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1. 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。

2. 发明授权

US07612082B2 Prostaglandin EP4 antagonists 有权
标题翻译：前列腺素EP4拮抗剂
公开(公告)号：US07612082B2
公开(公告)日：2009-11-03
申请号：US10976442
申请日：2004-10-28
申请人： Larry A. Wheeler , Michael E. Garst , Yanbin Liang , David F. Woodward , Achim H.-P. Krauss , Robert M. Burk , Yariv Donde , Mark Holoboski , David W. Old , June Chen
发明人： Larry A. Wheeler , Michael E. Garst , Yanbin Liang , David F. Woodward , Achim H.-P. Krauss , Robert M. Burk , Yariv Donde , Mark Holoboski , David W. Old , June Chen
IPC分类号： A61K43/42
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：本文公开了与作为前列腺素EP4受体的拮抗剂或前列腺素EP4拮抗剂的化合物1或化合物2或其药学上可接受的盐或其前药相关的方法和组合物。

3. 发明授权

US06710072B2 &OHgr;-cycloalkyl 17-heteroaryl prostaglandin E2 analogs as EP2-receptor agonists 失效
标题翻译： ω-环烷基17-杂芳基前列腺素E2类似物作为EP2-受体激动剂
公开(公告)号：US06710072B2
公开(公告)日：2004-03-23
申请号：US10283629
申请日：2002-10-29
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： C07D33324
CPC分类号： C07D333/28 , A61K31/381 , A61K31/41 , A61K31/557 , C07D333/16 , C07F9/4018
摘要： The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
摘要翻译：本发明涉及E型前列腺素衍生物作为EP2激动剂的用途，一般而言，特别是作为眼睛低血压剂。根据本发明使用的PGE衍生物由下式I表示：其中阴影线段表示α键，实心三角形表示β键，波浪段表示α或β键，虚线表示双键或单键，X选自氢和卤素基团，R 3是杂芳基或取代的杂芳基，R 1和R 2独立地选自氢或低级具有至多6个碳原子的烷基或具有至多6个碳原子的低级酰基，R选自CO 2 R 4，CONR 4，CH 2 O 4，CONR 4 SO 2 R 4，P（O）（OR 4），R 4选自H，苯基和具有1至6个碳原子的低级烷基，n为0或1至 4。

4. 发明授权

US06538018B1 3, 7 or 3 and 7 thia or oxa prostanoic acid derivatives as agents for lowering intraocular pressure 有权
标题翻译： 3,7或3和7和硫代前列腺酸衍生物作为降低眼内压的药物
公开(公告)号：US06538018B1
公开(公告)日：2003-03-25
申请号：US10103301
申请日：2002-03-20
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： A61K31559
CPC分类号： A61K31/559 , A61K31/5575 , Y10S514/913
摘要： The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; where in A, B, D, X, Y, Z, R1, R3 and R4 are as defined in the specification.
摘要翻译：本发明提供一种治疗眼高血压或青光眼的方法，其包括向具有高眼压症或青光眼的动物施用治疗有效量的由通式I表示的化合物;其中在A，B，D，X，Y，Z， R1，R3和R4如说明书中所定义。

5. 发明授权

US09591935B2 Therapeutic substituted cyclopentanes 有权
标题翻译：治疗性取代环戊烷
公开(公告)号：US09591935B2
公开(公告)日：2017-03-14
申请号：US12667197
申请日：2008-06-30
申请人： David W. Old , Vinh X. Ngo , Mark Holoboski , Mari Posner
发明人： David W. Old , Vinh X. Ngo , Mark Holoboski , Mari Posner
IPC分类号： A61K31/38 , A61K31/381 , A61K31/41 , C07D333/10 , A47G19/06
CPC分类号： C07D409/08 , A47G19/06 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/5575 , A61K31/559 , C07C405/00 , C07C2601/08 , C07D257/04 , C07D277/56 , C07D333/10 , C07D333/40
摘要： Disclosed herein are compounds having the formula (I) wherein a dashed line represents the presence or absence of a bond; Y is an organic acid functional group, or an amide or ester thereof; or Y is hydroxymethyl or an ether thereof; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH═CH—(CH2)3—, or —CH2C═C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 —CH2— may be replaced by S or O, and 1 —CH2—CH2— may be replaced by —CH═CH— or —C≡C—; U1 and U2 are independently selected from —H, ═O, —OH, —F, —Cl, and —CN; and B is aryl or heteroaryl, for use as acular hypotensive agent.
摘要翻译：本文公开了具有式（I）的化合物，其中虚线表示键的存在或不存在; Y是有机酸官能团，或其酰胺或酯; 或Y为羟甲基或其醚; 或Y为四唑基官能团; A是 - （CH 2）6 - ，顺式-CH 2 CH = CH-（CH 2）3 - 或-CH 2C≡C-（CH 2）3 - ，其中1或2个碳原子可被S或O取代; 或A是 - （CH 2）m -Ar-（CH 2）o-，其中Ar是亚芳基或杂亚环烷基，m和o的总和是1,2,3或4，并且其中1 -CH 2可以被S 或O和1 -CH 2 -CH 2 - 可以被-CH = CH-或-C≡C-取代; U1和U2独立地选自-H，= O，-OH，-F，-Cl和-CN; 和B是芳基或杂芳基，用作眼压降低剂。

6. 发明申请

US20090239930A1 THERAPEUTIC COMPOUNDS 有权
标题翻译：治疗化合物
公开(公告)号：US20090239930A1
公开(公告)日：2009-09-24
申请号：US12405349
申请日：2009-03-17
申请人： Mark HOLOBOSKI , Robert M. BURK , Mari POSNER
发明人： Mark HOLOBOSKI , Robert M. BURK , Mari POSNER
IPC分类号： A61K31/381 , C07D333/24 , A61K31/277 , C07C255/46
CPC分类号： C07C255/46 , C07C405/00 , C07C2601/04 , C07C2601/08 , C07D295/088 , C07D333/24 , C07D333/28 , C07D333/38
摘要： Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, R1, R2, Z, and G are as described. Methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：公开了包含其药学上可接受的盐或其前药的化合物，其中Y，A，R 1，R 2，Z和G如上所述。还公开了与之相关的方法，组合物和药物。

7. 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。

8. 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。

9. 发明授权

US06376533B1 Omega-cycloalkyl 17-heteroaryl prostaglandin E2 analogs as EP2-receptor agonists 有权
标题翻译： ω-环烷基17-杂芳基前列腺素E2类似物作为EP2-受体激动剂
公开(公告)号：US06376533B1
公开(公告)日：2002-04-23
申请号：US09693722
申请日：2000-10-20
申请人： Robert M. Burk , Mark Holoboski , Mari F. Posner
发明人： Robert M. Burk , Mark Holoboski , Mari F. Posner
IPC分类号： A61K3138
CPC分类号： C07D333/22 , A61K31/38 , A61K31/41 , C07D333/16
摘要： The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
摘要翻译：本发明涉及E型前列腺素衍生物作为EP2激动剂的用途，一般而言，特别是作为眼睛低血压剂。根据本发明使用的PGE衍生物由下式I表示：其中阴影线段表示α键，实心三角形表示β键，波浪段表示α或β键，虚线表示双键或单键，R 3是杂芳基或取代的杂芳基，R 1和R 2独立地选自氢或具有至多6个碳原子的低级烷基或具有至多6个碳原子的低级酰基，R 选自CO 2 R 4，CONR 42，CH 2 OR 4，CONR 4 SO 2 R 4，P（O）（OR 4），其中R 4选自H，苯基和具有1至6个碳原子的低级烷基，n为0或从1到4的整数。

10. 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。

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