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21. 发明授权

US08557860B2 Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚烷（ENE）OIC酸，2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US08557860B2
公开(公告)日：2013-10-15
申请号：US12967115
申请日：2010-12-14
申请人： Yariv Donde , Robert M. Burk , Michael Garst
发明人： Yariv Donde , Robert M. Burk , Michael Garst
IPC分类号： A61K31/381 , C07D333/06 , C07D333/16 , C07D333/22 , C07D333/28
CPC分类号： C07D333/28
摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
摘要翻译：公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。还公开了与其相关的药物制备的组合物和方法。

22. 发明授权

US07964634B2 Therapeutic compounds 有权
标题翻译：治疗化合物
公开(公告)号：US07964634B2
公开(公告)日：2011-06-21
申请号：US12427298
申请日：2009-04-21
申请人： Yariv Donde , Jeremiah H. Nguyen , Mark Holoboski , Mari Posner , Robert M. Burk
发明人： Yariv Donde , Jeremiah H. Nguyen , Mark Holoboski , Mari Posner , Robert M. Burk
IPC分类号： A61K31/38 , C07D333/24
CPC分类号： C07D333/38 , C07C69/732 , C07C405/00 , C07C2601/08 , C07D295/088
摘要： Compounds having a structure are disclosed herein. Compositions, methods, and medicaments related to the therapeutic use of these compounds are also disclosed.
摘要翻译：具有结构的化合物在本文中公开。还公开了与这些化合物的治疗用途有关的组合物，方法和药物。

23. 发明申请

US20110082184A1 CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS 有权
公开(公告)号：US20110082184A1
公开(公告)日：2011-04-07
申请号：US12967115
申请日：2010-12-14
申请人： Yariv Donde , Robert M. Burk , Michael Garst
发明人： Yariv Donde , Robert M. Burk , Michael Garst
IPC分类号： A61K31/381 , A61P27/02
CPC分类号： C07D333/28
摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

24. 发明授权

US07427685B2 Therapeutic substituted cyclopentanes 有权
标题翻译：治疗性取代环戊烷
公开(公告)号：US07427685B2
公开(公告)日：2008-09-23
申请号：US11553143
申请日：2006-10-26
申请人： Yariv Donde , Robert M. Burk
发明人： Yariv Donde , Robert M. Burk
IPC分类号： C07D333/38 , C07C63/00 , C07C69/76
CPC分类号： C07D333/40 , C07C405/00 , C07D333/38
摘要： Therapeutic compounds according to one of the structures below are disclosed herein.
摘要翻译：本文公开了根据以下结构之一的治疗化合物。

25. 发明授权

US07217725B2 Prostaglandin D2 antagonist 有权
标题翻译：前列腺素D2拮抗剂
公开(公告)号：US07217725B2
公开(公告)日：2007-05-15
申请号：US10780441
申请日：2004-02-12
申请人： Achim H. Krauss , David Woodward , Yariv Donde , Robert M. Burk
发明人： Achim H. Krauss , David Woodward , Yariv Donde , Robert M. Burk
IPC分类号： A61K31/421 , C07D263/32
CPC分类号： C07D493/08 , A61K31/422
摘要： Disclosed herein is compound 1 or a pharmaceutically acceptable salt, or a prodrug thereof. Compound 1 is useful for treating or preventing a variety of diseases or conditions. Results presented herein also demonstrate that Compound 1 is a prostaglandin D2 antagonist, and as such is useful in the treatment or prevention of prostaglandin D2 mediated conditions or diseases. A method comprising administering a prostaglandin D2 antagonist to a mammal suffering from a disease or condition selected from the group consisting of the gastrointestinal tract disorders or diseases, hyperalgesia, allodynia, abdominal cramping, glaucoma, ocular hypertension, and ocular hypotension is also disclosed herein.Pharmaceutical compositions and products comprising compound 1 are also disclosed.
摘要翻译：本文公开了化合物1或其药学上可接受的盐或其前药。化合物1可用于治疗或预防各种疾病或病症。本文提供的结果还表明化合物1是前列腺素D 2拮抗剂，因此可用于治疗或预防前列腺素D 2 N介导的病症或疾病。一种方法，其包括向患有选自以下的疾病或病症的哺乳动物施用前列腺素D 2拮抗剂：胃肠道疾病或疾病，痛觉过敏，异常性疼痛，腹部绞痛，青光眼，高眼压症，并且本文还公开了眼部低血压。还公开了包含化合物1的药物组合物和产品。

26. 发明授权

US06369089B1 Interheteroaryl 7-oxabicyclic [2.2.1]heptane oxazoles as prostaglandin F2&agr; antagonists 有权
标题翻译：杂环芳基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2α拮抗剂
公开(公告)号：US06369089B1
公开(公告)日：2002-04-09
申请号：US09840675
申请日：2001-04-23
申请人： Robert M. Burk , Yariv Donde
发明人： Robert M. Burk , Yariv Donde
IPC分类号： A61K31422
CPC分类号： C07D493/08
摘要： The present invention provides novel compounds represented by the general formula I. wherein m is an integer of from 1 to 3; n is 0 or an integer of from 1 to 4; R is selected from the group consisting of CO2H, CO2 R6, CH2OH, CH2O R6 P(O)(OH)2, and CONR3R4; R1 and R2 are independently selected from the group consisting of H, R6, C1-C6 alkenyl, C1-C6 alkynyl, C3-C7 cycloalkyl, C4-C12 alkylcycloalkyl, C6-C10 aryl, C7-C12 alkyl aryl radicals and heteroatom-substituted derivatives thereof, wherein one or more of the hydrogen or carbon atoms in said radicals is replaced with a halogen, nitrogen or sulfur-containing radical; R3 and R4 are selected from the group consisting of H and R6; and X is selected from the group consisting of H, R6, hydroxy, N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl; Y is O or S; Z is N or CH and pharmaceutically acceptable salts thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
摘要翻译：本发明提供由通式Ⅰ表示的新型化合物，其中m为1〜3的整数，n为0或1〜4的整数，R选自CO 2 H，CO 2 R 6，CH 2 OH， CH 2 O 6 P（O）（OH）2和CONR 3 R 4; R 1和R 2独立地选自H，R 6，C 1 -C 6烯基，C 1 -C 6炔基，C 3 -C 7环烷基，C 4 -C 12烷基环烷基，C 6 -C 10芳基，C 7 -C 12烷基芳基和其杂原子取代的衍生物，其中所述基团中的一个或多个氢或碳原子被卤素，氮或含硫基团取代; R 3和R 4选自由H和R6组成的组; 和X选自H，R6，羟基，N（R6）2，CON（R6）2，SR6，磺氧基，砜，卤素，COOR6，NO2，CN和OR6，其中R6是C1-C6烷基; Y为O或S; Z是N或CH及其药学上可接受的盐。新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病，血小板聚集和血栓形成。

27. 发明授权

US07863319B2 Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚（烯）酸，2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US07863319B2
公开(公告)日：2011-01-04
申请号：US11623417
申请日：2007-01-16
申请人： Yariv Donde , Robert M. Burk , Michael E. Garst
发明人： Yariv Donde , Robert M. Burk , Michael E. Garst
IPC分类号： A61K31/381 , C07D333/28
CPC分类号： C07D333/28
摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
摘要翻译：公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。还公开了与其相关的药物制备的组合物和方法。

28. 发明授权

US07101906B2 2,3,4-substituted cyclopentanones as therapeutic agents 有权
标题翻译： 2,3,4-取代环戊酮作为治疗剂
公开(公告)号：US07101906B2
公开(公告)日：2006-09-05
申请号：US10991284
申请日：2004-11-16
申请人： Yariv Donde , Robert M. Burk , Michael E. Garst , Jeremiah H. Nguyen
发明人： Yariv Donde , Robert M. Burk , Michael E. Garst , Jeremiah H. Nguyen
IPC分类号： A61K31/881 , C07D333/56 , C07D333/62
CPC分类号： C07D333/62 , C07C405/0025 , C07D333/56
摘要： Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein a dashed line represents the presence or absence of a bond; Y is a carboxylic acid, sulfonic acid, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 0 to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2—CH═CH—(CH2)3—, or —CH2—C≡C—(CH2)3— wherein 1 or 2 carbons may be substituted with S or O; B is hydrogen, C1-6 hydrocarbyl, CN, CO2H, or —(CH2)mX(CH2)pH, wherein m is at least 1 and the sum of m and p is from 1 to 5; X is S or O; J is H, CH3, or CF3; D is a covalent bond, CH2, O, or S; and E is an aromatic heterobicyclic ring system which may have substituents comprising up to 6 non-hydrogen atoms each. Methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：本文公开了包含其药学上可接受的盐或其前药的化合物，其中虚线表示存在或不存在键; Y是羧酸，磺酸或膦酸官能团; 或其包含0至12个碳原子的酰胺或酯; 或Y是含有0至12个碳原子的羟甲基或其醚; 或Y为四唑基官能团; A是 - （CH 2 CH 2）6 - ，顺式-CH 2 -CH-CH-（CH 2 CH 2））3 - 或 - CH 2-C≡C-（CH 2）3 - 其中1或 2个碳可以被S或O取代; B是氢，C 1-6烃基，CN，CO 2 H或 - （CH 2 CH 2）m H 其中m至少为1，m和p之和为1至5; X是S或O; J是H，CH 3或CF 3; D是共价键，CH 2，O或S; 并且E是芳族杂双环系统，其可以具有各自包含多达6个非氢原子的取代基。还公开了与之相关的方法，组合物和药物。

29. 发明授权

US06716864B2 Interheteroaryl 7-oxabicyclic [2.2.1]heptane oxazoles as prostaglandin F2&agr; antagonists 有权
标题翻译：杂环芳基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2α拮抗剂
公开(公告)号：US06716864B2
公开(公告)日：2004-04-06
申请号：US10300492
申请日：2002-11-19
申请人： Robert M. Burk , Yariv Donde
发明人： Robert M. Burk , Yariv Donde
IPC分类号： A61K31422
CPC分类号： C07D493/08
摘要： The present invention provides novel compounds represented by the general formula I. wherein m, n, X, Y, Z, R, R1 and R2 are as defined in the specification or a pharmaceutically acceptable salt thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
摘要翻译：本发明提供由通式I表示的新化合物，其中m，n，X，Y，Z，R 1，R 1和R 2如本说明书中所定义或其药学上可接受的盐。新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病，血小板聚集和血栓形成。

30. 发明授权

US06509364B2 Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2&agr; antagonists 有权
标题翻译：亚麻基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2α拮抗剂
公开(公告)号：US06509364B2
公开(公告)日：2003-01-21
申请号：US10087547
申请日：2002-02-28
申请人： Robert M. Burk , Yariv Donde , Michael E. Garst
发明人： Robert M. Burk , Yariv Donde , Michael E. Garst
IPC分类号： C07D41310
CPC分类号： C07D493/08
摘要： The present invention provides novel compounds represented by the general formula I. and pharmaceutically acceptable salts thereof wherein m, n, X, R, R1 and R2 are as defined in the specification. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
摘要翻译：本发明提供由通式I表示的新化合物及其药学上可接受的盐，其中m，n，X，R 1，R 2和R 2如说明书中所定义。新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病，血小板聚集和血栓形成。

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