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1. 发明专利

CA2020288A1 AMINOALKYL-SUBSTITUTED 2-AMINOTHIAZOLES AND THERAPEUTIC AGENTS CONTAINING THEM 未知
公开(公告)号：CA2020288A1
公开(公告)日：1991-01-19
申请号：CA2020288
申请日：1990-07-03
申请人： RENDENBACH MUELLER BEATRICE , UNGER LILIANE , TESCHENDORF HANS JUERGEN
发明人： RENDENBACH-MUELLER BEATRICE , UNGER LILIANE , TESCHENDORF HANS-JUERGEN
IPC分类号： C07D277/20 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61P25/00 , A61P43/00 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/00 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/395
摘要： - 18 - O.Z. 0050/40949 Aminoalkyl-substituted 2aminothiazole derivatives of the general formula I where R1 and R2, which may be identical or different, are each hydrogen, C1-C5-alkyl, phenyl or C1-C5-alkanoyl, R3 is C1-C5-alkyl, phenyl which is unsubstituted or monosubstituted by halogen, C1-C5-alkyl or C1-C5-alkoxy, or thienyl, n is an integer of from 2 to 6, and NR4R5 is one of the groups a, b, c or d , , , , a b c d where Ar is a phenyl ring which is unsubstituted or monosubstituted by C1-C5-alkyl, C1-C5-alkoxy, halogen, hydroxyl, nitro or trifluoromethyl, or is pyridyl, pyrimidinyl or thienyl, R6 is H or C1-C5-alkyl and R7 is phenyl which is unsubstituted or monosubstituted by C1C5-alkyl, C1-C5 alkoxy, halogen, hydroxyl or trifluoromethyl, or R7 is thienyl, with the proviso that R3 is C1C5-alkyl only when either R1 and R2 are not both simultaneously H or when NR4R5 is the group d, and their salts with physiologically tolerated acids, their preparation, their use for the preparation of a drug, and the drugs.

2. 发明申请

WO2012059431A1 BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译：适用于治疗SEROTONIN 5-HT6受体调节障碍的苯并呋喃或磺酰胺化合物
公开(公告)号：WO2012059431A1
公开(公告)日：2012-05-10
申请号：PCT/EP2011/069007
申请日：2011-10-28
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , HAUPT, Andreas , POHLKI, Frauke , UNGER, Liliane , RELO, Ana Lucia , WICKE, Karsten , ZHANG, Min
发明人： HAUPT, Andreas , POHLKI, Frauke , UNGER, Liliane , RELO, Ana Lucia , WICKE, Karsten , ZHANG, Min
IPC分类号： C07D209/52 , C07D211/24 , C07D221/06 , A61K31/403 , A61P25/00 , A61K31/439
CPC分类号： C07D209/52 , C07D211/24 , C07D221/06
摘要： The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae (IA) and (IB) wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor.
摘要翻译：本发明涉及式（IA）和（IB）的苯磺酰基或磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

3. 发明申请

WO2010125134A1 N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译： N-苯基 - （哌嗪酰基或对羟基苯甲酰基） - 苯磺酰胺或苯并呋喃基 - 苯基 - （哌嗪或或邻苯二酚）化合物，适用于治疗调节SEROTONIN 5-HT6受体的病症
公开(公告)号：WO2010125134A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055789
申请日：2010-04-29
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , HAUPT, Andreas , POHLKI, Frauke , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , RELO, Ana-Lucia , BESPALOV, Anton , VOGG, Barbara , BACKFISCH, Gisela , DELZER, Juergen , ZHANG, Min , LAO, Yanbin
发明人： HAUPT, Andreas , POHLKI, Frauke , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , RELO, Ana-Lucia , BESPALOV, Anton , VOGG, Barbara , BACKFISCH, Gisela , DELZER, Juergen , ZHANG, Min , LAO, Yanbin
IPC分类号： C07D241/04 , C07D317/06 , C07D295/096 , A61K31/495 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D295/096 , C07D241/04 , C07D243/08 , C07D317/46
摘要： The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)- benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds,pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. wherein X is a bond or a group N-R 4 ; R 1 is hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen, C 1 -C 3 alkyl, fluorine, C 1 -C 2 alkoxy or fluorinated C1-C 2 alkoxy; R 4 is hydrogen, C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl, or C 3 -C 4 cycloalkyl-CH 2 -; R 5 is hydrogen, fluorine, chlorine, C 1 -C 2 alkyl, fluorinated C1-C2 alkyl, C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 6 is hydrogen, fluorine or chlorine; and n is 1 or 2.
摘要翻译：本发明涉及N-苯基 - （哌嗪基或高哌嗪基） - 苯磺酰胺或苯磺酰基 - 苯基 - （哌嗪或高哌嗪）化合物，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。其中X为键或基团N-R4; R1是氢或甲基; R2是氢或甲基; R3是氢，C1-C3烷基，氟，C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基，C3-C4环烷基或C3-C4环烷基-CH2-; R5是氢，氟，氯，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯; 且n为1或2。

4. 发明申请

WO2009071691A2 OXINDOL-DERIVATE UND IHRE VERWENDUNG ALS MEDIKAMENT 审中-公开
标题翻译：羟吲哚衍生物及其药物缓释
公开(公告)号：WO2009071691A2
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066937
申请日：2008-12-05
申请人： ABBOTT GMBH & CO. KG , NETZ, Astrid , OOST, Thorsten , GENESTE, Hervé , BRAJE, Wilfried , WERNET, Wolfgang , UNGER, Liliane , HORNBERGER, Wilfried , LUBISCH, Wilfried
发明人： NETZ, Astrid , OOST, Thorsten , GENESTE, Hervé , BRAJE, Wilfried , WERNET, Wolfgang , UNGER, Liliane , HORNBERGER, Wilfried , LUBISCH, Wilfried
CPC分类号： C07D401/14 , C07D401/04 , C07D401/12 , C07D487/04 , C07D487/08
摘要： Die vorliegende Erfindung betrifft neue substituierte Oxindol-Derivate, diese enthaltende pharmazeutische Mittel und ihre Verwendung zur Behandlung von Vasopressin-abhängigen Erkrankungen.
摘要翻译：本发明涉及新的取代的羟吲哚衍生物，含有它们以及它们用于加压素依赖性疾病的治疗中使用的药物组合物。

5. 发明申请

WO2009056632A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：WO2009056632A1
公开(公告)日：2009-05-07
申请号：PCT/EP2008/064811
申请日：2008-10-31
申请人： ABBOTT GMBH & CO. KG , BRAJE, Wilfried , TURNER, Sean Colm , HAUPT, Andreas , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , WERNET, Wolfgang , MAYRER, Matthias , JONGEN-RELO, Ana Lucia , BESPALOV, Anton , ZHANG, Min
发明人： BRAJE, Wilfried , TURNER, Sean Colm , HAUPT, Andreas , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , WERNET, Wolfgang , MAYRER, Matthias , JONGEN-RELO, Ana Lucia , BESPALOV, Anton , ZHANG, Min
IPC分类号： C07D295/12 , C07D405/12 , A61K31/495 , A61K31/496 , A61P3/04 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. wherein R 1 is hydrogen or methyl R 2 is hydrogen or methyl R 3 hydrogen, fluorine C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 4 is hydrogen, C 1 -C 4 alkyl or fluorinated C 1 -C 4 alkyl; R 5 is hydrogen, fluorine, C 1 -C 2 alkyl, fluorinated C 1 -C 2 alkyl, C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; and R 6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。其中R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

6. 发明申请

WO2006072458A3 SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：取代的氧杂吲哚衍生物，含有它们的药物及其用途
公开(公告)号：WO2006072458A3
公开(公告)日：2006-10-05
申请号：PCT/EP2005014150
申请日：2005-12-30
申请人： ABBOTT GMBH & CO KG , LUBISCH WILFRIED , OOST THORSTEN , WERNET WOLFGANG , UNGER LILIANE , HORNBERGER WILFRIED , GENESTE HERVE
发明人： LUBISCH WILFRIED , OOST THORSTEN , WERNET WOLFGANG , UNGER LILIANE , HORNBERGER WILFRIED , GENESTE HERVE
IPC分类号： C07D401/12 , A61K31/496 , A61P25/00 , C07D403/12 , C07D417/12
CPC分类号： C07D209/40 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/14
摘要： The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in Claim I, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
摘要翻译：本发明涉及其中取代基A，B，X和Y如权利要求1中定义的通式（I）的新的羟吲哚衍生物，含有它们以及它们用于加压素依赖性和/或预防和/或治疗的药物组合物催产素依赖性疾病。

7. 发明申请

WO2006058753A1 TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULAIONT OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：适用于治疗多巴胺D3受体调节症状的三唑化合物
公开(公告)号：WO2006058753A1
公开(公告)日：2006-06-08
申请号：PCT/EP2005/012856
申请日：2005-12-01
申请人： ABBOTT GMBH & CO. KG , UNGER, Liliane , HAUPT, Andreas , BEYERBACH, Armin , DRESCHER, Karla , BRAJE, Wilfried , DARBYSHIRE, John , TURNER, Sean, C. , BACKFISCH, Gisela
发明人： UNGER, Liliane , HAUPT, Andreas , BEYERBACH, Armin , DRESCHER, Karla , BRAJE, Wilfried , DARBYSHIRE, John , TURNER, Sean, C. , BACKFISCH, Gisela
IPC分类号： A61K31/506 , C07D403/12 , A61P25/18
CPC分类号： C07D403/12
摘要： The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R 1 on the remaining carbon atom and a radical R 1a on one of the nitrogen atoms; R 1 is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxymethyl, fluorinated C 1 -C 6 alkyl, fluorinated C 3 -C 6 cycloalkyl, fluorinated C 1 -C 4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R 1a is hydrogen or C 1 -C 4 alkyl; and R 2 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, fluorinated C 1 -C 6 alkyl or fluorinated C 3 -C 6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceuticaly composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D 3 receptor antagonists or dopamine D 3 agonists, said method comprising administering an effective amount of at least one traizole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.
摘要翻译：本发明涉及式（I）化合物，其中n是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基和其中一个氮原子上的基团R 1a; R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基，杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及该化合物的生理耐受酸加成盐。本发明还涉及包含至少一种式（I）的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D 3受体拮抗剂或多巴胺D 3激动剂，所述方法包括给受试者施用有效量的式（I）化合物或生理学耐受的酸加成盐，需要。

8. 发明申请

WO2006040178A1 ARYLSULFONYLMETHYL OR ARYLSULFONAMIDE SUBSTITUTED AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MADULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译： ARYLSULFONYLMETHYL或ARYLSULFANAMID替代芳香化合物适用于治疗多巴胺D3受体制剂的病症
公开(公告)号：WO2006040178A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011091
申请日：2005-10-14
申请人： ABBOTT GMBH & CO.KG , DRESCHER, Karla , HAUPT, Andreas , UNGER, Liliane , TURNER, Sean, C. , BRAJE, Wilfried , GRANDEL, Roland , HENRY, Christophe
发明人： DRESCHER, Karla , HAUPT, Andreas , UNGER, Liliane , TURNER, Sean, C. , BRAJE, Wilfried , GRANDEL, Roland , HENRY, Christophe
IPC分类号： C07D311/04 , C07D215/38 , C07C211/19 , A61K31/13 , A61K31/47 , A61K31/35 , A61P25/16
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH 2i O or S; E is CR 6 R 7 or NR 3 ; R 1 is C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C4-cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C,-C 3 -alkylcarbonyl; R 1a is H, C 2 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, or R 1a and R 2 together are (CH 2 ) n with n being 2 or 3, or R 1 a and R 2a together are (CH 2 ) n with n being 2 or 3; R 2 and R 2a are independently of each other H, CH 3 , CH 2 F, CHF 2 or CF 3 ; R 3 is H or C 1 -C 4 -alkyl; R 6 , R 7 independently of each other are selected from H, C 1 -C 2 -alkyl and fluorinated C 1 -C 2 -alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式（I）的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以携带1个基团R 1

9. 发明申请

WO2004089905A1 N-[(PIPERAZINYL)HETARYL]ARYLSULFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译： N - [（PIPERAZINYL）HETARYL]具有多巴胺D3受体亲和性的芳香酰胺化合物
公开(公告)号：WO2004089905A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003872
申请日：2004-04-13
申请人： ABBOTT GMBH & CO. KG , BRAJE, Wilfried , HAUPT, Andreas , LUBISCH, Wilfried , GRANDEL, Roland , DRESCHER, Karla , GENESTE, Hervé , UNGER, Liliane , SAUER, Daryl, R. , TURNER, Sean, C.
发明人： BRAJE, Wilfried , HAUPT, Andreas , LUBISCH, Wilfried , GRANDEL, Roland , DRESCHER, Karla , GENESTE, Hervé , UNGER, Liliane , SAUER, Daryl, R. , TURNER, Sean, C.
IPC分类号： C07D213/76
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I ) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R a which is/are selected, independently of each other, from halogen, CN, NO 2 , C0 2 R 4 , COR 5 , C 1 -C 4 -alkyl and C 1 -C 4 -haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R b , which is/are selected from halogen, NO 2 , CN, C0 2 R 4 , COR 5 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl and C 1 -C 4 -haloalkyl, with it also being possible for two radicals R b which are bonded to adjacent C atoms of Ar to be together C 3 -C 4 -alkylene; R 1 is hydrogen, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 4 -hydroxyalkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 3 -C 4 -alkenyl or C 3 -C 4 -alkynyl; with the radicals n, R 1 , R 2 , R 3 , R 4 and R 5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D 3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.
摘要翻译：本发明涉及通式（I）的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员的二价，6元杂芳族基团，并且任选地带有一个或两个取代基R a彼此独立地选自卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4烷基和C 1 -C 4卤代烷基; Ar是苯基或6元杂芳族基，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4， COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4烷基和C 1 -C 4卤代烷基，对于与Ar的相邻C原子键合在一起为C 3 -C 4亚烷基的两个基团R b是可能的; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 C 1-4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与N-氧化物和生理上耐受的酸添加这些化合物的盐和包含至少一种如权利要求1至10中任一项所述的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物和/或至少一种I和/或N的生理上耐受的酸加成盐的药物组合物氧化物，其中适当地与生理上可接受的载体和/或辅助物质一起用于治疗对由多巴胺D3受体拮抗剂或激动剂影响的疾病，特别是用于治疗中枢神经系统疾病和肾功能紊乱。

10. 发明申请

WO1998027070A1 HETEROCYCLIC CARBOXYLIC ACID DERIVATIVES, THE PRODUCTION AND USE THEREOF AS ENDOTHELIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：杂环羧酸衍生物的生产和使用内皮素
公开(公告)号：WO1998027070A1
公开(公告)日：1998-06-25
申请号：PCT/EP1997006778
申请日：1997-12-04
申请人： BASF AKTIENGESELLSCHAFT , AMBERG, Wilhelm , JANSEN, Rolf , KLING, Andreas , KLINGE, Dagmar , RIECHERS, Hartmut , HERGENRÖDER, Stefan , RASCHACK, Manfred , UNGER, Liliane
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07D241/18
CPC分类号： C07D403/12 , C07D237/14 , C07D237/16 , C07D241/18 , C07D253/07 , C07D253/075 , C07D253/10 , C07D491/04
摘要： The present invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning cited in the description, as well as to the production and use of said substances as endothelin receptor antagonists.
摘要翻译：本发明涉及羧酸的式（I）其中取代基是在说明书，制备如所解释和作为内皮素受体拮抗剂使用的衍生物。

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