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：US20100216758A1

公开(公告)日：2010-08-26

申请号：US11989876

申请日：2006-08-03

申请人： Makoto Ando ,  Etsuko Sekino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

发明人： Makoto Ando ,  Etsuko Sekino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

IPC分类号： A61K31/397 ,  C07D401/02 ,  A61K31/4439 ,  C07D213/04 ,  A61K31/44 ,  C07D401/14 ,  A61K31/444 ,  C07D239/36 ,  A61K31/513 ,  C07D213/89 ,  C07D403/14 ,  A61K31/55 ,  C07D211/94 ,  A61K31/4545 ,  C07D221/24 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P1/00 ,  A61P13/00 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D213/69 ,  C07D213/64 ,  C07D213/89 ,  C07D239/52 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10 ,  C07D487/08

摘要： An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.

摘要翻译： 活性成分是由通式[I]表示的化合物：[其中R1和R2表示低级烷基，C3-6环烷基等，X1和X2表示次甲基，Ar-Y1-Y2-Y3 - 取代的次甲基等，但是它们都是Ar-Y1-Y2-Y3-取代的次甲基，X3至X8表示次甲基，-N-等，Y1和Y3表示单键，-O-或 类似的，Y2表示单键，低级亚烷基等，W表示 - （O） - （CH2）n-（O） - 等，n表示1〜4的整数，L和Z2表示 单键或亚甲基，Z1表示单键，C1-4亚烷基等，Ar表示芳香族碳环基等]。 该化合物作为黑色素浓缩激素受体拮抗剂起作为肥胖症等的治疗剂的作用。

公开(公告)号：US20110071129A1

公开(公告)日：2011-03-24

申请号：US12993928

申请日：2009-06-11

申请人： Makoto Ando ,  Etsuki Hirose ,  Kouta Masutani ,  Minoru Moriya ,  Takao Suzuki

发明人： Makoto Ando ,  Etsuki Hirose ,  Kouta Masutani ,  Minoru Moriya ,  Takao Suzuki

IPC分类号： A61K31/4427 ,  C07D487/10 ,  A61K31/444 ,  A61P3/04 ,  A61P3/10 ,  A61P1/16 ,  A61P25/24 ,  A61P25/22 ,  A61K31/5025 ,  A61K31/497

CPC分类号： C07D471/20 ,  A61K31/13 ,  C07D487/10 ,  C07D519/00

摘要： [Problem] To provide a melanin concentrating hormone receptor antagonist useful as medicines for central system disorders, cardiovascular disorders, metabolic disorders.[Means for Resolution] Provided are compound of a formula (I): [wherein R1 a and R1 b each are a hydrogen atom, etc.; R2 is a hydrogen atom, a C1-6 alkyl, etc.; Ar1 is a 6-membered aromatic carbocyclic group or a 6-membered aromatic nitrogen-containing heterocyclic group; Ar2 is a group to be formed by removing two hydrogen atoms from a 6-membered aromatic carbon ring, a 6-membered aromatic nitrogen-containing hetero ring, etc.; Ar3 is a mono- or bi-cyclic aromatic carbon ring or aromatic hetero ring; m1, m2, m3 and m4 each are independently 0, 1, 2, 3 or 4, provided that the total of m1 and m2 is from 2 to 6, the total of m3 and m4 is from 2 to 6]. The compounds are useful as medicines for central system disorders, cardiovascular disorders, metabolic disorders.

摘要翻译： [问题]提供可用作中枢系统疾病，心血管疾病，代谢紊乱的药物的黑色素浓缩激素受体拮抗剂。 [分解方法]提供式（I）的化合物：[其中R1 a和R1b各自为氢原子等; R2是氢原子，C1-6烷基等; Ar 1是6元芳族碳环基或6元芳族含氮杂环基; Ar 2是通过从6元芳族碳环，6元芳族含氮杂环等除去2个氢原子而形成的基团; Ar 3是单环或双环芳族碳环或芳族杂环; m1，m2，m3和m4各自独立为0,1,2,3或4，条件是m1和m2的总和为2至6，m3和m4的总和为2至6]。 该化合物可用作中枢系统疾病，心血管疾病，代谢紊乱的药物。

公开(公告)号：US20070249659A1

公开(公告)日：2007-10-25

申请号：US11579570

申请日：2005-05-09

申请人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

发明人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

IPC分类号： A61K31/44 ,  C07D471/02

CPC分类号： A61K31/501 ,  A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  C07D471/04

摘要： The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

摘要翻译： 本发明提供由式（I）表示的咪唑并吡啶化合物，其中R 1和R 2各自独立地表示C 1-6烷基 集团等 R 3和R 4各自独立地表示氢原子，甲基等; Ar 1是表示单环或双环的3至8元芳族或脂族杂环基等的二价取代基; Ar 2表示芳族碳环基或芳族杂环基; W表示 - （CH 2）2，m表示0〜10的整数。该化合物作为黑色素浓缩激素受体拮抗剂起作用， 作为肥胖症的治疗剂。

公开(公告)号：US20090264426A1

公开(公告)日：2009-10-22

申请号：US11991334

申请日：2006-09-05

申请人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

发明人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

IPC分类号： A61K31/5377 ,  C07D401/10 ,  C07D413/14 ,  A61K31/47 ,  A61P9/10

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/04 ,  C07D471/04

摘要： Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

摘要翻译： 公开了由式（I）表示的化合物：其中R1和R2独立地表示氢原子，低级烷基等; X1，X2和X3独立地表示次甲基或氮原子; Y1和Y3独立地表示单键，-O-等; Y2表示低级亚烷基等; W1至W4独立地表示单键，亚甲基等; L表示单键，亚甲基等; Z 1和Z 2独立地表示单键，C 1-4亚烷基等; Ar 1表示芳香族碳环等， Ar 2表示双环芳香族碳环等。 该化合物可用作中枢性疾病，心血管疾病或代谢性疾病的药物。

公开(公告)号：US07566781B2

公开(公告)日：2009-07-28

申请号：US11579570

申请日：2005-05-09

申请人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

发明人： Shunji Sakuraba ,  Minoru Moriya ,  Hidekazu Takahashi ,  Hiroyuki Kishino ,  Makoto Jitsuoka ,  Minoru Kameda ,  Akio Kanatani

IPC分类号： C07D491/02 ,  C07D237/02 ,  C07F9/02 ,  A61K31/519

CPC分类号： A61K31/501 ,  A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  C07D471/04

摘要： The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4 each independently represent a hydrogen atom, a methyl et al; Ar1 is a divalent substituent representing a monocyclic or bicyclic, 3- to 8-membered aromatic or aliphatic heterocyclic group et al; Ar2 represents an aromatic carbocyclic group, or an aromatic heterocyclic group; W represents —(CH2)m et al, and m indicates an integer of from 0 to 10. This compound acts as a melanin concentrating hormone receptor antagonist, and is useful as treating agents for obesity.

摘要翻译： 本发明提供由式（I）表示的咪唑并吡啶化合物，其中R 1和R 2各自独立地表示C 1-6烷基等; R3和R4各自独立地表示氢原子，甲基等; Ar 1是代表单环或双环的3-至8-元芳族或脂族杂环基团的二价取代基; Ar 2表示芳香族碳环基或芳香族杂环基; W表示 - （CH 2）m等，m表示0〜10的整数。该化合物作为黑色素浓缩激素受体拮抗剂起作用，可用作肥胖症的治疗剂。

公开(公告)号：US20110015198A1

公开(公告)日：2011-01-20

申请号：US12919036

申请日：2009-03-26

申请人： Kaori Kamijo ,  Minoru Moriya ,  Takao Suzuki ,  Akihiro Takezawa

发明人： Kaori Kamijo ,  Minoru Moriya ,  Takao Suzuki ,  Akihiro Takezawa

IPC分类号： A61K31/438 ,  C07D491/107 ,  C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/437 ,  A61K31/5025 ,  A61P3/04 ,  A61P3/10 ,  A61P1/16 ,  A61P25/24 ,  A61P25/22

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/20

摘要： [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases.[Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form —O—CH2—, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.

摘要翻译： [问题]提供可用作中枢疾病，循环系统疾病和代谢疾病的药剂的黑色素浓缩激素受体拮抗剂。 [解决方法]提供由式（I）表示的二芳基甲基酰胺衍生物：其中R1a，R1b，R2a，R2b，R3a和R3b独立地表示氢原子等，R4表示氢原子，C1-6烷基， 等等，R 5表示氢原子等，Z表示C 1-6烷基等，或者R 4和Z一起形成4至6元含氮杂环，Y1表示H等，Y2表示H等 表示H或Y1和Y2一起形成-O-CH 2 - ，W表示C，SO等，Ar 1表示6元芳基等，Ar 2表示6元芳基等，环A表示 苯环，吡啶环等。

公开(公告)号：US20070299070A1

公开(公告)日：2007-12-27

申请号：US11663038

申请日：2005-09-30

申请人： Takao Suzuki ,  Minoru Moriya ,  Shunji Sakuraba ,  Sayaka Mizutani ,  Hisashi Iwaasa ,  Akio Kanatani

发明人： Takao Suzuki ,  Minoru Moriya ,  Shunji Sakuraba ,  Sayaka Mizutani ,  Hisashi Iwaasa ,  Akio Kanatani

IPC分类号： A61K31/5377 ,  A61K31/4025 ,  A61K31/4045 ,  A61P1/00 ,  A61P13/00 ,  A61P21/00 ,  A61P27/00 ,  A61P37/00 ,  A61P5/00 ,  C07D413/14 ,  C07D413/10 ,  C07D403/10 ,  C07D401/12 ,  C07D401/10 ,  C07D401/02 ,  C07D209/04 ,  A61P9/00 ,  A61P7/00 ,  A61P43/00 ,  A61P3/00 ,  A61P25/00 ,  A61P15/00 ,  A61P11/00 ,  A61K31/4439 ,  A61K31/454

CPC分类号： C07D209/42 ,  C07D235/24 ,  C07D401/12

摘要： A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y, represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.

摘要翻译： 由式[I]表示的化合物：其中R 1和R 2相同或不同，各自表示C 1-6烷基， 烷基，C 3-8环烷基等; R 3a，R 3b和R 4相同或不同，各自表示氢，C 1-6 烷基等; X表示-N-，-CH-等; Y表示单键，C 1-3亚烷基等; Y 2表示C 1-4亚烷基，氧（C 1-4烷基亚烷基）等; Ar 1表示单环芳族碳环基团，单环芳族杂环基团等; 和Ar 2代表5或6元芳族碳环基团，芳族杂环基团等。 该化合物起着黑色素浓缩激素受体拮抗剂的作用，可用作例如肥胖症的治疗剂等。

公开(公告)号：US07531668B2

公开(公告)日：2009-05-12

申请号：US11663038

申请日：2005-09-30

申请人： Takao Suzuki ,  Minoru Moriya ,  Shunji Sakuraba ,  Sayaka Mizutani ,  Hisashi Iwaasa ,  Akio Kanatani

发明人： Takao Suzuki ,  Minoru Moriya ,  Shunji Sakuraba ,  Sayaka Mizutani ,  Hisashi Iwaasa ,  Akio Kanatani

IPC分类号： C07D235/12 ,  C07D209/12 ,  C07D211/06 ,  C07D401/12 ,  C07D291/04 ,  C07D291/06 ,  C07D279/02 ,  C07D279/06 ,  C07D279/12 ,  C07D265/02 ,  C07D265/06 ,  C07D265/30 ,  C07D257/04 ,  C07D257/08 ,  C07D251/04 ,  C07D237/04

CPC分类号： C07D209/42 ,  C07D235/24 ,  C07D401/12

摘要： A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.

摘要翻译： 由式[I]表示的化合物：其中R 1和R 2相同或不同，各自表示C 1-6烷基，C 3-8环烷基等; R3a，R3b和R4相同或不同，各自表示氢，C1-6烷基等; X表示-N-，-CH-等; Y1表示单键，C1-3亚烷基等; Y2代表C1-4亚烷基，氧基（C1-4亚烷基）等; Ar 1表示单环芳族碳环基团，单环芳族杂环基团等; 和Ar 2表示5或6元芳族碳环基团，芳族杂环基团等。 该化合物起着黑色素浓缩激素受体拮抗剂的作用，可用作例如肥胖症的治疗剂等。