公开(公告)号：US07855294B2

公开(公告)日：2010-12-21

申请号：US10590585

申请日：2005-03-04

申请人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

发明人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

IPC分类号： C07D215/26 ,  C07D491/20 ,  C07D491/107 ,  C07D401/06 ,  A61K31/438 ,  A61K31/4709 ,  A61K31/46

CPC分类号： C07D451/02 ,  C07D239/70 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

摘要翻译： 提供式[I]的环烷基吡啶衍生物：其中符号与说明书中所述的相同。 该化合物作为伤害感受肽受体拮抗剂起作用，并且可用作与伤害感受肽受体相关疾病的药物，例如作为抵抗麻醉止痛剂的缓解剂; 减轻对麻醉止痛药依赖或成瘾的缓解; 镇痛增强剂; 抗生素或食欲抑制剂; 用于认知障碍和痴呆/健忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救办法 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 或补救低血压。

公开(公告)号：US20090247560A1

公开(公告)日：2009-10-01

申请号：US12310951

申请日：2007-09-27

申请人： Makoto Ando ,  Minoru Kameda ,  Hiroshi Miyazoe ,  Minoru Moriya ,  Etsuko Sekino ,  Takao Suzuki

发明人： Makoto Ando ,  Minoru Kameda ,  Hiroshi Miyazoe ,  Minoru Moriya ,  Etsuko Sekino ,  Takao Suzuki

IPC分类号： A61K31/438 ,  C07D401/14 ,  A61P3/04 ,  A61P3/10 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D491/20

摘要： Provided is a compound of a formula (I): [wherein R1a and R1b are the same or different, representing a hydrogen atom, etc.; R2a and R2b are the same or different, representing a hydrogen atom, etc., or R2a and R2b, taken together, form —CH2CH2—, R3a and R3b are the same or different, representing a hydrogen atom, etc.; or R3a and R3b, taken together, form —CH2CH2-etc.; Y1 and Y2 represent —C(R)2—, etc.; Z represents OR, NR2, etc.; R represents a hydrogen atom, a C1-6 alkyl group, etc.; Ar1 represents a 6-membered aromatic carbocyclic group, etc.; Ar2 represents a 6-membered aromatic carbocyclic group, etc; A3 represents a 6-membered aromatic carbocyclic group etc.]. The compound is useful as a medicine for central disorders, cardiovascular disorders, metabolic disorders.

摘要翻译： 提供式（I）的化合物：其中R 1a和R 1b相同或不同，表示氢原子等; R2a和R2b相同或不同，表示氢原子等，或者R 2a和R 2b一起形成-CH 2 CH 2 - ，R 3a和R 3b相同或不同，表示氢原子等; 或R3a和R3b一起形成-CH 2 CH 2等; Y1和Y2表示-C（R）2-等; Z表示OR，NR2等; R表示氢原子，C 1-6烷基等; Ar 1表示6元芳族碳环基等。 Ar2表示6元芳族碳环基团等; A3表示6元芳族碳环基等]。 该化合物可用作中枢性疾病，心血管疾病，代谢紊乱的药物。

公开(公告)号：US20100324049A1

公开(公告)日：2010-12-23

申请号：US12676938

申请日：2008-09-26

申请人： Makoto Ando ,  Minoru Kameda ,  Hiroshi Miyazoe ,  Minoru Moriya ,  Etsuko Hirose ,  Takao Suzuki

发明人： Makoto Ando ,  Minoru Kameda ,  Hiroshi Miyazoe ,  Minoru Moriya ,  Etsuko Hirose ,  Takao Suzuki

IPC分类号： A61K31/4545 ,  C07D401/14 ,  C07D401/04 ,  C07D211/52 ,  C07D211/26 ,  C07D471/04 ,  A61K31/451 ,  A61K31/501 ,  A61K31/437 ,  A61K31/4985 ,  C07D487/04 ,  A61K31/5025 ,  A61K31/497 ,  A61P3/04 ,  A61P3/10 ,  A61P25/24 ,  A61P25/22 ,  A61P1/16 ,  A61P3/00

CPC分类号： C07D487/04 ,  C07D211/26 ,  C07D211/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  C07D451/04 ,  C07D471/04

摘要： [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease.[Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.

摘要翻译： [问题]提供黑色素浓缩激素受体的拮抗剂，其可用作中枢神经系统疾病，心血管疾病或代谢性疾病的药物。 解决问题的手段拮抗剂作为活性成分包含式（I）表示的化合物，其中R 1a和R 1b独立地表示氢原子或C 1-6烷基; R2a，R2b，R3a和R3b独立地表示氢原子，C1-6烷基等; Y表示H或-OH; Z表示-OR8等; R8表示氢原子，可以具有取代基的C1-6烷基等; R9a和R9b独立地表示氢原子，C1-6烷基等; Ar 1表示芳香族碳环基或芳香族杂环基; Ar2表示通过从芳香族碳环等除去2个氢原子而生成的基团等。 并且环组A表示不饱和杂环基团。

公开(公告)号：US20070191419A1

公开(公告)日：2007-08-16

申请号：US10590585

申请日：2005-03-04

申请人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

发明人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

IPC分类号： A61K31/435 ,  C07D221/04

CPC分类号： C07D451/02 ,  C07D239/70 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

摘要翻译： 提供式[I]的环烷基吡啶衍生物：其中符号与说明书中所述的相同。 该化合物作为伤害感受肽受体拮抗剂起作用，并且可用作与伤害感受肽受体相关疾病的药物，例如作为抵抗麻醉止痛剂的缓解剂; 减轻对麻醉止痛药依赖或成瘾的缓解; 镇痛增强剂; 抗生素或食欲抑制剂; 用于认知障碍和痴呆/健忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救办法 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 或补救低血压。

公开(公告)号：US20110015181A1

公开(公告)日：2011-01-20

申请号：US12920916

申请日：2009-03-04

申请人： Makoto Ando ,  Hirokatsu Ito ,  Minoru Kameda ,  Hiroshi Kawamoto ,  Kensuke Kobayashi ,  Hiroshi Miyazoe ,  Chisato Nakama ,  Nagaaki Sato ,  Toshiaki Tsujino

发明人： Makoto Ando ,  Hirokatsu Ito ,  Minoru Kameda ,  Hiroshi Kawamoto ,  Kensuke Kobayashi ,  Hiroshi Miyazoe ,  Chisato Nakama ,  Nagaaki Sato ,  Toshiaki Tsujino

IPC分类号： A61K31/55 ,  C07D498/04 ,  A61K31/5386 ,  C07D401/14 ,  A61K31/4545 ,  C07D417/14 ,  A61K31/541 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/439 ,  A61P3/00

CPC分类号： C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D451/02 ,  C07D498/08

摘要： The present invention relates to a compound that is useful for treatment of, for example, hypertension, arteriosclerosis, bulimia and obesity because of having an antagonistic action to a neuropeptide Y receptor and is represented by formula (I) [wherein R1 represents hydrogen, cyano, or the like; R represents a group represented by formula (II); X1 represents C1-4 lower alkylene or the like; X2 represents lower alkylene or the like; and Het represents a 5-membered heteroaromatic ring that has at least one nitrogen atom and, in addition, one or two hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms] or to a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及由于对神经肽Y受体具有拮抗作用而由式（I）表示的化合物，其可用于治疗例如高血压，动脉硬化，贪食症和肥胖症[其中R1表示氢，氰基 ，等等; R表示由式（II）表示的基团。 X1表示C1-4低级亚烷基等; X2表示低级亚烷基等; Het表示具有至少一个氮原子，另外还有一个或两个选自氮，硫和氧原子的杂原子的5元杂芳环]或其药学上可接受的盐。