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1. 发明申请

WO2005065416A3 PROCESS FOR THE PREPARATION OF PYRIDOPYRIMIDONES 审中-公开
公开(公告)号：WO2005065416A3
公开(公告)日：2005-07-21
申请号：PCT/US2004/044064
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
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.

2. 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。

3. 发明申请

WO1994006784A1 1,2-DISUBSTITUTED ETHYL AMIDES AS INHIBITORS OF ACAT 审中-公开
标题翻译：作为ACAT的抑制剂的1,2-取代的乙基胺
公开(公告)号：WO1994006784A1
公开(公告)日：1994-03-31
申请号：PCT/US1993008705
申请日：1993-09-21
申请人： SCHERING CORPORATION , DUGAR, Sundeep
发明人： SCHERING CORPORATION
IPC分类号： C07D295/12
CPC分类号： C07D221/20 , C07C233/09 , C07C2601/14 , C07D211/44 , C07D211/58 , C07D211/72 , C07D211/74 , C07D295/125 , C07D295/185 , C07D491/10
摘要： Amides of formula (I), wherein: R is A and R is B; R is B and R is A; or R and R are independently selected from the group B; A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl; B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl; R is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain; R is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl; R and R are both H, or R and R together represent =O; or a pharmaceutically acceptable salt thereof; useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.
摘要翻译：式（I）的酰胺，其中：R 1是A且R 2是B; R 1是B，R 2是A; 或R 1和R 2独立地选自B组; A是苯基，取代的苯基，杂芳基或取代的杂芳基; B是环烷基，取代的环烷基，杂环烷基或取代的杂环烷基; R 3是分支或直链的1至25个碳原子的烷基链; 2至25个碳原子的链烯基，分支或直链; 取代的烷基链; 取代烯基链; 中断的烷基链; 中断的烯基链; 取代的中断的烷基链; 或取代的中断的烯基链; R 4是氢，低级烷基，苯基，Q-取代的苯基，杂芳基或Q-取代的杂芳基; R 6和R 7均为H或R 6，R 7一起表示= O; 或其药学上可接受的盐; 可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

4. 发明申请

WO2008079105A1 METHODS TO SYNTHESIZE INDOLES AS PRECURSORS FOR PHARMACEUTICALS 审中-公开
标题翻译：合成作为药物前提剂的方法
公开(公告)号：WO2008079105A1
公开(公告)日：2008-07-03
申请号：PCT/US2006/032736
申请日：2006-08-22
申请人： SCIOS INC. , DUGAR, Sundeep , GIANNOUSIS, Peter
发明人： DUGAR, Sundeep , GIANNOUSIS, Peter
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D209/08 , C07C233/54 , C07F7/0818
摘要： The invention provides improved methods for the synthesis of indoles, especially useful for making indoles having an ester or amide group at C-5. The methods involve cyclization of a protected ortho-acetylene-substituted aniline derivative to produce an indole.
摘要翻译：本发明提供了用于合成吲哚的改进方法，特别可用于在C-5制备具有酯或酰胺基团的吲哚。所述方法包括环化受保护的邻乙炔取代的苯胺衍生物以产生吲哚。

5. 发明申请

WO2007005863A1 CRYSTALLINE FORMS OF (2R-TRANS)-6-CHLORO-5[[4-[(4-FLUOROPHENYL)METHYL]-2,5-DIMETHYL-1-PIPERAZINYL]CARBONYL]-N,N, 1-TRIMETHYL-ALPHA-OXO-1H-INDOLE-3-ACETAMIDE MONOHYDROCHLORIDE 审中-公开
标题翻译：（2R-TRANS）-6-氯代-5 [[4 - [（4-氟代甲基）甲基] -2,5-二甲基-1-哌嗪基]] - ，N，1-三甲基-AlPHA- OXO-1H-吲哚-3-乙酰胺一氢氯化物
公开(公告)号：WO2007005863A1
公开(公告)日：2007-01-11
申请号：PCT/US2006/026030
申请日：2006-06-30
申请人： SCIOS INC. , GIANNOUSIS, Peter , LEE, Kathleen, M. , DUGAR, Sundeep
发明人： GIANNOUSIS, Peter , LEE, Kathleen, M. , DUGAR, Sundeep
IPC分类号： C07D403/06 , A61K31/496 , A61P35/00
CPC分类号： C07D209/24
摘要： The present invention relates to novel crystalline forms of (2R-trans)-6-chloro-5-[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N, 1-trimethyl-alpha-oxo-1H-indole-3-acetamide monochloride, methods for their preparation, and pharmaceutical compositions comprising the novel pseudopolymorphs.
摘要翻译：本发明涉及（2R-反式）-6-氯-5 - [[4 - [（4-氟苯基）甲基] -2,5-二甲基-1-哌嗪基]羰基] -N，N 1-三甲基-α-氧代-1H-吲哚-3-乙酰胺一氯化物，其制备方法和包含新型假多晶型物的药物组合物。

6. 发明申请

WO2006112828A1 AZAINDOLE DERIVATIVES AS INHIBITORS OF P38 KINASE 审中-公开
标题翻译：作为P38激酶的抑制剂的氨基衍生物
公开(公告)号：WO2006112828A1
公开(公告)日：2006-10-26
申请号：PCT/US2005/012969
申请日：2005-04-15
申请人： SCIOS, INC. , DUGAR, Sundeep , GOYAL, Bindu , LU, Qing , LUEDTKE, Gregroy, R. , MAVUNKEL, Babu, J. , NASHASHIBI, Imad , PERUMATTAM, John, J. , TAN, Xuefei , TESTER, Richland , WANG, Dan, Xiong
发明人： DUGAR, Sundeep , GOYAL, Bindu , LU, Qing , LUEDTKE, Gregroy, R. , MAVUNKEL, Babu, J. , NASHASHIBI, Imad , PERUMATTAM, John, J. , TAN, Xuefei , TESTER, Richland , WANG, Dan, Xiong
IPC分类号： A61K31/496 , A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through an azacyclic linker to another cyclic moiety.
摘要翻译：本发明涉及使用作为氮杂吲哚的化合物抑制p38激酶，优选p38-a的方法，其中所述氮杂吲哚通过氮杂环链接体与另一个环状部分偶联。

7. 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.

8. 发明申请

WO2012137225A1 SUBSTITUTED METHYLFORMYL REAGENTS AND METHOD OF USING SAME TO MODIFY PHYSICOCHEMICAL AND/OR PHARMACOKINETIC PROPERTIES OF COMPOUNDS 审中-公开
标题翻译：取代的甲基试剂及其使用方法来改变化合物的化学和/或药物动力学性质
公开(公告)号：WO2012137225A1
公开(公告)日：2012-10-11
申请号：PCT/IN2012/000248
申请日：2012-04-09
申请人： SPHAERA PHARMA PVT. LTD , DUGAR, Sundeep , MAHAJAN, Dinesh , HOLLINGER PETER, Frank
发明人： DUGAR, Sundeep , MAHAJAN, Dinesh , HOLLINGER PETER, Frank
IPC分类号： A01N35/00 , A01N35/02 , A61K31/11
CPC分类号： C07D495/14 , C07D213/80 , C07D213/803 , C07D213/81 , C07D213/82 , C07D295/20 , C07D305/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D471/04 , C07D487/04 , C07D487/22 , C07D491/147 , C07D491/22
摘要： The present invention relates to the synthesis and application of novel chiral/ achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
摘要翻译：本发明涉及新型手性/非手性取代的甲酰甲基试剂的合成和应用，以修饰药物和/或生物活性物质，以改变未经修饰的原始药剂所得化合物的物理化学，生物学和/或药代动力学性质。

9. 发明申请

WO2009055828A1 NEW TETRACYCLIC COMPOUNDS 审中-公开
标题翻译：新型四环化合物
公开(公告)号：WO2009055828A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/081390
申请日：2008-10-27
申请人： MEDIVATION TECHNOLOGIES, INC. , HUNG, David, T. , PROTTER, Andrew, Asher , JAIN, Rajendra, Parasmal , DUGAR, Sundeep , CHAKRAVARTY, Sarvajit , BACHURIN, Sergey, Olegovich , USTINOV, Anatoly, Konstantinovich , BEZNOSKO, Bogdan, Konstantinovich , SHEVTSOVA, Elena, Feofanovna , GRIGORIEV, Vladimir, Viktorovich
发明人： HUNG, David, T. , PROTTER, Andrew, Asher , JAIN, Rajendra, Parasmal , DUGAR, Sundeep , CHAKRAVARTY, Sarvajit , BACHURIN, Sergey, Olegovich , USTINOV, Anatoly, Konstantinovich , BEZNOSKO, Bogdan, Konstantinovich , SHEVTSOVA, Elena, Feofanovna , GRIGORIEV, Vladimir, Viktorovich
IPC分类号： C07D471/04 , C07D471/14 , A61K31/437 , A61P25/18 , A61P25/24 , A61P25/28
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , C07D417/10 , C07D471/10 , C07D471/14
摘要： This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3- 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：本公开涉及可用于调节个体中组胺受体的新四环化合物。一个实施方案中的化合物是四环[4,3-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。

10. 发明申请

WO2005032481A2 QUINAZOLINE DERIVATIVES AS MEDICAMENTS 审中-公开
标题翻译：喹诺酮衍生物作为药物
公开(公告)号：WO2005032481A2
公开(公告)日：2005-04-14
申请号：PCT/US2004/032430
申请日：2004-09-30
申请人： SCIOS INC. , DUGAR, Sundeep , CHAKRAVARTY, Sarvajit , MURPHY, Alison , MCENROE, Glen , CONTE, Aurelia , PERUMATTAM, John, J.
发明人： DUGAR, Sundeep , CHAKRAVARTY, Sarvajit , MURPHY, Alison , MCENROE, Glen , CONTE, Aurelia , PERUMATTAM, John, J.
IPC分类号： A61K
CPC分类号： C07D471/04 , C07D475/10 , C07D487/04
摘要： Quinazoline derivatives have the formula (I) or the pharmaceutically acceptable salts thereof; wherein each of Z 5 , Z 6 , Z 7 and Z 8 is N or CH and wherein one or two Z 5 , Z 6 , Z 7 and Z 8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R 1 is independently OH, SH, NH 2 , OR, SR, NHR, halo or R-halide; wherein two adjacent R 1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R 2 is independently R, halo, R-halide, OR-halide, NH 2 , CONH 2 or CONHR; wherein R is optionally substituted C 1 -C 12 alkyl, C 1 -C 12 alkenyl, C 1 -C 12 alkynyl, or aryl C 1 -C 12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are =O, =N, or OH; and wherein R 3 is H or CH 3 . Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.
摘要翻译：喹唑啉衍生物具有式（I）或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8中的每一个是N或CH，并且其中一个或两个Z 5，Z 6，Z 7和Z 8，是N，其中两个相邻的Z位置不能是N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1基团可以连接形成5-6个成员的脂族杂环; 其中R 2独立地是R，卤素，卤化物，或者卤化物，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12链烯基，C 1 -C 12炔基或芳基C 1 -C 12烷基，其含有0-4个杂原子代替碳主链中的碳，其中任选取代基为= = N或OH; 并且其中R 3是H或CH 3。这样的化合物可用于治疗以增强的TGFbeta活性为特征的病症的药物组合物和方法。

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