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1. 发明申请

US20060094742A1 Prostaglandin EP4 antagonists 有权
标题翻译：前列腺素EP4拮抗剂
公开(公告)号：US20060094742A1
公开(公告)日：2006-05-04
申请号：US10976442
申请日：2004-10-28
申请人： Larry Wheeler , Michael Garst , Yanbin Liang , David Woodward , Achim Krauss , Robert Burk , Yariv Donde , Mark Holoboski , David Old , June Chen
发明人： Larry Wheeler , Michael Garst , Yanbin Liang , David Woodward , Achim Krauss , Robert Burk , Yariv Donde , Mark Holoboski , David Old , June Chen
IPC分类号： A61K31/473
CPC分类号： A61K31/473 , Y10S514/913
摘要： Disclosed herein are methods and compositions related to compound 1 or compound 2 or pharmaceutically acceptable salts, or prodrugs thereof, which are antagonists of a prostaglandin EP4 receptor, or are prostaglandin EP4 antagonists.
摘要翻译：本文公开的是与作为前列腺素EP4受体的拮抗剂的化合物1或化合物2或其药学上可接受的盐或前药相关的方法和组合物，或者是前列腺素EP 4 >拮抗剂。

2. 发明申请

US20060111430A1 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：US20060111430A1
公开(公告)日：2006-05-25
申请号：US10997039
申请日：2004-11-23
申请人： Yariv Donde , Mark Holoboski , Mari Posner , Robert Burk , Michael Garst
发明人： Yariv Donde , Mark Holoboski , Mari Posner , Robert Burk , Michael Garst
IPC分类号： A61K31/558 , A61K31/557 , C07D333/72 , C07C317/24
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。

3. 发明申请

US20060106088A1 2,3,4-Substituted cyclopentanones as therapeutic agents 有权
标题翻译： 2,3,4-取代的环戊酮作为治疗剂
公开(公告)号：US20060106088A1
公开(公告)日：2006-05-18
申请号：US10991284
申请日：2004-11-16
申请人： Yariv Donde , Robert Burk , Michael Garst , Jeremiah Nguyen
发明人： Yariv Donde , Robert Burk , Michael Garst , Jeremiah Nguyen
IPC分类号： A61K31/381 , C07D333/52
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。

4. 发明申请

US20060035960A1 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：US20060035960A1
公开(公告)日：2006-02-16
申请号：US10915933
申请日：2004-08-10
申请人： Yariv Donde , Robert Burk , Michael Garst
发明人： Yariv Donde , Robert Burk , Michael Garst
IPC分类号： A61K31/558 , C07D333/24
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。

5. 发明申请

US20070112051A1 CYCLOPENTANE HEPTAN(ENE)OIC ACID, 2-HETEROARYLALKENYL DERIVATIVES AS THERAPEUTIC AGENTS 有权
标题翻译：环丙沙星（ENE）OIC酸，作为治疗剂的2-异亮氨酸衍生物
公开(公告)号：US20070112051A1
公开(公告)日：2007-05-17
申请号：US11623417
申请日：2007-01-16
申请人： Yariv Donde , Robert Burk , Michael Garst
发明人： Yariv Donde , Robert Burk , Michael Garst
IPC分类号： A61K31/558
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。

6. 发明申请

US20060035961A1 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：US20060035961A1
公开(公告)日：2006-02-16
申请号：US10915987
申请日：2004-08-10
申请人： Yariv Donde , Robert Burk , Michael Garst
发明人： Yariv Donde , Robert Burk , Michael Garst
IPC分类号： A61K31/558 , C07D333/22 , C07D333/24
CPC分类号： C07D333/16 , C07D333/28
摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein A, B, R1, R2, D, and E are defined herein. Use of the diseases for the treatment of diseases, and compositions and medicaments related thereto are also disclosed.
摘要翻译：其中A，B，R 1，R 2，D和E的化合物包括其药学上可接受的盐或前体药物，其定义如下。还公开了用于治疗疾病的疾病的使用，以及与其相关的组合物和药物。

7. 发明申请

US20060035949A1 Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
公开(公告)号：US20060035949A1
公开(公告)日：2006-02-16
申请号：US10916243
申请日：2004-08-10
申请人： Yariv Donde , Robert Burk , Michael Garst
发明人： Yariv Donde , Robert Burk , Michael Garst
IPC分类号： A61K31/557 , C07C61/06
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.

8. 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。

9. 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.

10. 发明申请

US20080091028A1 IMIDAZOLE-2-THIONES 有权
标题翻译：咪唑-2 -THIONES
公开(公告)号：US20080091028A1
公开(公告)日：2008-04-17
申请号：US11873537
申请日：2007-10-17
申请人： Ken Chow , Todd Heidelbaugh , Daniel Gil , Michael Garst , Larry Wheeler
发明人： Ken Chow , Todd Heidelbaugh , Daniel Gil , Michael Garst , Larry Wheeler
IPC分类号： C07D215/12 , C07D215/02 , C07D215/22 , C07D233/06 , C07D233/30
CPC分类号： C07D233/84 , C07D233/70 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
摘要翻译：式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先选择于α2B2和/或α2C2肾上腺素能受体 2A肾上腺素能受体，因此没有或仅有最小的血管内和/或镇静作用。式1的这些化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

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