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1. 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。

2. 发明授权

US09006464B2 Substituted cyclopentanes having prostaglandin activity 有权
标题翻译：具有前列腺素活性的取代的环戊烷
公开(公告)号：US09006464B2
公开(公告)日：2015-04-14
申请号：US12265062
申请日：2008-11-05
申请人： Yariv Donde , Jeremiah H. Nguyen , Robert M. Burk
发明人： Yariv Donde , Jeremiah H. Nguyen , Robert M. Burk
IPC分类号： C07D333/40 , A61K31/381 , C07D263/34
CPC分类号： C07D333/40 , C07D263/34
摘要： Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
摘要翻译：本文公开了具有下式的化合物：还公开了治疗方法，药物和与其有关的组合物。

3. 发明申请

US20090239869A1 THERAPEUTIC SUBSTITUTED CYCLOPENTANES 有权
标题翻译：治疗性替代性CYCLOPENTANES
公开(公告)号：US20090239869A1
公开(公告)日：2009-09-24
申请号：US12404753
申请日：2009-03-16
申请人： Yariv Donde , Robert M. Burk , Jeremiah H. Nguyen
发明人： Yariv Donde , Robert M. Burk , Jeremiah H. Nguyen
IPC分类号： A61K31/5375 , A61K31/216 , A61K31/192 , C07D295/192 , C07C69/732 , C07C59/54
CPC分类号： C07C405/00 , C07C2601/08 , C07D295/08 , C07D333/38
摘要： Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness.
摘要翻译：本文公开了治疗性化合物。还公开了与之相关的方法，组合物和药物。本文所述的化合物用于治疗眼部病症，肠病和秃发。

4. 发明授权

US07732443B2 Therapeutic substituted cyclopentanes 有权
标题翻译：治疗性取代环戊烷
公开(公告)号：US07732443B2
公开(公告)日：2010-06-08
申请号：US12404753
申请日：2009-03-16
申请人： Yariv Donde , Robert M. Burk , Jeremiah H. Nguyen
发明人： Yariv Donde , Robert M. Burk , Jeremiah H. Nguyen
IPC分类号： A61K31/216 , A61K31/5377 , C07D265/30 , C07C57/26
CPC分类号： C07C405/00 , C07C2601/08 , C07D295/08 , C07D333/38
摘要： Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness.
摘要翻译：本文公开了治疗性化合物。还公开了与之相关的方法，组合物和药物。本文所述的化合物用于治疗眼部病症，肠病和秃发。

5. 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。

6. 发明申请

US20090275646A1 THERAPEUTIC COMPOUNDS 有权
标题翻译：治疗化合物
公开(公告)号：US20090275646A1
公开(公告)日：2009-11-05
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： A61K31/381 , C07C69/732 , A61K31/216 , C07D333/38 , A61P17/14
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。

7. 发明授权

US07906552B2 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：US07906552B2
公开(公告)日：2011-03-15
申请号：US10916243
申请日：2004-08-10
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： A61K31/38 , A61K31/5575 , C07D333/24 , C07C405/00
CPC分类号： C07C405/00 , 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。

8. 发明授权

US07183324B2 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：US07183324B2
公开(公告)日：2007-02-27
申请号：US10997039
申请日：2004-11-23
申请人： Yariv Donde , Mark Holoboski , Mari F. Posner , Robert M. Burk , Michael E. Garst
发明人： Yariv Donde , Mark Holoboski , Mari F. Posner , Robert M. Burk , Michael E. Garst
IPC分类号： A61K31/095 , A61K31/38 , C07C331/00 , C07D333/56
CPC分类号： C07D333/62 , C07C323/52 , C07C405/0033 , C07C2601/08 , C07D333/56
摘要： Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, B, J, and E are further described. 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; 其中进一步描述Y，A，B，J和E。还公开了与之相关的方法，组合物和药物。

9. 发明授权

US06407250B1 Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2a antagonists 有权
标题翻译： 2-亚麻基7-氧杂双环[2.2.1]庚烷恶唑作为前列腺素F2a拮抗剂
公开(公告)号：US06407250B1
公开(公告)日：2002-06-18
申请号：US09661771
申请日：2000-09-14
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： C07D41304
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 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 R6, hydroxy, N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl, 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， CH2O R6和CONR3R4; R1和R2独立地选自H，R6，C1-C6烯基，C1-C6炔基，C3-C7环烷基，C4-C12烷基环烷基，C6-C10芳基，C7-C12烷基芳基基团和杂原子取代的衍生物，其中所述基团中的一个或多个氢原子或碳原子被卤素，氮或含硫基团取代; R 3和R 4选自H和R 6; 和X选自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，其可接受的盐。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。

10. 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。

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