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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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3773. Отображено 100.
17-05-2012 дата публикации

Bicyclic compound and use thereof for medical purposes

Номер: US20120122964A1
Автор: Kousuke Tani, Satoshi Nakayama, Shinsaku Yamane, Tohru Kambe, Toru Maruyama
Принадлежит: Ono Pharmaceutical Co Ltd

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

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Номер записи: 1
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.

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Номер записи: 2
13-12-2012 дата публикации

Synthesis of epothilones, intermediates thereto and analogues thereof

Номер: US20120316348A1
Автор: Alexey Rivkin, Ana E. Gabarda, Huajin Dong, Samuel J. Danishefsky, Ting-Chao Chou, Yoshimura Fumikiko
Принадлежит: SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

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Номер записи: 3
03-01-2013 дата публикации

Macrocyclic lactones

Номер: US20130005641A1
Автор: Bernhard Brunner, Christoph Stock, Klaus Ebel, Ralf Pelzer
Принадлежит: BASF SE

The present invention relates to novel macrocyclic lactones, to processes for their preparation and to their use as fragrances and also to products comprising the novel macrocyclic lactones.

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Номер записи: 4
21-03-2013 дата публикации

18ß-GLYCYRRHETINIC ACID DERIVATIVES AND SYNTHETIC METHOD THEREOF

Номер: US20130072694A1
Автор: Hung Chi-Feng, Lin Chun-Nan, Liou Ya-Ting, Maitraie Dravidum, Tu Huang-Yao, Wang Jih-Pyang, Wei Bai-Luh, Yang Shyh-Chyun
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

The present invention provides a chemical compound having the structure being one selected from a group consisting of 2. The method according to further comprising a step of using an isopropylamine solution as the amine solution when Ris CONHCH(CH) claim 1 , and using an aniline solution as the amine solution when Ris CONHCH.3. The method according to further comprising steps of:methylating the 18β-glycyrrhetinic acid to obtain a methylated 18β-glycyrrhetinic acid; andoxidizing the methylated 18β-glycyrrhetinic acid to obtain a second compound.4. The method according to further comprising a step of esterifying the lactone compound to obtain a first derivative of the lactone compound.5. The method according to further comprising a step of cleaving a lactone ring of the lactone compound to obtain a second derivative of the lactone compound.6. The method according to further comprising a step of treating the second derivative with an alcohol solution to obtain a third derivative of the lactone compound.7. The method according to claim 6 , wherein the alcohol solution is one of an isopropyl alcohol solution and a benzyl alcohol solution.8. The method according to further comprising a step of esterifying the second compound with an alcohol solution to obtain a fourth derivative of the lactone compound.9. The method according to further comprising a step of cleaving a lactone ring of the fourth derivative by an acidic solution to obtain a fifth derivative of the lactone compound.13. The method according to claim 12 , wherein the chemical compound with Rbeing one of CONHCH(CH)and CONHCHis obtained by steps of:oxidizing the 18β-glycyrrhetinic acid to form a first compound;treating the first compound with an m-chloroperbenzoic acid to afford a lactone compound; andtreating the lactone compound with an amine solution to obtain the chemical compound being a first derivative of the chemical compound.14. The method according to further comprising a step of using an ...

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Номер записи: 5
09-05-2013 дата публикации

NOVEL POLY(ETHYLENE OXIDE)-BLOCK-POLY(ESTER) BLOCK COPOLYMERS

Номер: US20130116428A1
Автор: LAVASANIFAR Afsaneh, MAHMUD ABDULLAH
Принадлежит: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA

The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer. 125.-. (canceled)27. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris benzyl.28. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris α-cholestryl.29. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris hydrogen.3031.-. (canceled) This application claims the benefit of U.S. provisional patent application No. 60/783,837, filed Mar. 21, 2006.The present invention relates to novel poly(ethylene oxide)-block-poly(ester) block copolymers, particularly poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups and/or bioactive compounds on the polyester block. The invention also relates to a composition and method of use thereof for delivering bioactive agents.Amphiphilic block copolymers can self-assemble to nanoscopic, core/shell structures in which the hydrophobic core acts as a microreservoir for the encapsulation of drugs, proteins or DNA; and the hydrophilic shell interfaces the media. Among different block copolymers designed for drug delivery, those with polyethylene oxide (PEO), as the shell-forming block, and polyester or poly amino acids (PLAA), as the core-forming block, are of increasing interest. This is owed to the biocompatibility of PEO and potential biodegradability of polyester and PLAA, which make them safe for human administration.It is generally known that poly amino acids (PLAA) structures are ...

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Номер записи: 6
30-05-2013 дата публикации

Preparation of caprolactone, caprolactam, 2,5-tetrahydrofuran-dimethanol, 1,6-hexanediol or 1,2,6-hexanetriol from 5-hydroxymethyl-2-furfuraldehyde

Номер: US20130137863A1
Автор: Hero Jan Heeres, Ignacio Vladimiro Melián Cabrera, Johannes Gerardus De Vries, Pim Huat Phua, Teddy
Принадлежит: NEDERLANDSE ORGANISATIE VOOR WETENSCHAPPELIJK ONDERZOEK (NWO)

The present invention relates to a method for preparing caprolactone, comprising converting 5-hydroxymethyl-2-furfuraldehyde by hydrogenation into at least one intermediate compound selected from the group of 2,5-tetrahydrofuran-dimethanol, 1,6-hexanediol and 1,2,6-hexanetriol,and preparing caprolactone from said intermediate compound. Further, the invention relates to a method for preparing 1,2,6-hexanetriol comprising preparing 5-hydroxymethyl-2-furfaldehyde from a renewable source, converting 5-hydroxymethyl-2-furfaldehyde into 2,5-tetrahydrofuran-dimethanol and converting 2,5-tetrahydrofuran-dimethanol into 1,2,6-hexanetriol. Further, the invention relates to a method for preparing 1,6-hexanediol from 1,2,6-hexanetriol, wherein 1,2,6-hexanetriol is subjected to a ring closure reaction, thereby forming (tetrahydro-2H-pyran-2-yl)methanol, and the (tetrahydro-2H-pyran-2-yl)methanol is hydrogenated, thereby forming 1,6-hexane diol.

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Номер записи: 7
06-06-2013 дата публикации

HOMOADAMANTANE DERIVATIVES, PROCESS FOR PREPARING SAME, AND PHOTORESIST COMPOSITIONS

Номер: US20130143157A1
Автор: Ito Katsuki, Kawano Naoya, Ono Hidetoshi, Tanaka Shinji, Uenoyama Yoshitaka
Принадлежит: IDEMITSU KOSAN CO., LTD.

A compound represented by the following formula (I), wherein Ris a hydrogen atom, a halogen atom, a methyl group or a trifluoromethyl group. 3. The production method according to claim 1 , wherein the 5-oxo-4-oxa-5-homoadamantan-2-ol is reacted with methacrylic anhydride.4. A (meth)acrylic polymer obtained by polymerizing the compound according to .5. A positive photoresist composition comprising the (meth)acrylic polymer according to and a photoacid generator.6. A method for forming a resist pattern comprising the steps of:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'forming a photoresist film on a substrate by using the positive photoresist composition according to ;'}selectively exposing the photoresist film to light; andsubjecting the photoresist film which has been selectively exposed to an alkaline development treatment to form a resist pattern. The invention relates to a novel homoadamantane derivative, a method for producing the same, a (meth)acrylic polymer, a positive photoresist composition, and a method for forming a resist pattern.In recent years, a photolithographic process used to produce semiconductor devices has been desired to form a finer pattern along with miniaturization of semiconductor devices. Various methods for forming a fine pattern using a photoresist material that responds to short-wavelength light such as KrF excimer laser light, ArF excimer laser light, or Fexcimer laser light have been studied, and a novel photoresist material that responds to short-wavelength light such as excimer laser light has been desired.Various phenol resin-based photoresist materials have been developed. However, since these materials absorb light to a large extent due to the aromatic ring, it is difficult to obtain pattern accuracy that can deal with miniaturizationIn order to deal with the above problem, a polymer obtained by copolymerizing polymerizable compounds having an alicyclic skeleton (e.g., 2-methyl-2-adamantyl methacrylate) has been proposed ...

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Номер записи: 8
06-06-2013 дата публикации

Microorganisms and methods for the production of caprolactone

Номер: US20130144029A1
Автор: Anthony P. Burgard, Mark J. Burk, Priti Pharkya, Robin E. Osterhout
Принадлежит: Genomatica Inc

The invention provides non-naturally occurring microbial organisms containing caprolactone pathways having at least one exogenous nucleic acid encoding a butadiene pathway enzyme expressed in a sufficient amount to produce caprolactone. The invention additionally provides methods of using such microbial organisms to produce caprolactone by culturing a non-naturally occurring microbial organism containing caprolactone pathways as described herein under conditions and for a sufficient period of time to produce caprolactone.

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Номер записи: 9
13-06-2013 дата публикации

THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS

Номер: US20130150390A1
Автор: Kaino Mie, Meguro Hiroyuki
Принадлежит:

A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect. 16-. (canceled)8. The therapeutic or prophylactic agent of claim 7 , wherein in said Formula (I) claim 7 ,V is —CH═CH—, andwhen Y is represented by the Formula (II), m is 0; orwhen Y is represented by the Formula (III), p is 1.9. The therapeutic or prophylactic agent of claim 8 , wherein in Formula (I) claim 8 ,{'sup': '1', 'Ris hydrogen; and'}{'sup': 4', '4, 'sub': 1', '3, 'when Y is represented by the Formula (II), W is —N(R)— and Ris C-Calkyl, cyanoethyl, tetrahydropyranyl or phenyl; or'}{'sup': '3', 'sub': 1', '3, 'when Y is represented by the Formula (III), n is 0 and Ris C-Calkyl.'}11. A method of producing a therapeutic or prophylactic agent for allergic dermatitis comprising using the compound of the Formula (I) or the pharmaceutically acceptable salt thereof recited for the production of the therapeutic or prophylactic agent for allergic dermatitis.13. A method of producing a therapeutic or prophylactic agent for allergic dermatitis comprising using the compound of the Formula (I) or the pharmaceutically acceptable salt thereof recited for the production of the therapeutic or prophylactic agent for allergic dermatitis.14. The therapeutic method for allergic dermatitis of claim 12 , wherein claim 12 , in said Formula (I) claim 12 ,V is —CH═CH—, andwhen Y is represented by the Formula (II), m is 0; orwhen Y is represented by the Formula (III), p is 1.15. A method of producing a therapeutic or prophylactic agent for allergic dermatitis comprising ...

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Номер записи: 10
13-06-2013 дата публикации

Compositions and methods for treatment of cystic fibrosis and diseases associated with aberrant protein cellular processing

Номер: US20130150422A1
Автор: Agata Trzcinska-Daneluti, Daniela Rotin
Принадлежит: Hospital for Sick Children HSC

The disclosure relates to resorcylic acid lactones and indolinone-containing compounds for use in treatment of diseases associated with aberrant protein processing, such as cystic fibrosis (CF; mucoviscidosis). The disclosure more generally relates to treatment of aberrant protein processing, such as errors in protein folding, trafficking or post-translational modification.

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Номер записи: 11
13-06-2013 дата публикации

BIODEGRADABLE SHAPE MEMORY POLYMER

Номер: US20130150533A1
Автор: Budhlall Bridgette M., Garle Amit L.
Принадлежит:

A shape-memory polymers comprising at least one monomer subunit represented by the following structural formula (1). 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rand Rfor each occurrence is independently selected from a hydrogen claim 1 , a C1-C12 alkyl claim 1 , a C3-C12 cycloalkyl claim 1 , a C2-C12 alkenyl claim 1 , a C3-C12 cycloalkenyl claim 1 , a C3-C12 cycloalkynyl claim 1 , a C2-C12 alkynyl claim 1 , a (C6-C18)aryl(C6-C12)alkyl claim 1 , or a (C6-C18)heteroaryl(C6-C12)alkyl.3. The compound of claim 2 , wherein L is selected from —X— claim 2 , —C(X)— claim 2 , —N(R)— claim 2 , —C(X)X— claim 2 , —XC(X)— claim 2 , —C(X)NR— claim 2 , —NRC(X)—.4. The compound of claim 3 , wherein R claim 3 , R claim 3 , Rand Reach is hydrogen.5. The compound of claim 4 , wherein k and n are each independently is from 0 to 3.6. The compound of claim 5 , wherein X is O.7. The compound of claim 6 , wherein Ar is a C6-C18 aryl.8. The compound of claim 7 , wherein:R for each occurrence is independently selected from a hydrogen, a C1-C12 alkyl, a C3-C12 cycloalkyl, a C2-C12 alkenyl, a (C6-C18)aryl(C6-C12)alkyl, or a (C6-C18)heteroaryl(C6-C12)alkyl; andL is selected from —C(X)—, —C(O)O—, or —OC(O)—.9. The compound of claim 8 , wherein k and n are each independently from 0 to 2.14. The polymer of claim 13 , wherein the polymer comprises from 1 to 99% by weight of the repeat units of structural formula (III).15. The polymer of claim 14 , wherein the polymer comprises from 20 to 50% by weight of the repeat units of structural formula (III).16. The polymer of claim 12 , further comprising at least one initiator.17. The polymer of claim 15 , wherein the initiator is of 2 claim 15 ,2′-(ethane-1 claim 15 ,2-diylbis(oxy))diethanol.18. The polymer of claim 13 , wherein R claim 13 , R claim 13 , R claim 13 , Rand Rfor each occurrence is independently selected from a hydrogen claim 13 , a C1-C12 alkyl claim 13 , a C3-C12 cycloalkyl claim 13 , a C2-C12 alkenyl claim 13 ...

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Номер записи: 12
13-06-2013 дата публикации

PROCESSES FOR THE PRODUCTION OF HYDROGENATED PRODUCTS AND DERIVATIVES THEREOF

Номер: US20130150551A1
Автор: Albin Brooke A., Clinton Nye A., Dombek Bernard D., Dunuwila Dilum, Fruchey Olan S., Keen Brian T., Manzer Leo E.
Принадлежит: BIOAMBER S.A.S.

Processes for making hydrogenated products including caprolactame (CL) caprolactone (CLO) or 1,6-hexanediol (HDO) and derivative thereof from monoammonium adipate (MAA) and/or adipic acid (AA) obtained from a clarified diammonium adipate-containing (DAA-containing) fermentation broth or monoammonium adipate-containing (MAA-containing) fermentation broth. 1. A process for making a hydrogenated product from a clarified DAA-containing fermentation broth comprising;(a) distilling the broth to form an overhead that comprises water and ammonia, and a liquid bottoms that comprises MAA, at least some DAA, and at least about 20 wt % water;(b) cooling and/or evaporating the bottoms, and optionally adding an antisolvent to the bottoms, to attain a temperature and composition sufficient to cause the bottoms to separate into a DAA-containing liquid portion and a MAA-containing solid portion that is substantially free of DAA;(c) separating the solid portion from the liquid portion;(d) recovering the solid portion;(e) hydrogenating the solid portion in the presence of at least one hydrogenation catalyst to produce the hydrogenated product comprising at least one of CL, CLO or HDO; and(f) recovering the hydrogenated product.2. A process for making a hydrogenated product from a DAA-containing fermentation broth comprising:(a) distilling the broth to form a first overhead that includes water and ammonia, and a first liquid bottoms that includes MAA, at least some DAA, and at least about 20 wt % water;(b) cooling and/or evaporating the bottoms, and optionally adding an antisolvent to the bottoms, to attain a temperature and composition sufficient to cause the bottoms to separate into a DAA-containing liquid portion and a MAA-containing solid portion that is substantially free of DAA;(c) separating the solid portion from the liquid portion;(d) recovering the solid portion;(e) dissolving the solid portion in water to produce an aqueous MAA solution;(f) distilling the aqueous MAA ...

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Номер записи: 13
20-06-2013 дата публикации

Processes for the production of hydrogenated products and derivatives thereof

Номер: US20130158229A1
Автор: Bernard D. Dombek, Brian T. Keen, Brooke A. Albin, Dilum Dunuwila, Leo E. Manzer, Nye A. Clinton, Olan S. Fruchey
Принадлежит: Bioamber SAS

A process for making a hydrogenated product comprising caprolactone (CLO) and 1,6-hexanediol (HDO) and derivatives thereof from adipic acid (AA) obtained from fermentation broths containing diammonium adipate (DAA) or monoammonium adipate (MAA).

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Номер записи: 14
27-06-2013 дата публикации

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Номер: US20130165649A1
Автор: Cazin Catherine
Принадлежит:

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

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Номер записи: 15
01-08-2013 дата публикации

MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS

Номер: US20130196987A1
Автор: Boivin Roch, CHIBA Kenichi, Chow Jesse, Du Hong, Eguchi Yoshihito, FUJITA MASANORI, GOTO Masaki, Gusovsky Fabian, Harmange Jean-Christophe, INOUE Atsushi, Jiang Yimin, Kawada Megumi, KAWAI Takatoshi, Kawakami Yoshiyuki, Kimura Akifumi, Kotake Makoto, Kuboi Yoshikazu, Lemelin Charles-Andre, Li Xiang-Yi, Matsushima Tomohiro, Mizui Yoshiharu, Muramoto Kenzo, Sakurai Hideki, Shen Yong-Chun, SHIROTA Hiroshi, Spyvee Mark, Tanaka Isao, Wang John (Yuan), YAMAMOTO Satoshi, YONEDA Naoki
Принадлежит: EISAI CO., LTD.

The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis. 2. (canceled)3. The compound of claim 1 , wherein:{'sub': 1', '1-6', '1-6, 'Ris hydrogen, straight or branched Calkyl, straight or branched Cheteroalkyl, or aryl,'}wherein the alkyl, heteroalkyl, and aryl groups may optionally be substituted with one or more occurrences of halogen, hydroxyl or protected hydroxyl; and{'sub': '3', 'Ris hydrogen.'}4. The compound of claim 3 , where X is oxygen.5. (canceled)6. The compound of claim 3 , where Ris hydrogen.7. The compound of claim 3 , where Y and Z together represent —CH═CH—.8. The compound of claim 3 , where Y and Z together represent trans —CH═CH—.10126-. (canceled)127. The compound of claim 9 , wherein X is oxygen claim 9 , Ris hydrogen and Y and Z together represent —CH═CH—.130. The pharmaceutical composition of claim 129 , wherein:{'sub': 1', '1-6', '1-6, 'Ris hydrogen, straight or branched Calkyl, straight or branched Cheteroalkyl, or aryl; wherein the alkyl, heteroalkyl, and aryl groups may optionally be substituted with one or more occurrences of halogen, hydroxyl or protected hydroxyl; and'}{'sub': '3', 'Ris hydrogen.'}131. The pharmaceutical composition of claim 129 , wherein X is oxygen.132. The pharmaceutical composition of claim 129 , wherein X is oxygen claim 129 , Ris hydrogen and Y and Z together represent —CH═CH—.134. The pharmaceutical composition of claim 129 , wherein the composition is formulated for topical administration.135. A method for treating an inflammatory and/or autoimmune disorder or a disorder resulting from increased angiogenesis and/or cell proliferation comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a subject in need thereof a therapeutically effective amount of a compound according to .'}136. The method ...

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Номер записи: 16
08-08-2013 дата публикации

PROCESS FOR PREPARING A LACTONE

Номер: US20130204015A1
Автор: Jacquot Roland, Marion Philippe
Принадлежит: Rhodia Operations

A method for preparing a lactone is described. Also described, is the preparation of butyrolactone, valerolactone and caprolactone. The method for preparing a lactone can include a reduction of a dicarboxylic acid using hydrogen, in a gaseous phase and in the presence of an effective amount of a catalyst including an active ruthenium-tin phase including at least one RuSnalloy and an RuSnalloy. 1. A process for preparing a lactone , wherein the process comprises reducing a dicarboxylic acid using hydrogen , in a gas phase and with an effective amount of a catalyst present , the catalyst comprising a ruthenium-tin active phase comprised of at least an alloy RuSnand of an alloy RuSn.2. The process as described by claim 1 , wherein the dicarboxylic acid used corresponds to formula (I) below:{'br': None, 'HOOC—R—COOH\u2003\u2003(I)'}wherein in said formula (I), R represents a substituted or unsubstituted divalent group, comprising a linear sequence of atoms in a sufficient number to form the desired lactone.3. The process as described by claim 1 , wherein the dicarboxylic acid used corresponds to formula (I) in which the group R comprises a linear sequence of 2 to 8 atoms.4. The process as described by claim 1 , wherein the dicarboxylic acid used corresponds to formula (I) in which the group R has a total carbon condensation ranging from 2 to 15 carbon atoms claim 1 , and comprises a linear sequence of 2 to 8 atoms which is then included in a ring obtained.5. The process as described by claim 1 , wherein the dicarboxylic acid used corresponds to formula (I) in which the group R represents:a saturated or unsaturated, linear or branched aliphatic group,a saturated or unsaturated, linear or branched aliphatic group in which two vicinal carbon atoms optionally form a ring.6. The process as described by claim 1 , wherein the dicarboxylic acid of formula (I) used is selected from the group consisting of:succinic acid,2-ethylsuccinic acid,malic acid,glutaric acid,2- ...

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Номер записи: 17
15-08-2013 дата публикации

Intermediates and methods for making zearalenone macrolide analogs

Номер: US20130211103A1
Автор: Charles-Andre Lemelin, Francis G. Fang, Hong Du, Jing Li, Kevin (kuo-ming) Wu, Matthew J. Schnaderbeck, Pamela Mcguinness, Roch Boivin, Silvio A. Campagna, Thomas Horstmann, Xiang Niu, Xiaojie (Jeff) Zhu
Принадлежит: Eisai R&D Management Co Ltd

Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R 1 -R 12 are as defined herein.

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Номер записи: 18
22-08-2013 дата публикации

METHOD FOR MANUFACTURING ESTER

Номер: US20130217898A1
Автор: Ishihara Kazuaki, Uyanik Muhammet
Принадлежит: National University Corporation Nagoya University

The present invention relates to a method for manufacturing an ester from a ketone or an aldehyde, which is a reactive substrate, by a Baeyer-Villiger oxidation reaction using hydrogen peroxide, and in this method, as a catalyst, M(BAr), which is a metal borate, is used (M represents an alkali metal or an alkaline earth metal; Ar represents an aryl; and n is the same number as the valence of M). For example, when cyclohexanone was used as the reactive substrate, and Sr[B(3,5-CFCH)]was used as the catalyst, ε-caprolactone was obtained at an isolated yield of 82%. 1. A method for manufacturing an ester from a ketone or an aldehyde , which is a reactive substrate , by a Baeyer-Villiger oxidation reaction using hydrogen peroxide ,{'sub': 4', 'n, "wherein M(BAr), which is a borate salt, is used as a catalyst (M represents an alkali metal, an alkaline earth metal, or a triarylmethyl; four Ar's each represent an aryl having an electron withdrawing group and are identical to or different from each other; and n is the same number as the valence of M)."}2. The method for manufacturing an ester according to claim 1 ,wherein Ar of the borate salt represents pentafluorophenyl or 3,5-bistrifluoromethylphenyl.3. The method for manufacturing an ester according to claim 1 ,wherein the catalyst is used in an amount of 0.1 to 5 percent by mole with respect to that of the reactive substrate.4. The method for manufacturing an ester according towherein the reactive substrate has a carbon-carbon double bond, a carbon-carbon triple bond, a halogen group, a hydroxyl group, a silyl group, or a siloxy group.5. The method for manufacturing an ester according to claim 1 ,wherein the reactive substrate comprises a cyclic ketone, a chain ketone, a chromanone, or an aromatic aldehyde.6. The method for manufacturing an ester according to claim 1 ,wherein the method uses a Brønsted acid as a promoter.7. The method for manufacturing an ester according to claim 6 ,wherein the promoter comprises a ...

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Номер записи: 19
29-08-2013 дата публикации

CHIRAL COMPOUNDS, COMPOSITIONS, PRODUCTS AND METHODS EMPLOYING SAME

Номер: US20130224136A1
Автор: Boissy Raymond, deLong Mitchell A., Kvalnes Kalla Lynn
Принадлежит: LASYA, INC.

Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein. 15. A composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) from about 0.0001% to about 99.999% of a compound according to formula (I) of ;'}{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, '(b) from about 99.999% to about 0.0001% of a compound according to formula (II) of ; and'}(c) optionally, a pharmaceutically acceptable carrier,{'sup': 1', '2', '1, 'claim-ref': [{'@idref': 'CLM-00001', 'claim 1'}, {'@idref': 'CLM-00008', 'claim 8'}], 'wherein at least one of the substituents X, X, A, B, Z and Rin the compound according to formula (I) of is different from the corresponding substituent in the compound according to formula (II) of .'}16. A product comprising a compound according to .1722-. (canceled)2318. The product according to claim claim 1 , wherein said product is a skin care composition.24. The product according to claim 23 , further comprising a dermatologically acceptable carrier.25. (canceled)26. (canceled)27. A method of lightening mammalian skin claim 1 , said method comprising topically applying a compound according to to an area of skin in need of treatment.2831-. (canceled)32. A product comprising a compound according to .33. The product according to claim 32 , wherein said product is a skin care composition.34. The product according to claim 33 , further comprising a dermatologically acceptable carrier.35. A method of lightening ...

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Номер записи: 20
29-08-2013 дата публикации

SKIN LIGHTENING COMPOSITIONS

Номер: US20130224137A1
Автор: Chambournier Gilles, deLong Mitchell A., Ewell Kevin R., Kvalnes Kalla Lynn, Witwit Moe
Принадлежит: LASYA, INC.

Compositions and methods for lightening mammalian skin are described herein. 2. The composition of claim 1 , wherein Z is O.3. The composition of claim 1 , wherein A and B are taken together with the atoms to which they are attached to form an optionally substituted ring having from 4-9 member atoms.4. The composition of claim 1 , wherein A and B are taken to taken together with the atoms to which they are attached to form a ring having 6 member atoms.12. The composition of claim 1 , wherein the compound of formula I is 4-(tetrahydro-2H-pyran-2-yloxy)phenol.13. The composition of claim 1 , wherein the compound of formula I is present in the composition at a concentration of about 0.5 wt. % to about 10 wt. %.14. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid claim 1 , tocopherol claim 1 , butylated hydroxybenzoic acid claim 1 , butylated hydroxytoluene claim 1 , butylated hydroxyanisole claim 1 , uric acid claim 1 , gallic acid claim 1 , sorbic acid claim 1 , glutathione claim 1 , and esters and salts of any thereof.15. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant comprises at least one of ascorbic acid or a salt thereof claim 1 , ascorbyl phosphate or a salt thereof claim 1 , ascorbyl palmitate or a salt thereof claim 1 , tocopherol or a salt thereof claim 1 , tocopheryl acetate and sodium metabisulfite.16. The composition of claim 1 , comprising at least two antioxidants.17. The composition of claim 1 , comprising at least three antioxidants.18. The composition of claim 1 , comprising at least four antioxidants.19. The composition of claim 1 , comprising at least five antioxidants.20. The composition of claim 1 , wherein the composition comprises an antioxidant and the antioxidant is present in an amount of about 0.01 wt. % to about 3.0 wt. %.21. The composition of claim 1 , wherein the composition comprises an antioxidant ...

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Номер записи: 21
29-08-2013 дата публикации

NOVEL PROCESS FOR THE PREPARATION OF ASENAPINE

Номер: US20130225835A1
Автор: Dalmases Barjoan Pere, Huguet Clotet Juan, Peirats Masia Jordi
Принадлежит: LABORATORIOS LESVI, S.L.

The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I). 2. A compound according to selected from the group consisting of trans-N-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-formamide claim 1 , trans-N-(2-Chloro-11 -hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-formamide claim 1 , trans-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid benzyl ester claim 1 , trans-(2-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid benzyl ester claim 1 , trans-(8-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid ethyl ester claim 1 , trans-(2-Chloro-11-hydroxymethyl-10 claim 1 ,11-dihydro-dibenzo[b claim 1 ,f]oxepin-10-ylmethyl)-carbamic acid ethyl ester claim 1 , or a salt thereof.4. A process according to wherein the formic acid anhydride of formula III is selected from the group consisting of formic acetic anhydride claim 3 , formic propionic anhydride or formic isobutyric anhydride.6. A process according to wherein the reducing agent of step (a) or step (b-i) is a boron hydride or an aluminum hydride.7. A process according to wherein the leaving group is a halogen.8. A process according to wherein steps (b) and (c) are performed in one-pot manner without isolating intermediate compound of formula VI.9. A process for preparing asenapine or a salt of asenapine comprising treating compound of formula I according to with a reducing agent.15. Use of one or more compounds of for the preparation of asenapine or salts thereof.16. Use of compound of formula II prepared ...

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Номер записи: 22
03-10-2013 дата публикации

CATALYST COMPLEX WITH CARBENE LIGAND

Номер: US20130261296A1
Автор: HUANG Jinkun, NOLAN Steven P.
Принадлежит:

Catalytic complexes including a metal atom having anionic ligands, at least one nucleophilic carbene ligand, and an alkylidene, vinylidene, or allenylidene ligand. The complexes are highly stable to air, moisture and thermal degradation. The complexes are designed to efficiently carry out a variety of olefin metathesis reactions. 2. A catalytic complex according to wherein Ar is η—CHN or an alkyl substituted derivative thereof claim 1 , p-cymene claim 1 , fluorene claim 1 , or indene.3. A catalytic complex according to wherein the complex is linked to a solid support by means of a link between said anionic ligand and said solid support.4. A catalytic complex according to wherein the complex is linked to a solid support by means of a link between said nucleophilic carbene and said solid support.5. A method of performing ring closing metathesis claim 1 , said method comprising contacting a diene with a catalytic complex of under conditions appropriate claim 1 , and for a time sufficient to produce a cyclic alkene.6. A method according to wherein Ar is η—CHN or an alkyl substituted derivative thereof claim 5 , p-cymene claim 5 , fluorene claim 5 , or indene.8. A method as in wherein the terminal acetylene is substituted at the y-position with hydrogen claim 7 , a vinyl claim 7 , group or a phenyl group claim 7 , wherein the vinyl or phenyl group is optionally substituted with one or more moieties selected from C-Calkyl claim 7 , C-Calkoxy claim 7 , phenyl claim 7 , or a functional group selected from chloride claim 7 , bromide claim 7 , iodide claim 7 , fluoride claim 7 , nitro claim 7 , or dimethylamine.9. A method as in wherein the precursor species is formed from a dimer of the formula [ArMXX]by exposing the dimer to a nucleophilic carbene in a suitable solvent. This application is a continuation of application Ser. No. 13/041,573, filed Mar. 7, 2011, which is continuation of U.S. Pat. No. 7,902,389, issued Mar. 8, 2011, which is a continuation of U.S. Pat. No. 7, ...

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Номер записи: 23
14-11-2013 дата публикации

BENZYLPIPERIZINE COMPOUND

Номер: US20130303786A1
Автор: TOYODA Tomohiro, YOSHINAGA Hidefumi
Принадлежит:

Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), Rrepresents a hydrogen atom or a methyl group; Ris a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.) 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein LGrepresents a bromine atom claim 1 , or a substituted sulfonyloxy group.3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein LGrepresents a benzenesulfonyloxy group claim 1 , or a p-toluenesulfonyloxy group.4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound represented by the formula (12) is selected from the group consisting of the following compounds:(2-(4-Oxo-3,4-dihydro-2H-chromen-6-yl)ethyl 4-methylbenzenesulfonate,2-(8-Oxo-5,6,7,8-tetrahydronaphthalen-2-yl)ethyl 4-methylbenzenesulfonate,2-(3-Oxo-2,3-dihydro-1H-inden-5-yl)ethyl 4-methylbenzenesulfonate,2-(5-Oxo-2,3,4,5-tetrahydro-1-benzoxepin-7-yl)ethyl 4-methylbenzenesulfonate, and(2-(4-Oxo-3,4-dihydro-2H-chromen-6-yl)ethyl benzenesulfonate).5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound represented by the formula (12) is selected from the group consisting of the following compounds:(2-(4-Oxo-3,4-dihydro-2H-chromen-6-yl)ethyl 4-methylbenzenesulfonate, and(2-(4-Oxo-3,4-dihydro-2H-chromen-6-yl)ethyl benzenesulfonate). This application is a Divisional Application of U.S. application Ser. No. 13/527,612, filed Jun. 20, 2012, now allowed, which is a Continuation ...

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Номер записи: 24
05-12-2013 дата публикации

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Номер: US20130324577A1
Автор: Kambe Tohru, SUGIMOTO Isamu
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. 4. The compound according to claim 1 , which is a compound selected from the group consisting of(1) 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3S)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(2) 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-5-phenyl-1-penten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(3) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-5-(3-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(4) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3S)-5-(3-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(5) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-5-(4-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(6) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3S)-5-(4-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(7) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-5-(2-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(8) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3S)-5-(2-fluorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(9) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-5-(3-chlorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(10) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3S)-5-(3-chlorophenyl)-3-hydroxy-1-penten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(11) 4-[(3S,5aR,6R,7R,8aS)-7-hydroxy-6-{(1E,3R)-3-hydroxy-5-[3-(trifluoromethyl)phenyl]-1-penten-1-yl}octahydro-2H-cyclopenta[b]oxepin-3-yl]butanoic acid,(12) 4-[(3S,5aR,6R,7R,8aS)-7-hydroxy-6-{(1E,3S)-3-hydroxy-5-[3-(trifluoromethyl)phenyl]-1-penten-1-yl}octahydro-2H-cyclopenta[b]oxepin-3-yl]butanoic acid,(13) 4-[(3S,5aR,6R,7R,8aS)-7-hydroxy-6-{(1E,3S)-3- ...

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Номер записи: 25
05-12-2013 дата публикации

MACROCYCLIC TRIENE LACTONES HAVING UNCONJUGATED TRIENE STRUCTURE, ITS PRODUCTION METHOD AND ITS SYNTHETIC INTERMEDIATE

Номер: US20130324744A1
Автор: Inaba Teruhiko, Ishida Kenya
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention provides a novel macrocyclic compound exhibiting superior odor qualities and having a musk-like aroma, a method for producing the same, and a novel flavor or fragrance composition, and food products or beverages, fragrances or cosmetics, daily necessities or household goods and oral products using the novel macrocyclic compound. The invention relates to a compound represented by the formula (1), wherein each of wavy lines represents at least one of an E-configuration of C═C double bond and an Z-configuration of C═C double bond; m represents an integer of 0 to 10; and n represents an integer of 1 to 11, and n represents an integer of 1 to 11 when m is 0 to 4 or 6 to 10, and n is an integer of 1 or 3 to 11 when m is 5. 2. The compound according to claim 1 , wherein all of the wavy lines are the Z-configuration of C═C double bond.3. The compound according to claim 1 , which has a musk aroma.5. The method according to claim 4 , wherein all of the wavy lines in the formula (1) are the Z-configuration of C═C double bond.6. The method according to claim 4 , wherein the compound represented by the formula (1) in which all of the wavy lines are the Z-configuration of C═C double bond is produced in a ratio of 95% or more based on the whole of the produced compounds represented by the formula (1) claim 4 , and the rest can either be geometrical isomers.7. The method according to claim 4 , wherein the ω-hydroxytriene esters represented by the formula (3) is lactonized with titanate.10. The ω-hydroxytriene esters according to claim 9 , wherein all of the wavy lines are the Z-configuration of C═C double bond.11. A flavor or fragrance composition comprising the compound according to .12. A product comprising the compound according to claim 1 , wherein the product is selected from the group consisting of a food product or beverage claim 1 , a fragrance or cosmetic claim 1 , a daily necessities and household goods and an oral product.13. A product comprising ...

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Номер записи: 26
09-01-2014 дата публикации

Migrastatin analogs and uses thereof

Номер: US20140011844A1
Автор: Christoph Gaul, Jon T. Njardarson, Samuel J. Danishefsky
Принадлежит: SLOAN KETTERING INSTITUTE FOR CANCER RESEARCH

The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R 1 -R 6 , R a -R c , Q, Y 1 , Y 2 and n are as defined herein.

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Номер записи: 27
16-01-2014 дата публикации

Use of 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2,4-dienoic acid as a cosmetic

Номер: US20140017187A1
Автор: ANZALI Soheila, CONTARD Francis, ZEILLER Jean Jacques
Принадлежит: Merck Patent GmBH

The invention relates to 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2,4-dienoic acid and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound. 15.-. (canceled)6. A method of manufacturing a cosmetic composition , comprising combining together 5-(7-methoxy-3 ,3-dimethyl-2 ,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2 ,4-dienoic and/or a salt or solvate , with one or more cosmetically acceptable vehicles , and optionally one or more further active compounds having a skin-care and/or inflammation-inhibiting action.7. A method for the prophylaxis and/or treatment of skin diseases which are associated with defective keratinisation relating to differentiation and cell proliferation , acne vulgaris , acne comedonica , polymorphic acne , acne rosaceae , nodular acne , acne conglobata , age-related acne , acne occurring as a side effect , acne solaris , medicament-related acne or acne professionalis , for the treatment of other defects of keratinisation , ichthyosis , ichthyosiform states , Darier's disease , keratosis palmoplantaris , leukoplakia , leukoplakiform states , skin and mucosal (buccal) eczema (lichen) , for the treatment of other skin diseases which are associated with defective keratinisation and have an inflammatory and/or immunoallergic component , all forms of psoriasis relating to the skin , mucous membranes and finger- and toenails , and psoriatic rheumatism and skin atopy , eczema , respiratory atopy , or hypertrophy of the gums , said method comprising applying an effective amount of 5-(7-methoxy-3 ,3-dimethyl-2 ,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2 ,4-dienoic and/or a salt or solvate , with one or more cosmetically acceptable vehicles , and optionally one or more further active compounds having a skin-care and/or inflammation-inhibiting action to a patient in need thereof.8. A method for the care , preservation or improvement of the ...

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Номер записи: 28
23-01-2014 дата публикации

PROCESS FOR THE PREPARATION OF OLOPATADINE

Номер: US20140024704A1
Автор: Castellin Andrea, Ferrari Clark, Galvagni Marco
Принадлежит:

A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate. 2. The process of wherein R is n-butyl.3. The process of claim 1 , wherein the obtained olopatadine hydrochloride has an HPLC purity equal or higher than about 99.90% (Area %) and each single impurity lower than about 0.05% (HPLC Area %).4. The process of claim 1 , containing less than about 30 ppm of bromide ion.5. Olopatadine hydrochloride containing less than 300 ppm of bromide ion.6. The olopatadine hydrochloride of claim 5 , containing less than 30 ppm of bromide ion.7. Oloptadine hydrochloride having an HPLC purity equal or higher than about 99.90% (Area %) and each single impurity lower than about 0.05% (HPLC Area %).8. A pharmaceutical composition comprising the olopatadine hydrochloride of .9. A pharmaceutical composition comprising the olopatadine hydrochloride of .10. A method for the treatment of pathologies comprising allergic rhinitis claim 8 , urticaria claim 8 , dermatitis claim 8 , asthma claim 8 , conjunctivitis and/or of their symptoms claim 8 , comprising administering the pharmaceutical composition of .11. A method for the treatment of pathologies comprising allergic rhinitis claim 9 , urticaria claim 9 , dermatitis claim 9 , asthma claim 9 , conjunctivitis and/or of their symptoms claim 9 , comprising administering the pharmaceutical composition of . This is a divisional of application Ser. No. 12/990,442, filed Nov. 18, 2010, which is a 371 of International Application No. PCT/EP2010/053783, filed Mar. 23, 2010, which claims priority to Italian Application No. MI2009A000659, filed Apr. 21, 2009, the disclosures of which are incorporated by reference in their entireties.The present invention relates to a novel process for the preparation of olopatadine hydrochloride.Olopatadine hydrochloride, chemical name dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro hydrochloride, (11Z), of formula (I)is a novel antihistamine ...

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Номер записи: 29
23-01-2014 дата публикации

MIGRASTATINS AND USES THEREOF

Номер: US20140024705A1
Автор: Cortes Manuel Valiente, Danishefsky Samuel J., Lecomte Nicolas, Massague Joan, Moore Malcom, Oskarsson Thordur, Ouerfelli Ouathek, Yang Guangli
Принадлежит: Sloan-Kettering Institute for Cancer Research

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. 2. The compound of claim 1 , wherein Ris Caliphatic substituted with one or more halogens or Ris -T-Y wherein -T- is CHand —Y is acyl.3. The compound of claim 2 , wherein Ris —CFor Ris -T-Y wherein -T- is CHand —Y is —COH.6. The compound of or claim 2 , wherein Ris hydrogen or Caliphatic substituted with one or more halogens claim 2 , Ris Caliphatic claim 2 , Ris Caliphatic claim 2 , Ris hydrogen or -T-Y wherein -T- is a covalent bond or —CH— and Y is selected from the group consisting of —COR and —C(O)N(R) claim 2 , wherein R is hydrogen or Caliphatic claim 2 , Ris Caliphatic claim 2 , and is a single bond.7. The compound of or claim 2 , wherein Ris hydrogen or Caliphatic substituted with one or more halogens claim 2 , Ris Caliphatic claim 2 , Ris Caliphatic claim 2 , Ris hydrogen or -T-Y wherein -T- is a covalent bond or —CH— and Y is selected from the group consisting of —COR and —C(O)N(R) claim 2 , wherein R is hydrogen or Caliphatic claim 2 , Ris Caliphatic claim 2 , and is a (Z)-double bond.8. The compound of or claim 2 , wherein Ris hydrogen or Caliphatic substituted with one or more halogens claim 2 , Ris Caliphatic claim 2 , Ris Caliphatic claim 2 , Ris hydrogen or -T-Y wherein -T- is a covalent bond or —CH— and Y is selected from the group consisting of —COR and —C(O)N(R) claim 2 , wherein R is hydrogen or Caliphatic claim 2 , Ris Caliphatic claim 2 , and is an (E)- double bond.9. The compound of or claim 2 , wherein Ris hydrogen claim 2 , Ris methyl claim 2 , Ris methyl claim 2 , Ris -T-Y wherein -T- is —CH— and Y is selected from the group consisting of —COR and —C(O)N(R) claim 2 , wherein R is methyl claim 2 , Ris methyl claim 2 , and is a single bond.10. The compound of or claim 2 , wherein Ris hydrogen claim 2 , Ris methyl claim 2 , Ris methyl claim 2 , Ris -T-Y wherein -T- is —CHCHO— and Y is hydrogen claim 2 , wherein R is ...

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Номер записи: 30
30-01-2014 дата публикации

POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES

Номер: US20140031302A1
Автор: BARLUENGA Sofia, WINSSINGER Nicolas
Принадлежит: Universite De Strasbourg

The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90). 2. The compound of claim 1 , wherein X is O or NR.3. The compound of claim 1 , wherein Y is —OR claim 1 , —O—(CH)COOR or —O—(CH)CON(R).4. The compound of claim 1 , wherein Rand Rare independently hydrogen claim 1 , halogen claim 1 , or lower alkyl.5. The compound of claim 4 , wherein{'sup': '1', 'Ris hydrogen, halogen, or lower alkyl; and'}{'sup': '2', 'Ris hydrogen.'}6. The compound of claim 1 , wherein Ris lower alkyl claim 1 , alkoxy-substituted lower alkyl claim 1 , or aryl-substituted lower alkyl.7. The compound of claim 6 , wherein Ris methyl claim 6 , ethyl claim 6 , isopropyl claim 6 , n-propyl claim 6 , n-butyl claim 6 , isobutyl claim 6 , t-butyl claim 6 , methoxy-ethyl claim 6 , methoxy-methyl claim 6 , chloromethyl claim 6 , or benzyl.8. The compound of claim 1 , wherein L-TM is an oxygen or nitrogen-based functional group.14. A compound selected from the group consisting of the compounds exemplified by Scheme 2 as described in the specification claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , and/or prodrug thereof.15. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.16. A method of treating a patient with a disease comprising administering to the patient with the disease an effective amount of a compound of claim 1 , wherein the disease is mediated by kinases and Heat Shock Protein 90 (HSP90).17. The method of claim 16 , wherein the disease is an autoimmune disease claim 16 , inflammatory disease claim 16 , neurological or neurodegenerative disease claim 16 , cancer claim 16 , cardiovascular disease claim 16 , ...

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Номер записи: 31
13-03-2014 дата публикации

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Номер: US20140073676A1
Автор: Kambe Tohru, Maruyama Toru, Nakayama Satoshi, TANI Kousuke, Yamane Shinsaku
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. 4. The compound according to claim 3 , wherein the ring 2 is a C3-7 carbocycle; or a salt thereof claim 3 , a solvate thereof claim 3 , or a prodrug thereof.6. The compound according to claim 3 , wherein the compound represented by the general formula (I-2) is a compound selected from:(1) 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(2) ethyl 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(3) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(4) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(3-chlorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(5) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(3-chlorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(6) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid, and(7) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate;or a salt thereof, a solvate thereof, or a prodrug thereof.7. A pharmaceutical composition containing a compound represented by the general formula (I) according to claim 1 , or a salt thereof claim 1 , a solvate thereof ...

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Номер записи: 32
27-03-2014 дата публикации

ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS

Номер: US20140088158A1
Автор: Kleemann Heinz-Werner, PATEK Marcel, PERNERSTORFER Josef, SAFAROVA Alena, Schaefer Matthias
Принадлежит: SANOFI

The present invention relates to compounds of the formula I, 2. The compound according to claim 1 , wherein ring A is a 3-membered to 8-membered monocyclic ring which comprises 0 or 1 hetero ring members chosen from the series consisting of O claim 1 , S claim 1 , S(O) and S(O) claim 1 , and which is saturated claim 1 , wherein ring A is optionally substituted on ring carbon atoms by one or more identical or different substituents chosen from the series consisting of halogen claim 1 , R claim 1 , R claim 1 , (C-C)-alkenyl claim 1 , HO— claim 1 , R—O— claim 1 , phenyl-(C-C)-alkyl-O— claim 1 , R—C(O)—O— claim 1 , R—S(O)—O— claim 1 , HO—C(O)— claim 1 , R—O—C(O)— claim 1 , HN—C(O)— claim 1 , R—NH—C(O)— claim 1 , R—N(R)—C(O)— and oxo;or a stereoisomeric form thereof or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof.3. The compound according to claim 1 , wherein ring A is a cyclohexane ring or cycloheptane ring claim 1 , each of which is optionally substituted by one or more identical or different substituents chosen from the series consisting of halogen claim 1 , R claim 1 , R claim 1 , (C-C)-alkenyl claim 1 , HO— claim 1 , R—O— claim 1 , phenyl-(C-C)-alkyl-O— claim 1 , R—C(O)—O— claim 1 , R—S(O)—O— claim 1 , HO—C(O)— claim 1 , R—O—C(O)— claim 1 , HN—C(O)— claim 1 , R—NH—C(O)— claim 1 , R—N(R)—C(O)— and oxo;or a stereoisomeric form thereof or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof.4. The compound according to claim 1 , wherein{'sup': 12', '13', '15, 'Y is chosen from the series consisting of C(R)═C(R) and C(R)═N; and'}{'sup': '16', 'Z is C(R);'}or a stereoisomeric form thereof or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof.5. The compound according to claim 1 , wherein{'sup': 21', '1', '13', '14', '13', '14, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', 'm', '1', '4, 'Ris ...

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Номер записи: 33
03-04-2014 дата публикации

HIGHLY PURE PENTAMYCIN

Номер: US20140094602A1
Автор: Krimmer Dieter, Meier Victor, Reuter Karl, Stolz Florian, Winninps Cees
Принадлежит: Biolotus Biotechnology AG

Described is pentamycin in a purity exceeding 95%, certain polymorphs and solvates of pentamycin, processes for their manufacture, and a method for decreasing the rate of degradation of pentamycin. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. Pentamycin with a chemical purity exceeding 95%.20. Pentamycin in the form of a solvate with a heterocyclic compound.21. The pentamycin according to in the form of a morpholine solvate.22. A method for significantly decreasing the rate of degradation of pentamycin with a purity exceeding 95% comprising the step of transforming pentamycin with a purity exceeding 95% into its polymorph A.23. The method according to wherein the transformation into polymorph A is effected by crystallization from a solution of more than 95% pure pentamycin in dimethylsulfoxide after adding ethyl acetate. The invention relates to highly pure pentamycin, certain polymorphs and solvates of pentamycin, processes for their manufacture, and to a method for decreasing the rate of degradation of more than 95% pure pentamycin.Pentamycin, like Amphotericin B and Nystatin A1, belongs to the class of polyene macrolide antibiotics having antifungal activity. Pentamycin is obtainable from natural sources, e.g. it may be isolated from certain strains, like the mycelium of the actinomyces as described by S. Umezawa and Y. Tanaka in J. Antibiotics, Ser. A, vol. XI, no. 1, pages 26 to 29 (1958), or from luteus (NRRL 2776, NCIB 8984) as described in British patent 884711 to Glaxo. Said patent is directed to the production of the antibiotic lagosin which has been shown in the below-mentioned Pandey et al. article in J. Antibiotics vol. XXXV no. 8, pages 988-996 (1982) to be identical to fungichromin and cogomycin. Lagosin, both as a solid and in solution is stated in said British ...

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Номер записи: 34
10-04-2014 дата публикации

Oligomer-tricyclic conjugates

Номер: US20140100268A1
Автор: Jennifer Riggs-Sauthier, Stephanie Allums-Donald, Wen Zhang, Xuyuan Gu
Принадлежит: Nektar Therapeutics

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer.

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Номер записи: 35
04-01-2018 дата публикации

MACROCYCLIC PICOLINAMIDE COMPOUNDS WITH FUNGICIDAL ACTIVITY

Номер: US20180002319A1
Автор: ARNOLD Amela, Bravo-Altamirano Karla, Daeuble, DeLorbe Johnathan E., Herrick Jessica, Jones David M., LaLonde Rebecca Lyn K.C., Li Fangzheng, Meyer Kevin G., Renga James M., SR. John F., Wilmot Jeremy, Yao Chenglin
Принадлежит:

This disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides. 2. The compound according to claim 1 , wherein X and Y are hydrogen.3. The compound according to claim 2 , wherein Ris selected from the group consisting of hydrogen claim 2 , alkyl claim 2 , alkenyl claim 2 , and aryl claim 2 , each optionally substituted with 0 claim 2 , 1 claim 2 , or multiple R.4. (canceled)5. The compound according to claim 2 , wherein Ris independently selected for Rand Rfrom the group consisting of hydrogen claim 2 , alkyl claim 2 , alkenyl claim 2 , and aryl claim 2 , each optionally substituted with 0 claim 2 , 1 claim 2 , or multiple R.6. The compound according to claim 1 , wherein X is C(O)Rand Y is hydrogen.7. The compound according to claim 6 , wherein Ris selected from the group consisting of hydrogen claim 6 , alkyl claim 6 , alkenyl claim 6 , and aryl claim 6 , each optionally substituted with 0 claim 6 , 1 claim 6 , or multiple R.8. (canceled)9. The compound according to claim 6 , wherein Ris independently selected for Rand Rfrom the group consisting of hydrogen claim 6 , alkyl claim 6 , alkenyl claim 6 , and aryl claim 6 , each optionally substituted with 0 claim 6 , 1 claim 6 , or multiple R.10. The compound according to claim 1 , wherein X is hydrogen and Y is Q.11. The compound according to claim 10 , wherein Ris alkoxy.12. The compound according to claim 11 , wherein Ris hydrogen.13. The compound according to claim 12 , wherein Ris selected from the group consisting of hydrogen claim 12 , alkyl claim 12 , alkenyl claim 12 , and aryl claim 12 , each optionally substituted with 0 claim 12 , 1 claim 12 , or multiple R.14. (canceled)15. The compound according to claim 12 , wherein Ris independently selected for Rand Rfrom the group consisting of hydrogen claim 12 , alkyl claim 12 , alkenyl claim 12 , and aryl claim 12 , each optionally substituted with 0 claim 12 , 1 claim 12 , or multiple R.16. The compound according to claim 11 , ...

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Номер записи: 36
04-01-2018 дата публикации

USE OF MACROCYCLIC PICOLINAMIDES AS FUNGICIDES

Номер: US20180002320A1
Автор: ARNOLD Amela, Bravo-Altamirano Karla, Daeuble, DeLorbe Johnathan E., Herrick Jessica, Jones David M., LaLonde Rebecca Lyn K.C., Li Fangzheng, Meyer Kevin G., Renga James M., SR. John F., Wilmot Jeremy, Yao Chenglin
Принадлежит:

This disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides. 2. A composition according to claim 1 , wherein X is hydrogen and Y is Q.3. A composition according to claim 2 , wherein Ris alkoxy.4. A composition according to claim 3 , wherein Ris hydrogen.5. A composition according to claim 4 , wherein Ris selected from the group consisting of hydrogen claim 4 , alkyl claim 4 , alkenyl claim 4 , and aryl claim 4 , each optionally substituted with 0 claim 4 , 1 claim 4 , or multiple R.6. (canceled)7. A composition according to claim 4 , wherein Ris independently selected for Rand Rfrom the group consisting of hydrogen claim 4 , alkyl claim 4 , alkenyl claim 4 , and aryl claim 4 , each optionally substituted with 0 claim 4 , 1 claim 4 , or multiple R.8. A composition according to claim 3 , wherein Ris selected from the group consisting of —C(O)Rand —CHOC(O)R.9. A composition according to claim 8 , wherein Ris alkyl claim 8 , optionally substituted with 0 claim 8 , 1 claim 8 , or multiple R.10. A composition according to claim 9 , wherein Ris selected from the group consisting of hydrogen claim 9 , alkyl claim 9 , alkenyl claim 9 , and aryl claim 9 , each optionally substituted with 0 claim 9 , 1 claim 9 , or multiple R.11. (canceled)12. A composition according to claim 9 , wherein Ris independently selected for Rand Rfrom the group consisting of hydrogen claim 9 , alkyl claim 9 , alkenyl claim 9 , and aryl claim 9 , each optionally substituted with 0 claim 9 , 1 claim 9 , or multiple R.13. A composition according to claim 12 , wherein Ris selected from the group consisting of —CH claim 12 , —CH(CH) claim 12 , and —CHOCHCH.14. A composition for the control of a fungal pathogen including at least one of the compositions of and a phytologically acceptable carrier material.15. A composition for the control of a fungal pathogen including at least one of the compositions of and a phytologically acceptable carrier material.16. (canceled)17. A ...

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Номер записи: 37
07-01-2021 дата публикации

COMPOUND AND POLYMER COMPOUND CONTAINING THE COMPOUND

Номер: US20210002284A1
Автор: Abe Hiroya, SAITO Shohei, YABU Hiroshi
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

Provided is a compound having higher fluorescence quantum yield and higher optical stability than a conventional FLAP and a polymer compound containing the compound. 4. The compound according to claim 1 , wherein the E claim 1 , E claim 1 , and Eeach denote a polymerizable substituent group.7. The compound according to claim 3 , wherein in the general Formula (1) claim 3 , the Band Bhave any of structures of the general Formulas (5-1) and (5-2).8. The compound according to claim 3 ,{'sup': 1', '2, 'wherein in the general Formula (1), the Band Bhave a structure of the general Formula (5-3), and'}wherein m and n of a compound represented by the general Formula (1) are 0 or 3.9. The compound according to claim 1 , wherein in the general Formula (1) claim 1 ,the a1denotes an integer of 0 to 3 when m is 0, and{'sup': '1', 'denotes an integer that Ycan be substituted in accordance with the number 0 to m when m is an integer greater than or equal to 1 and less than or equal to 3,'}the a2denotes an integer of 0 to 3 when n is 0, and{'sup': '2', 'denotes an integer that Ycan be substituted in accordance with the number 0 to n when n is an integer greater than or equal to 1 and less than or equal to 3, and'}the b denotes an integer greater than or equal to 0 and less than or equal to 4,10. The compound according to claim 2 , wherein in the general Formula (1) claim 2 , the A is the general Formula (4).11. The compound according to claim 1 , wherein in the general Formula (1) claim 1 , the b is an integer greater than or equal to 1 and less than or equal to 4.12. A polymer compound made by polymerizing the compound described in .13. The polymer compound according to claim 12 , wherein the compound is bound to the polymer compound via a urethane binding in the polymer compound.14. The polymer compound according to further comprising claim 12 , in a main chain of the polymer compound claim 12 , a chemical structure included in the compound.15. The polymer compound according to ...

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Номер записи: 38
14-01-2016 дата публикации

Tricyclic compound and use thereof

Номер: US20160009677A1
Автор: Jae-Sun Kim, Jaeseung AHN, Je Ho Ryu, Jeong A Lee, Joon Ho Sa, Ju Young Lee, Min-Young Han, Taekyung Yoo
Принадлежит: SK Chemicals Co Ltd

The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.

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Номер записи: 39
10-01-2019 дата публикации

DEZOCINE ANALOGUE

Номер: US20190010114A1
Автор: CHEN Shuhui, FANG Yongbo, Gu Wei, Li Jian, Li Zhixiang, WANG FEI, Wu Wentao, Yang Guangwen, Zhang Tao, Zhang Yang
Принадлежит:

Disclosed in the present disclosure is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof. 2. The compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to claim 1 , wherein Ris selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , OH claim 1 , NH claim 1 , or the group consisting of Calkyl or heteroalkyl claim 1 , 3-5 membered cycloalkyl or heterocycloalkyl claim 1 , and 5-6 membered aryl or heteroaryl claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , or 3 R; and claim 1 , when X is CH claim 1 , Ris not H.5. The compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to claim 1 , wherein each of Rand Ris independently selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , OH claim 1 , NH claim 1 , or the group consisting of Calkyl or heteroalkyl claim 1 , 3-5 membered cycloalkyl or heterocycloalkyl and 5-6 membered aryl or heteroaryl claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , or 3 R.14. A method for treating pain in a subject in need thereof claim 1 , comprising: administering an effective amount of the compound claim 1 , the pharmaceutically acceptable salt or tautomer thereof according to to the subject. This application is a National Stage of International Application No. PCT/CN2017/070126, filed on Jan. 4, 2017, and published in Chinese as WO2017/118375 A1 on Jul. 13, 2017. This application claims the priority to Chinese Patent Application No. 201610003868.6, filed on Jan. 4, 2016. The entire disclosures of the above applications are incorporated herein by reference.Disclosed in the present disclosure is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof. ...

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Номер записи: 40
19-01-2017 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20170015646A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 2. A compound according to wherein is single bond.4. A compound according to wherein Ris methyl claim 3 , phenyl claim 3 , or p-phenylphenyl. This application is a Divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013, the content of which is incorporated herein by reference.The present invention relates to novel processes and intermediates for the preparations of isomer free Prostaglandins and the derivatives thereof.Prostaglandin ester analogues of the following Formula I-2whereinisis a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl; and Ris C-alkyl, such as, Latanoprost, Isoproyl unoprostone, Isoproyl cloprostenol, Travoprost and Tafluprost have been used in the management of open-angle glaucoma. The Prostaglandin ester analogues of Formula I-2 have been shown to have significantly greater hypotensive potency than the parent compound, presumably as a result of their more effective penetration through the cornea. They reduce intra-ocular pressure by enhancing uveoscleral outflow, and may also have some effect on trabecular meshwork as well.As shown in the following Scheme A:most of the Prostaglandin ester analogues of Formula I-2 disclosed in the prior art, such as in WO02096898, EP1886992, EP2143712, JP2012246301, U.S. Pat. No. 6,720,438, US2008033176, WO2010097672, and U.S. Pat. No. 7,582,779 were obtained by first synthesizing a Lactone VIII, whereinisor is a protective group of carbonyl group; Pand Pare protective groups for the hydroxyl groups; is a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl and then conducting a semi- ...

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Номер записи: 41
21-01-2016 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20160016883A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 1. A compound selected from the group consisting of travoprost free acid substantially free of 5 ,6-trans isomer , latanoprost free acid substantially free of 5 ,6-trans isomer , bimatoprost free acid substantially free of 5 ,6-trans isomer , tafluprost free acid substantially free of 5 ,6-trans isomer , fluprostenol substantially free of 5 ,6-trans isomer , cloprostenol substantially free of 5 ,6-trans isomer , and unoprostone substantially free of 5 ,6-trans isomer.2. A compound according to containing less than 0.1% of 5 claim 1 ,6-trans isomer.4. Latanoprost according to containing less than 0.2% of 5 claim 3 ,6-trans isomer.5. Latanoprost according to containing less than 0.1% of 5 claim 3 ,6-trans isomer7. Travoprost according to containing less than 0.2% of 5 claim 6 ,6-trans isomer.8. Travoprost according to containing less than 0.1% of 5 claim 6 ,6-trans isomer10. Tafluprost according to having a purity of greater than 99.8%.11. Tafluprost according to having a purity of greater than 99.9%.12. Unoprostone Isopropyl ester having a purity of greater than 99.5%.13. Unoprostone Isopropyl ester having a purity of greater than 99.7%.14. Unoprostone Isopropyl ester having a purity of greater than 99.9%. This application is a Divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013, the content of which is incorporated herein by reference.The present invention relates to novel processes and intermediates for the preparations of isomer free Prostaglandins and the derivatives thereof.Prostaglandin ester analogues of the following Formula I-2whereinis a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl; and Ris C-alkyl, such as, Latanoprost, Isopropyl unoprostone, Isopropyl cloprostenol, ...

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Номер записи: 42
15-01-2015 дата публикации

Catalyst complex with carbene ligand

Номер: US20150018557A1
Автор: Jinkun Huang, Steven P. Nolan
Принадлежит: Materia Inc

Catalytic complexes including a metal atom having anionic ligands, at least one nucleophilic carbene ligand, and an alkylidene, vinylidene, or allenylidene ligand. The complexes are highly stable to air, moisture and thermal degradation. The complexes are designed to efficiently carry out a variety of olefin metathesis reactions.

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Номер записи: 43
15-01-2015 дата публикации

TUBULIN BINDING AGENTS

Номер: US20150018566A1
Автор: Breen Elaine Carmel, Coogan Adrian, Hudson Gillian Joy, McCormack Emmet Martin, Moran Brian William, Shah Richard, Stack Gary Daniel, Walsh John Jarlath, White Martina
Принадлежит:

The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene. The second substituent on the B ring may for example be a substituent which has been found to provide enhanced tubulin binding activity (for example a carbonyl group), or may be a substituent that facilitates functionalisation of the B ring (for example an hydroxyl or amine group), or it may be a binding agent for a target that is preferentially expressed on vasculature undergoing angiogenesis, and not expressed on quiescent vasculature. 143-. (canceled)45. A compound of in which at least one of X claim 44 , Y and Z is C═O.46. A compound of in which Rand Rare each independently selected from H and a halogen.47. A compound of in which Rand Rare each claim 44 , independently claim 44 , selected from H claim 44 , OH claim 44 , amino and L(W).48. A compound according to in which Rand Rare each claim 44 , independently claim 44 , selected from H claim 44 , NH claim 44 , lower alkoxy claim 44 , alkylthio and OH.49. A compound according to in which Ris a lower alkoxy group in the para position.50. A compound according to in which Rand Rare each independently selected from H and a halogen claim 44 , Rand Rare each claim 44 , independently claim 44 , selected from OH claim 44 , amino and L(W) claim 44 , and Rand Rare each claim 44 , independently claim 44 , ...

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Номер записи: 44
16-01-2020 дата публикации

16-METHYL-OXACYCLOHEXADECAN-2-ONE AND 16-METHYL-AZACYCLOHEXADECAN-2-ONE DERIVATIVES AS ANTIMICROBIAL AGENTS

Номер: US20200017460A1
Автор: PRIESTLEY Nigel, STIERLE Andrea, STIERLE Donald
Принадлежит: The University of Montana

16-membered macrolide compounds inhibit growth of various microbial species and have utility in the treatment of systemic or topical microbial infections, including methicillin-resistant strains (Formula I). 7. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl or —Calkylene-OH; and Rand Rare each hydrogen.8. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl; Ris hydrogen; and Ris OH , —OCalkyl , or —OC(O)Calkyl.9. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl; Ris OH , —OCalkyl , —OC(O)Calkyl , or —OC(O)C(CF)(OCH)Ph; and Ris hydrogen.10. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris methyl.11. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen; and Ris OH.12. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris OH , —OC(O)CH , or —OC(O)C(CF)(OCH)Ph; and Ris hydrogen.13. The compound of any of or - , or a pharmaceutically acceptable salt thereof , wherein Ris —S—CH—CH(R)—X.14. The compound of any of - or - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen , CH , —C(O)CH , —C(O)CHCH—X , or —C(O)C(CF)(OCH)Ph.15. The compound of any of - , , or - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen , —C(O)Calkyl , —C(O)Calkylene-X , or —C(O)C(CF)(OCH)Ph; and Ris hydrogen , —C(O)Calkyl , or —C(O)C(CF)(OCH)Ph.16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris hydrogen claim 15 , —C(O)CH claim 15 , —C(O)CHCH—X claim 15 , or —C(O)C(CF)(OCH)Ph; and Ris hydrogen claim 15 , —C(O)CH claim 15 , or —C(O)C(CF)(OCH)Ph.17. The compound of any of - claim 15 , claim 15 , or - claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris hydrogen claim 15 , —C(O)Calkyl claim 15 , or —C(O)C(CF)(OCH)Ph; and Ris hydrogen claim 15 , — ...

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Номер записи: 45
03-02-2022 дата публикации

SECONDARY BATTERY AND DEVICE COMPRISING THE SAME

Номер: US20220037697A1
Автор: Fu Chenghua, HAN Changlong, WU Zeli
Принадлежит: Contemporary Amperex Technology Co., Limited

This application provides a secondary battery and a device comprising the same. The secondary battery includes a negative electrode plate and an electrolyte. The negative electrode plate includes a negative electrode active material. The electrolyte includes an electrolyte salt, an organic solvent, and an additive. The negative electrode active material includes a silicon-based material. The organic solvent includes ethylene carbonate (EC) and diethyl carbonate (DEC). A mass ratio of EC in the organic solvent is less than or equal to 20%, and a mass ratio of DEC in the organic solvent is less than or equal to 20%. The additive includes an additive A and an additive B. The additive A is selected from one or more of compounds represented by Formula 1 or Formula 2, and the additive B is selected from one or more of compounds represented by Formula 3, as described in the application. 2. The secondary battery according to claim 1 , wherein the mass ratio of EC in the organic solvent is 10%˜20%.3. The secondary battery according to claim 1 , wherein the mass ratio of DEC in the organic solvent is 10%˜20%.4. The secondary battery according to claim 1 , wherein a mass ratio of the additive A in the electrolyte is less than or equal to 1% claim 1 , and optionally the mass ratio of the additive Ain the electrolyte is 0.1%˜0.5%.5. The secondary battery according to claim 1 , wherein a mass ratio of the additive B in the electrolyte is less than or equal to 2% claim 1 , and optionally the mass ratio of the additive B in the electrolyte is 0.1%˜1%.6. The secondary battery according to claim 1 , wherein the organic solvent further comprises ethyl methyl carbonate (EMC) claim 1 , and a mass ratio of EMC in the organic solvent is greater than 50% claim 1 , optionally 55%˜65%.8. The secondary battery according to claim 1 , wherein the additive B is selected from one or more of the tris(trimethylsilane) phosphate claim 1 , tris(triethylsilane) phosphate claim 1 , or tris( ...

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Номер записи: 46
26-01-2017 дата публикации

Catalysts for (e)-selective olefin metathesis

Номер: US20170022231A1
Автор: Choon Woo Lee, Pablo E. GUZMAN, Robert H. Grubbs, T. Patrick MONTGOMERY, Tonia S. AHMED
Принадлежит: California Institute of Technology CalTech

This invention relates generally to olefin metathesis catalyst compounds, to the preparation of such compounds, and the use of such catalysts in the metathesis of olefins and olefin compounds, more particularly, in the use of such catalysts in (E)-selective olefin metathesis reactions. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.

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Номер записи: 47
22-01-2015 дата публикации

PROCESS FOR PRODUCING DODECANE-1,12-DIOL BY REDUCTION OF LAURYL LACTONE PRODUCED FROM THE OXIDATION OF CYCLODODECANONE

Номер: US20150025279A1
Автор: Hastings James D., HERKES Frank E., Rajendran Gurusamy, SUN Qun
Принадлежит: INVISTA North America S.a.r.l.

A process for synthesizing dodecane-1,12-diol, and by-products thereof, by the reduction of lauryl lactone produced from the oxidation of cyclododecanone. 2. The method of claim 1 , wherein the oxidizing comprises at least one of hydrogen peroxide claim 1 , a peracetic acid claim 1 , a trifluoro peracetic acid claim 1 , and a peracid.3. The method of claim 1 , wherein the oxidizing comprises at least one of hydrogen peroxide claim 1 , meta-chloroperoxybenzoic acid (mCPBA) claim 1 , trifluoro peracetic acid (CFCOH) claim 1 , permaleic acid (HOCHC═CCOH) claim 1 , performic acid (CHO) claim 1 , peracetic acid (CHCOH) claim 1 , magnesium monoperoxyphthalate (MMPP) claim 1 , perbenzoic acid (PBA) and monoperphthalic acid (MPPA).4. The method of claim 1 , wherein the oxidizing comprises hydrogen peroxide claim 1 , maleic anhydride claim 1 , and methyl acetate.5. The method of claim 1 , wherein the oxidizing comprises hydrogen peroxide claim 1 , maleic anhydride claim 1 , and methyl acetate claim 1 , which is carried out by the simultaneous addition of the hydrogen peroxide and the maleic anhydride in the methyl acetate claim 1 , to a solution of the cyclododecanone in the methyl acetate.6. The method of claim 1 , wherein the oxidizing comprises hydrogen peroxide claim 1 , maleic anhydride claim 1 , and methyl acetate claim 1 , which is carried out by the addition of the cyclododecanone to a preformed solution of hydrogen peroxide and maleic anhydride.7. The method of claim 1 , wherein the oxidizing comprises hydrogen peroxide claim 1 , maleic anhydride claim 1 , and methyl acetate claim 1 , which is carried out by the addition of hydrogen peroxide to a solution of cyclododecanone and maleic anhydride in a solvent.8. The method of claim 1 , wherein the oxidizing comprises hydrogen peroxide claim 1 , present in about 1.5 molar equivalents to about 2.5 molar equivalents claim 1 , relative to the cyclododecanone.9. The method of claim 1 , wherein the oxidizing comprises ...

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Номер записи: 48
28-01-2021 дата публикации

HETEROCYLCOALKENYL DERIVATIVES USEFUL AS AGONISTS OF THE GPR120 AND / OR GPR40

Номер: US20210024483A1
Автор: Lanter James C., Sui Zhihua, Wall Mark
Принадлежит:

The present invention is directed to heterocycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and/or GPR40 receptors. More particularly, the compounds of the present invention are agonists of GPR120 and/or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc. 2. A compound as in claim 1 , whereina is an integer from 1 to 2;b is an integer from 1 to 2;{'sub': '2', 'Z is selected from the group consisting of —O—, —S—, —SO— and —SO—; provided that when a is 1 and b is 2, or when a is 2 and b is 1 or when a is 2 and b is 2, then Z is —O—;'}c is an integer from 0 to 2;{'sup': '0', 'sub': 1-4', '1-2', '1-2', '1-2, 'each Ris independently selected from the group consisting of halogen, oxo, hydroxy, Calkyl, fluorinated Calkyl, Calkoxy and fluorinated Calkoxy;'}{'sup': '1', 'sub': 1-6', '3-6', '1-2', '3-6', '5-6', '1-2, 'Ris selected from the group consisting of Calkyl, Ccycloalkyl, —(Calkyl)-Ccycloalkyl, Ccycloalkenyl, 2,2-difluoro-benzo[d][1,3]dioxol-4-yl, phenyl, —(Calkyl)-phenyl, —C(═CH)-phenyl, —C(O)-phenyl, pyrimidinyl, pyridyl, thienyl, and 1-methyl-imidazol-4-yl;'}{'sub': 3-6', '5-6', '1-2', '1-2, 'wherein the Ccycloalkyl or Ccycloalkenyl, whether alone or as part of a substituent group is optionally substituted with one to two substituents independently selected from the group consisting of halogen, Calkyl and fluorinated Calkyl;'}{'sub': 1-4', '1-2', '1-4', '1-2, 'and wherein the phenyl, pyrimidinyl or pyridyl, whether alone or as part of a substituent group is optionally substituted with one to three substituents independently selected from the group consisting of halogen, hydroxy, Calkyl, fluorinated Calkyl, Calkoxy, fluorinated Calkoxy, and phenyl;'}{'sup': '2', 'sub': 1-4', '1-2, 'Ris selected from the group consisting of hydrogen, halogen, Calkyl and fluorinated Calkyl;'}{'sup': '3', 'sub': 1-2', '1-2, 'Ris ...

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Номер записи: 49
01-02-2018 дата публикации

COMPOUNDS AND COMPOSITIONS AND USES THEREOF

Номер: US20180028492A1
Автор: Alexandrov Vadim, Bowen Carrie A., HANANIA Taleen G., Powell Noel Aaron
Принадлежит:

Compounds of formula I: 2. The method according to claim 1 , wherein the neurological or psychiatric disease or disorder is depression claim 1 , bipolar disorder claim 1 , pain claim 1 , schizophrenia claim 1 , obsessive compulsive disorder claim 1 , addiction claim 1 , social disorder claim 1 , attention deficit hyperactivity disorder claim 1 , an anxiety disorder claim 1 , a movement disorder claim 1 , epilepsy claim 1 , autism or cognitive impairments.3. The method according to claim 2 , wherein the neurological or psychiatric disease or disease or disorder is depression.4. The method according to claim 3 , wherein the depression is treatment-resistant depression (TRD) claim 3 , major depressive disorder (MDD) claim 3 , unipolar depression claim 3 , bipolar depression or depression associated with another disease or disorder.5. The method according to claim 2 , wherein the neurological or psychiatric disease or disorder is a movement disorder or epilepsy.6. The method according to claim 1 , wherein said neurological disease or disorder is selected from Alzheimer's disease and Parkinson's disease.7. The method according to claim 1 , wherein any two of R claim 1 , R claim 1 , Rand Rattached to adjacent carbon atoms claim 1 , together with the carbon atoms to which they are attached claim 1 , form a 5 to 8-membered carbocycle or heterocycle which is optionally substituted with one or more substituents independently selected from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , (C-C)alkylamino claim 1 , di(C-C)alkylamino claim 1 , (C-C)alkyl claim 1 , (C-C)haloalkyl claim 1 , (C-C)alkoxy claim 1 , and (C-C)haloalkoxy.8. The method according to claim 7 , wherein any two of R claim 7 , R claim 7 , Rand Rform a phenyl ring.9. The method according to claim 1 , wherein:{'sup': 8', '9', '11, '(a) at least one of R, R, and Ris chosen from halogen, methyl and ethyl; or'}{'sup': '10', '(b) Ris methoxy; or'}{'sup': 8', '9', '10', '11', '7a', '7b', '4a', '4b, '(c) R, R, R, ...

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Номер записи: 50
04-02-2016 дата публикации

IN-SITU GENERATION OF RUTHENIUM CATALYSTS FOR OLEFIN METATHESIS

Номер: US20160031845A1
Автор: Beller Matthias, Dumrath Andreas, Dumrath Christa, Kadyrov Renat, NEUMANN Helfried
Принадлежит:

The present invention relates to a process for preparing olefins by means of metathesis, which comprises the following steps 2. The process according to claim 1 , wherein the anionic ligands X are identical and are each chlorine and Lis selected from the group consisting of nitrogen bases claim 1 , phosphanes claim 1 , phosphinites claim 1 , phosphonites claim 1 , phosphites and arsanes.3. The process according to claim 2 , wherein Lis selected from the group consisting of benzene claim 2 , toluene claim 2 , xylene claim 2 , cymene claim 2 , trimethylbenzene claim 2 , tetramethylbenzene claim 2 , hexamethylbenzene claim 2 , tetrahydronaphthalene and naphthalene claim 2 , and Lis selected from the group consisting of N-heterocyclic carbenes and phosphanes.4. The process according to claim 3 , wherein Lis selected from the group consisting of P(phenyl) claim 3 , P(cyclohexyl)and N-heterocyclic carbenes of the formula VI claim 3 , VII claim 3 , VIII claim 3 , IX claim 3 , X and XI.6. The process according to claim 5 , wherein the ruthenium compound is a compound of the general formula RuXLL(II) claim 5 , wherein the anionic ligands X are identical and are each chlorine and Lis selected from the group consisting of N-heterocyclic carbenes and phosphanes.7. The process according to claim 6 , wherein Lis selected from the group consisting of benzene claim 6 , toluene claim 6 , xylene claim 6 , cymene claim 6 , trimethylbenzene claim 6 , tetramethylbenzene claim 6 , hexamethylbenzene claim 6 , tetrahydronaphthalene and naphthalene claim 6 , and Lis selected from the group consisting of P(cyclohexyl)and the N-heterocyclic carbenes of the formulae VI claim 6 , VII claim 6 , VIII claim 6 , IX claim 6 , X and XI.8. The process according to claim 7 , wherein the ruthenium compound is selected from the group consisting of compounds of the formulae A claim 7 , B and C.9. The process according to claim 5 , wherein the ruthenium compound is a compound of the general formula RuXL( ...

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Номер записи: 51
01-02-2018 дата публикации

COMPOUNDS AND COMPOSITIONS AND USES THEREOF

Номер: US20180030064A1
Автор: HANANIA Taleen G., Heffernan Michele L.R., Jones Philip Glyn, Xie Linghong
Принадлежит:

Disclosed are compounds of formula (I): 3. The compound according to claim 1 , wherein Ris hydrogen and Ris hydrogen or methyl.4. The compound according to claim 1 , wherein Ris hydrogen and Ris hydrogen or methyl.5. The compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare hydrogen.6. The compound according to claim 2 , wherein Rand Rare both hydrogen.7. The compound according to claim 1 , wherein Rand Rare chosen independently from H claim 1 , fluoro claim 1 , and methyl.8. The compound according to claim 6 , wherein Rand Rare chosen independently from H claim 6 , fluoro claim 6 , and methyl.9. The compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare H.10. The compound according to claim 1 , wherein one of R claim 1 , R claim 1 , Rand Ris fluoro claim 1 , chloro claim 1 , methyl or cyano and the remaining three are H.11. The compound according to claim 1 , wherein two of R claim 1 , R claim 1 , R claim 1 , and Rare fluoro claim 1 , chloro claim 1 , methyl or cyano and the remaining two are H.12. The compound according to claim 1 , wherein two of R claim 1 , R claim 1 , Rand Rform a fused 1 claim 1 ,3-dioxole and the remaining two are H.13. The compound according to claim 1 , wherein two of R claim 1 , R claim 1 , R claim 1 , and Rform a fused dihydro-1 claim 1 ,4-dioxine and the remaining two are H.14. The compound according to claim 10 , wherein Rand Rare H claim 10 , one of Rand Ris chosen from fluoro claim 10 , chloro claim 10 , methyl and cyano claim 10 , and the other of Rand Ris H.15. The compound according to claim 11 , wherein Rand Rare H claim 11 , and Rand Rare chosen from fluoro claim 11 , chloro claim 11 , methyl and cyano.16. The compound according to claim 2 , wherein Ris hydrogen; Ris hydrogen or methyl; Ris hydrogen; Ris hydrogen or methyl; R claim 2 , R claim 2 , Rand Rare hydrogen.17. The compound according to claim 16 , wherein two of R claim 16 , R claim 16 , R claim 16 , and Rform ...

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Номер записи: 52
17-02-2022 дата публикации

ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

Номер: US20220052272A1
Автор: LEE Ga-Won, LEE Tae-Jin, OH Hong-Se
Принадлежит:

The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device having improved driving voltage and/or luminous efficiency characteristics can be provided. 4. The organic electroluminescent compound according to claim 1 , wherein in Rto R claim 1 , the substituents of the substituted alkyl claim 1 , the substituted aryl claim 1 , the substituted heteroaryl claim 1 , the substituted cycloalkyl claim 1 , the substituted alkoxy claim 1 , the substituted trialkylsilyl claim 1 , the substituted dialkylarylsilyl claim 1 , the substituted alkyldiarylsilyl claim 1 , the substituted triarylsilyl claim 1 , the substituted mono- or di-alkylamino claim 1 , the substituted mono- or di-arylamino claim 1 , and the substituted alkylarylamino each independently are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C3-C30)cycloalkyl; a (C3-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (3- to 30-membered)heteroaryl unsubstituted or substituted with a (C6-C30)aryl(s); a (C6-C30)aryl unsubstituted or substituted with one or more of a (C1-C30)alkyl(s) and a (3- to 30-membered)heteroaryl(s); a tri(C1-C30)alkylsilyl; a tri(C6-C30)arylsilyl; a di(C1-C30)alkyl(C6-C30)arylsilyl; a (C1-C30)alkyldi(C6-C30)arylsilyl; an amino; a mono- or di-(C1-C30)alkylamino; a mono- or di-(C6-C30)arylamino unsubstituted or substituted with a (C1-C30)alkyl(s); a (C1-C30)alkyl(C6-C30)arylamino; a (C1-C30)alkylcarbonyl; a (C1-C30)alkoxycarbonyl; a (C6-C30)arylcarbonyl; a di(C6-C30)arylboronyl; a di(C1-C30)alkylboronyl; a (C1-C30)alkyl(C6-C30)arylboronyl; a (C6-C30)aryl(C1- ...

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Номер записи: 53
24-02-2022 дата публикации

REACTIONS OF OLEFIN DERIVATIVES IN THE PRESENCE OF METHATHESIS CATALYSTS

Номер: US20220055025A1
Автор: Johns Adam M., PEDERSON Richard
Принадлежит:

The invention provides a method for synthesizing musk macrocycles comprising contacting an easily accessible diene starting materials bearing a Z-olefin moiety and performing a ring closing metathesis reaction in the presence of a Group 8 olefin metathesis catalyst. 112.-. (canceled)14. The olefin metathesis catalyst according to claim 13 , wherein:M is Ru;n is 0;m is 0;{'sup': 'a', 'sub': 1', '10', '1', '10', '3', '10', '3', '10', '5', '24', '5', '24, 'Ris unsubstituted C-Calkyl, substituted C-Calkyl, unsubstituted C-Ccycloalkyl, substituted C-Ccycloalkyl, unsubstituted C-Caryl or substituted C-Caryl;'}{'sup': b', 'a', 'b, 'sub': 1', '10', '1', '10', '3', '10', '3', '10', '5', '24', '5', '24, 'Ris unsubstituted C-Calkyl, substituted C-Calkyl, unsubstituted C-Ccycloalkyl, substituted C-Ccycloalkyl, unsubstituted C-Caryl or substituted C-Caryl; or Rand Rare linked together to form a five or a six-heterocyclic membered ring with the sulfoxide group;'}{'sup': 1', '2, 'Xand Xare independently halogen;'}{'sup': '1', 'Ris hydrogen;'}{'sup': 2', '1', '2, 'sub': 1', '6, 'Ris unsubstituted phenyl, substituted phenyl, C-Calkyl or substituted 1-propenyl; or Rand Rare linked together to form an optionally substituted indenylidene;'}{'sup': 5', '5, 'Xand Yare independently N;'}{'sup': 11', '12', '13', '14, 'sub': s', 't, 'Q is a two-atom linkage having the structure —[CRR]—[CRR]—;'}{'sup': 11', '12', '13', '14, 'R, R, R, and Rare independently hydrogen;'}“s” and “t” are independently 1;{'sup': '3', 'sub': 3', '10', '3', '10', '5', '24', '5', '24', '1', '20', '1', '2M', '1', '20', '1', '20', '5', '24', '5', '24', '5', '24', '5', '24', '6', '24', '6', '24', '6', '24', '6', '24, 'Ris unsubstituted C-Ccycloalkyl, substituted C-Ccycloalkyl, unsubstituted C-Caryl, or C-Caryl substituted with up to three substituents selected from: unsubstituted C-Calkyl, substituted C-Calkyl, unsubstituted C-Cheteroalkyl, substituted C-Cheteroalkyl, unsubstituted C-Caryl, substituted C-Caryl, ...

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Номер записи: 54
07-02-2019 дата публикации

BICYCLIC COMPOUND, PRODUCTION AND USE THEREOF

Номер: US20190038604A1
Автор: AIKAWA Katsuji, BABA Masanori, IIZAWA Yuji, KANZAKI Naoyuki, SETO Masaki, SHIRAISHI Mitsuru
Принадлежит: Tobira Therapeutics, Inc.

The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: 156.-. (canceled)58. The method of claim 57 , wherein the compound according to Formula (I) is administered as a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.59. The method of claim 57 , wherein the compound of Formula (I) is selected from the group consisting of(a) 8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-N-[4-[[N-methyl-N-(tetrahydropyran-4-yl)amino]methyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide;(b) (S)-8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-N-[4-[[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide methanesulfonate;(c) (S)-8-[4-(2-butoxyethoxy)phenyl]-1-propyl-N-[4-[[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamaide methanesulfonate;(d) (S)-1-isobutyl-8-[4-(2-propoxyethoxy)phenyl]-N-[4-[[(1-propyl-1H-imidazol-5-yl)methyl]sulfiyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide;(e) (S)-8-[4-(2-butoxyethoxy)phenyl]-1-[(1-methyl-1H-pyrazol-4-yl)methyl]-N-[4-[[(1-propyl-1H-imidazol-5-yl]methyl]sulfinyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide; and(f) (S)-8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-N-[4-[[(4-propyl-4H-1,2,4-triazol-3-yl)methyl]sulfinyl]phenyl]-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide.61. The method of claim 60 , wherein Zis SO.62. The method of claim 60 , wherein Zis SO whose configuration is (S).63. A method for inhibiting a biological function of CCR5 claim 60 , comprising contacting CCR5 with an effective amount of a compound according to Formula (I) or pharmaceutic ally acceptable salt thereof or a salt or hydrate thereof claim 60 , wherein the compound is selected from the group consisting of:(a) 8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-N-[4-[[N-methyl-N-( ...

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Номер записи: 55
07-02-2019 дата публикации

Novel molecule with anti-cancer activity

Номер: US20190040032A1
Автор: Ahmed ZEIN, Judith BOBBITT
Принадлежит: Oceans Ltd

The present invention provides a new compound of formula (I): extracted from a seaweed, and its use for inhibiting the growth of cancer cells, as well as methods for its extraction and isolation.

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Номер записи: 56
07-02-2019 дата публикации

Novel antibiotic

Номер: US20190040033A1
Автор: den Hertog Jeroen, Hoeksma Jelmer, van der Velden Gisela Johanna
Принадлежит: Koninklijke Nederlandse Akademie van Wetenschappen

The present invention relates to novel compounds, comprising an 8- or 9-membered cyclic structure, wherein an (E)-1,4-dioxo-but-2-ene moiety is embedded in said cyclic structure and to pharmaceutical compositions comprising these compounds. The compounds may be used as medicaments, in particular as medicaments for treating and preventing microbial infections, such as infections by multidrug resistant and/or Gram-positive bacteria. The invention further relates to fermentation processes wherein fungi of the genus are used for producing the novel compounds. 1. A compound comprising an (E)-7-hydroxy-4-oxo-hept-2-enoic acid lactone ring.2. The compound according to claim 1 , wherein the cyclic structure is unsubstituted or substituted with one or more substituents selected from halogen claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , aryl claim 1 , amino claim 1 , hydroxyl claim 1 , alkoxy claim 1 , acyl claim 1 , acyloxy claim 1 , carbamoyl claim 1 , cyano and nitro.3. The compound according to claim 1 , which is (E)-7-hydroxy-4-oxo-oct-2-enoic acid lactone.4. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.5. A method of treating a microbial infection comprising administering to a subject in need thereof a compound comprising an (E)-7-hydroxy-4-oxo-hept-2-enoic acid lactone ring.6. The method according to claim 5 , wherein the microbial infection is a bacterial infection.7. The method according to claim 6 , wherein the bacterial infection is an infection by a multidrug resistant bacterium.8. The method according to claim 6 , wherein the bacterial infection is an infection by a Gram-positive bacterium.9Staphylococcus.. The method according to claim 8 , wherein the Gram-positive bacterium is a methicillin-resistant10Staphylococcus aureus.. The method according to claim 9 , wherein the Gram-positive bacterium is a methicillin-resistant11. A method for producing a compound comprising an (E)-7-hydroxy-4 ...

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Номер записи: 57
18-02-2021 дата публикации

REACTIONS OF OLEFIN DERIVATIVES IN THE PRESENCE OF METHATHESIS CATALYSTS

Номер: US20210046466A1
Автор: Johns Adam M., Pederson Richard L.
Принадлежит:

The invention provides a method for synthesizing musk macrocycles comprising contacting an easily accessible diene starting materials bearing a Z-olefin moiety and performing a ring closing metathesis reaction in the presence of a Group 8 olefin metathesis catalyst. 112.-. (canceled)13. (canceled)14. (canceled)17. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 62/629,857, filed Feb. 13, 2018.Since its discovery in the 1950s, olefin metathesis has emerged as a valuable synthetic method for the formation of carbon-carbon double bonds. Recent advances in applications to organic syntheses and polymer syntheses mostly rely on developments of well-defined olefin metathesis catalysts.The technology of ruthenium metathesis catalysts has enabled the development of several research platforms including: ring opening metathesis polymerization (ROMP), ring opening cross metathesis (ROCM), cross metathesis (CM), ring closing metathesis (RCM).In another embodiment, the invention provides methods for the synthesis of macrocyclic compounds utilized in the fragrance industry.The odor of musk is perhaps the most universally appreciated fragrance. The natural macrocyclic musk compounds turned out to be ketones (animal sources) and lactones (plant materials). They are 15- or 17-membered ring systems. The type of odor is influenced by the ring size. Starting from 14 ring atoms, a weak musk scent is perceived. Compounds with 15-16 ring atoms exhibit strong musk odor.Macrocyclic musk compounds are expected to be of increasing importance in the future, especially because many of them are naturally occurring and even the synthetic representatives closely resemble the natural counterparts. In addition, the progress in synthetic chemistry contributes to declining prices and will stimulate increased use of this type of musk compounds.Synthetic musk compounds can be divided into three major classes: aromatic nitro musk compounds, polycyclic musk ...

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Номер записи: 58
19-02-2015 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20150051410A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 2. A process according to claim 1 , wherein said transesterification comprises hydrolysis of the macrolactone to form a compound containing a hydroxyl group and a carboxylic acidand then esterification of the carboxylic acid.3. A process according to claim 1 , wherein said transesterification comprises reacting the macrolactone with a nucleophile selected from the group consisting of a Calkanol claim 1 , a Calkoxide claim 1 , a Calkoxide salt claim 1 , or a mixture thereof to form a compound containing a hydroxyl group and an ester group.4. A process according to claim 3 , wherein the nucleophile is 2-propanol claim 3 , sodium 2-propoxide claim 3 , or a mixture thereof.6. A process according to claim 5 , wherein the silylating agent is selected from chlorotrimethylsilane claim 5 , chlorotriethylsilane claim 5 , chlorodimethyl(octyl)silane claim 5 , and tert-butylchlorodimethylsilane.7. A process according to claim 1 , wherein the compound of Formula I-2 is selected from the group consisting of Latanoprost claim 1 , Travoprost claim 1 , Tafluprost claim 1 , Isopropyl Cloprostenol claim 1 , and Isopropyl Unoprostone.9. A process according to claim 8 , wherein said transesterification comprises hydrolysis of the compound of Formula IIa to form Travoprost acid and then esterification of the Travoprost acid to form Travoprost.11. A process according to claim 10 , wherein said transesterification comprises hydrolysis of the compound of Formula IIb to form Latanoprost acid and then esterification of the Latanoprost acid to form Latanoprost.13. A process according to claim 12 , wherein said transesterification comprises hydrolysis of the compound of Formula IIc to form Tafluprost acid and then esterification of the Tafluprost acid to form Tafluprost.15. A process according to claim 14 , wherein said transesterification comprises opening the macrolactone ring and ...

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Номер записи: 59
03-03-2022 дата публикации

MACROLIDE BREFELDIN A ESTER DERIVATIVES AND USE THEREOF

Номер: US20220064138A1
Автор: JIANG Yaoyao, Liu Ming, SHAO Changlun, Wang Changyun, WANG Cuifang, WEI Meiyan
Принадлежит:

The present disclosure relates to the field of medicinal chemistry, and specifically to the use in the inhibition of tumor proliferation activity of ester derivatives of brefeldin A represented by Formula (I). The new compounds provided herein are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Bart's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer and colorectal cancer, and have the potential to be developed as novel antitumor agents.

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Номер записи: 60
14-02-2019 дата публикации

PREPARATION OF MACROCYCLIC LACTONES

Номер: US20190047974A1
Автор: DAVEY Paul Nicholas, ELLWOOD Simon
Принадлежит: Givaudan SA

A process for preparing a macrocyclic lactone comprising 14 to 17 ring carbon atoms, the process comprising the steps of i) subjecting a reaction mixture comprising an olefin-containing random polyester, formed by metathesis to a cyclo-depolymerization reaction to form the macrocyclic lactone, and ii) concomitant removal of the macrocyclic lactone from the reaction mixture. 1. A process for preparing and isolating a macrocyclic lactone by the cyclo-depolymerization of an olefin-containing random polyester contained in a reaction mixture , the process comprising the steps of:i) depolymerizing the olefin-containing random polyester in a reaction mixture to form fragments capable of intramolecular cyclisation;ii) intramolecular cyclization of said fragments to form a desired macrocyclic lactone; andiii) concomitant separation of the macrocyclic lactone from the reaction mixture.4. The process according to claim 1 , wherein the polyester contains at least 5 to 50 units.5. The process according to claim 1 , wherein the cyclo-depolymerization reaction is effected by trans-esterification or metathesis.7. The process according to claim 1 , wherein the concomitant separation of the macrocyclic lactone from the reaction mixture is effected by distillation.8. The process according to claim 1 , wherein the macrocyclic lactone is selected from the group consisting of E/Z-17-oxacyclohentadec-7-en-1-one; E/Z-17-oxacycloheptadec-9-en-1-one; E/Z-13-methyloxacyclopentadec-10-en-2-one; and E/Z-1-oxacyclohexadec-12-en-2-one.9. The process according to claim 8 , wherein the macrocyclic lactone is hydrogenated to form the hydrogenated macrocyclic lactone corresponding to E/Z-17-oxacycloheptadec-7-en-l-one; E/Z-17-oxacycloheptadec-9-en-1-one; E/Z-13-methyloxacyclopentadec-10-en-2-one; or E/Z-1-oxacyclohexadec-12-en-2-one.10. The process according to claim 1 , wherein the polyester is prepared by acyclic diene metathesis polymerization of a diene-ester.11. The process according to claim 10 ...

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Номер записи: 61
13-02-2020 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING alpha,omega-DICARBOXYLIC ACID-TERMINATED DIALKANE ETHERS

Номер: US20200048181A1
Автор: Geoffroy Otto Joseph, Oniciu Carmen Daniela
Принадлежит:

The present disclosure provides a process for the preparation of compounds of formula (III), 2. The process of claim 1 , further comprising the step of performing an aqueous work-up of the solution of step (b) to isolate an organic solution of the compound of formula (III).3. The process of claim 1 , further comprising the step of treating the crude compound of formula (III) with an aqueous solution of a hydroxide or oxide of an alkali or earth alkaline metal.5. The process of claim 1 , further comprising the step of removing the organic layer by evaporation to afford crude crystalline α claim 1 ,ω-dicarboxylic acid-terminated dialkane ether salt of formula (IV) in the form of an alcohol solvate or hydrate claim 1 , wherein the alcohol solvate or hydrate is stirred with tetrahydrofuran with subsequent addition of one or more anti-solvents to obtain the crystalline form of the α claim 1 ,ω-dicarboxylic acid-terminated dialkane ether salt of formula (IV).6. The process of claim 1 , further comprising the step of adding one or more anti-solvents so that the salt of the α claim 1 ,ω-dicarboxylic acid-terminated dialkane ether of formula (IV) is insoluble.7. The process of claim 1 , further comprising the step of humidifying the precipitate to obtain a crystalline salt of a α claim 1 ,ω-dicarboxylic acid-terminated dialkane ether of formula (IV).9. The process of claim 1 , comprising treating a solution of a compound of formula (III) in a water-miscible solvent with an aqueous solution of a base claim 1 , wherein the water-miscible solvent is selected from DMSO claim 1 , DMF claim 1 , methanol claim 1 , isopropyl alcohol claim 1 , and ethanol; or treating a solution of a compound of formula (III) in a water-immiscible solvent with an aqueous solution of a base claim 1 , wherein the water-immiscible solvent is selected from toluene claim 1 , xylene claim 1 , methyl ethyl ketone claim 1 , and methyl isobutyl ketone. This application is a continuation of U.S. application ...

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Номер записи: 62
13-02-2020 дата публикации

CYCLIZATION PROCESSES OF HYDROXYALKENOIC AICDS AND PRODUCTS THEREOF

Номер: US20200048233A1
Автор: TSVELIKHOVSKY Dmitry
Принадлежит: Yissum Research Development Company, of The Hebrew University of Jerusalem Ltd.

The invention provides efficient cyclization processes of hydroxyalkenoic acids and products produced therefrom. The following reactions are claimed: Formula (I), (II), (V) and (VI). 3. A process according to claim 1 , wherein Ris selected from C-Caryl or C-Cheteroaryl claim 1 , optionally substituted by at least one OH claim 1 , amine claim 1 , amide claim 1 , halide claim 1 , straight or branched C-Calkyl claim 1 , straight or branched C-Calkenyl claim 1 , straight or branched C-Calkynyl claim 1 , —O(C-Cakyl) claim 1 , —OC(═O)(C-Calkyl) claim 1 , —C(—O)(C-Calkyl) claim 1 , —C(═O)O(C-Calkyl); C-Caryl claim 1 , C-Cheteroaryl.4. A process according to claim 1 , wherein Ris selected from straight or branched C-Calkyl claim 1 , straight or branched C-Calkenyl claim 1 , straight or branched C-Calkynyl claim 1 , optionally substituted by at least one OH claim 1 , amine claim 1 , amide claim 1 , halide; —O(C-Cakyl) claim 1 , —OC(═O)(C-Calkyl) claim 1 , —C(═O)(C-Calkyl) claim 1 , —C(═O)O(C-Calkyl); C-Caryl claim 1 , C-Cheteroaryl claim 1 , C-Ccycloalkyl claim 1 , C-Cheterocycloalkyl5. A process according to claim 1 , wherein R2 is H6. A process according to claim 2 , wherein Rand Rtogether with the two carbon atoms they are each attached to form a 5 to 15 membered ring.7. A process according to claim 2 , wherein Rand Rtogether with the two carbon atoms they are each attached to form a 5 to 1.5 membered ring.8. A process according to claim 2 , wherein R5 and Rtogether with the two carbon atoms they re each attached to form a 5 to 15 membered ring.9. A process according to claim 1 , wherein said at least one Pd catalyst is selected from is selected from Pd(PPh) claim 1 , Pd(dba) claim 1 , Pd(OAc) claim 1 , PdCl claim 1 , Pd(acac)and any combinations thereof.10. A process according to claim 1 , wherein said at least one base is selected from KPO claim 1 , CsCO claim 1 , KCO claim 1 , NaOAc and any combinations thereof.11. A process according to claim 1 , being performed in ...

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Номер записи: 63
08-05-2014 дата публикации

Process for the Oxidation of Organic Carbonyl Compounds

Номер: US20140128622A1
Автор: Müller Ulrich, Parvulescu Andrei-Nicolae, Teles Joaquim Henrique, Vautravers Nicolas
Принадлежит: BASF SE

A process for the oxidation of an organic carbonyl compound comprising reacting the organic carbonyl compound, optionally in the presence of a solvent, with hydrogen peroxide in the presence of a catalyst comprising a tin-containing zeolitic material having an MWW-type framework structure. 2. The process of claim 1 , wherein Rand Rare independently from one another a linear or branched alkyl residue having from 1 to 20 carbon atoms claim 1 , a linear or branched alkenyl residue having from 2 to 20 carbon atoms claim 1 , an aryl or heteroaryl residue having from 4 to 20 carbon atoms claim 1 , or a hydrogen atom and wherein claim 1 , if neither Rnor Ris a hydrogen atom claim 1 , Rand Rmay form claim 1 , together with the carbonyl group or the carboxyl group claim 1 , a ring having from 4 to 20 carbon atoms.3. The process of claim 1 , wherein the compound of formula (I) contains at least one C—C double bond.4. The process of claim 3 , wherein the compound of formula (I) contains a C—C double bond in alpha position to the carbonyl group.5. The process of claim 1 , wherein at least 99 weight-% of the framework structure of the Sn-MWW consist of BOand SiO claim 1 , wherein the molar ratio of BOrelative to SiOis in the range of from 0.0005:1 to 0.0025:1.6. The process of claim 1 , wherein the Sn-MWW has a tin content in the range of from 0.1 to 4.0 weight-% claim 1 , calculated as element and based on the weight of the Sn-MWW.7. The process of claim 1 , wherein the Sn-MWW has a tin content in the range of from 0.1 to 1.0 weight-% or in the range of from 0.1 to 0.5 weight-% claim 1 , calculated as element and based on the weight of the Sn-MWW.8. The process of claim 1 , wherein at the beginning of the reaction according to (i) claim 1 , the molar ratio of Sn claim 1 , calculated as element and contained in the Sn-MWW claim 1 , relative to the compound according to formula (I) is in the range of from 0.001:1 to 0.05:1.9. The process of claim 1 , wherein at the beginning of ...

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Номер записи: 64
22-02-2018 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20180050999A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 2. A compound according to wherein Ris methyl claim 1 , phenyl claim 1 , or p-phenylphenyl. This application is a Divisional of U.S. patent application Ser. No. 14/802,026 filed Jul. 17, 2015, which is a divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013 (now U.S. Pat. No. 9,115,109 issued Aug. 25, 2015), the contents of which are incorporated herein by reference.The present invention relates to novel processes and intermediates for the preparations of isomer free Prostaglandins and the derivatives thereof.Prostaglandin ester analogues of the following Formula I-2whereinis a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl; and Ris C-alkyl, such as, Latanoprost, Isoproyl unoprostone, Isoproyl cloprostenol, Travoprost and Tafluprost have been used in the management of open-angle glaucoma. The Prostaglandin ester analogues of Formula I-2 have been shown to have significantly greater hypotensive potency than the parent compound, presumably as a result of their more effective penetration through the cornea. They reduce intra-ocular pressure by enhancing uveoscleral outflow, and may also have some effect on trabecular meshwork as well.As shown in the following Scheme A:most of the Prostaglandin ester analogues of Formula I-2 disclosed in the prior art, such as in WO02096898, EP1886992, EP2143712, JP2012246301, U.S. Pat. No. 6,720,438, US2008033176, WO2010097672, and U.S. Pat. No. 7,582,779 were obtained by first synthesizing a Lactone VIII, whereinor is a protective group of carbonyl group; Pand Pare protective groups for the hydroxyl groups; is a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or ...

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Номер записи: 65
26-02-2015 дата публикации

Photoacid generator and photoresist comprising same

Номер: US20150056558A1
Автор: Cheng-Bai Xu, Emad Aqad, Mingqi Li, Shintaro Yamada, William Williams, III
Принадлежит: Rohm and Haas Electronic Materials LLC

A photoacid generator compound has the formula (I): [A—(CHR 1 ) p ] k -(L)—(CH 2 ) m —(C(R 2 ) 2 ) n SO 3 − Z +   (I) wherein A is a substituted or unsubstituted, monocyclic, polycyclic, or fused polycyclic C 5 or greater cycloaliphatic group optionally comprising O, S, N, F, or a combination comprising at least one of the foregoing, R 1 is H, a single bond, or a substituted or unsubstituted C 1-30 alkyl group, wherein when R 1 is a single bond, R 1 is covalently bonded to a carbon atom of A, each R 2 is independently H, F, or C 1-4 fluoroalkyl, wherein at least one R 2 is not hydrogen, L is a linking group comprising a sulfonate group, a sulfonamide group, or a C 1-30 sulfonate or sulfonamide-containing group, Z is an organic or inorganic cation, p is an integer of 0 to 10, k is 1 or 2, m is an integer of 0 or greater, and n is an integer of 1 or greater. A precursor compound to the photoacid generator, a photoresist composition including the photoacid generator, and a substrate coated with the photoresist composition, are also disclosed.

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Номер записи: 66
22-02-2018 дата публикации

COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME

Номер: US20180053899A1
Автор: Chen Chi-Chung, LIAO Liang-Di, SHIEH Shwu-Ju, WU Hui-Ling
Принадлежит: NICHEM FINE TECHNOLOGY CO., LTD.

Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): 6. The compound as claimed in claim 5 , wherein Qand Qare each independently selected from the group consisting of: a substituted or unsubstituted phenyl group claim 5 , a substituted or unsubstituted biphenylyl group claim 5 , a substituted or unsubstituted terphenyl group claim 5 , a substituted or unsubstituted naphthyl group claim 5 , a substituted or unsubstituted phenanthryl group claim 5 , a substituted or unsubstituted anthryl group claim 5 , a substituted or unsubstituted benzanthryl group claim 5 , a substituted or unsubstituted pyrenyl group claim 5 , a substituted or unsubstituted fluorenyl group claim 5 , and any deuterated analogs thereof.12. The compound as claimed in claim 1 , wherein L claim 1 , L claim 1 , and Lare the same.14. An organic electronic device claim 1 , comprising a first electrode claim 1 , a second electrode claim 1 , and an organic layer disposed between the first electrode and the second electrode claim 1 , wherein the organic layer comprises the compound as claimed in .15. The organic electronic device as claimed in claim 14 , wherein the organic electronic device is an organic light emitting device.16. The organic electronic device as claimed in claim 15 , wherein the organic light emitting device comprises:a hole injection layer formed on the first electrode;a hole transport layer formed on the hole injection layer, wherein the organic layer is the hole transport layer;an emission layer formed on the hole transport layer;an electron transport layer formed on the emission layer, andan electron injection layer formed between the electron transport layer and the second electrode.17. The organic electronic device as claimed in claim 15 , wherein the organic light emitting device comprises:a hole injection layer formed on the first electrode, wherein the organic layer is the hole injection ...

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Номер записи: 67
02-03-2017 дата публикации

MACROCYCLIC PICOLINAMIDES AS FUNGICIDES

Номер: US20170055528A1
Автор: Boebel Timothy A., Bravo-Altamirano Karla, Daeuble, Li Fangzheng, Lu Yu, Meyer Kevin G., SR. John F., Yao Chenglin
Принадлежит:

This disclosure relates to macrocyclic picolinamides of Formula (I) and their use as fungicides. 2. A compound according to claim 1 , wherein X and Y are hydrogen.3. A compound according to claim 2 , wherein Ris chosen from alkyl or aryl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.4. A compound according to claim 2 , wherein Ris chosen from alkyl or aryl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.5. A compound according to claim 1 , wherein X is C(O)Rand Y is hydrogen.6. A compound according to claim 5 , wherein Ris chosen from alkyl or aryl claim 5 , each optionally substituted with 0 claim 5 , 1 or multiple R.7. A compound according to claim 5 , wherein Ris chosen from alkyl or aryl claim 5 , each optionally substituted with 0 claim 5 , 1 or multiple R.8. A compound according to claim 1 , wherein Xis hydrogen and Y is Q.9. A compound according to claim 8 , wherein Ris chosen from alkyl or aryl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R.10. A compound according to claim 8 , wherein Ris chosen from alkyl or aryl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R.11. A compound according to claim 9 , wherein Ris hydrogen.12. A compound according to claim 9 , wherein Ris —C(O)Ror —CHOC(O)R.13. A compound according to claim 12 , wherein Ris chosen from alkyl or alkoxy claim 12 , each optionally substituted with 0 claim 12 , 1 claim 12 , or multiple R.14. A compound according to claim 13 , wherein Ris chosen from —CH claim 13 , —CH(CH) claim 13 , —CHOCHCH claim 13 , or —CHCHOCH.15. A composition for the control of a fungal pathogen including at least one of the compounds of and a phytologically acceptable carrier material.16. A composition for the control of a fungal pathogen including mixtures of at least one of the compounds of with other pesticides including fungicides claim 1 , insecticides claim 1 , nematocides claim 1 , miticides claim 1 , arthropodicides claim 1 ...

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Номер записи: 68
20-02-2020 дата публикации

STEREOCHEMICALLY DEFINED POLYPROPIONATES AND METHODS FOR MAKING AND USING THE SAME

Номер: US20200055866A1
Автор: Campagna Silvio, CHOI Hyeong-Wook, Fang Francis G., MATHIEU Steven
Принадлежит: Eisai R&D Management Co., Ltd.

The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries. 23-. (canceled)7. (canceled)957-. (canceled)60. The compound of claim 1 , wherein R is —C(O)Rand Ris substituted with —COOH.64. The process of claim 63 , wherein the reducing agent is a hydride.65. The process of claim 63 , wherein the reducing agent is sodium borohydride.66. The process of claim 63 , wherein the acid is hydrochloric acid.68. The process of claim 67 , further comprising claim 67 , prior to reacting the racemic mixture of phthalates of Formulas 2A and 2B with the first chiral amine in the solvent to form the pair of diastereomeric salts thereof in the solution claim 67 , dissolving the racemic mixture of phthalates of Formulas 2A and 2B in the solvent.69. The process of claim 68 , wherein the racemic mixture of phthalates of Formulas 2A and 2B are dissolved in the solvent at a volume ratio in a range of about 1:12 to about 1:20 (phthalates:solvent).70. The process of claim 67 , wherein the solvent is acetone.71. The process of claim 67 , wherein the first chiral amine is (S)-α-methylbenzylamine. This application is a divisional of and claims priority to pending U.S. Utility patent application Ser. No. 15/906,401 which is a divisional of and claims priority to pending U.S. Utility patent application Ser. No. 15/501,658, which was the U.S. national phase under 35 U.S.C. § 371 of PCT International Patent Application Serial No. PCT/US2015/043535, filed on Aug. 4, 2015, which claims the benefit of and priority to U.S. Provisional Application Ser. No. 62/032,757, filed Aug. 4, 2014, the disclosure of which is hereby incorporated by reference herein in its entirety.The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically ...

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Номер записи: 69
05-03-2015 дата публикации

7-MEMBERED FUSED HETEROCYCLES AND METHODS OF THEIR SYNTHESIS

Номер: US20150065703A1
Автор: Ferrer Javier Izquierdo, Scheidt Karl A.
Принадлежит: Northwestern University

Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds. 4. The compound of claim 1 , wherein Ris an aromatic system selected from a group consisting of phenyl claim 1 , naphthyl claim 1 , and pyridinyl claim 1 , which optionally is substituted with C-Calkyl claim 1 , halo claim 1 , or C-Calkoxy.6. The compound of claim 1 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.10. The compound of claim 7 , wherein Ris an aromatic system selected from a group consisting of phenyl claim 7 , naphthyl claim 7 , and pyridinyl claim 7 , which optionally is substituted with C-Calkyl claim 7 , halo claim 7 , or C-Calkoxy.12. The compound of claim 7 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.17. The compound of claim 13 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.20. The method of claim 18 , wherein LG is Br claim 18 , Cl claim 18 , or a sulfonate ester. The present application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 61/870,966, filed on Aug. 28, 2013, the content of which is incorporated herein by reference in its entirety.This invention was made with government support under grant number R01 GM073072 awarded by the National Institutes of Health. The government has certain rights in the invention.The field of the invention relates to 7-membered fused heterocycles and their methods of synthesis. In particular, the field of the ...

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Номер записи: 70
28-02-2019 дата публикации

USE OF PICOLINAMIDE COMPOUNDS AS FUNGICIDES

Номер: US20190059383A1
Автор: Bravo-Altamirano Karla, Buchan Zachary A., Daeuble, DeKorver Kyle A., Herrick Jessica, Jones David M., LOY Brian A., Lu Yu, Meyer Kevin G., Rigoli Jared W., SR. John F., Wang Xuelin, Wilmot Jeremy, Yao Chenglin
Принадлежит:

This disclosure relates to picolinamides of Formula I and their use as fungicides. 2. The composition according to claim 1 , wherein X is hydrogen and Y is Q.3. (canceled)4. The composition according to claim 2 , wherein Ris alkoxy.5. The composition according to claim 4 , wherein Ris hydrogen.6. The composition according to claim 5 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 5 , Rand Rare independently aryl claim 5 , each optionally substituted with 0 claim 5 , 1 or multiple R claim 5 , and Ris H.7. The composition according to claim 4 , wherein Ris chosen from —C(O)R claim 4 , or —CHOC(O)R.8. The composition according to claim 7 , wherein Ris alkyl claim 7 , optionally substituted with 0 claim 7 , 1 or multiple R.9. The composition according to claim 8 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 8 , Rand Rare independently aryl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R claim 8 , and Ris H.10. The composition according to claim 9 , wherein Ris chosen from —CH claim 9 , —CHOCHCH claim 9 , —CHCHOCH claim 9 , —CH(CH) claim 9 , —CHCHCHCH claim 9 , -cyclopropyl.11Zymoseptoria triticiPuccinia triticinaPuccinia striiformisVenturia inaequalisUstilago maydisUncinula necatorRhynchosporium secalisPyricularia oryzaePhakopsora pachyrhiziLeptosphaeria nodorumBlumeria graminis f.triticiBlumeria graminis f.hordeiErysiphe cichoracearumColletotrichum lagenariumCercospora beticolaAlternaria solaniPyrenophora teres. The composition according to wherein the fungal pathogen is one of Leaf Blotch of Wheat () claim 1 , Wheat Brown Rust () claim 1 , Stripe Rust () claim 1 , Scab of Apple () claim 1 , Blister Smut of Maize () claim 1 , Powdery Mildew of Grapevine () claim 1 , Barley scald () claim 1 , Blast of Rice () claim 1 , Rust of Soybean () claim 1 , Glume Blotch of Wheat () claim 1 , Powdery Mildew of Wheat (sp. ) claim 1 , Powdery Mildew of Barley (sp. ) claim 1 , Powdery Mildew of Cucurbits () claim 1 ...

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Номер записи: 71
10-03-2016 дата публикации

HIGHLY ACTIVE, SELECTIVE, ACCESSIBLE, AND ROBUST ZEOLITIC SN-BAEYER-VILLIGER OXIDATION CATALYST

Номер: US20160067692A1
Автор: Katz Alexander S., Ouyang Xiaoying, Zones Stacey Ian
Принадлежит:

Provided is a process of conducting a Baeyer-Villiger oxidation which comprises contacting a ketone and an oxidant in the presence of an Sn-DZ-1 catalyst to thereby oxidize the ketone to an ester. The Sn-DZ-1 catalyst comprises Sn heteroatoms on the external surface of the zeolitic material lattice framework, and B heteroatoms, or silanols created from boron hydrolysis, throughout the remainder of the lattice framework. 1. A process of conducting a Baeyer-Villiger oxidation which comprises contacting a ketone and an oxidant in the presence of a Sn-DZ-1 catalyst to thereby oxidize the ketone to an ester.2. The process of claim 1 , wherein the ketone comprises a cyclic ketone such that its Baeyer-Villiger-oxidation product is a lactone.3. The process of claim 1 , wherein the ketone comprises 2-adamantanone.4. The process of claim 1 , wherein the ketone comprises 5-hydroxyl-2-adamantanone.5. The process of claim 1 , wherein the ketone comprises 5-bromo-2-adamantanone.6. The process of claim 1 , wherein the oxidant comprises a peroxy acid.7. The process of claim 1 , wherein the oxidant comprises hydrogen peroxide.8. The process of claim 1 , wherein the oxidant comprises an organic hydroperoxide.9. The process of claim 1 , wherein a solvent is used for the reaction which comprises dioxane.10. The process of claim 1 , wherein the Sn-DZ-1 catalyst is prepared by a method comprising delaminating a borosilicate zeolite precursor by contacting the zeolite precursor in a solution with a metal salt.11. The process of claim 10 , wherein the metal salt comprises an Al claim 10 , Zn claim 10 , or Mn cation.12. The process of claim 10 , wherein the metal salt comprises a Ga cation.13. The process of claim 10 , wherein the borosilicate zeolite precursor is ERB-1.14. The process of claim 1 , wherein the Sn-DZ-1 comprises Sn heteroatoms on the external surface of the zeolitic material lattice framework claim 1 , and B heteroatoms claim 1 , or silanols created from boron hydrolysis ...

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Номер записи: 72
17-03-2016 дата публикации

SYNTHESIS OF RESORCYLIC ACID LACTONES USEFUL AS THERAPEUTIC AGENTS

Номер: US20160075677A1
Автор: BARLUENGA Sofia, KARPLUS Martin, WINSSINGER Nicolas
Принадлежит: Universite De Strasbourg

Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90. 2. The compound of claim 1 , wherein X is O or NR.3. The compound of claim 1 , wherein X is O or NR; and Y is —OR claim 1 , —O—(CH)COOR or —O—(CH)CON(R).4. The compound of claim 1 , wherein Rand Rare independently hydrogen or halogen.6. The compound of claim 5 , wherein Rand Rare hydrogen or halogen.7. The compound of claim 5 , wherein Rand are Rare alkyl or hydrogen.8. The compound of claim 5 , wherein claim 5 , Rand Rare independently hydrogen or aliphatic.9. The compound of claim 5 , wherein X is O; Y is —O—(CH)COOR or —O—(CH)CON(R) claim 5 , wherein the groups bound to the nitrogen atom may be in the Z- or E-configuration; R claim 5 , Rare independently hydrogen or halogen; and Rand Rare independently hydrogen or aliphatic.11. The compound of claim 10 , wherein X is O or NR.12. The compound of claim 10 , wherein Y is —O—(CH)COOR or —O—(CH)CON(R) claim 10 , wherein the groups bound to the nitrogen atom may be in the Z- or E-configuration.13. The compound of claim 10 , wherein X is O claim 10 , Y is —O—(CH)COOR or —O—(CH)CON(R) claim 10 , wherein the groups bound to the nitrogen atom may be in the Z- or E-configuration; Rand Rare independently hydrogen or halogen; and Rand Rare hydrogen.17. A pharmaceutical composition comprising an effective HSP 90-inhibiting amount of a compound of claim 1 , in combination with a pharmaceutically acceptable carrier.18. A pharmaceutical composition comprising an effective kinase-inhibiting amount of a compound of claim 1 , in combination with a pharmaceutically acceptable carrier.19. The composition of claim 17 , wherein the composition comprises particles that are less than about 2 microns average particle ...

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Номер записи: 73
16-03-2017 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Номер: US20170073323A1
Автор: HSU Min-Kuan, Kao Li-Ta, WEI Shih-Yi, Yeh Yu-Chih
Принадлежит: CHIROGATE INTERNATIONAL INC.

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: 1. A compound selected from the group consisting of:and Pand Pare protecting groups for hydroxyl groups, which are independently selected from the group consisting of methoxymethyl, methoxythiomethyl, tert-butylthiomethyl, benzyloxymethyl, 2-methoxyethoxymethyl, bis(2-chloroethoxy)methyl, tetrahydropyranyl, tetrahydrothiopyranyl, 4-methoxytetrahydropyranyl, 4-methoxytetrahydrothiopyranyl, tetrahydrofuranyl, tetrahydrothiofuranyl, 1-ethoxyethyl, 1-methyl-1-methoxyethyl, and triphenylmethyl. This application is a Divisional of U.S. patent application Ser. No. 14/801,999 filed Jul. 17, 2015, which is a Divisional of U.S. patent application Ser. No. 13/967,473 filed Aug. 15, 2013 (now U.S. Pat. No. 9,115,109 granted, Aug. 25, 2015) the content of which is incorporated herein by reference.The present invention relates to novel processes and intermediates for the preparations of isomer free Prostaglandins and the derivatives thereof.Prostaglandin ester analogues of the following Formula I-2whereinis a single or double bond; Ris a single bond or a C-alkylene or —CHO—; and Ris a C-alkyl or an aryl or an aralkyl, each of which is unsubstituted or substituted by a C-alkyl, a halogen or a trihalomethyl; and Ris C-alkyl, such as, Latanoprost, Isopropyl unoprostone, Isopropyl cloprostenol, Travoprost and Tafluprost have been used in the management of open-angle glaucoma. The Prostaglandin ester analogues of Formula I-2 have been shown to have significantly greater hypotensive potency than the parent compound, presumably as a result of their more effective penetration through the cornea. They reduce intra-ocular pressure by enhancing uveoscleral outflow, and may also have some effect on trabecular meshwork as well.As shown in the following Scheme A:most of the Prostaglandin ester analogues of Formula I-2 disclosed in the prior art, such as in WO02096898, EP1886992, ...

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Номер записи: 74
05-06-2014 дата публикации

RESORCYLIC ACID LACTONE COMPOUNDS

Номер: US20140155635A1
Автор: Kim Ji Nyeo, Sim Tae Bo, YOON Ho Jong
Принадлежит: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Disclosed are a novel resorcyclic acid lactone compound with inhibitory activity against protein kinases, a pharmaceutically acceptable salt thereof, a method for the synthesis thereof, and a pharmaceutical composition for the treatment and prevention of various cancer diseases comprising the same as an active ingredient. The novel resorcyclic acid lactone compound is useful as a therapeutic for cancer diseases, especially blood cancer, inter alia, acute myeloid leukemia (AML). 2. The compound of claim 1 , being in an optically pure form or as a racemate.3. The compound of claim 2 , wherein Ris C1˜C10 alkyl claim 2 , and Rand Rare each a hydrogen atom.4. The compound of claim 3 , being (7S claim 3 ,12S claim 3 ,13R claim 3 ,Z)-4 claim 3 ,12 claim 3 ,13-trihydroxy-2-methoxy-7-methyl-7 claim 3 ,8 claim 3 ,13 claim 3 ,14-tetrahydro-5H-dibenzo[c claim 3 ,e][1]oxacyclotetradecen-5 claim 3 ,11(12H)-dione.5. An anti-cancer composition comprising the compound defined in .6. The anti-cancer composition of claim 5 , having inhibitory activity against a kinase selected from the group consisting of FLT3 (D835Y) claim 5 , FLT3 (ITD) claim 5 , FLT3 claim 5 , FLT1/VEGFR1 claim 5 , FLT4/VEGFR3 claim 5 , PDGFRa claim 5 , PDGFRb claim 5 , PDGFRa (D842V) claim 5 , PDGFRa (T674I) claim 5 , and PDGFRa (V561 D).7. The anti-cancer composition of for use in treatment and prevention of blood cancer.8. The anti-cancer composition of claim 7 , wherein the blood cancer is acute myeloid leukemia (AML).10. An intermediate compound for use in synthesis of the resorcyclic acid lactone compound of claim 1 , selected from the group consisting of:5-(3-(hydroxymethyl)phenyl)-7-methoxy-2,2-dimethyl-4H-benzo[d][1,3]dioxin-4-one);3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)benzaldehyde;(E)-methyl 3-(3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)phenyl)acrylate;(2S,3R)-methyl 2,3-dihydroxy-3-(3-(7-methoxy-2,2-dimethyl-4-oxo-4H-benzo[d][1,3]dioxin-5-yl)phenyl)propanoate;(4S,5R ...

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Номер записи: 75
12-06-2014 дата публикации

Tin-Containing Zeolitic Material Having an MWW-Type Framework Structure

Номер: US20140163243A1
Автор: COX Gerhard, Hinrichsen Bernd, Jacubinas Richard, Müller Ulrich, Parvulescu Andrei-Nicolae, Teles Joaquim Henrique, Vautravers Nicolas
Принадлежит: BASF SE

A tin containing zeolitic material having an MWW-type framework structure (Sn-MWW), having a tin content of at most 2 weight-%, calculated as element and based on the weight of the Sn-MWW, and having an X-ray diffraction pattern comprising peaks at 2 theta diffraction angles of (6.6±0.1)°, (7.1±0.1)°, and (7.9±0.1)°. 1. A process for preparing a tin-containing zeolitic material having an MWW-type framework structure (Sn-MWW) comprising{'sub': 2', '2', '3, '(i) providing a boron-containing zeolitic material having an MWW framework structure comprising SiOand BO(B-MWW);'}(ii) deboronating the B-MWW by treating the B-MWW provided in (i) with a liquid solvent system having a pH in the range of from 5.5 to 8; [{'sub': 2', '2, '(iii.1) preparing an aqueous synthesis mixture containing the deboronated B-MWW obtained from (ii), an MWW template compound, and a tin source, wherein in the synthesis mixture, the molar ratio of Sn, calculated as SnO, relative to Si, calculated as SiOand contained in the deboronated B-MWW, is at most 0.015:1;'}, '(iii.2) hydrothermally synthesizing a tin-containing zeolitic material having an MWW-type framework structure from the synthesis mixture obtained from (iii.1) thereby obtaining a tin-containing zeolitic material having an MWW-type framework structure in its mother liquor;', '(iii.3) separating the tin-containing zeolitic material having an MWW-type framework structure obtained from (iii.2) from its mother liquor;, '(iii) incorporating Sn into the deboronated B-MWW obtained from (ii) by a process comprising'}(iv) treating the tin-containing zeolitic material having an MWW-type framework structure obtained from (iii) with an aqueous solution having a pH of at most 5 thereby obtaining the Sn-MWW having an Sn content of at most 2 weight-%, calculated as element and based on the weight of the Sn-MWW, and optionally separating the Sn-MWW from the aqueous solution.2. The process of claim 1 , wherein in (i) claim 1 , the B-MWW is provided by a ...

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Номер записи: 76
25-03-2021 дата публикации

THERAPEUTIC AGENT FOR GLAUCOMA COMPRISING FP AGONIST AND ß BLOCKER

Номер: US20210085636A1
Автор: Kazufumi NAGAI, Kazumi MORIYUKI, Satoshi Nakayama, Shinsaku Yamane, Tomohiro KARAKAWA
Принадлежит: Ono Pharmaceutical Co Ltd

A combination of the present invention is an effective therapy for glaucoma, in particular a combination of 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate and a β-blocker, is useful as an agent for treating glaucoma since the combination enhances intraocular pressure lowering action compared to a single administration of each drug and has an effect of maintaining intraocular pressure lowering action.

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Номер записи: 77
29-03-2018 дата публикации

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Номер: US20180086730A1
Автор: BECKER Cyrus K., Pfister Jürg, Venkatraman Meenakshi S., Zhang Xiaoming
Принадлежит:

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 147-. (canceled)49. The compound of claim 48 , wherein R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , and Rare H.50. The compound of claim 48 , wherein at least one of R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , and Rare is deuterium.51. The compound of claim 48 , wherein Lis —O-alkylene-C(O)—.52. The compound of claim 48 , wherein Lis —O-alkylene-OC(O)—.53. The compound of claim 48 , wherein Lis a bond.54. The compound of claim 48 , wherein the alkylene group is a C-Calkylene group.55. The compound of claim 48 , wherein the alkylene group is a Calkylene group.56. (canceled)5863-. (canceled)66. A composition comprising a compound of claim 48 , or and one or more pharmaceutically acceptable excipients.67. The composition of claim 66 , which is formulated for transdermal delivery.6870-. (canceled)71. A method of treating pulmonary hypertension claim 66 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of claim 66 , or or a pharmaceutically acceptable salt thereof.72. The method of claim 71 , wherein the pulmonary hypertension is pulmonary arterial hypertension.73. The method of claim 71 , wherein the compound is administered transdermally. This application claims priority to U.S. provisional application 61/751,608 filed Jan. 11, 2013 ...

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Номер записи: 78
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 ...

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Номер записи: 79
21-03-2019 дата публикации

CHEMICAL TOOLS FOR IMAGING PHOSPHOLIPASE D ACTIVITY

Номер: US20190085373A1
Автор: BASKIN Jeremy, BUMPUS Timothy, LIANG Dongjun
Принадлежит:

A method for detecting phospholipase D (PLD) activity in a cell, comprising: (i) stimulating endogenous PLD in said cell for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and an exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein the functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form; (ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its second functional group, with the first functional group to form a linkage between said detectable label and said phosphatidyl alcohol so as to form a labeled phosphatidyl alcohol containing said detectable label; and (iii) detecting said labeled phosphatidyl alcohol. 1. A method for detecting phospholipase D (PLD) activity in a cell , the method comprising:(i) stimulating endogenous PLD in said cell while said cell is in contact with an exogenous functionalized alcohol containing at least one carbon atom in order for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and said exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein said exogenous functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form, as provided by the exogenous functionalized alcohol;(ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its ...

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Номер записи: 80
02-04-2015 дата публикации

USE OF MACROCYCLIC PICOLINAMIDES AS FUNGICIDES

Номер: US20150094281A1
Автор: Boebel Timothy, Bravo-Altamirano Karla, Herrick Jessica, Li Fangzheng, Meyer Kevin G., Renga James M., Wilmot Jeremy, Yao Chenglin
Принадлежит:

The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides. 2. The method according to claim 1 , wherein X and Y are independently chosen from H claim 1 , C(O)R claim 1 , or CHOR.3. The method according to claim 2 , wherein Ris chosen from H claim 2 , alkyl claim 2 , alkenyl claim 2 , aryl claim 2 , —Si(R) claim 2 , or —C(O)R claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.4. The method according to claim 3 , wherein Ris chosen from CHR claim 3 , aryl claim 3 , alkyl claim 3 , or alkenyl claim 3 , each optionally substituted with 0 claim 3 , 1 claim 3 , or multiple R.5. The method according to claim 4 , wherein Ris chosen from H claim 4 , alkyl claim 4 , alkenyl claim 4 , aryl claim 4 , or heteroaryl claim 4 , each optionally substituted with 0 claim 4 , 1 claim 4 , or multiple R.6. The method according to claim 1 , wherein X is H and Y is Q.7. The method according to claim 6 , wherein Ris chosen from H claim 6 , alkyl claim 6 , alkenyl claim 6 , aryl claim 6 , —Si(R) claim 6 , or —C(O)R claim 6 , each optionally substituted with 0 claim 6 , 1 or multiple R.8. The method according to claim 7 , wherein Ris chosen from CHR claim 7 , aryl claim 7 , alkyl claim 7 , or alkenyl claim 7 , each optionally substituted with 0 claim 7 , 1 claim 7 , or multiple R.9. The method according to claim 8 , wherein Ris chosen from H claim 8 , alkyl claim 8 , alkenyl claim 8 , aryl claim 8 , or heteroaryl claim 8 , each optionally substituted with 0 claim 8 , 1 claim 8 , or multiple R.10. The method according to claim 9 , wherein Ris H claim 9 , —C(O)Ror —CHOC(O)R.11. The method according to claim 10 , wherein Ris chosen from —C(O)Ror —CHOC(O)R.12. The method according to claim 11 , wherein Ris chosen from alkyl or alkoxy claim 11 , each optionally substituted with 0 claim 11 , 1 claim 11 , or multiple R.13. The method according to wherein:at least one compound of said Formula I is applied in combination with a phytologically ...

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Номер записи: 81
02-04-2015 дата публикации

MACROCYCLIC PICOLINAMIDES COMPOUNDS WITH FUNGICIDAL ACTIVITY

Номер: US20150094341A1
Автор: Boebel Timothy, Bravo-Altamirano Karla, Herrick Jessica, Li Fangzheng, Meyer Kevin G., Renga James M., Wilmot Jeremy, Yao Chenglin
Принадлежит:

The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi. 2. The compound according to claim 1 , wherein X and Y are independently chosen from H claim 1 , C(O)R claim 1 , or CHOR.3. The compound according to claim 2 , wherein Ris chosen from H claim 2 , alkyl claim 2 , alkenyl claim 2 , aryl claim 2 , —Si(R) claim 2 , or —C(O)R claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.4. The compound according to claim 3 , wherein Ris chosen from CHR claim 3 , aryl claim 3 , alkyl claim 3 , or alkenyl claim 3 , each optionally substituted with 0 claim 3 , 1 claim 3 , or multiple R.5. The compound according to claim 4 , wherein Ris chosen from H claim 4 , alkyl claim 4 , alkenyl claim 4 , aryl claim 4 , or heteroaryl claim 4 , each optionally substituted with 0 claim 4 , 1 claim 4 , or multiple R.6. The compound according to claim 1 , wherein X is H and Y is Q.7. The compound according to claim 6 , wherein Ris chosen from H claim 6 , alkyl claim 6 , alkenyl claim 6 , aryl claim 6 , —Si(R) claim 6 , or —C(O)R claim 6 , each optionally substituted with 0 claim 6 , 1 or multiple R.8. The compound according to claim 7 , wherein Ris chosen from CHR claim 7 , aryl claim 7 , alkyl claim 7 , or alkenyl claim 7 , each optionally substituted with 0 claim 7 , 1 claim 7 , or multiple R.9. The compound according to claim 8 , wherein Ris chosen from H claim 8 , alkyl claim 8 , alkenyl claim 8 , aryl claim 8 , or heteroaryl claim 8 , each optionally substituted with 0 claim 8 , 1 claim 8 , or multiple R.10. The compound according to claim 9 , wherein Ris H claim 9 , —C(O)Ror —CHOC(O)R.11. The compound according to claim 10 , wherein Ris chosen from —C(O)Ror —CHOC(O)R.12. The compound according to claim 11 , wherein Ris chosen from alkyl or alkoxy claim 11 , each optionally substituted with 0 claim 11 , 1 claim 11 , or multiple R.13. A formulation for the control of a fungal pathogen claim 11 , ...

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Номер записи: 82
19-03-2020 дата публикации

CHEMICAL PROCESS TO MANUFACTURE BRANCHED-CAPROLACTONE

Номер: US20200087276A1
Автор: Dauenhauer Paul J., Hillmyer Marc A., Lundberg Daniel J., Lundberg David J.
Принадлежит:

Synthesizing an alkyl-caprolactone includes hydrogenating an alkyl-phenol to yield a first mixture comprising an alkyl-cyclohexanone and an alkyl-cyclohexanol; separating the alkyl-cyclohexanone from the first mixture to yield a first portion of a purified alkyl-cyclohexanone; oxidizing the first portion of the purified alkyl-cyclohexanone to yield a second mixture comprising an alkyl-caprolactone, the alkyl-cyclohexanone, and the alkyl-cyclohexanol; separating the alkyl-caprolactone from the second mixture to yield a third mixture comprising the alkyl-cyclohexanone and the alkyl-cyclohexanol; combining the third mixture and the first mixture in to yield a fourth mixture; separating the alkyl-cyclohexanone from the fourth mixture to yield a second portion of the purified alkyl-cyclohexanone; oxidizing the second portion of the purified alkyl-cyclohexanone to yield a fifth mixture comprising the alkyl-caprolactone, the alkyl-cyclohexanone, and the alkyl-cyclohexanol; separating the alkyl-caprolactone from the fifth mixture; and combining the alkyl-caprolactone from the fifth mixture with the alkyl-caprolactone from the second mixture. 1. A method of synthesizing an alkyl-caprolactone , the method comprising:hydrogenating an alkyl-phenol in a first reactor to yield a first stream comprising an alkyl-cyclohexanone;providing the first stream to a first distillation column to yield a second stream comprising the alkyl-cyclohexanone;providing the second stream to a second distillation column to yield a third stream comprising purified alkyl-cyclohexanone;oxidizing the purified alkyl-cyclohexanone in a second reactor to yield a fourth stream comprising an alkyl-caprolactone and the alkyl-cyclohexanone;providing the fourth stream to a third distillation column to yield a fifth stream comprising the alkyl-caprolactone and a sixth stream comprising the alkyl-cyclohexanone and water;removing some of the water from the sixth stream to yield a seventh stream;providing the ...

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Номер записи: 83
26-03-2020 дата публикации

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Номер: US20200093781A1
Автор: Kambe Tohru, Maruyama Toru, Nakayama Satoshi, TANI Kousuke, Yamane Shinsaku
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. 1. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, or a solvate thereof:and a pharmaceutically acceptable solvent, wherein the composition is a parenteral solution. The present invention relates to a compound represented by the general formula (I)(wherein all symbols represent the same meanings as those described below), a salt thereof, or a solvate thereof, or a prodrug thereof (hereinafter, abbreviated as present invention compound in some cases).Glaucoma is an ocular disease having the characteristic of a visual functional disorder which causes a transient or permanent visual field defect and decreased vision.This is derived from that since an aqueous humor is accumulated by a circulatory disorder of an aqueous humor, and an intraocular pressure is continuously increased, an optic nerve is compressed. Decrease in an intraocular pressure is effective for treatment of glaucoma and, in order to decrease an intraocular pressure, for example, drug treatment (eye drops, internal remedy, infusion treatment), laser treatment, or operation treatment is performed.Previously, among prostaglandins (PGs) which are physiologically active substances, as those that decrease an intraocular pressure, PGFs and PGIs are known. Development of a drug for treating glaucoma or ocular hypertension is being progressed using derivatives of them, and there are some drugs which are actually sold (e.g. latanoprost etc.). However, the existing glaucoma ...

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Номер записи: 84
04-04-2019 дата публикации

Process Involving Cross Metathesis of Olefins

Номер: US20190100504A1
Автор: DAVEY Paul Nicholas, Goeke Andreas, LORINCZ Krisztian, LOVCHIK Martin Alan, Ondi Levente, TOTH Florian
Принадлежит: Givaudan S.A.

A method of forming a macrocyclic musk compound comprising the steps of: — 1. A method of forming a macrocyclic musk compound comprising the steps of: —i) cross-metathesizing a first olefin and a second olefin in the presence of a homogeneous transition metal catalyst comprising an alkylidene ligand, to form a statistical mixture of a hetero-dimer intermediate of said first and second terminal olefin, and homo-dimersii) separating the hetero-dimer from the statistical mixture of hetero- and homo-dimersiii) and cyclizing the hetero-dimer intermediate to form the macrocyclic musk compound.7. A method according to claim 1 , wherein the first olefin and second olefin are reacted in a 1:x molar ratio to produce a ratio of hetero-dimer:first homo-dimer:second homo-dimer of 2x:1:1x.8. A method according to claim 1 , wherein the hetero-dimer is formed in admixture with a protected alcohol homo-dimer and a carboxylic acid ester homo-dimer.9. A method according to wherein the mixture of protected alcohol hetero-dimer and each carboxylic acid ester homo-dimer is formed in a molar ratio of 2:1:1.10. A method according to claim 1 , wherein the hetero-dimer is separated from the homo-dimers by distillation at a temperature of 100 to 220 degrees centigrade and a pressure of 1 to 10 mbar.11. A method according to claim 1 , wherein the homo-dimers are recycled by metathesis with ethylene to regenerate the first and second olefins.12. A method according to wherein the homo-dimers are treated with ethylene gas at a pressure of 1 bar to 20 bar.13. A method according to claim 1 , wherein the hetero-dimer is cyclised by trans-esterification.14. A method according to wherein claim 13 , if the hetero-dimer contains a protected alcohol group claim 13 , it is first de-protected by hydrolysis before being subjected to cyclisation by tran-esterification.15. A method of forming E/Z 9-ambrettolide according to the method according to .16. A method of forming E/Z 9-ambrettolide according to claim ...

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Номер записи: 85
02-06-2022 дата публикации

Methods of carbon-carbon bond fragmentation

Номер: US20220169580A1
Автор: Andrew Smaligo, Ohyun Kwon
Принадлежит: UNIVERSITY OF CALIFORNIA

The present disclosure relates to methods of carbon-carbon bond fragmentation.

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Номер записи: 86
02-06-2022 дата публикации

DERIVATIVES OF 10-METHYLENE LIPIDS, PROCESS FOR PREPARING SUCH DERIVATIVES AND USE THEREOF

Номер: US20220169596A1
Автор: Raboin Jean-Christophe, STRUB Henri
Принадлежит:

The present invention relates to derivatives of 10-methylene lipids, their preparation and their use. 1. Intermediate product for preparing a product chosen at least from polyamides , polyesters , lactams and lactones , and optionally said intermediate product having a saturated aliphatic linear chain of 14-20 carbon atoms , said aliphatic linear chain havinga terminal group chosen from a carboxylic acid and a carboxylic acid ester,a methyl group branched in the Δ10 position,{'sub': '2', 'a functional group bound to the carbon of the said branched methyl group, this functional group being chosen from bromo (—Br), hydroxyl (—OH) and amino (—NH) groups, wherein bromo (—Br) is preferred.'}2. Intermediate product according to claim 1 , wherein the aliphatic linear chain has 16 claim 1 , 17 or 18 carbon atoms claim 1 , preferably claim 1 , 16 or 18.3. Intermediate product according to any one of or claim 1 , wherein the terminal group is an ester chosen from methyl claim 1 , ethyl claim 1 , propyl and isopropyl esters.4. Composition comprising at least one intermediate product of any one of to claim 1 , optionally in mixture with other lipids.5. Process for preparing the intermediate product of any one of to or the composition of claim 1 , said process comprising the following steps:{'sub': '2', 'a) providing at least one 10-methylene-substituted lipid comprising an aliphatic linear chain of 14-20 carbon atoms having a methylene (═CH) group branched in the Δ10 position and a terminal group chosen from a carboxylic acid and a carboxylic acid ester, optionally in mixture with other lipids,'} a saturated aliphatic linear chain with the same number of carbon atoms than the aliphatic linear chain of the 10-methylene-substituted lipid,', 'a methyl group branched in the Δ10 position, and', {'sub': '2', 'a functional group bound to the carbon of the branched methyl group, chosen from bromo (—Br), hydroxyl (—OH) and amino (—NH) groups, preferably bromo (—Br).'}], 'b) reacting ...

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Номер записи: 87
08-04-2021 дата публикации

CONDENSED CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20210104673A1
Автор: HWANG Seokhwan, JUN Mieun, Kim Jongwoo, Kim Youngkook
Принадлежит:

Provided are a condensed cyclic compound and an organic light-emitting device including the same. The organic light-emitting device may include a first electrode, a second electrode, and an organic layer disposed between the first electrode and the second electrode. The organic layer may include the condensed cyclic compound represented by Formula 1: 3. An organic light-emitting device comprising:a first electrode;a second electrode facing the first electrode; andan organic layer disposed between the first electrode and the second electrode,{'claim-ref': [{'@idref': 'CLM-00001', 'claim 1'}, {'@idref': 'CLM-00002', 'claim 2'}], 'wherein the organic layer comprises an emission layer and the condensed cyclic compound of or .'}4. The organic light-emitting device of claim 3 ,wherein the first electrode is an anode, the second electrode is a cathode, the organic layer further comprises a hole transport region between the first electrode and the emission layer, and an electron transport region between the emission layer and the second electrode, the hole transport region comprises a hole injection layer, a hole transport layer, an emission auxiliary layer, an electron blocking layer, or any combination thereof, and the electron transport region comprises a hole blocking layer, a buffer layer, an electron transport layer, an electron injection layer, or any combination thereof.5. The organic light-emitting device of claim 4 ,wherein at least one of the hole transport region and the emission layer comprises the condensed cyclic compound.6. The organic light-emitting device of claim 4 ,wherein the hole transport region comprises a hole transport layer, and the hole transport layer comprises the condensed cyclic compound.7. The organic light-emitting device of claim 4 ,wherein the hole transport region comprises a hole injection layer, and the hole injection layer comprises the condensed cyclic compound. This application is a continuation of U.S. application Ser. No. 15/868, ...

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Номер записи: 88
23-04-2015 дата публикации

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Номер: US20150112079A1
Автор: Kambe Tohru, Maruyama Toru, Nakayama Satoshi, TANI Kousuke, Yamane Shinsaku
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. 113-. (canceled)17. The method of preparing a compound according to claim 16 , wherein the ring 2 is a C3-7 carbocycle claim 16 , or a salt thereof claim 16 , a solvate thereof claim 16 , or a prodrug thereof.181. The method of preparing a compound according to claim 16 , wherein Z is (1) —(CH)— claim 16 , or (2) —(CH)-A-CH—; and all symbols represent the same meanings as those described claim claim 16 ,or a salt thereof, a solvate thereof, or a prodrug thereof.19. The method of preparing a compound according to claim 16 , wherein the compound represented by the general formula (I-2) is a compound selected from:(1) 4-{(3S,5 aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(2) ethyl 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(3) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-7-hydroxy-6-[(1E,3R)-3-hydroxy-4-phenoxy-1-buten-1-yl]octahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(4) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(3-chlorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid,(5) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(3-chlorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate,(6) 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid, and(7) 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E ...

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Номер записи: 89
03-07-2014 дата публикации

BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES

Номер: US20140187557A1
Автор: DOYON Julien Georges Pierre-Olivier, LINDERS Joannes Theodorus Maria, Meerpoel Lieven, PONCELET Alain Philippe, Schoentjes Bruno, VER DONCK Luc August Laurentius
Принадлежит: Janssen Pharmaceutica NV

The present invention relates to a compound of formula (I) 2. The method as claimed in wherein A represents phenyl or phenyl substituted with 1 claim 1 , 2 or 3 Rsubstituents.4. The method as claimed in wherein A represents pyridyl claim 1 , pyrimidinyl or quinolinyl claim 1 , each of said pyridyl claim 1 , pyrimidinyl or quinolinyl optionally being substituted with 1 claim 1 , 2 or 3 Rsubstituents.5. The method as claimed in wherein Z represents CH.6. The method as claimed in wherein Z represents O.7. The method as claimed in wherein Rrepresents halo claim 1 , hydroxyl claim 1 , Calkyl or Calkyloxy.8. The method as claimed in wherein Rrepresents hydrogen.11. The method as claimed in wherein n represents an integer of value 1 or 2.12. The method as claimed in wherein n is 0.13. The method as claimed in wherein A represents phenyl claim 1 , 1 claim 1 ,3-benzodioxolyl claim 1 , 2 claim 1 ,3-dihydro-1 claim 1 ,4-benzodioxinyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , quinolinyl; each of said rings optionally being substituted with 1 or 2 substituents each independently selected from halo claim 1 , hydroxyl claim 1 , Calkyl or Calkyloxy; Rand Reach independently represent hydrogen claim 1 , Calkyl claim 1 , CalkyloxyCalkyl claim 1 , phenylCalkyl; or Rand Rare taken together with the nitrogen to which they are attached to form pyrrolidinyl optionally substituted in position 3 with hydroxyl; piperidinyl; morpholinyl; piperazinyl optionally substituted with Calkyl or Calkylcarbonyl; Rrepresents hydrogen or methyl.14. The method as claimed in wherein the substituents on the cycloheptane or oxepine ring have a cis configuration.15. The method as claimed in wherein the compound is an enantiomeric pure form.16. The method as claimed in wherein the compound is selected from(±) cis-6-(4-Chloro-3-methoxy-phenyl)-5-(3-diethylamino-propyl)-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol oxalate;(±) cis-6-(3-Chloro-phenyl)-5-(3-diethylamino-propyl)-6,7,8,9-tetrahydro-5H- ...

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Номер записи: 90
02-04-2020 дата публикации

A HIGHLY EFFICIENT SYNTHESIS OF Z-MACROCYLCES USING STEREORETENTIVE, RUTHENIUM-BASED METATHESIS CATALYSTS

Номер: US20200102285A1
Автор: Ahmed Tonia S., GRUBBS Robert H.
Принадлежит:

A highly efficient, Z-selective ring-closing metathesis system for the formation of macrocycles using a stereoretentive, ruthenium-based catalyst supported by a dithiolate ligand is reported. This catalyst is demonstrated to be remarkably active as observed in initiation experiments showing complete catalyst initiation at −20° C. within 10 min. Using easily accessible diene starting materials bearing a Z-olefin moiety, macrocyclization reactions generated products with significantly higher Z-selectivity in appreciably shorter reaction times, in higher yield, and with much lower catalyst loadings than in previously reported systems. Macrocyclic lactones ranging in size from twelve-membered to seventeen-membered rings are synthesized in moderate to high yields (68-79% yield) with excellent Z-selectivity (95%-99% Z). 2. The method according to claim 1 , wherein:R′ is methyl or ethyl;n is 1, 3, or 4;m is 6 or 7;the Z-macrocyclic product of Formula (VI) is a thirteen, fourteen, sixteen, or seventeen-membered ring with a Z-selectivity of 95;R is nil, iso-propyl or butyl;{'sub': '0', 'Ris nil;'}{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10, 'R, R, R, R, R, R, R, R, R, and Rare H, methyl, iso-propyl, or fluoro;'}{'sub': 11', '12', '13', '14, 'R, R, R, and Rare independently H, phenyl, iso-propoxy, nitro, or dimethylaminosulfonate;'}{'sub': 15', '16', '17', '18, 'R, R, R, and Rare H or methyl;'}{'sub': 1', '2', '3', '4, 'X, X, X, and Xare H, fluoro, or chloro; and'}Y is oxygen, sulfur, or iodo.3. The method according to claim 1 , wherein:R′ is methyl;n is 2;m is 6;the Z-macrocyclic product of Formula (VI) is a sixteen-membered ring with a Z-selectivity of 98;R is nil, iso-propyl, or butyl;{'sub': '0', 'Ris nil;'}{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10, 'R, R, R, R, R, R, R, R, R, and Rare H, methyl, iso-propyl, or fluoro;'}{'sub': 11', '12', '13', '14, 'R, R, R, and Rare H, phenyl, iso-propoxy, nitro, or dimethylaminosulfonate;'}{'sub': 15', '16', ' ...

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Номер записи: 91
11-04-2019 дата публикации

Photoactive fluorophores and methods of in vivo labeling

Номер: US20190106573A1
Автор: Jonathan B. Grimm, Luke D. Lavis
Принадлежит: HOWARD HUGHES MEDICAL INSTITUTE

Provided are a photoactive fluorophore, a photoactive ligand, and a photoactive complex. The photoactive fluorophore includes a photoactivatable derivative of an azetidine-containing Janelia-Fluor dye. The photoactive ligand includes a photoactive fluorophore and a protein tag. The photoactive complex includes a photoactive ligand conjugated to a protein. Also provided are methods of in vivo labeling with and photoactivation of the photoactive fluorophore, ligand, and complex.

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Номер записи: 92
10-07-2014 дата публикации

CYTOTOXIN COMPOUNDS AND METHODS OF ISOLATION

Номер: US20140194495A1
Автор: AMSLER CHARLES D., Baker Bill J., DIYABALANAGE THUSHARA, MCCLINTOCK JAMES B.
Принадлежит:

The present invention concerns groups of compounds derived from tunicates of the species, as well as to pharmaceutical compositions comprising these compounds, and uses thereof. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines. 126-. (canceled)28. The Palmerolide compound according to claim 27 , wherein at least one Ris —OC(NH)O.29. The Palmerolide compound according to claim 27 , wherein Ris methyl.30. The Palmerolide compound according to claim 27 , wherein at least one Ris methyl.31. The Palmerolide compound according to claim 27 , wherein both Rare methyl.32. The Palmerolide compound according to claim 27 , wherein Ris —CHCHNHC(O)CHC(CH).33. The Palmerolide compound according to claim 27 , wherein Ris —CHCHNHC(O)CHC(CH)CHC(CH)CH.34. The Palmerolide compound according to claim 27 , wherein Ris —CHCHNHC(O)CHC(CH)CHC(CH)CH.35. The Palmerolide compound according to claim 27 , wherein Ris —CH═O.36. The Palmerolide compound according to claim 27 , wherein at least one Ris —OH.37. The Palmerolide compound according to claim 27 , wherein at least one Ris —OSOH.38. The Palmerolide compound according to claim 27 , wherein at least two Rare —OH and at least one Ris —OC(NH)O claim 27 , and optionally Rand Rare —CH.42. A method for isolating a Palmerolide claim 27 , said method comprising:{'i': 'Synoicum', 'a) subjecting a tunicate to solvent extraction;'}b) removing said solvent to provide an extract; andc) fractionating said extract to isolate said Palmerolide.43. The method according to claim 42 , wherein said solvent is CHCH/MeOH.44. The method according to claim 42 , wherein said extract is fractionated using flash chromatography.45. The method according to claim 44 , wherein said flash chromatography is gradient flash chromatography over silica.46. The ...

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Номер записи: 93
27-04-2017 дата публикации

Process for Preparing Cyclic Esters and Cyclic Amides

Номер: US20170114036A1
Автор: DUSSELIER Michiel, SELS Bert
Принадлежит:

The invention relates to a process for preparing a cyclic ester or a cyclic amide, comprising the step of: 115-. (canceled)17. The process according to claim 16 , wherein at least one of said interconnected and non-parallel channel systems comprises 12- or more-membered ring channels.18. The process according to claim 16 , wherein said zeolite has a Brønsted acid density between 0.05 and 6.5 mmol/g dry weight.19. The process according to claim 16 , wherein said zeolite comprises a BEA topology claim 16 , a MFI topology claim 16 , a FAU topology claim 16 , a MEL topology claim 16 , a FER topology claim 16 , and a MWW topology.20. The process according to claim 16 , wherein said zeolite comprises a BEA topology.21. The process according to claim 16 , wherein X is Al.22. The process according to claim 16 , wherein said zeolite comprises at least three interconnecting and non-parallel channel systems.23. The process according to claim 16 , wherein said aminocarboxylic acid is provided in a composition comprising said amino-carboxylic acid in a concentration of at least 1 wt % based on a total weight of the composition.24. The process according to claim 16 , wherein said process is performed under conditions of water removal.25. The process according to claim 24 , wherein said water removal is performed via azeotropic distillation. The invention relates to a process for preparing cyclic esters and cyclic amides, which may be used as starting products for the preparation of polymers such as biopolymers.Cyclic esters are useful compounds that can be polymerized into polymeric materials. Such polymeric materials are useful in the preparation of biodegradable plastic materials and other plastic materials. Cyclic esters are also useful as plasticizers and as intermediates for production of surface-active agents and plasticizers.Cyclic esters are usually prepared by condensing hydroxy acids to an oligomeric prepolymer. The prepolymer is then depolymerized to a cyclic ester. ...

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Номер записи: 94
18-04-2019 дата публикации

Bicyclic compound and use thereof for medical purposes

Номер: US20190111019A1
Автор: Kousuke Tani, Satoshi Nakayama, Shinsaku Yamane, Tohru Kambe, Toru Maruyama
Принадлежит: Ono Pharmaceutical Co Ltd

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

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Номер записи: 95
03-05-2018 дата публикации

BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES

Номер: US20180116995A1
Автор: Kambe Tohru, Maruyama Toru, Nakayama Satoshi, TANI Kousuke, Yamane Shinsaku
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc. 113-. (canceled)14. 4-{(3S ,5aR ,6R ,7R ,8aS)-6-[(1E ,3R)-4-(2 ,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid.15. A pharmaceutical composition containing 4-{(3S ,5aR ,6R ,7R ,8aS)-6-[(1E ,3R)-4-(2 ,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoic acid.16. The pharmaceutical composition according to claim 15 , which is a FP agonist.17. The pharmaceutical composition according to claim 15 , which is an agent for treating an ocular disease.18. The pharmaceutical composition according to claim 17 , wherein the ocular disease is glaucoma claim 17 , ocular hypertension claim 17 , macular edema claim 17 , macular degeneration claim 17 , retina and optic nerve tensile force rise claim 17 , myopia claim 17 , hypermetropia claim 17 , astigma claim 17 , dry eye claim 17 , amotio retinae claim 17 , cataract claim 17 , intraocular pressure rise due to trauma or inflammation claim 17 , intraocular pressure rise due to a drug claim 17 , or intraocular pressure rise after operation.19. The pharmaceutical composition according to claim 17 , wherein the ocular disease is glaucoma claim 17 , or ocular hypertension.20. The pharmaceutical composition according to claim 15 , wherein a dosage form is an eye drop.21. A method of treating an ocular disease claim 15 , comprising administering an effective amount of 4-{(3S claim 15 ,5aR claim 15 ,6R claim 15 ,7R claim 15 ,8aS)-6-[(1E claim 15 ,3R)-4-(2 ...

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Номер записи: 96
25-08-2022 дата публикации

POLYCYCLIC CARBOGENIC MOLECULES AND USES THEREOF AS ANTI-CANCER AGENTS

Номер: US20220267241A1
Автор: Robinson Emily E., Thomson Regan J.
Принадлежит:

Disclosed are new polycyclic carbogenic molecules and their methods of synthesis. The new polycyclic carbogenic molecules may be utilized in anti-cancer therapies. In particular, the polycyclic carbogenic molecules may be formulated as pharmaceutical compositions that comprise the small molecules, which compositions may be administered in methods of treating and/or preventing cell proliferative diseases and disorders such as cancer. The new polycyclic carbogenic molecules may be prepared from vinyl- or allyl-substituted cyclohexenone precursors via preparation of a silyl bis-enol ether intermediate. 118.-. (canceled)2023.-. (canceled)24. A synthesis method for a polycyclic molecule comprising: (i) first precursor comprising a cyclohexanone substituted at the 5-position or the 6-position with a vinyl group or an allyl group,', '(ii) a second precursor which is a cyclohexanone substituted at the 5-position or the 6-position with a vinyl group or an allyl group, or a second precursor which is an alkyl vinyl ketone; and', '(iii) a dialkyl silyl dihalide to form a symmetrical or unsymmetrical silyl bis-enol ether; and, '(a) reacting a(b) performing oxidative coupling and ring-closing metathesis of the symmetrical or unsymmetrical silyl bis-enol ether to provide the polycyclic molecule.25. The method of claim 19 , wherein m and n are 0.28. The method of claim 27 , wherein m and n are 0.31. The method of claim 30 , wherein m and n are 0.34. The method of claim 33 , wherein m and n are 0. The present application claims the benefit of priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 62/561,464, filed on Sep. 21, 2017, the content of which is incorporated herein by reference in its entirety.The field of the invention relates to new small molecules and uses of the new small molecules as anti-cancer agents. The new small molecules are polycyclic carbogenic molecules that are potent to a variety of cancer cells.While treatment options have improved in recent ...

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Номер записи: 97
27-05-2021 дата публикации

Alpha,Beta-UNSATURATED AMIDE COMPOUND

Номер: US20210155612A1
Автор: Hiroki Yamada, Takahiro Nakajima, Tomohiro Danjo
Принадлежит: Kyowa Kirin Co Ltd

An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, “A” represents optionally substituted heterocyclic diyl, R 1 represents hydrogen atom or optionally substituted lower alkyl, R 2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO 2 —, —NR X1 — (wherein, R X1 represents hydrogen atom or lower alkyl), —CHR X2 — (wherein, R X2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

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Номер записи: 98
14-05-2015 дата публикации

ANTI-CANCER POLYKETIDE COMPOUNDS

Номер: US20150133535A1
Автор: Burkart Michael D., Castro Januario E., Jones Brian D., Kashyap Manoj Kumar, Kumar Deepak, La Clair James J., MANDEL Alexander, Villa Reymundo
Принадлежит:

Provided herein, inter alia, are anticancer polyketides. The uses of the polyketides described herein include treatment of cancer, for example, through regulation of the spliceosome and detection of spliceosome inhibition. 3. The compound of claim 1 , wherein Ris hydrogen or C-Cunsubstituted alkyl.4. (canceled)5. The compound of wherein Ris methyl.6. The compound of claim 4 , wherein Ris hydrogen.7. The compound of claim 5 , wherein Xis O.8. The compound of claim 1 , wherein when Ris attached to a chiral carbon having (S) stereochemistry claim 1 , Ris attached to a chiral carbon having (S) or (R) stereochemistry.9. The compound of claim 1 , wherein when Ris attached to a chiral carbon having (R) stereochemistry claim 1 , Ris attached to a chiral carbon having (S) stereochemistry.10. The compound of claim 1 , wherein Xis C(R)(R).11. The compound of claim 10 , wherein Rand Rare independently hydrogen claim 10 , halogen claim 10 , or methyl.12. The compound of claim 11 , wherein Rand Rare hydrogen or -F.13. (canceled)14. The compound of claim 13 , wherein when Ris attached to a chiral carbon having (S) stereochemistry claim 13 , Ris attached to a chiral carbon having (S) or (R) stereochemistry.15. The compound of claim 13 , wherein when Ris attached to a chiral carbon having (R) stereochemistry claim 13 , Ris attached to a chiral carbon having (S) or (R) stereochemistry.17. (canceled)18. A pharmaceutical composition comprising the compound of and a pharmaceutical excipient.19. A method of treating cancer claim 1 , the method comprising administering to a subject in need thereof a therapeutically effective amount of the compound of .20. The method of claim 19 , wherein the cancer is leukemia claim 19 , lymphoma claim 19 , metastatic cancer claim 19 , or bone cancer.21. (canceled)22. A method of detecting splicesome inhibition with a test compound claim 19 , the method comprising:(i) contacting a cell with a test compound;(ii) extracting an mRNA from said cell thereby ...

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Номер записи: 99
14-05-2015 дата публикации

DIRECT ANTI-MARKOVNIKOV ADDITION OF ACIDS TO ALKENES

Номер: US20150133680A1
Автор: Hamilton David S., Nicewicz David A., Perkowski Andrew J.
Принадлежит:

A method of making an anti-Markovnikov addition product is carried out by reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product; the dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst. Compositions useful for carrying out such methods are also described. 1. A method of making an anti-Markovnikov addition product , comprising:reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product;said dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst.2. The method of claim 1 , wherein said anti-Markovnikov addition product is produced regioselectively in a ratio of at least 5:1 of anti-Markovnikov addition product as compared to the corresponding Markovnikov addition product.4. The method of claim 3 , wherein A claim 3 , B claim 3 , and C are each independently selected from the group consisting of halo claim 3 , aryl claim 3 , cyano claim 3 , carboxyl claim 3 , and carbonyl groups.5. The method of claim 1 , wherein said single electron oxidation catalyst is a photocatalyst.6. The method of claim 5 , wherein said photocatalyst comprises a carbocyclic or heterocyclic aromatic compound containing ring nitrogen heteroatoms.7. The method of claim 6 , wherein said photocatalyst comprises an anthracene claim 6 , aza-anthracene or polyaza-anthracene nucleus which is unsubstituted claim 6 , substituted or polysubstituted at any position with halogen claim 6 , and/or with one or more lower alkyl or cycloalkyl radicals claim 6 , and/or with other phenyl substituents.8. The method of claim 5 , wherein said photocatalyst has a reduction potential of about −1.0 V to +0.1 V against a saturated calomel reference electrode in 100 percent acetonitrile ...

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Номер записи: 100