公开(公告)号：CA2172354A1

公开(公告)日：1996-09-24

申请号：CA2172354

申请日：1996-03-21

Applicant: WALDECK HARALD ,  HOELTJE DAGMAR ,  MESSINGER JOSEF ,  ANTEL JOCHEN ,  WURL MICHAEL ,  THORMAEHLEN DIRK

Inventor： WALDECK HARALD ,  HOELTJE DAGMAR ,  MESSINGER JOSEF ,  ANTEL JOCHEN ,  WURL MICHAEL ,  THORMAEHLEN DIRK

IPC: C07D223/16 ,  A61K31/33 ,  A61K31/423 ,  A61K31/428 ,  A61K31/55 ,  A61K31/554 ,  A61K38/00 ,  A61K38/05 ,  A61P7/10 ,  A61P9/00 ,  A61P43/00 ,  C07D267/14 ,  C07D281/10 ,  C07K5/078 ,  C07D267/02 ,  C07D281/02 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds with neutral endopeptidase (NEP) inhibitory activity corresponding to the formula I I in which R1 is a lower alkoxy-lower-alkyl group whose lower alkoxy radical is substituted by a lower alkoxy group, or a phenyl-lower-alkyl or phenyloxy-lower-alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or a naphthyl-lower-alkyl group, A is CH2, O or S, R2 is hydrogen or halogen, R3 is hydrogen or halogen, R4 is hydrogen or a group forming a biolabile ester, and R5 is hydrogen or a group forming a biolabile ester, and the physiologically acceptable acid addition salts thereof.

公开(公告)号：CA2172354C

公开(公告)日：2002-10-08

申请号：CA2172354

申请日：1996-03-21

Applicant: WALDECK HARALD ,  HOELTJE DAGMAR ,  MESSINGER JOSEF ,  ANTEL JOCHEN ,  WURL MICHAEL ,  THORMAEHLEN DIRK

Inventor： WALDECK HARALD ,  HOELTJE DAGMAR ,  MESSINGER JOSEF ,  ANTEL JOCHEN ,  WURL MICHAEL ,  THORMAEHLEN DIRK

IPC: C07D223/16 ,  A61K31/33 ,  A61K31/423 ,  A61K31/428 ,  A61K31/55 ,  A61K31/554 ,  A61K38/00 ,  A61K38/05 ,  A61P7/10 ,  A61P9/00 ,  A61P43/00 ,  C07D267/14 ,  C07D281/10 ,  C07K5/078 ,  C07D267/02 ,  C07D281/02 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds with neutral endopeptidase (NEP) inhibitory activity corresponding to the formula I I in which R1 is a lower alkoxy-lower-alkyl group whose lower alkoxy radical is substituted by a lower alkoxy group, or a phenyl-lower-alkyl or phenyloxy-lower-alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or a naphthyl-lower-alkyl group, A is CH2, O or S, R2 is hydrogen or halogen, R3 is hydrogen or halogen, R4 is hydrogen or a group forming a biolabile ester, and R5 is hydrogen or a group forming a biolabile ester, and the physiologically acceptable acid addition salts thereof.

公开(公告)号：WO2002092592A1

公开(公告)日：2002-11-21

申请号：PCT/EP2002/004904

申请日：2002-05-04

Applicant: SOLVAY PHARMACEUTICALS GmbH ,  JASSERAND, Daniel ,  ANTEL, Jochen ,  PREUSCHOFF, Ulf ,  BRÜCKNER, Reinhard ,  SANN, Holger ,  WURL, Michael ,  EICKELMANN, Peter

Inventor： JASSERAND, Daniel ,  ANTEL, Jochen ,  PREUSCHOFF, Ulf ,  BRÜCKNER, Reinhard ,  SANN, Holger ,  WURL, Michael ,  EICKELMANN, Peter

IPC: C07D401/06

CPC classification number: C07D401/06 ,  C07D211/32 ,  C07D405/14

Abstract: Es werden neue, Motilin-agonistisch wirksame Verbindungen der allgemeinen Formel I, worin R 1 , R 2 , R 3 , Ar und n die in der Beschreibung angegebenen Bedeutungen besitzen, sowie diese Verbindungen enthaltende Arzneimittel beschrieben. Ferner werden Verfahren zur Herstellung der neuen Verbindungen und Zwischenprodukte dieses Verfahrens beschrieben.

Abstract translation: 通式的新胃动素激动剂有效的化合物，其中R <1>，R <2>，R <3>中，Ar和n具有在说明书中给出的含义，以及被描述含有它们的药物组合物，这些化合物。 此外，用于制备本工艺的新的化合物和中间产物的方法进行说明。

公开(公告)号：WO2009050252A1

公开(公告)日：2009-04-23

申请号：PCT/EP2008/064007

申请日：2008-10-17

Applicant: SOLVAY PHARMACEUTICALS GMBH ,  SCHOEN, Uwe ,  WALDECK, Harald ,  REINECKER, Uwe ,  GREGORY, Peter-Colin ,  REICHE, Dania ,  SANN, Holger ,  WURL, Michael ,  ANTEL, Jochen

Inventor： SCHOEN, Uwe ,  WALDECK, Harald ,  REINECKER, Uwe ,  GREGORY, Peter-Colin ,  REICHE, Dania ,  SANN, Holger ,  WURL, Michael ,  ANTEL, Jochen

IPC: C07C307/02 ,  A61K31/095 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07C307/02 ,  C07C2602/42

Abstract: This invention relates to sulfamates of Formula (I), wherein R1 to R3 and n are defined in the claims, having carbonic anhydrase enzyme inhibitory activity, to medicaments comprising these compounds, to pharmaceutical compositions comprising these compounds, and to processes for the preparation of these compounds. The invention is also directed to the use of such compounds, medicaments and compositions, particularly to their use in administering them to patients to achieve a therapeutic effect.

Abstract translation: 本发明涉及式（I）的氨基磺酸盐，其中R1至R3和n在权利要求书中具有碳酸酐酶抑制活性，包含这些化合物的药物，包含这些化合物的药物组合物，以及制备 这些化合物。 本发明还涉及这些化合物，药物和组合物的用途，特别是其用于将它们施用于患者以达到治疗效果的用途。

公开(公告)号：WO2005110413A2

公开(公告)日：2005-11-24

申请号：PCT/EP2005/052281

申请日：2005-05-18

Applicant: SOLVAY PHARMACEUTICALS GMBH ,  ANTEL, Jochen ,  GREGORY, Peter-Colin ,  REINECKER, Uwe ,  WURL, Michael ,  SCHOEN, Uwe ,  WALDECK, Harald ,  FIRNGES, Michael ,  REICHE, Dania

Inventor： ANTEL, Jochen ,  GREGORY, Peter-Colin ,  REINECKER, Uwe ,  WURL, Michael ,  SCHOEN, Uwe ,  WALDECK, Harald ,  FIRNGES, Michael ,  REICHE, Dania

IPC: A61K31/495

CPC classification number: A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/519 ,  A61K31/53 ,  C07D213/74 ,  C07D295/26

Abstract: The present invention relates to the use of known and novel N-sulfamoyl-N'­arylpiperazines and their physiologically compatible acid addition salts for the prophylaxis or treatment of obesity and related conditions.

Abstract translation: 本发明涉及已知和新型N-氨磺酰-N-芳基哌嗪及其生理上相容的酸加成盐在预防或治疗肥胖症及相关病症中的用途。

公开(公告)号：WO2007054580A1

公开(公告)日：2007-05-18

申请号：PCT/EP2006/068416

申请日：2006-11-14

Applicant: SOLVAY PHARMACEUTICALS GMBH ,  ANTEL, Jochen ,  WALDECK, Harald ,  SCHOEN, Uwe ,  GREGORY, Peter-Colin ,  WURL, Michael ,  FIRNGES, Michael ,  REICHE, Dania ,  REINECKER, Uwe

Inventor： ANTEL, Jochen ,  WALDECK, Harald ,  SCHOEN, Uwe ,  GREGORY, Peter-Colin ,  WURL, Michael ,  FIRNGES, Michael ,  REICHE, Dania ,  REINECKER, Uwe

IPC: C07D491/10 ,  C07D491/20 ,  A61K31/438 ,  A61P27/06 ,  A61P25/00 ,  A61P3/00 ,  A61P35/00

CPC classification number: C07D491/10

Abstract: The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.

Abstract translation: 本发明涉及通式（I）的新型N-氨磺酰基-N'-苯并吡喃哌啶及其生理上可接受的酸加成盐，包括它们的药物组合物，其制备方法及其用于预防和/或治疗和 /或预防和/或抑制青光眼，癫痫，双相性精神障碍，偏头痛，神经性疼痛，肥胖症，II型糖尿病，代谢综合征，酒精依赖和/或癌症及其并发症和/或继发性疾病或病症。

公开(公告)号：WO2005110413A3

公开(公告)日：2006-07-13

申请号：PCT/EP2005052281

申请日：2005-05-18

Applicant: SOLVAY PHARM GMBH ,  ANTEL JOCHEN ,  GREGORY PETER-COLIN ,  REINECKER UWE ,  WURL MICHAEL ,  SCHOEN UWE ,  WALDECK HARALD ,  FIRNGES MICHAEL ,  REICHE DANIA

Inventor： ANTEL JOCHEN ,  GREGORY PETER-COLIN ,  REINECKER UWE ,  WURL MICHAEL ,  SCHOEN UWE ,  WALDECK HARALD ,  FIRNGES MICHAEL ,  REICHE DANIA

IPC: A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D213/74 ,  C07D295/22 ,  C07D295/26

CPC classification number: A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/519 ,  A61K31/53 ,  C07D213/74 ,  C07D295/26

Abstract: The present invention relates to the use of known and novel N-sulfamoyl-N'­arylpiperazines and their physiologically compatible acid addition salts for the prophylaxis or treatment of obesity and related conditions.

Abstract translation: 本发明涉及已知和新型N-氨磺酰-N-芳基哌嗪及其生理上相容的酸加成盐在预防或治疗肥胖症及相关病症中的用途。

公开(公告)号：WO2007065948A1

公开(公告)日：2007-06-14

申请号：PCT/EP2006/069482

申请日：2006-12-08

Applicant: SOLVAY PHARMACEUTICALS GMBH ,  ANTEL, Jochen ,  SCHOEN, Uwe ,  WALDECK, Harald ,  WURL, Michael ,  FIRNGES, Michael ,  REICHE, Dania ,  GREGORY, Peter-Colin

Inventor： ANTEL, Jochen ,  SCHOEN, Uwe ,  WALDECK, Harald ,  WURL, Michael ,  FIRNGES, Michael ,  REICHE, Dania ,  GREGORY, Peter-Colin

IPC: C07D211/58 ,  C07D401/04 ,  C07D409/12 ,  C07D401/12 ,  A61K31/4545 ,  A61P3/04

CPC classification number: C07D409/12 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12

Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and/or related conditions.

Abstract translation: 本发明涉及通式（I）的新型N-氨磺酰 - 哌啶酰胺及其生理上可接受的酸加成盐，涉及包含它们的药物组合物，其制备方法及其用于治疗肥胖及其伴随和/或 继发性疾病和/或相关病症。