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1. 发明申请

WO2007039470A1 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 审中-公开
标题翻译： 4-苯基-6-取代的嘧啶-2-羰基衍生物
公开(公告)号：WO2007039470A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066562
申请日：2006-09-21
申请人： N.V. ORGANON , RANKOVIC, Zoran , CAI, Jiaqiang
发明人： RANKOVIC, Zoran , CAI, Jiaqiang
IPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/36 , C07D403/04 , C07D401/04 , C07D403/12 , C07D401/12 , A61K31/505 , A61K31/506 , A61P19/10 , A61P9/10
CPC分类号： C07D239/34 , C07D239/36 , C07D239/38 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12
摘要： The invention relates to 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula (I) wherein R represents 1-3 optional substituents independently selected from (C 1-4 )- alkyl (optionally substituted with one or more halogens), (C 1-4 )alkyloxy (optionally substituted with one or more halogens) and halogen; X is NR 1 , O or S; R 1 is H or (C 1-4 )alkyl; Y is (C 1-4 )alkyl, benzyl or (C 2-6 )alkyl, substituted with a group selected from OH, (C 1-4 )alkyloxy, NR 2 R 3 , a 4-8 membered saturated heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S and NR 4 , and a 5 or 6-membered aromatic heterocyclic group comprising 1-4 N atoms; or R 1 and Y form together with the nitrogen to which they are bonded a 5-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S, NR 4 and NO; the ring being optionally substituted with NR 2 R 3 or with 1 to 4 (C 1-3 )alkyl groups; R 2 and R 3 are independently H or (C 1-4 )alkyl; or R 2 and R 3 form together with the nitrogen to which they are bonded a 4-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S and NR 4 ; R 4 is H, (C 1-6 )alkyl,(C 3-6 ) cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-4 )alkyloxy-(C 1-4 )alkyl, benzyl, amido- (C 1-4 )alkyl, (C 1-6 )alkyloxycarbonyl(C 1-4 )alkyl or carboxy(C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the preparation of a medicament for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.
摘要翻译：本发明涉及具有式（I）的4-苯基-6-取代 - 嘧啶-2-甲腈衍生物，其中R表示1-3个任选的取代基，其独立地选自（C 1-4 - ） - 烷基（任选被一个或多个卤素取代），（C 1-4烷基）烷氧基（任选被一个或多个卤素取代）和卤素; X是NR 1，O或S; R 1是H或（C 1-4烷基）烷基; Y是（C 1-4 - ）烷基，苄基或被选自OH，（C 1-4）烷基的（C 1-6）烷基取代的（C 1-6 - NR 3 R 3，含有1或2个选自O，S和NR 4的杂原子的4-8元饱和杂环和含有1-4个N原子的5或6元芳族杂环基; 或R 1和Y与它们所键合的氮一起形成5-8元饱和杂环，任选地包含另外的选自O，S，NR 4的杂原子 >和NO; 该环任选地被NR 2 R 3 3或与1至4个（C 1-3 - ）烷基取代; R 2和R 3独立地是H或（C 1-4烷基）烷基; 或R 2和R 3 3与它们所连接的氮一起形成4-8元饱和杂环，任选地包含另外的选自O，S的杂原子和 NR _{4 ; R 4是H，（C 1-6）烷基，（C 3-6）环烷基，（C 3-6）（C 1-4）烷基，（C 1-4烷基）烷氧基 - （C 1-4 - ）烷基，苄基，酰氨基 - （C 1-4 - ）烷基，（C 1-6 - ）烷氧基羰基（C 1-4 - ）烷基或羧基（C _{1-4 ）烷基; 或其药学上可接受的盐，包含其的药物组合物，以及这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物在制备用于治疗组织蛋白酶K和组织蛋白酶的药物中的用途 S相关疾病，例如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛。}}

2. 发明申请

WO2006040300A1 4-CYCLOALKYL-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 审中-公开
标题翻译： 4-环丙基 - 嘧啶-2-羰基衍生物
公开(公告)号：WO2006040300A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/055091
申请日：2005-10-07
申请人： AKZO NOBEL N.V. , CAI, Jiaqiang , RANKOVIC, Zoran
发明人： CAI, Jiaqiang , RANKOVIC, Zoran
IPC分类号： C07D239/28 , C07D401/12 , C07D401/06
CPC分类号： C07D239/28 , C07D401/06 , C07D401/12
摘要： The invention relates to 4-cycloalkyl-pyrimidine-2-carbonitrile derivatives having the general formula (I) wherein n is 0, 1, 2 or 3; R 1 is H or (C 1-6 )alkyl; R 2 is (C 2-6 )alkyl, optionally substituted with one or more halogens, OH, (C 1-4 )alkyloxy or NR 3 R 4 ; R 3 and R 4 are independently H, (C 1-4 )alkyl, (C 3-8 )cycloalkyl, (C 3-8 )cycloalkyl(C 1-4 )alkyl, (C 6-10 )aryl, (C 6-10 )aryl(C 1-4 )alkyl, (C 2-9 )heteroaryl, (C 2-9 )heteroaryl(C 1-4 )alkyl or (C 1-4 )alkyl substituted with a 4-8 membered saturated heterocyclic ring comprising 1-3 heteroatoms selected from O, S and NR 5 ; or R 3 and R 4 together with the nitrogen to which they are bound form a 4-8 membered saturated heterocyclic ring, which ring optionally comprises NR 5 , and which ring is optionally substituted with (C 6-10 )aryl, (C 6-10 )aryloxy, (C 6-10 )aryl(C 1-4 )alkyloxy, (C 2-9 )heteroaryl, NR 6 ,R 7 , CONR 6 R 7 or NR 6 COR 7 ; R 5 is H, (C 1-4 )alkyl, (C 6-10 )aryl, (C 6-10 )aryl(C 1-4 )alkyl, (C 2-5 ) heteroaryl or (C 2-5 )heteroaryl(C 1-4 )alkyl; R 6 and R 7 are independently H or (C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said compounds as well as to the use thereof in the treatment of osteoporosis, atherosclerosis and related disorders.
摘要翻译：本发明涉及具有通式（I）的4-环烷基 - 嘧啶-2-甲腈衍生物，其中n为0,1,2或3; R 1是H或（C 1-6 - ）烷基; R 2是（C 2-6）烷基，任选被一个或多个卤素OH，（C 1-4烷基）烷氧基或 NR _{3 - [R _{4 ; R 3和R 4独立地为H，（C 1-4烷基）烷基，（C 1-3 - ）环烷基，（C 3-8）环烷基（C 1-4-4烷基）烷基，（C 1-6-10）芳基，（C < （C 1-4-20）芳基（C 1-4 - ）烷基，（C 2-9）杂芳基，（C 2-9 < （C 1-4）烷基或被含有1-3个选自以下杂原子的4-8元饱和杂环取代的（C 1-4烷基）烷基由O，S和NR 5取代; 或R 3和R 4与它们所连接的氮一起形成4-8元饱和杂环，该环任选地包含NR 5，（C 6〜10）芳基，（C 6〜10）芳氧基，（C 6〜10）芳基，（C 1-4）烷氧基，（C 2-9）杂芳基，NR 6，R 7， CONR 6，R 7或NR 6 COR 7;和/或NR 6。 R 5是H，（C 1-4）烷基，（C 6-10）芳基，（C 6-10）（C 1-4）烷基，（C 2-5）杂芳基或（C 2-5）杂芳基（C 1-4）（C _{1-4 ）烷基; R 6和R 7独立地是H或（C 1-4 - ）烷基; 或其药学上可接受的盐。本发明还涉及包含所述化合物的药物组合物以及其在治疗骨质疏松症，动脉粥样硬化和相关病症中的用途。}}}

3. 发明申请

WO2004071445A3 2-(AMINOMETHYL)ARYLAMIDE ANALGESICS 审中-公开
标题翻译： 2-（氨基甲酰基）亚胺酰胺
公开(公告)号：WO2004071445A3
公开(公告)日：2004-09-16
申请号：PCT/US2004004017
申请日：2004-02-11
申请人： PHARMACOPEIA DRUG DISCOVERY , HO KOC-KAN , BALDWIN JOHN J , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , MCDONALD EDWARD , GUO TAO , MORPHY JOHN RICHARD , RANKOVIC ZORAN , HORLICK ROBERT , APPELL KENNETH C
发明人： HO KOC-KAN , BALDWIN JOHN J , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , MCDONALD EDWARD , GUO TAO , MORPHY JOHN RICHARD , RANKOVIC ZORAN , HORLICK ROBERT , APPELL KENNETH C
IPC分类号： C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04 , C07C237/30 , A61K31/166 , A61K31/4035 , A61K31/404 , A61K31/435 , A61K31/55 , C07C237/32 , C07D217/16
CPC分类号： C07C237/30 , C07C237/32 , C07C311/08 , C07C311/37 , C07C323/42 , C07C2602/10 , C07C2602/12 , C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04
摘要： A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the Formula I: a representative example is:
摘要翻译：公开了可用作止痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由式I表示：代表性的例子是：

4. 发明申请

WO2007080191A1 6-PHENYL-1H-IMIDAZO[4, 5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN K AND S INHIBITORS 审中-公开
标题翻译： 6-苯基-1H-咪唑并[4,5-C]吡啶-4-羰基酮衍生物作为CATHEPSIN K和S抑制剂
公开(公告)号：WO2007080191A1
公开(公告)日：2007-07-19
申请号：PCT/EP2007/050356
申请日：2007-01-15
申请人： N.V. ORGANON , CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , CUMMING, Iain , GILLESPIE, Jonathan
发明人： CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , CUMMING, Iain , GILLESPIE, Jonathan
IPC分类号： C07D471/04 , A61K31/437 , A61P19/00 , C07D519/00 , C07F7/10
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，涉及包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛如神经性疼痛的药物。

5. 发明申请

WO2005011703A1 2-CYANO-1,3,5-TRIAZINE-4,6-DIAMINE DERIVATIVES 审中-公开
标题翻译： 2-氰基-1,3,5-三嗪-4,6-二胺衍生物
公开(公告)号：WO2005011703A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051587
申请日：2004-07-23
申请人： AKZO NOBEL N.V. , RANKOVIC, Zoran , CAI, Jiaqiang , CUMMING, Iain
发明人： RANKOVIC, Zoran , CAI, Jiaqiang , CUMMING, Iain
IPC分类号： A61K31/53
CPC分类号： C04B35/632 , A61K31/53 , C07D251/48 , C07D401/12 , C07D405/12
摘要： The invention relates to the use of a 2-cyano-1,3,5-triazine -4,6-diamine derivative having general formula (I), wherein R 1 is (C 1-6 )alkyl, (C 3-8 )cycloalkyl, aryl, aryl(C 1-4 )alkyl, aryloxy(C 1-4 )alkyl, heteroaryl or heteroaryloxy(C 1-4 )alkyl; R 2 is H or (C 1-4 )alkyl; or R 1 and R 2 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR 5 , which ring may be substituted with (C 1-4 )alkyl, (C 3-8 )cycloalkyl, aryl, aryl(C 1-4 )alkyl or NR 6 R 7 ,and which ring may be fused to a benzene ring; R 3 is (C 1-6 )alkyl, (C 3-8 ) cycloalkyl (optionally comprising 1 or more heteroatoms selected from O, S or NR8), aryl, aryl(C 1-4 )alkyl or heteroaryl; R 4 is H or (C 1-4 )alkyl; or R 3 and R 4 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR 9 ; R 5 , R 8 and R 9 are independently H, (C 1-4 )alkyl, (C 3-8 ) cycloalkyl, aryl or aryl(C 1-4 )alkyl; R 6 and R 7 are independently H or (C 1-4 )alkyl; or R 6 and R 7 form together with the nitrogen to which they are bound a 4-8 membered heterocyclic ring; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of osteoporosis and atherosclerosis.
摘要翻译：本发明涉及具有通式（I）的2-氰基-1,3,5-三嗪-4,6-二胺衍生物，其中R 1为（C 1-6）烷基，（C 3-8）环烷基，芳基（C 1-4）烷基，芳氧基（C 1-4）烷基，杂芳基或杂芳氧基（C 1-4）烷基; R2是H或（C1-4）烷基; 或R 1和R 2与它们所连接的氮一起形成4-8元杂环，任选地还包含1个或多个选自O，S或NR 5的杂原子，该环可以被（C 1-4）烷基取代，（C 3-8）环烷基，芳基，芳基（C 1-4）烷基或NR 6 R 7，并且该环可以与苯环稠合; R 3是（C 1-6）烷基，（C 3-8）环烷基（任选地包含1个或多个选自O，S或NR 8的杂原子），芳基，芳基（C 1-4）烷基或杂芳基; R4是H或（C1-4）烷基; 或R 3和R 4与它们所连接的氮一起形成4-8元杂环，任选地还包含1个或多个选自O，S或NR 9的杂原子; R5，R8和R9分别是H，（C1-4）烷基，（C3-8）环烷基，芳基或芳基（C1-4）烷基; R 6和R 7独立地为H或（C 1-4）烷基; 或者R6和R7与它们所结合的氮一起形成4-8元杂环; 或其药学上可接受的盐，用于制备用于治疗骨质疏松症和动脉粥样硬化的药物。

6. 发明申请

WO2003068220A1 1-ARYLSULFONYL-3-SUBSTITUTED INDOLE AND INDOLINE DERIVATIVES USEFUL IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：用于治疗中枢神经系统疾病的1-ARYLSULFONYL-3替代的吲哚和吲哚衍生物
公开(公告)号：WO2003068220A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/050010
申请日：2003-02-05
申请人： AKZO NOBEL N.V. , SPINKS, Daniel , ARMER, Richard E. , MILLER, David J. , RANKOVIC, Zoran , SPINKS, Gayle , MESTRES, Jordi , JAAP, David, Robert
发明人： SPINKS, Daniel , ARMER, Richard E. , MILLER, David J. , RANKOVIC, Zoran , SPINKS, Gayle , MESTRES, Jordi , JAAP, David, Robert
IPC分类号： A61K31/40
CPC分类号： C07D401/12 , C07D209/18 , C07D209/42 , C07D401/14 , C07D403/12
摘要： The present invention relates to 1- arylsulfonyl-3 substituted indoline derivatives having the general formula (I) (I) wherein the dotted line represents an optional bond, n is 0 or 1, m is 0-5 and Ar, R6-R11 are as defined in the description. The invention further relates to pharmaceutical compositions comprising the said derivatives, and to the use of these 1- arylsulfonyl-3- substituted indole or indoline derivatives in the treatment of central nervous disorders such as psychosis, schizophrenia, manic depressions, depressions, neurological disorders, cognitive enhancement, Parkinson' s disease, amyotrophic lateral sclerosis, Alzheimer' s disease and Huntington' s disease.
摘要翻译：本发明涉及具有通式（I）（I）的1-芳基磺酰基-3取代的二氢吲哚衍生物，其中虚线表示任意键，n为0或1，m为0-5，Ar，R6-R11为如说明书中所定义。本发明还涉及包含所述衍生物的药物组合物，以及这些1-芳基磺酰基-3-取代的吲哚或二氢吲哚衍生物在治疗中枢神经障碍如精神病，精神分裂症，躁狂抑郁症，沮丧，神经障碍，认知增强，帕金森病，肌萎缩性侧索硬化，阿尔茨海默病和亨廷顿舞蹈病。

7. 发明申请

WO2009147167A1 INDANE DERIVATIVES AS AMPA RECEPTOR MODULATORS 审中-公开
标题翻译：印度衍生物作为AMPA受体调节剂
公开(公告)号：WO2009147167A1
公开(公告)日：2009-12-10
申请号：PCT/EP2009/056791
申请日：2009-06-03
申请人： N.V. ORGANON , GILLESPIE, Jonathan , JAMIESON, Craig , MACLEAN, John, Kinnaird, Ferguson , MOIR, Elizabeth, Margaret , RANKOVIC, Zoran
发明人： GILLESPIE, Jonathan , JAMIESON, Craig , MACLEAN, John, Kinnaird, Ferguson , MOIR, Elizabeth, Margaret , RANKOVIC, Zoran
IPC分类号： C07D231/12 , C07D231/14 , C07D231/18 , C07D405/12 , C07D409/12 , C07D471/04 , A61K31/415 , A61P25/00
CPC分类号： C07D231/14 , C07D231/12 , C07D231/18 , C07D405/12 , C07D409/12 , C07D471/04
摘要： The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
摘要翻译：本发明涉及式（I）的杂环衍生物; 其中变量如说明书中所定义，或其药学上可接受的盐或溶剂化物。本发明还涉及包含所述杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防需要由AMPA受体介导的突触应答增强的精神疾病，包括精神分裂症，抑郁症和阿尔茨海默病。

8. 发明申请

WO2008003452A1 PYRAZOLEALKANAMIDE SUBSTITUTED THIOPHENES AS AMPA POTENTIATORS 审中-公开
标题翻译：作为AMPA电位器的吡唑烷酰胺取代噻吩
公开(公告)号：WO2008003452A1
公开(公告)日：2008-01-10
申请号：PCT/EP2007/005851
申请日：2007-07-02
申请人： N.V. ORGANON , GILLEN, Kevin, James , JAMIESON, Craig , MACLEAN, John, Kinnaird, Ferguson , MOIR, Elizabeth, Margaret , RANKOVIC, Zoran
发明人： GILLEN, Kevin, James , JAMIESON, Craig , MACLEAN, John, Kinnaird, Ferguson , MOIR, Elizabeth, Margaret , RANKOVIC, Zoran
IPC分类号： C07D409/12 , C07D409/14 , A61K31/497 , A61P25/28 , C07D417/14 , C07D495/04
CPC分类号： C07D409/12 , C07D409/14 , C07D471/04 , C07D495/04
摘要： The present invention relates to a heterocyclic derivative according to Formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
摘要翻译：本发明涉及式（I）的杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防需要由AMPA受体介导的突触应答增强的精神疾病，包括精神分裂症，抑郁症和阿尔茨海默病。

9. 发明申请

WO2004071445A2 2-(AMINOMETHYL)ARYLAMIDE ANALGESICS 审中-公开
标题翻译： 2-（氨基甲基）丙酰胺解毒剂
公开(公告)号：WO2004071445A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/004017
申请日：2004-02-11
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
发明人： HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
IPC分类号： A61K
CPC分类号： C07C237/30 , C07C237/32 , C07C311/08 , C07C311/37 , C07C323/42 , C07C2602/10 , C07C2602/12 , C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04
摘要： A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the Formula I: a representative example is:
摘要翻译：公开了可用作镇痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由公式I表示：一个代表性的例子是：

10. 发明申请

WO2003010132A1 N-[(1-DIMETHYLAMINOCYCLOALKYL)METHYL]BENZAMIDE DERIVATIVES 审中-公开
标题翻译： N - [（1-二甲基氨基甲酰基）甲基]苯甲酰胺衍生物
公开(公告)号：WO2003010132A1
公开(公告)日：2003-02-06
申请号：PCT/EP2002/007892
申请日：2002-07-11
申请人： AKZO NOBEL N.V. , MORPHY, John, Richard , RANKOVIC, Zoran
发明人： MORPHY, John, Richard , RANKOVIC, Zoran
IPC分类号： C07C233/79
CPC分类号： C07D333/16 , C07C235/50 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18
摘要： The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide I derivatives having the general formula (I) wherein n is 0, 1, 2 or 3; R 1 and R 2 are independently H, (C 1-4 )alkyl or (C 1-4 )alkyloxy; R3 is (C 3-8 )alkyl, (C 4-7 )cycloalkyl, (C 4-7 )cycloalkyl (C 1-3 )alkyl, (C 6-12 )aryl(C 1-3 )alkyl (wherein the aryl moiety is optionailly substituted with 1-3 substituents selected from (C1-4)alkyl, (C 1-4 )alkyloxy, halogen, trifluoromethyl and methoxycarbonyl), or (C 4-9 )- heteroaryl(C 1-3 )alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives in the treatment of disorders or conditions which are responsive to inhibition of the GlyT-2 transporter, such as muscle spasticity, epilepsy and, particularly, acute, chronic and neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺I衍生物，其中n为0,1,2或3; R1和R2独立地为H，（C1-4）烷基或（C1-4）烷氧基; R3是（C3-8）烷基，（C4-7）环烷基，（C4-7）环烷基（C1-3）烷基，（C6-12）芳基（C1-3）烷基（其中芳基部分选择性地被 1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，卤素，三氟甲基和甲氧基羰基的取代基）或（C 4-9） - 杂芳基（C 1-3）烷基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物用于治疗对抑制GlyT-2转运蛋白有响应的病症或病症的用途，例如肌肉痉挛，癫痫，特别是急性，慢性和神经性疼痛。

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