公开(公告)号：WO2012031138A3

公开(公告)日：2013-03-21

申请号：PCT/US2011050229

申请日：2011-09-01

申请人： CONCERT PHARMACEUTICALS INC ,  BIS JOANNA A ,  IGO DAVID H ,  TURNQUIST DAVID J

发明人： BIS JOANNA A ,  IGO DAVID H ,  TURNQUIST DAVID J

IPC分类号： C07D473/04 ,  C07D473/08

CPC分类号： C07D473/10 ,  C07B2200/05 ,  C07D473/04 ,  C07D473/08

摘要： The present invention provides individual crystalline polymorphs of (S)-1- (4,4,6, 6,6-pentadeutero-5-hydroxyhexyl)-3,7 -dimethyl- 1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermo gravimetric analysis (TGA).

摘要翻译： 本发明提供了（S）-1-（4,4,6,6,6-五氘-5-羟基己基）-3,7-二甲基-1H-嘌呤-2,6（3H，7H） （a）粉末X射线衍射数据（“XRPD”）;和（c）粉末X射线衍射数据（“XRPD”）中的一种或多种来表征本文公开的每种多晶型物。 （b）差示扫描量热法（“DSC”）; 和（e）热重分析（TGA）。

公开(公告)号：WO2013016156A1

公开(公告)日：2013-01-31

申请号：PCT/US2012/047513

申请日：2012-07-20

申请人： GLAXO GROUP LIMITED ,  BIS, Joanna ,  IGO, David, H.

发明人： BIS, Joanna ,  IGO, David, H.

IPC分类号： A61K31/4409

CPC分类号： C07D213/89 ,  A61K31/44 ,  A61K31/4425 ,  A61K45/06 ,  C07B2200/13

摘要： Disclosed are novel novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[ 4-chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[ 4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter "Compound A-l,4-dioxane/water solvate"), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ku radiation, at about 4.0,8.1, 10.1, 14.2, 16.2, 18.6,20.3,24.7,25.0, and 26.5.

摘要翻译： 公开了4-叔丁基-N- [4-氯-2-（1-氧 - 吡啶-4-羰基）苯基] - 苯磺酰胺的钠盐的新型新型多晶型溶剂化和脱溶剂形式。 本发明的一个实施方案涉及4-叔丁基-N- [4-氯-2-（1-氧 - 吡啶-4-羰基） - 苯基]苯磺酰胺（以下称为“化合物A1， 4-二恶烷/水溶剂合物“），其中结晶形式的特征在于包括衍射角（°28）的X射线粉末衍射图，当使用Cu Ku辐射测量时，衍射角为约4.0,8.1,10.1,14.2,16.2， 18.6,20.3,24.7,25.0和26.5。

公开(公告)号：WO2012031138A9

公开(公告)日：2012-03-08

申请号：PCT/US2011/050229

申请日：2011-09-01

申请人： CONCERT PHARMACEUTICALS, INC. ,  BIS, Joanna, A. ,  IGO, David, H. ,  TURNQUIST, David, J.

发明人： BIS, Joanna, A. ,  IGO, David, H. ,  TURNQUIST, David, J.

IPC分类号： C07D473/04 ,  C07D473/08

摘要： The present invention provides individual crystalline polymorphs of ( S )-1- (4,4,6, 6,6-pentadeutero-5-hydroxyhexyl)-3,7 -dimethyl- 1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermo gravimetric analysis (TGA).

公开(公告)号：WO2012031138A2

公开(公告)日：2012-03-08

申请号：PCT/US2011050229

申请日：2011-09-01

申请人： CONCERT PHARMACEUTICALS INC ,  BIS JOANNA A ,  IGO DAVID H ,  TURNQUIST DAVID J

发明人： BIS JOANNA A ,  IGO DAVID H ,  TURNQUIST DAVID J

IPC分类号： A61K31/522

CPC分类号： C07D473/10 ,  C07B2200/05 ,  C07D473/04 ,  C07D473/08

摘要： The present invention provides individual crystalline polymorphs of (S)-1- (4,4,6, 6,6-pentadeutero-5-hydroxyhexyl)-3,7 -dimethyl- 1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data ("XRPD"); (b) differential scanning calorimetry ("DSC"); and (e) thermo gravimetric analysis (TGA).

摘要翻译： 本发明提供了（S）-1-（4,4,6,6,6-五氘代-5-羟基己基）-3,7-二甲基-1H-嘌呤-2,6（3H，7H） 指定为Form 1，Form 2，Form 3和Form 4的二酮。本文公开的每种多晶型物均根据（a）粉末X射线衍射数据（“XRPD”）中的一种或多种进行表征; （b）差示扫描量热法（“DSC”）; 和（e）热重分析（TGA）。

公开(公告)号：WO2005051383A1

公开(公告)日：2005-06-09

申请号：PCT/US2004/039528

申请日：2004-11-24

申请人： SB PHARMCO PUERTO RICO INC. ,  BROOK, Christopher, S. ,  CHEN, Pingyun, Y. ,  CHEN, Wei ,  DAI, Qunying ,  DELL'ORCO, Philip, C. ,  HISLER, Claire ,  IGO, David, H. ,  KATRINCIC, Lee, M. ,  LABAW, Clifford, S. ,  LOUVET, Ann, Marie ,  OH, Choon, K ,  PING, Li-Jen ,  SPOORS, Paul, G. ,  WANG, Jun ,  WERNER, Christopher

发明人： BROOK, Christopher, S. ,  CHEN, Pingyun, Y. ,  CHEN, Wei ,  DAI, Qunying ,  DELL'ORCO, Philip, C. ,  HISLER, Claire ,  IGO, David, H. ,  KATRINCIC, Lee, M. ,  LABAW, Clifford, S. ,  LOUVET, Ann, Marie ,  OH, Choon, K ,  PING, Li-Jen ,  SPOORS, Paul, G. ,  WANG, Jun ,  WERNER, Christopher

IPC分类号： A61K31/403

CPC分类号： C07D209/88

摘要： The present invention relates to a salt of carvedilol and/or corresponding solvates thereof, compositions containing such carvedilol and/or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to carvedilol phosphate salts, and/or solvates thereof, which include a novel crystalline form of carvedilol dihydrogen phosphate (i.e., which is the dihydrogen phosphate salt of 1­(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate,etc.) and/or other corresponding solvates thereof, compositions containing these carvedilol phosphate salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.

摘要翻译： 本发明涉及卡维地洛和/或其相应溶剂合物的盐，含有这种卡维地洛和/或其相应溶剂合物的组合物和/或使用上述化合物治疗哺乳动物某些疾病状态的方法， 特别的人 本发明还涉及卡维地洛磷酸盐和/或其溶剂合物，其包括新型的卡维地洛磷酸二氢盐结晶形式（即，其为磷酸二氢盐1（咔唑-4-基氧基-3 - [[2- （邻甲氧基苯氧基）乙基]氨基] -2-丙醇）和/或卡维地洛磷酸氢盐等）和/或其它相应的溶剂合物，含有这些卡维地洛磷酸盐和/或溶剂合物的组合物，以及使用上述盐 和/或溶剂化治疗高血压，充血性心力衰竭和心绞痛等

公开(公告)号：WO2004002472A8

公开(公告)日：2005-02-24

申请号：PCT/US0320346

申请日：2003-06-27

申请人： SB PHARMCO INC ,  CHEN PINGYUN Y ,  DAI QUNYING ,  DELL ORCO PHILLIP C ,  HISLER CLAIRE ,  IGO DAVID H ,  KATRINCIC LEE M ,  LABAW CLIFFORD S ,  PING LI-JEN

发明人： CHEN PINGYUN Y ,  DAI QUNYING ,  DELL ORCO PHILLIP C ,  HISLER CLAIRE ,  IGO DAVID H ,  KATRINCIC LEE M ,  LABAW CLIFFORD S ,  PING LI-JEN

IPC分类号： A61K31/403 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  C07D209/82 ,  C07D209/88

CPC分类号： C07D209/88

摘要： The present invention relates to a salt of carvedilol, corresponding compositions containing such a carvedilol salt or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to a novel crystalline form of carvedilol hydrobromide, which is the hydrobromide salt of 1-(carbazol-4-yloxy-3-[[2-(o­methoxyphenoxy)ethyl]amino]-2-propanol, and/or other carvedilol solvates thereof, compositions containing salts or solvates of carvedilol hydrobromide, and methods of using the aforementioned compound(s) to treat hypertension, congestive heart failure, and angina, etc.

摘要翻译： 本发明涉及卡维地洛的盐，含有这种卡维地洛盐或其相应溶剂合物的相应组合物，和/或使用上述化合物治疗哺乳动物，特别是人中某些疾病状态的方法。 本发明还涉及1-（咔唑-4-基氧基-3 - [[2-（甲氧基苯氧基）乙基]氨基] -2-丙醇的氢溴酸盐和/或 其它卡维地洛溶剂化物，含有盐酸卡维地洛盐酸盐或溶剂化物的组合物，以及使用上述化合物治疗高血压，充血性心力衰竭和心绞痛等的方法。

公开(公告)号：WO2007062333A3

公开(公告)日：2007-05-31

申请号：PCT/US2006/061066

申请日：2006-11-18

申请人： GLAXO GROUP LIMITED ,  IGO, David, H. ,  NORTON, Beth, A.

发明人： IGO, David, H. ,  NORTON, Beth, A.

IPC分类号： C07D211/80 ,  A61K31/445

摘要： The invention is directed to the L-tartrate salt of trans-3-aminocyclobutyl (lS,2R,3S,4S:,6R,7R,8R-,14R)-4-ethenyl-3-hydroxy-2,4,7, 14-tetramethyl-9- oxotricyclo[5.4.3.01,8]tetradec-6-yl imidodicarbonate (Compound IA.) Compound IA is useful for the treatment of a variety of diseases and conditions, such as respiratory tract and skin and skin structure infections. Accordingly, the invention is further directed to pharmaceutical compositions comprising Compound IA. The invention is still further directed to methods of treating respiratory tract and skin and skin structure infections using Compound IA or a pharmaceutical composition comprising Compound IA.

公开(公告)号：WO2004002472A1

公开(公告)日：2004-01-08

申请号：PCT/US2003/020346

申请日：2003-06-27

申请人： SB PHARMCO PUERTO RICO INC. ,  CHEN, Pingyun Y. ,  DAI, Qunying ,  DELL'ORCO, Phillip C. ,  HISLER, Claire ,  IGO, David, H. ,  KATRINCIC. Lee M. ,  LABAW, Clifford, S. ,  PING, Li-Jen

发明人： CHEN, Pingyun Y. ,  DAI, Qunying ,  DELL'ORCO, Phillip C. ,  HISLER, Claire ,  IGO, David, H. ,  KATRINCIC. Lee M. ,  LABAW, Clifford, S. ,  PING, Li-Jen

IPC分类号： A61K31/403

CPC分类号： C07D209/88

摘要： The present invention relates to a salt of carvedilol, corresponding compositions containing such a carvedilol salt or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to a novel crystalline form of carvedilol hydrobromide, which is the hydrobromide salt of 1-(carbazol-4-yloxy-3-[[2-(o­methoxyphenoxy)ethyl]amino]-2-propanol, and/or other carvedilol solvates thereof, compositions containing salts or solvates of carvedilol hydrobromide, and methods of using the aforementioned compound(s) to treat hypertension, congestive heart failure, and angina, etc.

摘要翻译： 本发明涉及卡维地洛的盐，含有这种卡维地洛盐或其相应溶剂合物的相应组合物，和/或使用上述化合物治疗哺乳动物，特别是人中某些疾病状态的方法。 本发明还涉及1-（咔唑-4-基氧基-3 - [[2-（甲氧基苯氧基）乙基]氨基] -2-丙醇的氢溴酸盐和/或 其它卡维地洛溶剂化物，含有盐酸卡维地洛盐酸盐或溶剂化物的组合物，以及使用上述化合物治疗高血压，充血性心力衰竭和心绞痛等的方法。

公开(公告)号：WO2009158377A1

公开(公告)日：2009-12-30

申请号：PCT/US2009/048389

申请日：2009-06-24

申请人： SMITH KLINE BEECHAM CORPORATION ,  DESCHAMPS, Nicole, Marie ,  IGO, David, H. ,  MITCHELL, Mark, Bryan

发明人： DESCHAMPS, Nicole, Marie ,  IGO, David, H. ,  MITCHELL, Mark, Bryan

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： C07D405/12

摘要： Disclosed are salts of methyl 2-((R)-(3-chlorophenyl)((R)-l-((S)-2-(methylamino)- 3 -((R)-tetrahydro-2H-pyran-3 -yl)propylcarbamoyl)piperidin-3 -yl)methoxy)ethylcarbamate and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

摘要翻译： 公开了2 - （（R） - （3-氯苯基）（（R）-1 - （（S）-2-（甲基氨基）-3 - （（R） - 四氢-2H-吡喃-3-基） 吡啶-3-基）丙基氨基甲酰基）哌啶-3-基）甲氧基）乙基氨基甲酸酯和含有它们的药物组合物。 还公开了其制备方法及其使用方法。

公开(公告)号：WO2007062333A2

公开(公告)日：2007-05-31

申请号：PCT/US2006061066

申请日：2006-11-18

申请人： GLAXO GROUP LTD ,  IGO DAVID H ,  NORTON BETH A

发明人： IGO DAVID H ,  NORTON BETH A

IPC分类号： A61K31/325 ,  C07C271/32

CPC分类号： C07C271/66 ,  C07C59/255 ,  C07C2601/04 ,  C07C2603/82

摘要： The invention is directed to the L-tartrate salt of trans-3-aminocyclobutyl (lS,2R,3S,4S:,6R,7R,8R-,14R)-4-ethenyl-3-hydroxy-2,4,7, 14-tetramethyl-9- oxotricyclo[5.4.3.01,8]tetradec-6-yl imidodicarbonate (Compound IA.) Compound IA is useful for the treatment of a variety of diseases and conditions, such as respiratory tract and skin and skin structure infections. Accordingly, the invention is further directed to pharmaceutical compositions comprising Compound IA. The invention is still further directed to methods of treating respiratory tract and skin and skin structure infections using Compound IA or a pharmaceutical composition comprising Compound IA.

摘要翻译： 本发明涉及反式-3-氨基环丁基（1S，2R，3S，4S：，6R，7R，8R-，14R）-4-乙烯基-3-羟基-2,4,7的L-酒石酸盐， 14-四甲基-9-氧代三环[5.4.3.01,8]十四碳-6-亚氨基二碳酸酯（化合物IA）化合物1A可用于治疗各种疾病和病症，例如呼吸道和皮肤和皮肤结构感染 。 因此，本发明进一步涉及包含化合物IA的药物组合物。 本发明还涉及使用化合物IA或包含化合物IA的药物组合物治疗呼吸道和皮肤和皮肤结构感染的方法。