is a single bond or an organic functional carbon chain,n is ≧1,m=0-1 andM is an anionic, cationic, amphoteric or non-ionic group14. A formulation according to claim 6 , characterised in that is in the form of a liquid pesticide formulation which can be applied by means of spraying methods.15. A formulation according to claim 6 , characterised in that it comprises one or more crop- ...

Подробнее
Номер записи: 77
07-05-2015 дата публикации

BICYCLIC SULFONE COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE

Номер: US20150126493A1
Автор: Aicher Thomas D., Barr Kenneth J., Simov Vladimir, Thomas Willam D., Toogood Peter L., Van Huis Chad A.
Принадлежит:

The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis. 2. The compound of claim 1 , wherein A is aryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , and Chaloalkoxy.3. The compound of claim 1 , wherein A is phenyl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , and Chaloalkoxy.4. The compound of claim 1 , wherein A is heteroaryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , and Chaloalkoxy.54. The compound of any one of - claims 1 , wherein X is —O—[C(R)(R)]—[C(R)]-ψ.64. The compound of any one of - claims 1 , wherein X is —C(R)-[C(R)(R)]—[C(R)]-ψ.74. The compound of any one of - claims 1 , wherein X is —C(O)—[C(R)(R)]—[C(R)]-ψ.87. The compound of any one of - claims 1 , wherein Yand Yare C(R).97. The compound of any one of - claims 1 , wherein at least one of Yand Yis N.109. The compound of any one of - claims 1 , wherein Ris hydrogen.1110. The compound of any one of - claims 1 , wherein Ris —C(O)-aryl or —C(O)-aralkyl;{'sub': 1-6', '1-6', '1-6', '1-6, 'each of which is optionally substituted with 1, 2, or 3 ...

Подробнее
Номер записи: 78
25-04-2019 дата публикации

ROR GAMMA (RORy) MODULATORS

Номер: US20190119204A1
Автор: CALS Joseph Maria Gerardus Barbara, MACHNIK David, NABUURS Sander Bernardus, SABUCO Jean-Francois
Принадлежит:

The present application relates to compounds according to (Formula IA) or (Formula IB): 113-. (canceled)17. The method according to claim 16 , wherein the at least one condition is selected from the group consisting of rheumatoid arthritis claim 16 , psoriasis claim 16 , inflammatory bowel disease claim 16 , Crohn's disease and multiple sclerosis.18. The method according to claim 16 , wherein the at least one condition is selected from the group consisting of osteoarthritis and asthma.19. The method according to claim 16 , wherein the at least one condition is mucosal leishmaniasis.21. The method according to claim 20 , wherein the at least one condition is selected from the group consisting of rheumatoid arthritis claim 20 , psoriasis claim 20 , inflammatory bowel disease claim 20 , Crohn's disease and multiple sclerosis.22. The method according to claim 20 , wherein the at least one condition is selected from the group consisting of osteoarthritis and asthma.23. The method according to claim 20 , wherein the at least one condition is mucosal leishmaniasis.26. A pharmaceutical composition comprising the compound according to claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , and one or more pharmaceutically acceptable excipients. This application is a continuation of U.S. patent application Ser. No. 15/829,226, filed Dec. 1, 2017, which claims priority benefit of European patent application 16202175.2, filed Dec. 5, 2016, the disclosures of each of which are incorporated herein by reference in their entireties.The present application relates to compounds that are modulators of RORγ, to pharmaceutical compositions comprising the same and to their use for the treatment of RORγ-mediated diseases or conditions, in particular autoimmune diseases and inflammatory diseases.T helper (T) cells play a crucial role in the adaptive immune system as they coordinate defense against specific pathogens. The interleukin 17 (IL-17) producing lineages of Tcells, such ...

Подробнее
Номер записи: 79
25-04-2019 дата публикации

ARYL ETHERS AND USES THEREOF

Номер: US20190119214A1
Автор: DIXON Darryl David, GRINA Jonas, Josey John A., Rizzi James P., Schlachter Stephen T., Wallace Eli M., Wang Bin, WEHN Paul, Xu Rui, Yang Hanbiao
Принадлежит:

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo. 164.-. (canceled)66. The process of claim 65 , wherein P is selected from acyl and methoxymethyl ether.67. The process of claim 66 , wherein P is —C(═O)R claim 66 , wherein R is C-Calkyl.68. The process of claim 67 , wherein P is —C(═O)CH.69. The process of claim 65 , wherein the fluorinating comprises adding (diethylamino)sulfur trifluoride to the compound of Formula A.71. The process of claim 70 , wherein the hydrolyzing comprises a silver salt.72. The process of claim 71 , wherein the silver salt is selected from AgCO claim 71 , AgClOand AgBF.76. The process of claim 75 , wherein the fluorinating comprises adding N-fluoro-o-benzendisulfonamide claim 75 , acetyl hypofluorite claim 75 , Accufluor® claim 75 , Selectfluor® claim 75 , Selectfluor® II claim 75 , or N-fluorobenzenesulfonamide to the 3-fluoro-5-(7-methylsulfonyl-1-oxo-indan-4-yl)oxy-benzonitrile.77. The process of claim 75 , wherein the reducing is an asymmetric reduction.78. The process of claim 77 , wherein the reducing provides the 3-fluoro-5-(((1S claim 77 ,2R)-2-fluoro-1-hydroxy-7-(methylsulfonyl)-2 claim 77 ,3-dihydro-1H-inden-4-yl)oxy)benzonitrile with greater than 90% enantioselectivity.79. The process of claim 77 , wherein the asymmetric reduction is selected from Corey-Bakshi-Shibata reduction claim 77 , asymmetric hydrogenation claim 77 , and asymmetric transfer hydrogenation.80. The process of claim 77 , further comprising a ruthenium catalyst. This application is a Continuation of U.S. application Ser. No. 15/805,390, filed on Nov. 7, 2017, which is a Continuation of U.S. application Ser. No. 14/905,776, filed Jan. 15, 2016, which is a National Stage Entry of PCT/US2014/054375, filed Sep. ...

Подробнее
Номер записи: 80
16-04-2020 дата публикации

TETRALIN AND INDANE DERIVATIVES AND USES THEREOF

Номер: US20200115333A1
Автор: Greenhouse Robert, Harris, III Ralph New, Jaime-Figueroa Saul, Kress James M., Repke David Bruce, Stabler Russell Stephen
Принадлежит: Roche Palo Alto LLC

The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, RR, Rand Rare as defined herein. 2. The method of wherein m is 0 claim 1 , s is 1 claim 1 , Ris 3-fluoro claim 1 , Ris hydrogen and Ris acetyl claim 1 , aminocarbonyl or methylsulfonyl or a pharmaceutically acceptable salt.3. The method of wherein the compound is (R)-[6-(3-fluoro-benzenesulfonyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-naphthalen-1-ylmethyl]-urea or a pharmaceutically acceptable salt.4. The method of claim 3 , wherein the central nervous system disease state is depression.5. The method of claim 3 , wherein the central nervous system disease state is a memory disorder.6. The method of claim 3 , wherein the central nervous system disease state is Parkinson's disease. This Application is a Continuation of U.S. application Ser. No. 15/597,478, filed May 17, 2017, which is a Continuation of U.S. application Ser. No. 14/531,465, filed Nov. 3, 2014, which is a Continuation U.S. application Ser. No. 13/314,525, filed on Dec. 8, 2011, which is a Continuation of U.S. application Ser. No. 11/985,459, filed on Nov. 15, 2007, which is a continuation of U.S. patent application Ser. No. 11/315,706, filed Dec. 21, 2005, which claims the benefit under Title 35 U.S.C. 119(e) of U.S. Provisional Patent Application Ser. No. 60/638,030, filed Dec. 21, 2004, the disclosure of which is incorporated herein by reference in its entirety.This invention relates to substituted indane and tetralin compounds, and associated compositions, methods for use as therapeutic agents, and methods of preparation thereof.The actions of 5-hydroxytryptamine (5-HT) as a major modulatory neurotransmitter in the brain are mediated through a number of receptor families termed 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HTS, 5-HT6, and 5-HT7. Based on a high level of 5-HT6 receptor mRNA in the brain, it has been stated that the 5-HT6 receptor may play a role in the pathology and treatment of ...

Подробнее
Номер записи: 81
24-07-2014 дата публикации

N-substituted isopropyldimethyl azulene sulfonamide derivatives, and preparation method and use thereof

Номер: US20140206741A1
Автор: FANG Yang, Luyun Zhang, Ping Zhang, Shufan Yin, Wanqi Shi, Ying Li
Принадлежит: Sichuan Guokang Pharmaceutical Co Ltd

The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.

Подробнее
Номер записи: 82
27-05-2021 дата публикации

AFFINITY ILLUDOFULVENE CONJUGATES

Номер: US20210155583A1
Автор: KELNER Michael
Принадлежит:

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker. 1. A compound , (a) the compound comprising an illudofulvene moiety , or (b) the compound being an illudofulvene analog , where the illudofulvene moiety or the illudofulvene analog is selected from the group consisting of analog 317 (2'S ,3′R ,6′R)-6′-hydroxy-2′-(hydroxymethyl)-2′ ,4′ ,6′-trimethyl-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-3′-yl 4-(fluorosulfonyl)benzoate; analog 318 ((2'S ,3′R ,6′R)-3′-((4-(fluorosulfonyl)benzoyl)oxy)-6′-hydroxy-2′ ,4′ ,6′-trimethyl-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-2′-yl)methyl 4-(fluorosulfonyl)benzoate; analog 333 ((2'S ,3′R ,6′R)-6′-hydroxy-2′ ,4′ ,6′-trimethyl-3′-(((4-nitrophenoxy)carbonyl)oxy)-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-2′-yl)methyl acetate; analog 334 ((2'S ,3′R ,6′R)-3′-(((2-((tert-butoxycarbonyl)(methyl)amino)ethyl)(methyl)carbamoyl)oxy)-6′-hydroxy-2′ ,4′ ,6′-trimethyl-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-2′-yl)methyl acetate; analog 335 tert-butyl ((2'S ,3′R ,6′R)-6′-hydroxy-2′-(hydroxymethyl)-2′ ,4′ ,6′-trimethyl-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-3′-yl) ethane-1 ,2-diylbis(methylcarbamate); analog 339 ((2'S ,3′R ,6′R)-3′ ,6′-dihydroxy-2′ ,4′ ,6′-trimethyl-7′-oxo-2′ ,3′ ,6′ ,7′-tetrahydrospiro[cyclopropane-1 ,5′-inden]-2′-yl)methyl 4-methylbenzenesulfonate; ...

Подробнее
Номер записи: 83
10-05-2018 дата публикации

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

Номер: US20180127368A1
Автор: Batt Douglas G, Beaudoin Bertrand Myra, Dhar T.G. Murali, Marcoux David, Weigelt Carolyn A., Xiao Hai-Yun, Xiao Zili, Yang Michael G., Zhu Yeheng
Принадлежит:

There are described RORγ modulators of the formula (I), 17. A compound selected from the following:1-(4-((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carbonyl)piperazin-1-yl)ethan-1-one,(3R,3aS,9bS)—N-((1,1-dioxidotetrahydrothiophen-3-yl)methyl)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide (diastereomeric mixture),methyl 4-((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamido)tetrahydro-2H-thiopyran-4-carboxylate 1,1-dioxide,(3R,3 aS,9bS)—N-(2,3-dihydroxy-3-methylbutyl)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N-(2-hydroxy-2-methylpropyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1r,4R)-4-hydroxycyclohexyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(1,1-dioxidothiomorpholino)((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalen-3-yl)methanone,(3R,3 aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N—((R)-2-hydroxypropyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxycyclopentyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxycyclobutyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxy cyclopropyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, ...

Подробнее
Номер записи: 84
01-09-2022 дата публикации

SULFONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS

Номер: US20220274922A1
Автор: Dewji Nazneen, Rideout Darryl, Rosse Gerard
Принадлежит:

Provided herein are sulfone compounds, for example, a compound of Formula A, or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, a tautomer, a mixture of two or more tautomers, or an isotopic variant thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof; and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disorder, disease, or condition. 2. The compound of claim 1 , wherein E is —C(R)—.3. The compound of or claim 1 , wherein G is —C(R)—.4. The compound of any one of to claim 1 , wherein J is —C(R)—.5. The compound of any one of to claim 1 , wherein L is —C(R)—.6. The compound of any one of to claim 1 , wherein M is —C(R)—.7. The compound of any one of to claim 1 , wherein E claim 1 , G claim 1 , J claim 1 , L claim 1 , and M are each —C(R)—.8. The compound of any one of to claim 1 , wherein Q is —C(R)—.9. The compound of any one of to claim 1 , wherein R is —C(R)—.10. The compound of any one of to claim 1 , wherein U is —C(R)—.11. The compound of any one of to claim 1 , wherein V is —C(R)—.12. The compound of any one of to claim 1 , wherein W is —C(R)—.13. The compound of any one of to claim 1 , wherein Q claim 1 , R claim 1 , U claim 1 , V claim 1 , and W are each —C(R)—.15. The compound of claim 14 , wherein:{'sup': 1', '1a', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1a', '1a', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1b', '1c', '1b', '1c', '1a', '1d', '1a', '1d', '1a', '1b', '1c', '1a', '1d', '1a', '1d', '1b', '1c', '1a', '1d', '1a', '1d', '1a', '1b', '1c', '1a', '1d', '1a', '1d', '1a', '1b', '1c', '1a', '1b', '1c', '1a', '1a', '1b', '1c', '1b', '1c, 'sub': 1-6', '2-6', '2-6', '3-10', '6-14', '7-15', '2', '2', '2', '2', '2', '2, 'each Ris independently (a) cyano, halo, or nitro; (b) Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, ...

Подробнее
Номер записи: 85
01-09-2022 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20220274926A1
Автор: Balog James Aaron, BECK Hilary Plake, Guo Weiwei, JAEN Juan Carlos, OSIPOV Maksim, POWERS Jay Patrick, REILLY Maureen Kay, SHUNATONA Hunter Paul, WALKER James Ross, Williams David K., ZIBINSKY Mikhail
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 238-. (canceled)39. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.40. A method of treating cancer claim 1 , said method comprising administering an effective amount of a compound of claim 1 , to a subject in need thereof.41. A method of claim 40 , wherein said compound is administered concurrently with claim 40 , subsequent to claim 40 , or prior to claim 40 , radiation treatment.4245-. (canceled)46. A method of claim 40 , wherein said cancer is a cancer of the prostate claim 40 , colon claim 40 , rectum claim 40 , pancreas claim 40 , cervix claim 40 , stomach claim 40 , endometrium claim 40 , brain claim 40 , liver claim 40 , bladder claim 40 , ovary claim 40 , testis claim 40 , head claim 40 , neck claim 40 , skin (including melanoma and basal carcinoma) claim 40 , mesothelial lining claim 40 , white blood cell (including lymphoma and leukemia) claim 40 , esophagus claim 40 , breast claim 40 , muscle claim 40 , connective tissue claim 40 , lung (including small-cell lung carcinoma and non-small-cell carcinoma) claim 40 , adrenal gland claim 40 , thyroid claim 40 , kidney claim 40 , or bone; or is glioblastoma claim 40 , mesothelioma claim 40 , renal cell carcinoma claim 40 , gastric carcinoma claim 40 , sarcoma (including Kaposi's sarcoma) claim 40 , choriocarcinoma claim 40 , cutaneous basocellular carcinoma claim 40 , or testicular seminoma.47. A method of claim 40 , wherein said cancer is selected from the group consisting of melanoma claim 40 , colon cancer claim 40 , pancreatic cancer claim 40 , breast cancer claim 40 , ...

Подробнее
Номер записи: 86
02-05-2019 дата публикации

S1PR2 ANTAGONISTS AND USES THEREFOR

Номер: US20190127372A1
Автор: McMaster Christopher, Simms Gordon
Принадлежит: DALHOUSIE UNIVERSITY

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are compounds which contain bioisosteric replacements of the urea group of JTE-013 and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis. 3. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH; and'}{'sup': '2', 'sub': '3', 'Ris CH.'}4. The method of claim 3 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}5. The method of claim 4 , wherein{'sup': '4', 'sub': 3', '2, 'Ris CH(CH).'}6. The method of claim 5 , wherein{'sup': '5', 'Ris halogen.'}7. The method of claim 6 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.8. The method of claim 2 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.9. The method of claim 1 , wherein the ocular diseases include familial exudative vitreoretinopathy.10. The method of claim 1 , wherein the compound of formula IX is a S1PR2 antagonist.13. The compound of claim 12 , wherein{'sup': '3', 'Ris H; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}14. The compound of claim 13 , wherein{'sup': '5', 'Ris Cl; and'}n is 2.15. The compound of claim 11 , wherein{'sup': '1', 'sub': '3', 'Ris CH;'}{'sup': '2', 'sub': '3', 'Ris CH;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'sub': 3', '2, 'Ris CH(CH);'}{'sup': '5', 'Ris Cl; and'}n is 2.16. The compound of claim 11 , wherein the eye condition includes familial exudative vitroretinopathy.17. The compound of claim 11 , wherein the eye condition includes an inability to normally vascularize the eye.18. The compound of claim 11 , wherein the eye condition includes secondary aberrant neovascularization.20. The method of claim 19 , wherein ...

Подробнее
Номер записи: 87
17-05-2018 дата публикации

Anthranilic acid ester compound or salt thereof, agricultural and horticultural microbicide comprising the compound, and method for using the microbicide

Номер: US20180132482A1
Автор: Atsushi Okada, Eiji YASUKOUCHI, Hiroto Harayama, Naoto Shimizu, Takashi Furuya, Yutaka Abe, Yutaka Kato
Принадлежит: Nihon Nohyaku Co Ltd

In crop production in the fields of agriculture, horticulture and the like, the damage caused by diseases etc. is still immense, and diseases resistant to existing microbicides have emerged. Under such circumstances, the development of novel agricultural and horticultural microbicides is desired. The present invention provides an anthranilic acid ester compound represented by the general formula (1): (wherein A 1 , A 3 and A 4 each represent a CH group, A 2 represents a C-haloalkyl group, R 1 represents an alkyl group, R 3 represents a hydrogen atom or an acyl group, R 4 , R 5 and R 7 each represent a hydrogen atom, R 6 represents a haloalkyl group, Z represents an alkyl group, and m represents 0, 1 or 2), or a salt thereof, an agricultural and horticultural microbicide comprising the compound or a salt thereof as an active ingredient, and a method for using the microbicide.

Подробнее
Номер записи: 88
21-05-2015 дата публикации

Compositions and methods for the treatment of neurological degenerative disorders and neurological diseases

Номер: US20150141513A1
Автор: Mahesh KANDULA
Принадлежит: Individual

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.

Подробнее
Номер записи: 89
17-05-2018 дата публикации

AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE

Номер: US20180134681A1
Автор: Banba Shinichi, CHIBA Yutaka, Daido Hidenori, Kai Akiyoshi, Kato Hiroko, Katsuta Hiroyuki, Kawahara Nobuyuki, Maki Junji, Nomura Michikazu, TAKAHASHI Kiyoshi, Wakita Takeo, YOSHIDA Kei
Принадлежит:

An object of the present invention is to provide a compound represented by Formula (1): 114-. (canceled) The present invention relates to a compound represented by Formula (1):wherein A, A, Aand Aeach represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom;Rand Reach represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group;Gand Geach represent an oxygen atom or a sulfur atom;X, which may be identical or different, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group;n is an integer of 0 to 4; andQand Qeach represent an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group,an insecticide comprising the compound as the active ingredient, and a process for preparation thereof and use thereof.International Publication WO 2000/55120 and U.S. Pat. No. 6,548,514 describe a compound similar to the compound of the present invention for the use as medicament, but they do not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.International Publication WO 2000/7980 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.US Patent Laid-Open No. 2002-032238 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.The object of the present invention is to provide a pesticide having a high insecticidal efficacy. Another object of the present invention is to provide a compound represented by Formula (1), a process for ...

Подробнее
Номер записи: 90
07-08-2014 дата публикации

Potassium Channel Blockers

Номер: US20140221337A1
Автор: FORD John, Garrett Sasha Louise, Hamlyn Richard John, Hartzoulakis Basil, John Derek Edward, Madge David, Mulla Mushtaq
Принадлежит: Xention Limited

The present invention provides a compound of formula (I) 2. A compound according to claim 1 , wherein Xis C(═O).3. A compound according claim 2 , wherein Ris NRR.4. A compound according to claim 3 , wherein Rand Rare the same or different and each represents hydrogen claim 3 , or optionally substituted Calkyl.8. A compound according to wherein{'sub': 3', '3, 'Ris H, F, or CH.'}9. A compound according to claim 8 , wherein Ris H or F.10. A compound according to wherein{'sub': '4', 'Ris preferably selected from the group consisting of optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl.'}12. A compound according to claim 11 , wherein Ris selected from hydrogen and CH claim 11 , or Rand Rtogether with the N to which they are attached form an optionally substituted saturated or partially saturated 4-6 membered ring with the general formula (II).13. A compound according to claim 12 , wherein the 4-6 membered ring is substituted azetidinyl claim 12 , substituted pyrrolidinyl claim 12 , substituted piperazinyl or substituted piperidinyl.16. A compound according to selected from the group consisting of:3-(Benzenesulfonyl-benzyl-amino)-N-(1H-indazol-6-yl)-benzamide;N-Benzyl-N-[3-(4-phenyl-piperidine-1-carbonyl)-phenyl]-benzenesulfonamide;N-Benzyl-N-[3-(3-phenyl-piperidine-1-carbonyl)-phenyl]-benzenesulfonamide;N-Benzyl-N-[3-(2-phenyl-morpholine-4-carbonyl)-phenyl]-benzenesulfonamide;N-Benzyl-N-[3-(4-phenoxy-piperidine-1-carbonyl)-phenyl]-benzenesulfonamide;N-Benzyl-N-[3-(3-phenyl-piperidine-1-carbonyl)-phenyl]-methanesulfonamide;N-Benzyl-N-[3-(2-phenyl-morpholine-4-carbonyl)-phenyl]-methanesulfonamide;N-Benzyl-N-[3-(4-phenoxy-piperidine-1-carbonyl)-phenyl]-methanesulfonamide;N-Benzyl-N-[3-(3-(4-phenyl-piperidine-1-carbonyl)-phenyl]-methanesulfonamide;1-Methyl-1H-imidazole-4-sulfonic acid benzyl-[3-(4-phenyl-piperidine-1-carbonyl)-phenyl]-amide;N-Benzyl-N-[3-(3-( ...

Подробнее
Номер записи: 91
07-08-2014 дата публикации

Sulfur derivatives as chemokine receptor modulators

Номер: US20140221481A1
Автор: Haiqing Yuan, John E. Donello, Michael E. Garst, Richard L. Beard, Veena Viswanath, Xiaoxia Liu
Принадлежит: Allergan Inc

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Подробнее
Номер записи: 92
08-09-2022 дата публикации

PROBE FOR SELECTIVELY CHARACTERIZING ENZYMES INVOLVED IN XENOBIOTIC METABOLISM AND METHOD OF MAKING AND USING THE SAME

Номер: US20220282317A1
Автор: Ramos-Hunter Susan, Whidbey Christopher, Wright Aaron T.
Принадлежит: BATTELLE MEMORIAL INSTITUTE

Activity-based probes that can be used to selectively identify and characterize enzymes that are involved in different phases of xenobiotic metabolism in a host and its microbiota population(s) are described. The activity-based probes described specifically label only their target active enzymes involved in xenobiotic metabolism and therefore provide a measurement of true protein functional activity rather than transcript or protein abundance. The activity-based probes also provide multimodal profiling of these active enzymes. Methods for preparing the activity based probes and exemplary methods for their use also are disclosed. 2. The method of claim 1 , further comprising exposing the probe-enzyme conjugate to a Tag-containing compound to form a probe-enzyme conjugate comprising a Tag moiety.3. The method of claim 1 , further comprising exposing the probe to a light source.4. The method of claim 1 , further comprising extracting a subject sample from the subject and analyzing the subject sample using a fluorescent detection technique claim 1 , a colorimetric detection technique claim 1 , a mass spectrometry technique claim 1 , or a combination thereof.8. The method of claim 1 , wherein one or more Tags are present and wherein each Tag independently is a fluorophore claim 1 , a binding partner of an affinity-based binding pair claim 1 , a quantum dot claim 1 , or a dye.9. The method of claim 1 , wherein the one or more Tags independently are rhodamine claim 1 , fluorescein claim 1 , or biotin.10. The method of claim 1 , wherein one or more Tags are present and wherein each Tag independently is an azide or an alkyne.13. The method of claim 1 , wherein Linkeris an ester group claim 1 , an —O(CH)NR′″C(O)(CH)— group claim 1 , or a —(CH)— group claim 1 , wherein each n′ independently is an integer ranging from 1 to 20 and wherein R′″ is hydrogen claim 1 , aliphatic claim 1 , or aromatic.14. The method of claim 1 , wherein m is 1 and Linkeris an —NR′″C(O)(CH)— group or ...

Подробнее
Номер записи: 93
25-05-2017 дата публикации

MODULATORS OF THE RELAXIN RECEPTOR 1

Номер: US20170144984A1
Автор: Agoulnik Alexander, Agoulnik Irina, Chen Catherine, Ferrer-Alegre Marc, Marugan Juan Jose, Southall Noel, Xiao Jingbo, Zheng Wei
Принадлежит:

Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R, and Rare as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1. 120-. (canceled)21. A method for therapeutic intervention in a facet of mammalian health that is mediated by a mammalian relaxin receptor 1 claim 104 , the method comprising administering to a mammal in need thereof an effective amount of a compound or salt of .2239-. (canceled)40. The method of claim 21 , whereinthe facet of mammalian health is cardiovascular disease.41. The method of claim 40 , wherein the cardiovascular disease is selected from myocardial ischemia-reperfusion injury claim 40 , cardiac fibrosis claim 40 , acute congestive heart failure claim 40 , cerebrovascular disease and stroke claim 40 , post-infarction heart claim 40 , cardiac anaphylaxis claim 40 , cerebral ischemia (stroke) claim 40 , intestinal ischemia-reperfusion injury claim 40 , systemic and pulmonary hypertension claim 40 , vascular inflammation claim 40 , hypertension claim 40 , high blood pressure; left ventricular hypertrophy (LVH); vasodilation; renal hypertension; diuresis; nephritis; natriuresis; scleroderma renal crisis; angina pectoris (stable and unstable); myocardial infarction; heart attack; coronary artery disease; coronary heart disease; cardiac arrhythmias; atrial fibrillation; portal hypertension; raised intraocular pressure; vascular restenosis; chronic hypertension; valvular disease; myocardial ischemia; acute pulmonary edema; acute coronary syndrome; hypertensive retinopathy; hypertensive pregnancy sickness; Raynaud's phenomenon; erectile dysfunction claim 40 , glaucoma claim 40 , ...

Подробнее
Номер записи: 94
14-08-2014 дата публикации

Cyclohexanone compounds and herbicides comprising the same

Номер: US20140228219A1
Автор: Masato Konobe, Yoshinobu Jin, Yosuke NAKASHIMA
Принадлежит: Sumitomo Chemical Co Ltd

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH 2 , O, S, S(O) or S(O) 2 ; R 1 represents a hydrogen atom or a methyl group; R 2 and R 3 represents a hydrogen atom, a C 1-6 alkyl group and the like; R 4 represents a C 6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C 1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Подробнее
Номер записи: 95
15-09-2022 дата публикации

Wdr5-myc inhibitors

Номер: US20220289673A1
Автор: Alex G. Waterson, Alexey Kuznetsov, Changho HAN, Jonathan D. Macdonald, Joseph R. Alvarado, Sameer S. Nikhar, Selena Chacon Simon, Shaun R. Stauffer, Stephen W. Fesik, William P. Tansey
Принадлежит: VANDERBILT UNIVERSITY

Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

Подробнее
Номер записи: 96
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: 97
21-08-2014 дата публикации

Benzamide Compounds and Related Methods of Use

Номер: US20140234939A1
Автор: Khanfar Mohammad, Silverman Richard B., Wang Hua
Принадлежит: Northwestern University

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease. 1. (canceled)5. The compound of wherein Y is selected from oxy claim 4 , alkylene claim 4 , alkyl-substituted alkylene claim 4 , amino and substituted amino moieties.6. The compound of wherein Ris a substituted benzyl moiety claim 5 , said substituents selected from 1-3 halo and cyano substituents and combinations thereof.7. The compound of wherein Y is a substituted amino moiety and Ris selected from phenyl claim 5 , substituted phenyl claim 5 , benzyl claim 5 , substituted benzyl claim 5 , heteroaryl claim 5 , substituted heteroaryl claim 5 , heteroarylalkyl and substituted heteroarylalkyl moieties.8. The compound of wherein said amino substituent is selected from alkyl and cycloalkyl moieties.9. The compound of wherein said amino substituent is selected from methyl claim 8 , ethyl claim 8 , isopropyl and cyclopropyl moieties.10. The compound of wherein said amino substituent is a divalent alkylene moiety claim 9 , where a said Rand said alkylene moiety together provide a cycloheteroalkyl moiety.11. The compound of wherein said amino substituent is a divalent alkylene moiety claim 7 , where a said Rsubstituent and said alkylene moiety together provide a cycloheteroalkyl moiety.13. The compound of wherein Ris selected from phenyl claim 12 , 2- claim 12 , 3- claim 12 , and 5-pyridinyl claim 12 , 2-pyrimidinyl claim 12 , 3-pyridazinyl claim 12 , 2-thiazolyl claim 12 , methylene-2-thiazolyl claim 12 , 2-oxadiazolyl claim 12 , 5-isoxazolyl claim 12 , 2-nicotintate and 2-nicotinamide moieties; and Ris selected from phenyl and 2-pyridinyl moieties.14. The compound of wherein a least one of Rand Ris substituted claim 13 , said substituents independently selected from halo claim 13 , cyano claim 13 , C-Calkyl claim 13 , substituted alkyl claim 13 , alkoxy claim 13 , methylsulfinyl claim 13 , hydroxy claim ...

Подробнее
Номер записи: 98
07-06-2018 дата публикации

ARYL ETHERS AND USES THEREOF

Номер: US20180155279A1
Автор: DIXON Darryl David, GRINA Jonas, Josey John A., Rizzi James P., Schlachter Stephen T., Wallace Eli M., Wang Bin, WEHN Paul, Xu Rui, Yang Hanbiao
Принадлежит:

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo. 164.-. (canceled)66. The method of claim 65 , wherein Ris phenyl or pyridyl claim 65 , wherein said phenyl or pyridyl is substituted with one or more substituents selected from the group consisting of halo claim 65 , C-Calkyl claim 65 , C-Calkoxy and cyano.67. The method of claim 65 , wherein Ris cyano claim 65 , fluoroalkyl claim 65 , sulfinyl claim 65 , sulfonamide claim 65 , sulfonyl or sulfoximinyl.68. The method of claim 65 , wherein Ris hydrogen.69. The method of claim 65 , wherein Ris hydroxy or amino and Ris hydrogen.70. The method of claim 65 , wherein Ris fluoro and n is 1 claim 65 , 2 or 3.73. The method of claim 72 , wherein Ris phenyl or pyridyl claim 72 , wherein said phenyl or pyridyl is substituted with one or more substituents selected from the group consisting of halo claim 72 , C-Calkyl claim 72 , C-Calkoxy and cyano.74. The method of claim 72 , wherein Ris cyano claim 72 , fluoroalkyl claim 72 , sulfinyl claim 72 , sulfonamide claim 72 , sulfonyl or sulfoximinyl.75. The method of claim 72 , wherein Ris hydrogen and Ris hydroxy or amino.76. The method of claim 72 , wherein the enantiomeric excess of said compound is at least about 80%.80. The method of claim 65 , wherein the cancer is hemangioblastoma claim 65 , pheochromocytoma claim 65 , a pancreatic neuroendocrine tumor claim 65 , renal cell carcinoma claim 65 , astrocytoma claim 65 , breast cancer claim 65 , cervical cancer claim 65 , colorectal cancer claim 65 , glioblastoma claim 65 , glioma claim 65 , head and neck cancer claim 65 , hepatocellular cancer claim 65 , non-small cell lung cancer claim 65 , melanoma claim 65 , neuroblastoma claim 65 , ovarian cancer or prostate cancer.81. The ...

Подробнее
Номер записи: 99
08-06-2017 дата публикации

Herbicidally Active Arylcarboxylic Acid Amides

Номер: US20170158629A1
Автор: AHRENS HARTMUT, DIETRICH Hansjörg, GATZWEILER ELMAR, ROSINGER CHRISTOPHER HUGH, SCHMUTZLER Dirk, TIEBES Jörg, WALDRAFF CHRISTIAN
Принадлежит:

Benzamides of the general formula (I) are described as herbicides. 3. A herbicidal composition comprising a herbicidally active content of at least one compound of the formula (I) or salt as claimed in .4. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.5. A method of controlling unwanted plants claim 1 , comprising applying an effective amount of at least one compound of formula (I) or salt as claimed in or a herbicidal composition thereof to one or more plants or to a site of unwanted vegetation.6. A product comprising a compound of formula (I) or salt as claimed in or a herbicidal composition thereof for controlling one or more unwanted plants.7. The product as claimed in claim 6 , wherein the compound of formula (I) or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.8. The product as claimed in claim 7 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2012/028579 A1 discloses N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and use thereof as herbicides. WO 2012/126932 A1 describes N-(1,3,4-oxadiazol-2-yl)arylcarboxamides and use thereof as herbicides. The active ingredients described therein do not always exhibit sufficient activity against harmful plants and/or some do not have sufficient compatibility with some important crop plants such as cereal species, corn and rice.It is an object of the present invention to provide alternative herbicidally active ingredients. This object is achieved by the arylcarboxamides of the invention that are described hereinafter, which bear an alkyl or cycloalkyl radical in the 2 position, a sulfur radical in the 3 position and a cycloalkyl radical in the 4 position.The present invention thus provides arylcarboxamides of the formula (I) ...

Подробнее
Номер записи: 100