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1. 发明申请

WO2007081835A3 MODULATORS OF HYPOXIA INDUCIBLE FACTOR-1 AND RELATED USES 审中-公开
标题翻译： HYPOXIA诱导因子-1的调节剂及相关用途
公开(公告)号：WO2007081835A3
公开(公告)日：2008-08-14
申请号：PCT/US2007000340
申请日：2007-01-09
申请人： BTG INT LTD , KHODADOUST MEHRAN , HESS HANS-JURGEN , HUSSON SAJJAT , BRUENING REIMAR C , GARDINER GREGORY E
发明人： KHODADOUST MEHRAN , HESS HANS-JURGEN , HUSSON SAJJAT , BRUENING REIMAR C , GARDINER GREGORY E
IPC分类号： C07J19/00 , A61K31/585 , A61P35/00 , C07J41/00 , C07J43/00
CPC分类号： C07J19/00 , C07J19/005 , C07J41/0005 , C07J41/0038 , C07J43/003
摘要： The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
摘要翻译：本发明具有式I或II化合物及其药学上可接受的盐和前药，以及使用该化合物调节局部和全身缺氧事件的作用的方法。

2. 发明申请

WO2004009552A1 PHOSPHODIESTERASE 4 INHIBITORS, INCLUDING N-SUBSTITUTED ANILINE AND DIPHENYLAMINE ANALOGS 审中-公开
标题翻译：磷酸二酯酶4抑制剂，包括N-取代的苯胺和二苯胺类似物
公开(公告)号：WO2004009552A1
公开(公告)日：2004-01-29
申请号：PCT/US2003/022543
申请日：2003-07-21
申请人： MEMORY PHARMACEUTICALS CORPORATION , SCHUMACHER, Richard, A. , HOPPER, Allen, T. , TEHIM, Ashok , HESS, Hans-Jurgen, Ernst , UNTERBECK, Axel , KUESTER, Erik , BRUBAKER, William, Frederick, Jr. , DUNN, Robert, F.
发明人： SCHUMACHER, Richard, A. , HOPPER, Allen, T. , TEHIM, Ashok , HESS, Hans-Jurgen, Ernst , UNTERBECK, Axel , KUESTER, Erik , BRUBAKER, William, Frederick, Jr. , DUNN, Robert, F.
IPC分类号： C07D213/38
CPC分类号： C07D241/12 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/92 , C07C229/60 , C07C2601/08 , C07C2601/14 , C07D213/38 , C07D213/61 , C07D213/68 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/80 , C07D215/12 , C07D215/14 , C07D215/38 , C07D217/22 , C07D239/42 , C07D241/20 , C07D261/08 , C07D261/14 , C07D277/28 , C07D295/13 , C07D307/14 , C07D307/20 , C07D317/58 , C07D333/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula (I): wherein R 1 , R 2 R 3 and R 4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4的抑制。本发明的化合物具有式（I）：其中R 1，R 2 R 3和R 4如本文所定义。

3. 发明申请

WO2007081835A2 MODULATORS OF HYPOXIA INDUCIBLE FACTOR-1 AND RELATED USES 审中-公开
标题翻译： HYPOXIA诱导因子-1的调节剂及相关用途
公开(公告)号：WO2007081835A2
公开(公告)日：2007-07-19
申请号：PCT/US2007/000340
申请日：2007-01-09
申请人： BIONAUT PHARMACEUTICALS, INC. , KHODADOUST, Mehran , HESS, Hans-jurgen , HUSSON, Sajjat , BRUENING, Reimar, C. , GARDINER, Gregory, E.
发明人： KHODADOUST, Mehran , HESS, Hans-jurgen , HUSSON, Sajjat , BRUENING, Reimar, C. , GARDINER, Gregory, E.
CPC分类号： C07J19/00 , C07J19/005 , C07J41/0005 , C07J41/0038 , C07J43/003
摘要： The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
摘要翻译：本发明具有式I或II化合物及其药学上可接受的盐和前药，以及使用该化合物调节局部和全身缺氧事件的作用的方法。

4. 发明申请

WO2006074192A2 TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：治疗炎症性疾病
公开(公告)号：WO2006074192A2
公开(公告)日：2006-07-13
申请号：PCT/US2006000132
申请日：2006-01-03
申请人： BIONAUT PHARMACEUTICALS INC , AN WENQIAN FRANK , PARK JUN YOUNG , KHODADOUST MEHRAN , HESS HANS-JURGEN , HUSSOIN MD SAJJAT
发明人： AN WENQIAN FRANK , PARK JUN YOUNG , KHODADOUST MEHRAN , HESS HANS-JURGEN , HUSSOIN MD SAJJAT
CPC分类号： A61K31/203 , A61K31/05 , A61K31/09 , A61K31/165 , A61K31/19 , A61K31/343 , A61K31/365 , A61K31/366 , A61K31/37 , A61K31/415 , A61K31/428 , A61K31/498 , A61K31/517 , A61K31/56 , A61K31/57 , C07F9/12
摘要： Methods of treating an inflammatory disorder include administering an effective amount of a compound represented by Structural Formula (I). Ring A is optionally substituted, contains zero, one, two, or three double bonds, and is optionally fused to an aliphatic, aryl or heteroaryl ring; X is an optionally substituted 1 to 3 carbon aliphatic chain that is optionally fused to a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring, wherein one or two carbons in X are optionally replaced with -O-, -S-, or -NR e -; Y is carbon or nitrogen; R 1 and R 2 are independently -H, -OH, -CN, -NO 2 , -NR f R g , halogen, optionally substituted alkyl, or optionally substituted alkoxy; or R 1 and R 2 together link the carbons to which they are bonded with a bond, -O-, -S-, or -NR h -; R 3 and R 4 are independently -H, -OH, -CN, -NO 2 , -NR i R j , halogen, optionally substituted alkyl, or optionally substituted alkoxy, or R 4 is =0; or R 3 and R 4 , taken together with the atoms to which they are bonded, form a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring that is optionally fused to a monocyclic or bicyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring; R e -R j are independently -H or optionally substituted alkyl; and each of the OSM signaling inhibitor compounds has at least one hydrogen atom bonded to an oxygen, nitrogen, or sulfur atom. The OSM signaling inhibitor compounds also include pharmaceutically acceptable salt or solvates of the compounds represented by Structural Formula (I).
摘要翻译：治疗炎性病症的方法包括施用有效量的结构式（I）表示的化合物。环A任选被取代，含有0,1,2或3个双键，并且任选地与脂族，芳基或杂芳基环稠合; X是任选被1至3个碳的脂族链，其任选地与单环，任选取代的脂族，杂环，芳基或杂芳基环稠合，其中X中的一个或两个碳任选被-O-，-S- ，或-NR e - Y是碳或氮; R 1和R 2独立地是-H，-OH，-CN，-NO 2，-NR f，卤素，任选取代的烷基或任选取代的烷氧基; 或R 1和R 2 2一起连接与它们键合的碳键，-O-，-S-或-NR“ SUP> - ; R 3和R 4独立地是-H，-OH，-CN，-NO 2，-NR O，卤素，任选取代的烷基或任选取代的烷氧基，或R 4是= O; 或R 3和R 4与它们所键合的原子一起形成单环，任选取代的脂族，杂环，芳基或杂芳基环，其是任选地与单环或双环，任选取代的脂族，杂环，芳基或杂芳基环稠合; R e独立地是-H或任选取代的烷基; 并且每个OSM信号传导抑制剂化合物具有至少一个与氧，氮或硫原子键合的氢原子。 OSM信号传导抑制剂化合物还包括由结构式（I）表示的化合物的药学上可接受的盐或溶剂合物。

5. 发明申请

WO2007103260A1 PHOSPHODIESTERASE 10 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶10抑制剂
公开(公告)号：WO2007103260A1
公开(公告)日：2007-09-13
申请号：PCT/US2007/005511
申请日：2007-03-01
申请人： AMGEN INC. , MEMORY PHARMACEUTICALS CORPORATION , ARRINGTON, Mark, P. , HOPPER, Allen, T. , CONTICELLO, Richard, D. , NGUYEN, Truc, M. , HESS, Hans-jurgen , GAUSS, Carla , HITCHCOCK, Stephen, A.
发明人： ARRINGTON, Mark, P. , HOPPER, Allen, T. , CONTICELLO, Richard, D. , NGUYEN, Truc, M. , HESS, Hans-jurgen , GAUSS, Carla , HITCHCOCK, Stephen, A.
IPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , A61K31/502 , A61K31/517 , A61P25/18
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D471/04
摘要： The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：本发明如果针对某些作为PDE10抑制剂的噌啉化合物，含有这些化合物的药物组合物和制备这些化合物的方法。本发明还涉及治疗由PDE10酶介导的疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。

6. 发明申请

WO2004014913A3 DERIVATIVES OF 2-TRIFLUORMETHYL-6-AMINOPURINE AS PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译： 2-三氟甲基-6-氨基嘌呤作为磷酸二酯酶4抑制剂的衍生物
公开(公告)号：WO2004014913A3
公开(公告)日：2004-07-29
申请号：PCT/US0324914
申请日：2003-08-08
申请人： MEMORY PHARM CORP , LIU RUIPING , HOPPER ALLEN T , TEHIM ASHOK , HESS HANS-JURGEN E , RONG YAJING
发明人： LIU RUIPING , HOPPER ALLEN T , TEHIM ASHOK , HESS HANS-JURGEN E , RONG YAJING
IPC分类号： A61K31/52 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/36 , A61P29/00 , A61P31/18 , A61P37/00 , A61P43/00 , C07D473/34 , C07D473/40
CPC分类号： C07D473/34 , C07D473/14
摘要： PDE4 inhibition is achieved by novel compounds of the Formula (I) wherein R and R are as defined herein.
摘要翻译：通过式（I）的新化合物（其中R 1和R 2如本文所定义）实现PDE4抑制。

7. 发明申请

WO2008093086A1 MODULATORS OF HYPOXIA INDUCIBLE FACTOR-1 AND RELATED USES 审中-公开
标题翻译： HYPOXIA诱导因子-1的调节剂及相关用途
公开(公告)号：WO2008093086A1
公开(公告)日：2008-08-07
申请号：PCT/GB2008/000320
申请日：2008-01-31
申请人： BTG INTERNATIONAL LIMITED , HESS, Hans-Jurgen , HUSSOIN, Sajjat , SCHWARZ, Oliver
发明人： HESS, Hans-Jurgen , HUSSOIN, Sajjat , SCHWARZ, Oliver
IPC分类号： C07J41/00 , C07J43/00 , A61K31/58 , A61P35/00
CPC分类号： C07J41/0016 , C07J43/003
摘要： The invention features compounds of formula (I): and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
摘要翻译：本发明的特征在于式（I）化合物及其药学上可接受的盐和前药，以及使用该化合物调节局部和全身缺氧事件的作用的方法。

8. 发明申请

WO2003032981A1 4-(4-ALKOXY-3-HYDROXYPHENYL)-2-PYRROLIDONE DERIVATIVES AS PDE-4 INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL SYNDROMES 审中-公开
标题翻译： 4-4-烷氧基-3-羟基苯基-2-吡咯烷酮衍生物作为PDE-4抑制剂治疗神经综合征
公开(公告)号：WO2003032981A1
公开(公告)日：2003-04-24
申请号：PCT/US2002/032834
申请日：2002-10-16
申请人： MEMORY PHARMACEUTICALS CORPORATION , LIU, Ruiping , DE VIVO, Michael , HESS, Hans-Jurgen, Ernst , HOPPER, Allen , KEUSTER, Erik , TEHIM, Ashok
发明人： LIU, Ruiping , DE VIVO, Michael , HESS, Hans-Jurgen, Ernst , HOPPER, Allen , KEUSTER, Erik , TEHIM, Ashok
IPC分类号： A61K31/4015
CPC分类号： C07D207/26 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula (I), wherein R 1 , R 2 and R 3 are as defined herein.
摘要翻译：选择性PDE4抑制由4-（取代的 - 苯基）-2-吡咯烷酮化合物实现。与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且在抑制其它类型的PDE方面表现出选择性。本发明的化合物具有式（I），其中R 1，R 2，R 3和R 3 - 3如本文所定义。

9. 发明申请

WO1996014845A1 NK-1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF EYE DISORDERS 审中-公开
标题翻译： NK-1受体拮抗剂治疗眼病
公开(公告)号：WO1996014845A1
公开(公告)日：1996-05-23
申请号：PCT/IB1995000811
申请日：1995-09-29
申请人： PFIZER INC. , HESS, Hans-Jurgen, Ernst
发明人： PFIZER INC.
IPC分类号： A61K31/445
CPC分类号： A61K31/439 , A61K31/137 , A61K31/40 , A61K31/438 , A61K31/451 , A61K31/4535 , A61K31/454 , A61K31/55 , A61K31/675
摘要： The present invention relates to a method of treating or preventing a disorder of the eye selected from glaucoma, ocular hypertension, miosis, excess lacrimation, hyperemia and breakdown of the blood aqueous barrier in mammals, including humans, using an NK-1 antagonist. It also relates to a method of treating or preventing such disorders in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds that are substance P receptor antagonists.
摘要翻译：本发明涉及一种使用NK-1拮抗剂治疗或预防选自青光眼，眼高血压，瞳孔缩小，过度流泪，充血以及哺乳动物（包括人）中的血液水屏障的分解的眼睛病症的方法。它还涉及使用作为P受体拮抗剂的某些奎宁环衍生物，哌啶衍生物，吡咯烷衍生物，氮杂降冰片烷衍生物，乙二胺衍生物和相关化合物来治疗或预防哺乳动物包括人类的这种疾病的方法。

10. 发明申请

WO2006074192A3 TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
公开(公告)号：WO2006074192A3
公开(公告)日：2006-07-13
申请号：PCT/US2006/000132
申请日：2006-01-03
申请人： BIONAUT PHARMACEUTICALS, INC. , AN, Wenqian, Frank , PARK, Jun, Young , KHODADOUST, Mehran , HESS, Hans-Jurgen , HUSSOIN, Md., Sajjat
发明人： AN, Wenqian, Frank , PARK, Jun, Young , KHODADOUST, Mehran , HESS, Hans-Jurgen , HUSSOIN, Md., Sajjat
IPC分类号： A61K31/09 , A61K31/415 , A61K31/19 , A61K31/365 , A61K31/343 , A61K31/165 , A61K31/56 , A61K31/498 , A61K31/05 , A61K31/37 , A61P29/00 , A61P19/02
摘要： Methods of treating an inflammatory disorder include administering an effective amount of a compound represented by Structural Formula (I). Ring A is optionally substituted, contains zero, one, two, or three double bonds, and is optionally fused to an aliphatic, aryl or heteroaryl ring; X is an optionally substituted 1 to 3 carbon aliphatic chain that is optionally fused to a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring, wherein one or two carbons in X are optionally replaced with -O-, -S-, or -NR e -; Y is carbon or nitrogen; R 1 and R 2 are independently -H, -OH, -CN, -NO 2 , -NR f R g , halogen, optionally substituted alkyl, or optionally substituted alkoxy; or R 1 and R 2 together link the carbons to which they are bonded with a bond, -O-, -S-, or -NR h -; R 3 and R 4 are independently -H, -OH, -CN, -NO 2 , -NR i R j , halogen, optionally substituted alkyl, or optionally substituted alkoxy, or R 4 is =0; or R 3 and R 4 , taken together with the atoms to which they are bonded, form a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring that is optionally fused to a monocyclic or bicyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring; R e -R j are independently -H or optionally substituted alkyl; and each of the OSM signaling inhibitor compounds has at least one hydrogen atom bonded to an oxygen, nitrogen, or sulfur atom. The OSM signaling inhibitor compounds also include pharmaceutically acceptable salt or solvates of the compounds represented by Structural Formula (I).

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