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1. 发明申请

WO2011103460A8 FUSED TETRACYCLIC PYRIDO[4,3-B]INDOLE AND PYRIDO[3,4-B]INDOLE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：熔融四环吡啶[4,3-B]吲哚和吡咯并[3,4-B]吲哚衍生物及其使用方法
公开(公告)号：WO2011103460A8
公开(公告)日：2012-10-18
申请号：PCT/US2011025475
申请日：2011-02-18
申请人： MEDIVATION TECHNOLOGIES INC , CHAKRAVARTY SARVAJIT , HART BARRY PATRICK , JAIN RAJENDRA PARASMAL
发明人： CHAKRAVARTY SARVAJIT , HART BARRY PATRICK , JAIN RAJENDRA PARASMAL
IPC分类号： A01N43/38 , A61K31/405 , A61K31/44
CPC分类号： C07D471/14 , C07D471/16 , C07D471/18 , C07D471/22 , C07D498/14 , C07D498/16 , C07D513/00 , C07D513/16
摘要： This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4- b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
摘要翻译：本公开涉及稠合的四环吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚。还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。

2. 发明申请

WO2012112964A3 PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：吡咯并[4,3-b]吲哚和吡咯并[3,4-b]吲哚衍生物及其使用方法
公开(公告)号：WO2012112964A3
公开(公告)日：2014-01-03
申请号：PCT/US2012025753
申请日：2012-02-17
申请人： MEDIVATION TECHNOLOGIES INC , CHAKRAVARTY SARVAJIT , HART BARRY PATRICK , JAIN RAJENDRA PARASMAL
发明人： CHAKRAVARTY SARVAJIT , HART BARRY PATRICK , JAIN RAJENDRA PARASMAL
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/437 , A61K31/4709 , A61K31/4745 , A61K31/55 , A61K45/06 , C07D471/04 , A61K2300/00
摘要： This disclosure is directed to pyrido[4,3-b]indole and pyrido [3, 4-b] indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. The compounds may bind to and antagonize receptor alpha2B, alpha1B or alpha2Alpha· The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.
摘要翻译：本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。还提供了包含化合物的药物组合物，以及在各种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。化合物可以结合并拮抗受体α2B，α1B或α2αα。该化合物可用于治疗，例如（i）降低血压和/或（ii）促进肾血流量和/或（iii）降低或抑制钠再吸收或调节血糖水平，增加胰岛素分泌并治疗对胰岛素产生增加或预期是有反应的疾病或病症。该化合物也可用于治疗预期对血压降低有反应的疾病或病症。具体描述了使用该化合物治疗心血管，肾脏疾病或2型糖尿病。

3. 发明申请

WO2010127177A8 PYRIDO [4,3-B] INDOLES AND METHODS OF USE 审中-公开
标题翻译：吡咯并[4,3-B]吲哚和使用方法
公开(公告)号：WO2010127177A8
公开(公告)日：2011-12-15
申请号：PCT/US2010033053
申请日：2010-04-29
申请人： MEDIVATION TECHNOLOGIES INC , JAIN RAJENDRA PARASMAL , CHAKRAVARTY SARVAJIT
发明人： JAIN RAJENDRA PARASMAL , CHAKRAVARTY SARVAJIT
IPC分类号： A01N43/42
CPC分类号： C07D471/04
摘要： New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
摘要翻译：描述了可用于调节个体中组胺受体的新杂环化合物。描述了吡啶并[4,3-b]吲哚，以及包含化合物的药物组合物以及在多种治疗应用中使用该化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元紊乱。

4. 发明申请

WO2011019417A8 PYRIDO [4, 3-B] INDOLES AND METHODS OF USE 审中-公开
标题翻译：吡啶[4,3-B]吲哚及其使用方法
公开(公告)号：WO2011019417A8
公开(公告)日：2011-12-15
申请号：PCT/US2010033055
申请日：2010-04-29
申请人： MEDIVATION TECHNOLOGIES INC , JAIN RAJENDRA PARASMAL , CHAKRAVARTY SARVAJIT
发明人： JAIN RAJENDRA PARASMAL , CHAKRAVARTY SARVAJIT
IPC分类号： A01N43/42
CPC分类号： C07D471/04
摘要： New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
摘要翻译：描述了可用于调节个体中组胺受体的新杂环化合物。描述了吡啶并[4,3-b]吲哚，以及包含化合物的药物组合物和在各种治疗应用中使用所述化合物的方法，包括治疗认知障碍，精神障碍，神经递质介导的障碍和/或神经元病症。

5. 发明申请

WO2009094668A8 NEW 2,3,4,5-TETRAHYDRO-1H-PYRIDO[ 4,3-B] INDOLE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新的2,3,4,5-四氢-1H-吡咯并[4,3-B]吲哚化合物及其使用方法
公开(公告)号：WO2009094668A8
公开(公告)日：2010-09-10
申请号：PCT/US2009032065
申请日：2009-01-26
申请人： MEDIVATION TECHNOLOGIES INC , HUNG DAVID T , PROTTER ANDREW ASHER , CHAKRAVARTY SARVAJIT , JAIN RAJENDRA PARASMAL
发明人： HUNG DAVID T , PROTTER ANDREW ASHER , CHAKRAVARTY SARVAJIT , JAIN RAJENDRA PARASMAL
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D487/14 , C07D471/04 , C07D471/14 , C07D487/04
摘要： This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5- tetrahydro-lH-pyrido[4,3-b]indole compounds. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
摘要翻译：本公开涉及可用于调节个体中组胺受体的新型三环化合物。描述了化合物，包括新的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚化合物。还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。

6. 发明申请

WO2009120717A3 PYRIDO [3, 4-B] INDOLES AND METHODS OF USE 审中-公开
标题翻译：吡咯并[3,4-B]吲哚和使用方法
公开(公告)号：WO2009120717A3
公开(公告)日：2009-12-03
申请号：PCT/US2009038138
申请日：2009-03-24
申请人： MEDIVATION TECHNOLOGIES INC , HUNG DAVID T , PROTTER ANDREW ASHER , CHAKRAVARTY SARVAJIT , JAIN RAJENDRA PARASMAL , DUGAR SUNDEEP
发明人： HUNG DAVID T , PROTTER ANDREW ASHER , CHAKRAVARTY SARVAJIT , JAIN RAJENDRA PARASMAL , DUGAR SUNDEEP
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00
CPC分类号： C07D471/14 , C07D471/04
摘要： This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
摘要翻译：本公开涉及可用于调节个体中组胺受体的新杂环化合物。描述吡啶并[3,4-b]吲哚，以及包含该化合物的药物组合物以及在各种治疗应用中使用该化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元紊乱。

7. 发明申请

WO2005065416A2 PROCESS FOR THE PREPARATION OF PYRIDOPYRIMIDONES 审中-公开
标题翻译：制备吡啶并嘧啶酮的方法
公开(公告)号：WO2005065416A2
公开(公告)日：2005-07-21
申请号：PCT/US2004044064
申请日：2004-12-31
申请人： SCIOS INC , CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , TESTER RICHLAND , CONTE AURELIA
发明人： CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , TESTER RICHLAND , CONTE AURELIA
IPC分类号： C07D239/90 , C07D239/91 , C07D471/04 , C07D487/02
CPC分类号： C07D239/91 , C07D471/04
摘要： The present invention is directed to a rpocess for making 2-substituted pyridopyrimidones. In particular, 2-substituted pyridopyrimidones are made through the single step reaction of suitable acid derivatives with desired derivatives of amidines.
摘要翻译：本发明涉及制备2-取代的吡啶并嘧啶酮的方法。具体地说，2-取代的吡啶并嘧啶酮是通过合适的酸衍生物与期望的脒衍生物的单步反应制备的。

8. 发明申请

WO2006105222A2 CARBOXAMIDE INHIBITORS OF TGFB 审中-公开
标题翻译： TGFB的羧酰胺抑制剂
公开(公告)号：WO2006105222A2
公开(公告)日：2006-10-05
申请号：PCT/US2006011509
申请日：2006-03-27
申请人： SCIOS INC , AXON JONATHAN , CHAKRAVARTY SARVAJIT , HART BARRY , MCENROE GLENN , MURPHY ALISON , PONTIUS KAREN , SHENG DANIEL , WANG GINA , YELLAPREGADA SHANTI
发明人： AXON JONATHAN , CHAKRAVARTY SARVAJIT , HART BARRY , MCENROE GLENN , MURPHY ALISON , PONTIUS KAREN , SHENG DANIEL , WANG GINA , YELLAPREGADA SHANTI
IPC分类号： C07D401/12 , A61K31/506 , C07D401/14 , C07D407/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D495/04
摘要： Certain appropriately substituted forms of pyrimidine having a pyridylamine group at C- 4 of the pyrimidine and an amide group on the pyridine ring are useful in the treatment of conditions associated with excessive TGFB activity.
摘要翻译：在嘧啶的C 4上具有吡啶基胺基的嘧啶的某些适当取代的形式和吡啶环上的酰胺基可用于治疗与过量TGFB活性相关的病症。

9. 发明申请

WO0012497B1 QUINAZOLINE DERIVATIVES AS MEDICAMENTS 审中-公开
公开(公告)号：WO0012497B1
公开(公告)日：2000-09-08
申请号：PCT/US9919846
申请日：1999-08-27
申请人： SCIOS INC , CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , PERUMATTAM JOHN J , SCHREINER GEORGE F , LIU DAVID Y , LEWICKI JOHN A
发明人： CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , PERUMATTAM JOHN J , SCHREINER GEORGE F , LIU DAVID Y , LEWICKI JOHN A
IPC分类号： A61K31/517 , A61K31/519 , A61K31/5355 , A61K39/395 , A61P1/16 , A61P1/18 , A61P7/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P19/02 , A61P29/00 , A61P43/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/02 , C07D239/91 , A61K31/47 , A61K31/505 , C07D215/00 , C07D239/72
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF- beta and/or p38- alpha kinase using compounds of formula (1) or the pharmaceutically acceptable salts thereof wherein R is a noninterfering substituent; each Z is CR or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar' is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

10. 发明申请

WO2004087056A3 BI-CYCLIC PYRIMIDINE INHIBITORS OF TGFbeta 审中-公开
标题翻译： TGFbeta的双循环嘧啶抑制剂
公开(公告)号：WO2004087056A3
公开(公告)日：2005-02-24
申请号：PCT/US2004009300
申请日：2004-03-26
申请人： SCIOS INC , DUGAR SUNDEEP , CHAKRAVARTY SARVAJIT , CONTE AURELIA , AXON JONATHAN , MCENROE GLENN
发明人： DUGAR SUNDEEP , CHAKRAVARTY SARVAJIT , CONTE AURELIA , AXON JONATHAN , MCENROE GLENN
IPC分类号： A61K31/517 , A61K31/519 , C07D239/94 , C07D401/12 , C07D487/02 , C07D487/04 , C07D491/02 , C07D491/04 , C07D495/04 , C07D498/02 , C07D498/04 , C07D239/70 , C07D491/048
CPC分类号： C07D487/04 , A61K31/517 , C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D498/04
摘要： Compounds in which a pyrimidine nucleus is bridged at the (5) and (6) position and are further substituted at positions (2) and (4) with substituents comprising aromatic moieties are useful in treating subjects with conditions ameliorated by inhibition of TGFbeta activity.
摘要翻译：其中嘧啶核在（5）和（6）位置桥连并在含有芳族部分的取代基在位置（2）和（4）进一步取代的化合物可用于治疗受抑制TGFbeta活性改善的病症的受试者。

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