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1. 发明申请

WO2007008942A3 PHENYLAMINO-ACETIC ACID [1-(PYRIDIN-4-YL)-METHYLIDENE]-HYDRAZIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF G PROTEIN-COUPLED RECEPTOR KINASES FOR THE TREATMENT OF EYE DISEASES 审中-公开
标题翻译：作为用于治疗眼病的G蛋白偶联受体激动剂的调节剂的苯甲酸乙酸[1-（吡啶-4-基） - 甲基] - 乙酰衍生物和相关化合物
公开(公告)号：WO2007008942A3
公开(公告)日：2007-04-12
申请号：PCT/US2006026976
申请日：2006-07-11
申请人： AERIE PHARMACEUTICALS INC , DELONG MITCHELL A , SZNAIDMAN MARCOS L , OAKLEY ROBERT H , ECKHARDT ALLEN E , HUDSON CHRISTINE , YINGLING JEFFREY D , PEEL MICHAEL , RICHARDSON THOMAS E , MURRAY CLAIRE LOUISE , RAO BYAPPANAHALLY N NARASINGA , HEASLEY BRIAN H , PATEL PARESMA R
发明人： DELONG MITCHELL A , SZNAIDMAN MARCOS L , OAKLEY ROBERT H , ECKHARDT ALLEN E , HUDSON CHRISTINE , YINGLING JEFFREY D , PEEL MICHAEL , RICHARDSON THOMAS E , MURRAY CLAIRE LOUISE , RAO BYAPPANAHALLY N NARASINGA , HEASLEY BRIAN H , PATEL PARESMA R
IPC分类号： C07D213/61 , A61K31/341 , A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/47 , A61K31/513 , A61P27/02 , C07C251/86 , C07D213/36 , C07D215/42 , C07D233/88 , C07D239/54 , C07D307/52 , C07D333/36
CPC分类号： C07D401/12 , C07D213/53 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/42 , C07D233/64 , C07D239/52 , C07D239/54 , C07D307/14 , C07D307/52 , C07D333/22 , C07D401/14
摘要： Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X 1 , X 2 , X 3 and X 4 are, independently, CH, O, S or N-R 6 , with the proviso that at least one of X 2 or X 3 is O, S or N-R 6 ; and a heteroaryl group (ii): wherein X 5 and X 9 are CH or C-halogen, X 6 and X 8 are CH, and X 7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R 1 , R 2 , R 3 , R 4 , and R 5 are, independently, hydrogen; halogen; C 1 -C 4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C 1 -C 4 alkyl-heterocycle; -C(O)NH-C 1 -C 4 alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C 1 -C 4 alkyl; aryl, heteroaryl, C 1 -C 4 alkyl aryl or C 1 -C 4 alkyl heteroaryl; R 6 is H or C 1 -C 4 alkyl; R 7 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and X is N-R 6 .
摘要翻译：提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。还提供了使用化合物和/或组合物影响疾病状态或病症如癌症骨质疏松症和青光眼的各种方法。（式（I））。 A选自杂芳基（i）：其中X 1，X 2，X 3和X 4 >独立地是CH，O，S或NR 6，条件是X 2或X 3中的至少一个是O ，S或NR 6; 和杂芳基（ii）：其中X 5和X 9是CH或C-卤素，X 6和X 8 H是CH，X 7是N，并且其中六元杂芳基可以进一步与未取代的六元芳基稠合; R 1，R 2，R 3，R 4和R 5，独立地是氢; 卤素; C 1 -C 4烷基; 氨基; 硝基; 氰基; 杂; 羧基，羰基氨基; 氨基磺酰基; 磺酰; 氨; 硫代; 磺酰基; 酰基; 杂环; -要么; -O-C _{1 -C _{4 烷基 - 杂环; -C（O）NH-C _{1 -C _{4 烷基 - 杂环; -C（O）NH杂芳基; -C（O）NH-芳基; 或羧基氨基; 其中R是C 1 -C 4烷基; 芳基，杂芳基，C 1 -C 4烷基芳基或C 1 -C 4烷基杂芳基; R 6是H或C 1 -C 4烷基; R 7是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 烷氧基; X为N-R 6。}}}}

2. 发明申请

WO2007008942A2 HYDRAZIDE COMPOUNDS 审中-公开
标题翻译：氢化物化合物
公开(公告)号：WO2007008942A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026976
申请日：2006-07-11
申请人： AERIE PHARMACEUTICALS, INC. , DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally, N. Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
发明人： DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally, N. Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
CPC分类号： C07D401/12 , C07D213/53 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/42 , C07D233/64 , C07D239/52 , C07D239/54 , C07D307/14 , C07D307/52 , C07D333/22 , C07D401/14
摘要： Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
摘要翻译：提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。

3. 发明申请

WO2005074654A2 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 审中-公开
标题翻译：制备1,3-二氧戊环核苷的方法
公开(公告)号：WO2005074654A2
公开(公告)日：2005-08-18
申请号：PCT/US2005003620
申请日：2005-02-03
申请人： UNIV EMORY , SZNAIDMAN MARCOS , PAINTER GEORGE R , ALMOND MERRICK R , CLEARY DARRYL G , PESYAN AMIR
发明人： SZNAIDMAN MARCOS , PAINTER GEORGE R , ALMOND MERRICK R , CLEARY DARRYL G , PESYAN AMIR
IPC分类号： C07D239/47 , C07D239/54 , C07D405/04 , C07D473/16
CPC分类号： C07D473/16 , C07D317/34 , C07D405/04
摘要： This aplication provides a process for preparing enantiomerically pure beta-D-dioxolane nucleosides. In particular, a new synthesis of (-)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure beta-D or beta-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D-or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifiying the nucleoside to obtain a substantially pure protected beta-D or beta-L-1,3-dioxolane nucleoside.
摘要翻译：该应用提供了制备对映体纯的β-D-二氧戊环核苷的方法。具体来说，描述了适用于大规模开发的（ - ） - DAPD的新合成。在一个实施方案中，本发明提供了制备基本上纯的β-D或β-L-1,3-二氧戊环核苷的方法，其包括a）制备或获得酯化的2,2-二烷氧基乙醇; b）用乙醇酸环化酯化的2,2-二烷氧基乙醇以获得1,3-二氧戊环内酯; c）分解1,3-二氧戊环内酯以获得基本上纯的D-或L-内酯; d）选择性还原和活化D-或L-手性内酯以获得基本上纯的D-或L-1,3-二氧戊环; e）将D-或L-1,3-二氧戊环偶联到活化和/或保护的嘌呤或嘧啶碱基上; 和f）任选纯化核苷以获得基本上纯的受保护的β-D或β-L-1,3-二氧戊环核苷。

5. 发明申请

WO2007008926A1 ISOQUINOLINE COMPOUNDS 审中-公开
标题翻译：异喹啉化合物
公开(公告)号：WO2007008926A1
公开(公告)日：2007-01-18
申请号：PCT/US2006/026947
申请日：2006-07-11
申请人： AERIE PHARMACEUTICALS, INC. , DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally N., Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
发明人： DELONG, Mitchell, A. , SZNAIDMAN, Marcos, L. , OAKLEY, Robert, H. , ECKHARDT, Allen, E. , HUDSON, Christine , YINGLING, Jeffrey, D. , PEEL, Michael , RICHARDSON, Thomas, E. , MURRAY, Claire, Louise , RAO, Byappanahally N., Narasinga , HEASLEY, Brian, H. , PATEL, Paresma, R.
IPC分类号： C07D217/02 , A61K31/472 , A61P27/06
CPC分类号： C07D217/02
摘要： Isoquinoline compounds are provided that influence, inhibit or reduce the action of a G-protein receptor kinase . Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
摘要翻译：提供了影响，抑制或降低G蛋白受体激酶作用的异喹啉化合物。还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。

6. 发明申请

WO2005074654A3 METHODS TO MANUFACTURE 1,3-DIOXOLANE NUCLEOSIDES 审中-公开
公开(公告)号：WO2005074654A3
公开(公告)日：2005-08-18
申请号：PCT/US2005/003620
申请日：2005-02-03
申请人： EMORY UNIVERSITY , SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
发明人： SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
IPC分类号： C07D239/47
摘要： This aplication provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (-)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D-or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifiying the nucleoside to obtain a substantially pure protected β-D or β-L-1,3-dioxolane nucleoside.

7. 发明申请

WO2004050613A2 2-SUBSTITUTED-3-PROPENAMIDE DERIVATIVES AND METHODS OF USING THE SAME 审中-公开
标题翻译： 2-取代-3-丙烯酰胺衍生物及其使用方法
公开(公告)号：WO2004050613A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/038233
申请日：2003-12-02
申请人： TRIANGLE PHARMACEUTICALS, INC. , SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
发明人： SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
IPC分类号： C07D
CPC分类号： C07D207/325 , C07C235/38 , C07C237/22 , C07D203/18 , C07D205/04 , C07D207/20 , C07D207/24 , C07D207/33 , C07D211/18 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/26 , C07D213/40 , C07D213/75 , C07D213/82 , C07D231/40 , C07D233/06 , C07D233/64 , C07D239/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D239/52 , C07D241/20 , C07D251/22 , C07D253/07 , C07D261/14 , C07D263/12 , C07D277/04 , C07D277/22 , C07D277/46 , C07D277/58 , C07D285/135 , C07D295/185 , C07D295/205 , C07D307/10 , C07D307/14 , C07D307/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/79 , C07D309/04 , C07D309/20 , C07D317/46 , C07D317/52 , C07D317/62 , C07D317/64 , C07D319/18 , C07D333/12 , C07D333/20 , C07D333/36 , C07D333/44 , C07D401/12 , C07D405/12 , C07D417/12 , C07D491/10
摘要： This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
摘要翻译：本发明提供2-取代的丙烯酰胺衍生物及其用于治疗乙型肝炎病毒和/或丙型肝炎病毒的组合物。

8. 发明申请

WO2002079213A1 PROCESS FOR THE PREPARATION OF 2'-HALO-$G(B)-L-ARABINOFURANOSYL NUCLEOSIDES 审中-公开
标题翻译：制备2'-HALO-DOLLAR G（B）-L-阿拉伯呋喃糖基核苷酸的方法
公开(公告)号：WO2002079213A1
公开(公告)日：2002-10-10
申请号：PCT/US2002/009848
申请日：2002-03-29
申请人： TRIANGLE PHARMACEUTICALS, INC. , SZNAIDMAN, Marcos
发明人： SZNAIDMAN, Marcos
IPC分类号： C07H15/04
CPC分类号： C07H15/04 , C07H19/06
摘要： The present invention is directed to the process for the preparation of 2'-deoxy-2'-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2'-deoxy-2'-fluoro-β-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.
摘要翻译：本发明涉及制备2'-脱氧-2'-卤代-β-阿拉伯呋喃糖基核苷的方法，特别是2'-脱氧-2'-氟-β-L-阿拉伯呋喃糖基胸腺嘧啶 L-FMAU），来自L-阿拉伯糖，其可商购并且比L-核糖或L-木糖便宜，分为十个步骤。所有的试剂和原料都是廉价的，不需要特殊的设备来进行反应。

9. 发明申请

WO2002059098A1 THIAZOLE AND OXAZOLE DERIVATIVES AS ACTIVATORS OF HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTORS 审中-公开
标题翻译：作为人类过氧化物酶促反应物激活受体的激活剂的噻唑和氧唑衍生物
公开(公告)号：WO2002059098A1
公开(公告)日：2002-08-01
申请号：PCT/US2001/051056
申请日：2001-12-19
申请人： GLAXO GROUP LIMITED , BANKER, Pierette , CADILLA, Rodolfo , LAMBERT, Millard, Hurst, III , RAFFERTY, Stephen, William , STERNBACH, Daniel, David , SZNAIDMAN, Marcos, Luis
发明人： BANKER, Pierette , CADILLA, Rodolfo , LAMBERT, Millard, Hurst, III , RAFFERTY, Stephen, William , STERNBACH, Daniel, David , SZNAIDMAN, Marcos, Luis
IPC分类号： C07D277/24
CPC分类号： C07D417/06 , C07D263/32 , C07D277/24 , C07D277/26 , C07D277/28 , C07D417/10 , C07D417/12
摘要： The present invention provides a compound of formula (I) wherein R 1 -R 5 , R 25 , R 26 , Y and X 2 are defined as in claim 1. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and are useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 5，R 26，Y和X 2定义如权利要求1中所述。化合物活化人过氧化物酶体增殖激活受体（hPPAR），并且可用于治疗相关疾病如心血管疾病和高胆固醇血症。

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