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1. 发明申请

WO2012004378A1 SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：作为S1P调节剂的螺旋环胺衍生物
公开(公告)号：WO2012004378A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061599
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , STOIT, Axel , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , VAN DONGEN, Maria J.P. , LEFLEMME, Nicolas J.-L.D.
发明人： STOIT, Axel , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , VAN DONGEN, Maria J.P. , LEFLEMME, Nicolas J.-L.D.
IPC分类号： C07D265/36 , C07D491/107 , C07D491/20 , A61K31/407 , A61K31/4355 , A61K31/5386 , A61P25/00
CPC分类号： C07D491/107 , C07D265/34 , C07D265/36 , C07D491/20 , C07F9/6561
摘要： The present invention relates spiro- cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; -W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
摘要翻译：本发明涉及式（I）的螺环胺衍生物，其中R1; R2; R3; Q; -W-T-; R5; Z者除外; 和A具有权利要求中提供的定义; 或其药学上可接受的盐，溶剂合物或水合物或其一种或多种N-氧化物。本发明的化合物对S1P受体具有亲和力，可用于治疗，缓解或预防（a）S1P受体涉及的疾病和病症。

2. 发明申请

WO2011092226A8 SYNTHESIS OF SUBSTITUTED PYRAZOLINE CARBOXAMIDINE DERIVATIVES 审中-公开
标题翻译：取代的吡唑啉甲酰胺衍生物的合成
公开(公告)号：WO2011092226A8
公开(公告)日：2011-08-04
申请号：PCT/EP2011/051100
申请日：2011-01-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , VAN LOEVEZIJN, Arnold , LANGE, Josephus H.M. , BARF, Gerrit A. , DEN HARTOG, Arnold P.
发明人： VAN LOEVEZIJN, Arnold , LANGE, Josephus H.M. , BARF, Gerrit A. , DEN HARTOG, Arnold P.
IPC分类号： C07D231/06 , C07D231/54 , C07D409/04 , C07D409/12 , C07D513/10 , C07D491/107
摘要： This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及有机化学，具体涉及制备式（I）的吡唑啉甲脒衍生物的方法，称为有效的5-HT 6拮抗剂。本发明还涉及这些化合物的新中间体。其中符号具有说明书中给出的含义。

3. 发明申请

WO2011023795A1 (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：（THIO）吗啉衍生物作为S1P调节剂
公开(公告)号：WO2011023795A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062552
申请日：2010-08-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
发明人： IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
IPC分类号： C07D265/30 , C07D265/32 , C07D413/12 , C07D419/12 , C07D471/04 , A61K31/5377 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , C07D279/12 , C07D417/12 , C07D487/04
CPC分类号： C07D295/15 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04 , C07F9/6533
摘要： The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO 2 -(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH 3 -O- and the linking group –Y-(CH 2 ) n -X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -CH 2 -O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH 2 ) 2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH 2 -R5, wherein R5 is -OH, -PO 3 H 2 , -OPO 3 H 2 , -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO 2 -; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的（硫代）吗啉衍生物，其中R 1选自氰基，（2-4C）炔基，（1-4C）烷基，（3-6C）环烷基，（4-6C）环烷基，（6-8C）双环烷基，（8-10C）双环基团，各自任选被（1-4C）烷基，苯基，联苯基，萘基取代，各自任选被一个或多个独立地选自卤素，（1- 氨基，二（1-4C）烷基氨基，-SO 2 - （1-4C）烷氧基，被一个或多个氟原子烷基取代的（2-4C）炔基，任选被一个或多个氟原子取代的（1-4C）） - （1-4C）烷基，-CO-O-（1-4C）烷基，-NH-CO-（1-4C）烷基和（3-6C）环烷基，被苯氧基取代的苯基（1-4C）烷基或任选被（1-4C）烷基任意取代的苯基的单环杂环，和任选被取代的（1-4C）烷基的双环杂环，与（1-4C）烷基; A选自-CO-O-，-O-CO-，-NH-CO-，-CO-NH，-C = C-，-CCH 3 -O-和连接基-Y-（CH 2）n X- 其中Y连接到R 1并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - CH 2 -O-，-CO-，-O-CO-，-CO-O-， -CO-NH-，-NH-CO-，-C≡C-和-C = C-; n为1〜10的整数，并且X连接到亚苯基/吡啶基上，并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH，-CO - ， - C = C - 和-C = C- ; 环结构B任选地含有一个氮原子; R2是H，任选被一个或多个氟原子取代的（1-4C）烷基，（1-4C）任选被一个或多个氟原子取代的烷氧基或卤素; 并且R 3是（1-4C）亚烷基-R 5，其中亚烷基可以被（CH 2）2取代以形成环丙基部分或一个或两个卤素原子，或者R 3是（3-6C）亚环烷基-R 5或-CO -CH 2 -R 5，其中R 5是-OH，-PO 3 H 2，-OPO 3 H 2，-COOH，-COO（1-4C）烷基或四唑-5-基; R4是H或（1-4C）烷基; R6是一个或多个独立地选自H，（1-4C）烷基或氧代的取代基; W是-O - ， - S - ， - SO-或-SO 2 - ; 或其药学上可接受的盐，溶剂合物或水合物; 条件是式（I）的衍生物不是2-（4-乙基苯基）-4-吗啉代乙醇或4- [4-（2-羟乙基）-2-吗啉基]苯乙腈或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物对S1P受体具有亲和力，可用于治疗，缓解或预防S1P受体介导的疾病和病症。

4. 发明申请

WO2011005098A1 PEPTIDE LIGANDS FOR TARGETING TO THE BLOOD-BRAIN BARRIER 审中-公开
标题翻译：用于靶向血脑屏障的肽配体
公开(公告)号：WO2011005098A1
公开(公告)日：2011-01-13
申请号：PCT/NL2010/050448
申请日：2010-07-12
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , UNIVERSITEIT LEIDEN , UNIVERSITEIT UTRECHT HOLDING B.V. , VAN ROOY, Inge , HENNINK, Wilhelmus Everhardus , MASTROBATTISTA, Enrico , SCHIFFELERS, Raymond Michel , DINTER-HEIDORN, Heike , BRINKHUIS, Rene Pascal , VAN HEST, Jan , RUTJES, Floris Peter Johannes Theodorus
发明人： VAN ROOY, Inge , HENNINK, Wilhelmus Everhardus , MASTROBATTISTA, Enrico , SCHIFFELERS, Raymond Michel , DINTER-HEIDORN, Heike , BRINKHUIS, Rene Pascal , VAN HEST, Jan , RUTJES, Floris Peter Johannes Theodorus
IPC分类号： C07K7/08 , A61K47/48
CPC分类号： B82Y5/00 , A61K47/66 , A61K47/6911 , A61K47/6915 , C07K7/08 , C07K2319/01
摘要： The present invention relates to peptides comprising defined amino acid sequences, compositions comprising said peptides and a pharmaceutically acceptable substance, use of said peptides as a central nervous system targeting principle in the treatment, prophylaxis or diagnosis of a central nervous system disorders, combinations of said peptides with pharmaceutically acceptable substances, use of said combinations for the treatment, prophylaxis or diagnosis of a central nervous system disorders, a method of delivery of said peptide and of a pharmaceutically acceptable substance and a nucleic acid sequence encoding for said peptide sequence.
摘要翻译：本发明涉及包含确定的氨基酸序列的肽，包含所述肽的组合物和药学上可接受的物质，所述肽用作中枢神经系统靶向原理在治疗，预防或诊断中枢神经系统疾病中的用途，所述具有药学上可接受的物质的肽，所述组合用于治疗，预防或诊断中枢神经系统病症，递送所述肽和药学上可接受的物质的方法以及编码所述肽序列的核酸序列。

5. 发明申请

WO2010070057A3 PRECOMPACTED FAST-DISINTEGRATING FORMULATIONS OF COMPOUNDS WITH A LOW ORAL BIOAVAILABILITY 审中-公开
公开(公告)号：WO2010070057A3
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067434
申请日：2009-12-17
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , MÖSCHWITZER, Jan P. , WU, Yu-San , VAN TOMME, Sophie R. , KUIL, Henny , KET, Aldo V. , DOESBURGH-DEWIT, Lucia M.
发明人： MÖSCHWITZER, Jan P. , WU, Yu-San , VAN TOMME, Sophie R. , KUIL, Henny , KET, Aldo V. , DOESBURGH-DEWIT, Lucia M.
IPC分类号： A61K9/26 , A61K31/4155 , A61K31/4353 , A61K9/20
摘要： This invention relates to the field of pharmaceutical chemistry. Embodiments of the present invention relate to, and provide precompacted fast-disintegrating formulations of compounds with a low oral bioavailability.

6. 发明申请

WO2010003760A3 FLUORO-SUBSTITUTED 3,4-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
公开(公告)号：WO2010003760A3
公开(公告)日：2010-01-14
申请号：PCT/EP2009/057323
申请日：2009-06-15
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , LANGE, Josephus H.M. , VLIET, VAN, Bernard J.
发明人： LANGE, Josephus H.M. , VLIET, VAN, Bernard J.
IPC分类号： C07D401/12 , A61K31/4439 , A61P25/00
摘要： This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB 1 receptor antagonists, methods for preparing these compounds, novel intermediates useful for the synthesis of said compounds, methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as active ingredient, as well as the use of these pharmaceutical compositions for the treatment of obesity and obesity-related cardiovascular disorders, drug addiction, cognition deficits, liver fibrosis and inflammatory disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

7. 发明申请

WO2012004375A1 BISARYL (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译： BISARYL（THIO）MORPHOLINE衍生物作为S1P调节剂
公开(公告)号：WO2012004375A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061590
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , IWEMA BAKKER, Wouter I. , BRONGER, Raymond
发明人： IWEMA BAKKER, Wouter I. , BRONGER, Raymond
IPC分类号： C07D265/30 , C07D413/10 , A61K31/5375 , A61K31/5377 , A61P25/00
CPC分类号： A61K31/5375 , A61K31/5377 , A61K31/54 , C07D265/30 , C07D295/15 , C07D413/10
摘要： The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, -SO 2 -(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl and -NH-CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from -CO-, -NH-, -O-, -S-, -SO- or -SO 2 -; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R6 wherein the alkylene group may be substituted with (CH 2 ) 2 to form a cyclopropyl moiety or with one or more halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or -CO-CH 2 -R6, wherein R6 is -OH, -PO 3 H 2 , -OPO 3 H 2 , -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R5 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO 2 -; or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chloro-phenyl]-4-morpholineethanol. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的二芳基（硫代）吗啉衍生物，其中R 1是选自苯基，吡啶基，嘧啶基，联苯基和萘基的芳基取代基，各自任选被一个或多个独立地选自卤素的取代基取代任选被一个或多个氟原子取代的（1-4C）烷氧基，氨基，二（1-4C）烷基氨基，-SO 2 - （1-4C）烷基，-CO - （1-4C）烷基，-CO-O-（1-4C）烷基和-NH-CO-（1-4C）烷基，或被苯氧基，苄基，苄氧基，苯基乙基或吗啉基取代，各自任选被（ 1-4C）烷基和（8-10C）双环基团，各自任选被（1-4C）烷基任意地被一个或多个氟原子或氧代取代的烷基取代; A选自-CO - ， - NH - ， - O - ， - S - ， - SO-或-SO 2 - ; 环结构B任选地含有一个氮原子; R2是H，任选被一个或多个氟原子取代的（1-4C）烷基，（1-4C）任选被一个或多个氟原子取代的烷氧基或卤素; 并且R 3是（1-4C）亚烷基-R 6，其中亚烷基可以被（CH 2）2取代以形成环丙基部分或与一个或多个卤素原子，或者R 3是（3-6C）亚环烷基-R 5或-CO -CH 2 -R 6，其中R 6是-OH，-PO 3 H 2，-OPO 3 H 2，-COOH，-COO（1-4C）烷基或四唑-5-基; R4是H或（1-4C）烷基; R5是一个或多个独立地选自H，（1-4C）烷基或氧代的取代基; W是-O - ， - S - ， - SO-或-SO 2 - ; 或其药学上可接受的盐，溶剂合物或水合物，条件是式（I）的衍生物不是2- [4-（4-氯苯氧基）-2-氯 - 苯基] -4-吗啉乙醇。本发明的化合物对S1P受体具有亲和性，可用于治疗，缓解或预防S1P受体介导的疾病和病症。

8. 发明申请

WO2011045270A1 MONOHYDRATE OF PARDOPRUNOX 审中-公开
标题翻译： PARDOPRUNOX MONOHYDRATE
公开(公告)号：WO2011045270A1
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065191
申请日：2010-10-11
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , VAN RHEENEN, Jeroen , MUIJSELAAR, Wilhelmus G.H.M. , TEUNISSEN, Hendrik
发明人： VAN RHEENEN, Jeroen , MUIJSELAAR, Wilhelmus G.H.M. , TEUNISSEN, Hendrik
IPC分类号： A61K31/496 , C07D413/04 , A61P25/24
CPC分类号： A61K31/496 , C07D263/58
摘要： This invention relates to a novel process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol- 2(3H)-one hydrochloride, a partial dopamine-D 2 receptor agonist and a full serotonin 5-HT 1A receptor agonist. The invention also relates to the monohydrate of said compound, as well as to pharmaceutical compositions containing this compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in affections or diseases of the central nervous system, caused by disturbances of the dopaminergic and/or serotonergic systems, for example: anxiety disorders (including generalised anxiety, panic disorder and obsessive compulsive disorder), depression, autism, schizophrenia, Parkinson's disease, restless leg syndrome, disturbances of cognition and memory.
摘要翻译：本发明涉及制备7-（4-甲基-1-哌嗪基）苯并恶唑-2（3H） - 酮盐酸盐，部分多巴胺-D 2受体激动剂和全5-羟色胺5-HT 1A受体激动剂的新方法。本发明还涉及所述化合物的一水合物，以及含有该化合物的药物组合物，制备化合物的方法，制备用于其合成的新中间体的方法，以及制备组合物的方法。本发明还涉及这些化合物和组合物的用途，特别是它们在将其给予患者以在由多巴胺能和/或血清素能系统的紊乱引起的中枢神经系统的感觉或疾病中的治疗效果方面的用途，例如：焦虑障碍（包括广泛性焦虑，恐慌症和强迫症），抑郁症，自闭症，精神分裂症，帕金森病，不宁腿综合症，认知障碍和记忆障碍。

9. 发明申请

WO2011023796A1 BIFEPRUNOX FOR TREATING ADDICTION 审中-公开
标题翻译： BIFEPRUNOX用于治疗ADDICTION
公开(公告)号：WO2011023796A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062555
申请日：2010-08-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , H. LUNDBECK A/S , ARNT, Jørn , MCCREARY, Andrew C. , KAM, VAN DER, Elizabeth
发明人： ARNT, Jørn , MCCREARY, Andrew C. , KAM, VAN DER, Elizabeth
IPC分类号： A61K31/496 , A61P25/30
CPC分类号： A61K31/496
摘要： The present invention relates to bifeprunox for use in the treatment of a patient with a substance use disorder, in particular wherein the substance is alcohol or nicotine and or food addiction, particularly where the addictive food is sucrose, a mono-or a polysaccharide.
摘要翻译：本发明涉及用于治疗患有物质使用障碍的患者的双歧，特别是其中所述物质是醇或尼古丁和/或食物成瘾，特别是上瘾食物是蔗糖，单糖或多糖的情况。

10. 发明申请

WO2012004373A1 FUSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：作为S1P调节剂的熔融杂环衍生物
公开(公告)号：WO2012004373A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061586
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , SMID, Pieter , IWEMA BAKKER, Wouter, I. , COOLEN, Hein, K.A.C. , SLIEDREGT, Leonardus, A.J.M. , VAN DONGEN, Maria, J.P. , DEN HARTOG, Jacobus, A.J.
发明人： SMID, Pieter , IWEMA BAKKER, Wouter, I. , COOLEN, Hein, K.A.C. , SLIEDREGT, Leonardus, A.J.M. , VAN DONGEN, Maria, J.P. , DEN HARTOG, Jacobus, A.J.
IPC分类号： C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , A61P25/28 , A61K31/429 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/55
CPC分类号： C07D491/048 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified substructures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
摘要翻译：本发明涉及式（I）的稠合杂环衍生物。变量R1-R4，z，A，Q，X和Y如权利要求中所定义。以下杂环是式（I）的亚结构：式（I）化合物是S1P受体（鞘氨醇-1-磷酸受体）的调节剂，更具体地说，它们是S1P5的激动剂。该化合物在治疗认知障碍，与年龄有关的认知衰退和痴呆方面具有治疗用途。

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