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1. 发明授权

US06649624B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06649624B2
公开(公告)日：2003-11-18
申请号：US10226225
申请日：2002-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof
摘要翻译：一种治疗中枢神经系统疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar 1表示可被取代的芳基或杂芳基，所选择的取代基卤代低级烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基，低级烷氧基羰基，任选被氧代取代的低级亚烷基和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，该取代基选自卤素，氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示单键或羰基; T，U，V和W各自独立地表示反应可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的氮原子或次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示亚氨基，被低级烷基或氧取代; 或其盐或酯

2. 发明授权

US06635653B2 Spiropyrazole compounds 有权
标题翻译：螺吡唑化合物
公开(公告)号：US06635653B2
公开(公告)日：2003-10-21
申请号：US10126506
申请日：2002-04-18
申请人： R. Richard Goehring , Gary Lee , Parviz Gharagozloo , Sam Victory , Donald Kyle
发明人： R. Richard Goehring , Gary Lee , Parviz Gharagozloo , Sam Victory , Donald Kyle
IPC分类号： A61K31438
CPC分类号： C07D471/10
摘要： A compound of the formula (I): wherein Z, W, A, B, C, R1, R2, Q and n are as disclosed herein.
摘要翻译：式（I）的化合物：其中Z，W，A，B，C，R 1，R 2，Q和n如本文所公开。

3. 发明授权

US06506764B1 Hydroxamic and carboxylic acid derivatives 失效
标题翻译：羟肟酸和羧酸衍生物
公开(公告)号：US06506764B1
公开(公告)日：2003-01-14
申请号：US09623669
申请日：2000-09-06
申请人： Andrew Douglas Baxter , David Alan Owen , Duncan Hannah , John Gary Montana
发明人： Andrew Douglas Baxter , David Alan Owen , Duncan Hannah , John Gary Montana
IPC分类号： A61K31438
CPC分类号： C07D221/20 , C07D211/96
摘要： Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y (I) have therapeutic utility as inhibitors of metalloproteinases etc.
摘要翻译：具有治疗作用的化合物作为金属蛋白酶抑制剂等

4. 发明授权

US06790854B2 Diphenylalkylamine derivatives useful as opioid receptor agonists 失效
标题翻译：用作阿片类受体激动剂的二苯基烷基胺衍生物
公开(公告)号：US06790854B2
公开(公告)日：2004-09-14
申请号：US10221172
申请日：2003-03-13
申请人： Masaki Tsushima , Kaori Tadauchi , Kenji Asai , Naoko Miike , Toshiaki Kudo
发明人： Masaki Tsushima , Kaori Tadauchi , Kenji Asai , Naoko Miike , Toshiaki Kudo
IPC分类号： A61K31438
CPC分类号： C07D211/32
摘要： A substance having affinity for an opioid &dgr; receptor, which is represented by the following general formula (I): wherein, X represents a group of the general formula: —CO—N(R5)(R6) (II) and the like, n represents 1 to 3, R1 and R2 represent a hydrogen atom, a halogen atom, a lower alkyl group and the like, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group and the like, R4 represents a saturated or unsaturated monocyclic or bicyclic carbocyclic group and the like, R5 to R12 represent a hydrogen atom, a lower alkyl group and the like, and R3 and R4, R5 and R6, R7 or R8 and R9 and R10 may bind to each other to form a cyclic structure, and a medicament useful for preventive and/or therapeutic treatment of central nervous system diseases and peripheral nervous system diseases comprising the substance as an active ingredient.
摘要翻译：由以下通式（I）表示的对阿片样物质δ受体有亲和力的物质：其中，X表示通式-CO-N（R 5）（R 6）（R 6） II）等，n表示1〜3，R 1，R 2表示氢原子，卤素原子，低级烷基等，R 3表示氢原子，卤素原子，低级烷基等，R 4表示饱和或不饱和的单环或双环碳环基等，R 5至R 12表示氢原子，低级烷基等，和 R 3和R 4，R 5和R 6，R 7或R 8和R 9和R 10可以彼此结合形成环状结构，以及可用于预防和/或治疗中枢神经系统疾病和包含该物质作为活性成分的周围神经系统疾病的药物。

5. 发明授权

US06645973B1 Spiro(2h-1-benzopyran-2,4-piperidine)derivatives as glycine transport inhibitors 有权
标题翻译：螺（2h-1-苯并吡喃-2,4-哌啶）衍生物作为甘氨酸转运抑制剂
公开(公告)号：US06645973B1
公开(公告)日：2003-11-11
申请号：US10130557
申请日：2002-05-17
申请人： Samuel George Gibson , David John Miller
发明人： Samuel George Gibson , David John Miller
IPC分类号： A61K31438
CPC分类号： C07D491/10
摘要： The present invention relates to spiro[2H-1-benzopyran-2,4′-piperidine] derivatives having general formula (I), wherein the substituents R1, R2, X and Y are ase defined in the claims or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these spiro[2H-1-benzopyran-2,4′-piperidine] derivatives in therapy, more specifically for the treatment of CNS disorders.
摘要翻译：本发明涉及具有通式（I）的螺[2H-1-苯并吡喃-2,4'-哌啶]衍生物，其中取代基R 1，R 2，X和Y如权利要求中所定义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，以及这些螺[2H-1-苯并吡喃-2,4'-哌啶]衍生物在治疗中的用途，更具体地涉及CNS病症的治疗。

6. 发明授权

US06479501B2 Spiro[cyclopent[b]indole-piperidines] 有权
公开(公告)号：US06479501B2
公开(公告)日：2002-11-12
申请号：US09768666
申请日：2001-01-24
申请人： Mark G. Palermo , Gerard J. O'Malley
发明人： Mark G. Palermo , Gerard J. O'Malley
IPC分类号： A61K31438
CPC分类号： C07D471/10
摘要： Novel spiro[cyclopent[b]indole-piperidines], intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro[cyclopent[b]indole-piperidines] and intermediates, or compositions thereof are disclosed.

7. 发明授权

US06376505B1 5-HT1A and 5-HT1D&agr;dalpha antagonists 失效
标题翻译： 5-HT1A和5-HT1Dalphadalpha拮抗剂
公开(公告)号：US06376505B1
公开(公告)日：2002-04-23
申请号：US09423348
申请日：1999-11-22
申请人： Vincent P. Rocco
发明人： Vincent P. Rocco
IPC分类号： A61K31438
CPC分类号： C07D491/20
摘要： A class of novel substituted-aryloxy-2-ol-3-(4-spiro-(alkanedioxy)isobenzofuranyl- and phthaloyl-piperidine) derivatives is disclosed useful as 5-HT1A and 5-HT1D&agr; antagonists.
摘要翻译：公开了一类新的取代 - 芳氧基-2-醇-3-（4-螺 - （烷二氧基）异苯并呋喃基 - 和邻苯二甲酰基 - 哌啶）衍生物，其用作5-HT1A和5-HT1Dalpha拮抗剂。

8. 发明授权

US06492378B1 Substituted isoquinoline derivatives and their use as anticonvulsivants 失效
标题翻译：取代的异喹啉衍生物及其作为抗惊厥药的用途
公开(公告)号：US06492378B1
公开(公告)日：2002-12-10
申请号：US09762613
申请日：2001-02-09
申请人： John David Harling , Jag Paul Heer , Mervyn Thompson
发明人： John David Harling , Jag Paul Heer , Mervyn Thompson
IPC分类号： A61K31438
CPC分类号： C07D221/20 , C07D217/02 , C07D217/04 , C07D217/06
摘要： This invention relates to novel substituted isoquinoline derivatives and their use as anticonvulsants.
摘要翻译：本发明涉及新型取代的异喹啉衍生物及其作为抗惊厥药的用途。

9. 发明授权

US06479486B2 Azabicyclic spiroether derivatives and their use as therapeutic agents 失效
标题翻译：氮杂双环螺醚衍生物及其作为治疗剂的用途
公开(公告)号：US06479486B2
公开(公告)日：2002-11-12
申请号：US10115629
申请日：2002-04-01
申请人： Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
发明人： Ian Thomas Huscroft , Janusz Jozef Kulagowski , Piotr Antoni Raubo
IPC分类号： A61K31438
CPC分类号： C07D491/20
摘要： The present invention relates compounds of the formula (I): wherein Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（I）的化合物：其中Z是-CR 9 R 10 CH 2 - 或-CH 2 CR 9 R 10 - ;且R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。这些化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。

10. 发明授权

US06326375B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06326375B1
公开(公告)日：2001-12-04
申请号：US09640784
申请日：2000-08-18
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.
摘要翻译：通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个代表所述次甲基; X表示氮; Y表示任选取代的亚氨基或氧原子，其表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，全身性疾病等。

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