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1. 发明申请

WO2003015785A1 2H-PHTHALAZIN-1-ONES AND METHODS FOR USE THEREOF 审中-公开
标题翻译： 2H-PHTHALAZIN-1-ONES及其使用方法
公开(公告)号：WO2003015785A1
公开(公告)日：2003-02-27
申请号：PCT/US2002/026271
申请日：2002-08-15
申请人： ICOS CORPORATION , BEATON, Graham , MOREE, Wilna, J. , RUETER, Jaimie, K. , DAHL, Russell, S. , MCELLIGOTT, David, L. , GOLDMAN, Phyllis , DEMAGGIO, Anthony, J. , CHRISTENSON, Erik , HERENDEEN, Dan , FOWLER, Kerry, W. , HUANG, Danwen , BERTINO, Jaimie, A. , BOURDON, Lisa, H. , FAIRFAX, David, J. , JIANG, QIN , REISCH, Helge, A. , SONG, Ren, Hua , ZHICHKIN, Pavel, E.
发明人： BEATON, Graham , MOREE, Wilna, J. , RUETER, Jaimie, K. , DAHL, Russell, S. , MCELLIGOTT, David, L. , GOLDMAN, Phyllis , DEMAGGIO, Anthony, J. , CHRISTENSON, Erik , HERENDEEN, Dan , FOWLER, Kerry, W. , HUANG, Danwen , BERTINO, Jaimie, A. , BOURDON, Lisa, H. , FAIRFAX, David, J. , JIANG, QIN , REISCH, Helge, A. , SONG, Ren, Hua , ZHICHKIN, Pavel, E.
IPC分类号： A61K31/502
CPC分类号： C07D401/12 , A61K41/0038 , A61K49/001 , C07D237/32 , C07D237/34 , C07D241/44 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds comprising a bicyclic aryl moiety, such as 2H-phthalazin-1-one or derivatives thereof, compositions comprising the same, and methods for producing and using the same. In particular, the present invention provides compounds of the formula: (I) or a pharmaceutically acceptable salt, a hydrate, a solvate, or a prodrug thereof; where Q 1 , Q 2 and Y are those defined herein.
摘要翻译：本发明提供包含双环芳基部分的化合物，例如2H-酞嗪-1-酮或其衍生物，包含它们的组合物，及其制备和使用方法。特别地，本发明提供下式的化合物：（I）或其药学上可接受的盐，水合物，溶剂合物或前药; 其中Q 1，Q 2和Y是本文定义的那些。

2. 发明申请

WO2007146838A3 SUBSTITUTED PHENYL ACETIC ACIDS AS DP-2 ANTAGONISTS 审中-公开
标题翻译：取代的苯乙酸作为DP-2拮抗剂
公开(公告)号：WO2007146838A3
公开(公告)日：2008-03-13
申请号：PCT/US2007070805
申请日：2007-06-08
申请人： ICOS CORP , DUDLER THOMAS , FAROUZ FRANCINE , FOWLER KERRY , HAWTHORN NATALY , HUANG DANWEN , BOHAN JIN , KIM MUSONG , LOVER ANDREW , ODINGO JOSHUA , OLIVER AMY , REED MARK , RUAN FUQIANG , THORSETT EUGENE
发明人： DUDLER THOMAS , FAROUZ FRANCINE , FOWLER KERRY , HAWTHORN NATALY , HUANG DANWEN , BOHAN JIN , KIM MUSONG , LOVER ANDREW , ODINGO JOSHUA , OLIVER AMY , REED MARK , RUAN FUQIANG , THORSETT EUGENE
IPC分类号： C07D209/18 , C07D211/30 , C07D211/96 , C07D217/06 , C07D223/04 , C07D401/12 , C07D407/12 , C07D409/12
CPC分类号： C07D267/14 , C07D207/337 , C07D211/34 , C07D217/06 , C07D217/08 , C07D223/04 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Substituted phenyl acetic acid compounds of formula (I), pharmaceutical compositions, methods for their preparation and methods are provided that are useful in the treatment and prevention of disorders or conditions responsive to DP-2 receptor modulation, in particular, inflammatory and immune-related disorders and conditions, such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：提供式（I）的取代的苯基乙酸化合物，药物组合物，其制备方法和方法，其可用于治疗和预防对DP-2受体调节，特别是炎症和免疫相关的病症或病症疾病和病症，如哮喘，过敏性鼻炎和特应性皮炎。

3. 发明申请

WO2007143745A2 SUBSTITUTED PHENYL ACETIC ACIDS AS DP-2 ANTAGONISTS 审中-公开
标题翻译：取代的苯乙酸作为DP-2拮抗剂
公开(公告)号：WO2007143745A2
公开(公告)日：2007-12-13
申请号：PCT/US2007/070803
申请日：2007-06-08
申请人： ICOS CORPORATION , DUDLER, Thomas , FAROUZ, Francine , FOWLER, Kerry , HAWTHORN, Nataly , HUANG, Danwen , JUDKINS, Angela , KIM, Musong , ODINGO, Joshua , OLIVER, Amy , REED, Mark , RUAN, Fuqiang , THORSETT, Eugene
发明人： DUDLER, Thomas , FAROUZ, Francine , FOWLER, Kerry , HAWTHORN, Nataly , HUANG, Danwen , JUDKINS, Angela , KIM, Musong , ODINGO, Joshua , OLIVER, Amy , REED, Mark , RUAN, Fuqiang , THORSETT, Eugene
CPC分类号： C07D295/205 , C07D207/273 , C07D211/46 , C07D211/54 , C07D211/76 , C07D213/71 , C07D215/36 , C07D223/12 , C07D225/02 , C07D239/42 , C07D241/08 , C07D261/10 , C07D295/155 , C07D295/185 , C07D295/26 , C07D313/12 , C07D333/34 , C07D405/04
摘要： Substituted phenyl acetic acid compounds of formula (I), pharmaceutical compositions, methods for their preparation and methods are provided that are useful in the treatment and prevention of disorders or conditions responsive to DP 2 receptor modulation, in particular, inflammatory and immune related disorders and conditions, such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：提供式（I）的取代的苯基乙酸化合物，药物组合物，其制备方法和方法，其可用于治疗和预防对DP 2受体调节，特别是炎症和免疫相关疾病的病症或病症，以及哮喘，过敏性鼻炎和特应性皮炎等病症。

4. 发明申请

WO2004035587A1 REVERSE-TURN MIMETICS AND COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：反向转换的MIME和组合物以及与之相关的方法
公开(公告)号：WO2004035587A1
公开(公告)日：2004-04-29
申请号：PCT/US2003/032411
申请日：2003-10-14
申请人： MYRIAD GENETICS, INC. , QABAR, Maher, N. , STASIAK, Marcin , MATHEW, Jessymol , LITTLE, Thomas , HUANG, Danwen
发明人： QABAR, Maher, N. , STASIAK, Marcin , MATHEW, Jessymol , LITTLE, Thomas , HUANG, Danwen
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Reverse-turn mimetics and methods relating to the same having Structure (I) are disclosed, including pharmaceutically acceptable salts and stereoisomers thereof, wherein R 1 , R 2 , R 3 and R 4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.
摘要翻译：公开了涉及具有结构（I）的反转模拟物和与其相同的方法，包括其药学上可接受的盐和立体异构体，其中R 1，R 2，R 3和R 4如本文所定义。这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。特别地，本发明的化合物和含有这些化合物的药物组合物是神经激肽（速激肽）拮抗剂。还公开了包含本发明的反转模拟物的文库。

5. 发明申请

WO2007143745A3 SUBSTITUTED PHENYL ACETIC ACIDS AS DP-2 ANTAGONISTS 审中-公开
标题翻译：取代的苯乙酸作为DP-2拮抗剂
公开(公告)号：WO2007143745A3
公开(公告)日：2008-04-17
申请号：PCT/US2007070803
申请日：2007-06-08
申请人： ICOS CORP , DUDLER THOMAS , FAROUZ FRANCINE , FOWLER KERRY , HAWTHORN NATALY , HUANG DANWEN , JUDKINS ANGELA , KIM MUSONG , ODINGO JOSHUA , OLIVER AMY , REED MARK , RUAN FUQIANG , THORSETT EUGENE
发明人： DUDLER THOMAS , FAROUZ FRANCINE , FOWLER KERRY , HAWTHORN NATALY , HUANG DANWEN , JUDKINS ANGELA , KIM MUSONG , ODINGO JOSHUA , OLIVER AMY , REED MARK , RUAN FUQIANG , THORSETT EUGENE
IPC分类号： C07D295/16 , A61P11/06 , A61P37/08 , C07D207/273 , C07D211/72 , C07D225/02 , C07D233/96 , C07D295/185 , C07D295/21
CPC分类号： C07D295/205 , C07D207/273 , C07D211/46 , C07D211/54 , C07D211/76 , C07D213/71 , C07D215/36 , C07D223/12 , C07D225/02 , C07D239/42 , C07D241/08 , C07D261/10 , C07D295/155 , C07D295/185 , C07D295/26 , C07D313/12 , C07D333/34 , C07D405/04
摘要： Substituted phenyl acetic acid compounds of formula (I), pharmaceutical compositions, methods for their preparation and methods are provided that are useful in the treatment and prevention of disorders or conditions responsive to DP 2 receptor modulation, in particular, inflammatory and immune related disorders and conditions, such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：提供式（I）的取代的苯基乙酸化合物，药物组合物，其制备方法和方法，其可用于治疗和预防对DP 2受体调节，特别是炎症和免疫相关疾病的病症或病症，以及哮喘，过敏性鼻炎和特应性皮炎等病症。

6. 发明申请

WO2007146838A2 SUBSTITUTED PHENYL ACETIC ACIDS AS DP-2 ANTAGONISTS 审中-公开
标题翻译：取代的苯乙酸作为DP-2拮抗剂
公开(公告)号：WO2007146838A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/070805
申请日：2007-06-08
申请人： ICOS CORPORATION , DUDLER, Thomas , FAROUZ, Francine , FOWLER, Kerry , HAWTHORN, Nataly , HUANG, Danwen , BOHAN, Jin , KIM, Musong , LOVER, Andrew , ODINGO, Joshua , OLIVER, Amy , REED, Mark , RUAN, Fuqiang , THORSETT, Eugene
发明人： DUDLER, Thomas , FAROUZ, Francine , FOWLER, Kerry , HAWTHORN, Nataly , HUANG, Danwen , BOHAN, Jin , KIM, Musong , LOVER, Andrew , ODINGO, Joshua , OLIVER, Amy , REED, Mark , RUAN, Fuqiang , THORSETT, Eugene
CPC分类号： C07D267/14 , C07D207/337 , C07D211/34 , C07D217/06 , C07D217/08 , C07D223/04 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Substituted phenyl acetic acid compounds of formula I, pharmaceutical compositions, methods for their preparation and methods are provided that are useful in the treatment and prevention of disorders or conditions responsive to DP-2 receptor modulation, in particular, inflammatory and immune related disorders and conditions, such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：提供式I的取代的苯基乙酸化合物，药物组合物，其制备方法和方法，其可用于治疗和预防对DP-2受体调节，特别是炎症和免疫相关疾病和病症有反应的病症或病症，如哮喘，过敏性鼻炎和特应性皮炎。

7. 发明申请

WO2005113556A1 QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA 审中-公开
标题翻译：喹诺酮类作为人类磷酸肌氨酸激酶3激酶的抑制剂
公开(公告)号：WO2005113556A1
公开(公告)日：2005-12-01
申请号：PCT/US2005/016778
申请日：2005-05-12
申请人： ICOS CORPORATION , FOWLER, Kerry, W. , HUANG, Danwen , KESICKI, Edward, A. , OOI, Hua Chee , OLIVER, Amy, R. , RUAN, Fuqiang , TREIBERG, Jennifer
发明人： FOWLER, Kerry, W. , HUANG, Danwen , KESICKI, Edward, A. , OOI, Hua Chee , OLIVER, Amy, R. , RUAN, Fuqiang , TREIBERG, Jennifer
IPC分类号： C07D487/04
CPC分类号： C07D473/34 , A61K31/52 , C07D239/91 , C07D473/16 , C07D487/04
摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.
摘要翻译：公开了抑制PI3Kdelta活性的化合物，包括选择性抑制PI3Kdelta活性的化合物。公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kdelta）活性的方法，以及使用该化合物治疗PI3Kdelta在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

8. 发明申请

WO1996022962A1 BUTYRYL-TYROSINYL SPERMINE, ANALOGS THEREOF AND METHODS OF PREPARING AND USING SAME 审中-公开
标题翻译：丁基吡咯烷酮，其类似物及其制备和使用方法
公开(公告)号：WO1996022962A1
公开(公告)日：1996-08-01
申请号：PCT/US1996001128
申请日：1996-01-23
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , NAKANISHI, Koji , HUANG, Danwen , CHOI, Seok-Ki , KALIVRETENOS, Aristotle , GOODNOW, Robert
发明人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
IPC分类号： C07C211/00
CPC分类号： C07C237/22 , C07C245/18 , C07C247/16 , C07C247/18 , C07C279/14 , C07D209/20
摘要： The present invention provides a compound having structure (I) wherein R1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R2 ia s 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl)aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl], (trifluoromethyl)-aminoacetyl or D- or L-arginyl group bonded through the alpha -carbonyl moiety thereof; R4 is H, or a linear or branched chain alkyl group; wherein R5, R6 and R7 are independently the same or different and are H, a linear or branched chain alkyl group, an aryl group or an arylalkyl group; wherein n, j and t are each 0 or 1; wherein m, o, p, q, r and s are independently the same or different and are 0, 1 or 2; wherein r+s and m+o are each equal to 2; wherein, j is 0, p+q is 2; wherein, if j is 1, then p is 1, q is 0 and R6 is H; and wherein * denotes a D or L configuration. The invention also provides a method of synthesizing the compound. Another aspect of the invention concerns a method of treating a subject afflicted by a disorder associated with binding of an etiological agent to a glutamate receptor.
摘要翻译：本发明提供具有结构（I）的化合物，其中R1是饱和或不饱和的直链或支链烷基或胆甾烷基; 其中R2是2-吲哚基，3-吲哚基，4-吲哚基，5-吲哚基，4-羟基苯基，4-（芳基烷氧基）苯基，3,4-二卤代苯基，4-羟基-3,5-二卤苯基，4-叠氮基苯基或4-卤代苯基; 其中R 3为H，直链或支链烷基或烯基，或苯基，2-叠氮基苯基，3-叠氮基苯基，4-叠氮基苯基或链烯基酰基，3-氨基-3-丁基丙基，N- [N-（ N-（4-叠氮基苯甲酰基）氨基丙基）氨丙基]，顺式或反式肉桂基，2-氨基-2 - [（4'-叠氮基苯基）乙酰基]，（三氟甲基） - 氨基乙酰基或D-或L-精氨酰基其α-羰基部分; R4是H或直链或支链烷基; 其中R5，R6和R7独立地相同或不同，为H，直链或支链烷基，芳基或芳基烷基; 其中n，j和t各自为0或1; 其中m，o，p，q，r和s独立地相同或不同，为0,1或2; 其中r + s和m + o各自等于2; 其中，j为0，p + q为2; 其中，如果j为1，则p为1，q为0且R6为H; 并且其中*表示D或L构型。本发明还提供了一种合成化合物的方法。本发明的另一方面涉及一种治疗受病原体与谷氨酸受体的结合相关疾病的受试者的治疗方法。

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