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91. 发明授权

US07732456B2 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US07732456B2
公开(公告)日：2010-06-08
申请号：US10591373
申请日：2005-03-04
申请人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号： A61K31/444 , C07D401/02
CPC分类号： C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译：本发明提供由通式（I）表示的吡啶酮衍生物[在该式中，R 1和R 2可以相同或不同，代表H等，或者R 1和R 2可以与脂族含氮杂环基一起形成他们绑定的N X1-X3可以相同或不同，代替次甲基或N，但不是全部同时代表氮; X4-X7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R1，L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

92. 发明授权

US07727998B2 Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient 失效
标题翻译：黑色素浓缩激素受体拮抗剂含有哌啶衍生物作为活性成分
公开(公告)号：US07727998B2
公开(公告)日：2010-06-01
申请号：US10544261
申请日：2004-02-09
申请人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
发明人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
IPC分类号： A61K31/4545 , C07D491/10
CPC分类号： C07D401/04 , A61K31/438 , A61K31/4439 , A61K31/445 , C07D211/26 , C07D491/10
摘要： The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
摘要翻译：本发明提供了含有作为活性成分的通式[I]表示的哌啶衍生物的黑色素浓缩激素受体拮抗剂：其中R1是氢，羟基，低级烷基等; R2，R3a，R3b，R4a，R4b，R5a，R5b和R6各自代表氢，卤素等; W1和W2各自独立地代表-O-，-CH2-等; Y1，Y2，Y3和Y4代表-CH-，-CF-，-N-等; Z代表低级烷基，脂族杂环基等; Ar是单环或双环脂族杂环或芳族杂环; n为1〜8的整数]。该化合物作为拮抗黑素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病或代谢疾病的药物。

93. 发明授权

US07718801B2 Substituted imidazole derivative 有权
标题翻译：取代的咪唑衍生物
公开(公告)号：US07718801B2
公开(公告)日：2010-05-18
申请号：US11661486
申请日：2005-08-30
申请人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
发明人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
IPC分类号： C07D239/00 , C07D239/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
摘要翻译：本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯：其中：X 1，X 2，X 3和X 4可以相同或不同，各自为C或N，条件是 X1，X2，X3和X4中的两个为N; Y是CH或N; R1，R1'，R2，R2'，R3，R3'，R4和R4'可以相同或不同，分别为氢原子，低级烷基等; R5是氢原子或甲基; R 6和R 7可以相同或不同，分别为氢原子，低级烷基等; R 8和R 8'可以相同或不同，分别为氢原子，低级烷基等; R9是可以被取代的芳基或杂芳基; n为1〜3的整数，PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

94. 发明授权

US07645756B2 Nitrogenous fused heteroaromatic ring derivative 失效
标题翻译：含氮稠合杂芳环衍生物
公开(公告)号：US07645756B2
公开(公告)日：2010-01-12
申请号：US10589832
申请日：2005-02-17
申请人： Toshiyuki Takahashi , Akio Kanatani , Shigeru Tokita , Ryo Yoshimoto
发明人： Toshiyuki Takahashi , Akio Kanatani , Shigeru Tokita , Ryo Yoshimoto
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/53 , A61P3/04 , A61P3/10 , A61P9/10
CPC分类号： C07D487/04
摘要： The invention provides a compound or its pharmaceutically-acceptable salt of formula wherein A1 is a hydrogen, etc.; j and k are 0 or 1; is a double bond, etc.; is a double bond, etc.; one of W1 and W2 is E—O—W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1): which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供了下式的化合物或其药学上可接受的盐：其中A1是氢等; j和k为0或1; “img id =”CUSTOM-CHARACTER-00001“he =”3.13mm“wi =”9.14mm“file =”US07645756-20100112-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>是双键等; “img id =”CUSTOM-CHARACTER-00002“he =”3.13mm“wi =”9.48mm“file =”US07645756-20100112-P00002.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>是双键等; W1和W2之一是E-O-W等，另一个是氢原子等; E是通过从其中除去两个氢原子而衍生自苯环等的二价基团; W是一组式（II-1）：其具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，并且可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

95. 发明授权

US07629362B2 2-pyridine carboxamide derivatives 有权
标题翻译： 2-吡啶甲酰胺衍生物
公开(公告)号：US07629362B2
公开(公告)日：2009-12-08
申请号：US10545424
申请日：2004-02-13
申请人： Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4436 , C07D417/14 , C07D401/14
CPC分类号： C07D471/04 , C07D417/14
摘要： The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物，其由式（I）表示：[其中X1表示氮原子，硫原子，氧原子等 ; R1表示6-至10-元芳基，5-至7-元杂芳基等; D表示氧原子或硫原子; R2和R3相同或不同，各自表示氢原子，低级烷基等; 式（II）表示任选取代的5〜7元杂芳基等; 式（III）表示单环或双环杂芳基]或其药学上可接受的盐。

96. 发明授权

US07541477B2 Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient 失效
标题翻译：黑色素浓缩激素受体的拮抗剂，其包含苯并咪唑衍生物作为活性成分
公开(公告)号：US07541477B2
公开(公告)日：2009-06-02
申请号：US10522718
申请日：2003-07-29
申请人： Minoru Moriya , Akio Kanatani , Hisashi Iwaasa , Akane Ishihara , Takehiro Fukami
发明人： Minoru Moriya , Akio Kanatani , Hisashi Iwaasa , Akane Ishihara , Takehiro Fukami
IPC分类号： A61K31/4184 , C07D235/30
CPC分类号： C07D403/12 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/04
摘要： This invention relates to a benzimidazole derivative of the general formula [I] [wherein B1, B2, and B3 represent hydrogen atom or lower alkyl; R1 and R2 are same or different and represent lower alkyl, etc.; R3 and R4 represent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.
摘要翻译：本发明涉及通式[I]的苯并咪唑衍生物[其中B1，B2和B3表示氢原子或低级烷基; R1和R2相同或不同，代表低级烷基等; R3和R4代表氢原子等; W表示3至8元芳族或脂肪杂环等; Ar表示取代或未取代的芳族杂环等。]该化合物作为黑色素浓缩激素受体的拮抗剂起作用，可用作中枢疾病，循环系统疾病和代谢性疾病的药物。

97. 发明申请

US20090118304A1 2-HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE 有权
标题翻译： 2-HETEROARYL取代的吲哚衍生物
公开(公告)号：US20090118304A1
公开(公告)日：2009-05-07
申请号：US11992555
申请日：2006-09-29
申请人： Keiji Takahashi , Yoshio Ogino , Teruyuki Nishimura
发明人： Keiji Takahashi , Yoshio Ogino , Teruyuki Nishimura
IPC分类号： A61K31/497 , C07D401/14 , A61K31/437 , A61P3/10 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D471/04
摘要： Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.
摘要翻译：公开了由下式（I）表示的化合物，其具有葡糖激酶活化作用，因此可用于治疗糖尿病或肥胖症或其药学上可接受的盐。在该式中，R 1表示芳基等; R11表示芳基等; R 2表示甲酰基等，R 3表示C 1-6烷基等; R3表示氢原子等; Z1表示-O-等; Z2表示-O-等; Y1-Y4分别表示碳原子或氮原子; 环A表示杂芳基; X表示碳原子等; m表示0-2的整数; q表示0-2的整数。

98. 发明授权

US07422898B2 Nucleic acid encoding monkey Gpr103 失效
标题翻译：编码猴Gpr103的核酸
公开(公告)号：US07422898B2
公开(公告)日：2008-09-09
申请号：US11578592
申请日：2005-04-14
申请人： Hideki Sano , Hisashi Iwaasa , Satoshi Mashiko
发明人： Hideki Sano , Hisashi Iwaasa , Satoshi Mashiko
IPC分类号： C12N5/10 , C12N15/12 , C12N15/63 , C12N1/21 , C07K14/00
CPC分类号： C07K14/705 , G01N33/6893 , G01N33/6896 , G01N2333/726
摘要： There are provided non-human primate and rat GPR103 genes and proteins and a compound evaluation method employing the genes or proteins. There are also provided highly useful novel ligands for functional analysis of the GPR103 genes and proteins and for the compound evaluation. The nucleic acids or proteins having the sequences listed as SEQ ID NOS: 1 to 4 provide non-human primate or rat GPR103 genes and proteins and information based on the genes and proteins. The genes and proteins can be used for evaluation of compounds. The nucleic acids or proteins having the sequence listed as SEQ ID NO: 5 or 6 provide a GPR103 ligand.
摘要翻译：提供了非人灵长类动物和大鼠GPR103基因和蛋白质，以及使用基因或蛋白质的化合物评估方法。还提供了非常有用的新配体，用于GPR103基因和蛋白质的功能分析以及化合物评估。具有SEQ ID NO：1至4列出的序列的核酸或蛋白质提供非人灵长类动物或大鼠GPR103基因和基于基因和蛋白质的蛋白质和信息。基因和蛋白质可用于评价化合物。具有SEQ ID NO：5或6所列序列的核酸或蛋白质提供GPR103配体。

99. 发明申请

US20070141642A1 Guanosine triphosphate (GTP)-binding protein-coupled receptor protein, BG37 失效
公开(公告)号：US20070141642A1
公开(公告)日：2007-06-21
申请号：US11704546
申请日：2007-02-08
申请人： Takaharu Maruyama , Takao Nakamura , Hiraku Itadani , Ken-Ichi Tanaka
发明人： Takaharu Maruyama , Takao Nakamura , Hiraku Itadani , Ken-Ichi Tanaka
IPC分类号： G01N33/567 , C07K14/72
CPC分类号： C07K14/705
摘要： The present inventors conducted a similarity search of the amino acid sequence of known G protein-coupled receptor proteins in GenBank, and obtained a novel human GPCR gene “BG37”. cDNA containing the ORF of the gene was cloned and its nucleotide sequence was determined. Moreover, novel GPCR “BG37” genes from mouse and rat were isolated. Use of the novel GPCR of the present invention enables screening of ligands, compounds inhibiting the binding to a ligand, and candidate compounds of pharmaceuticals which can regulate signal transduction from the “BG37” receptor.

100. 发明授权

US07148224B2 Pyrazinone derivatives 失效
标题翻译：吡嗪酮衍生物
公开(公告)号：US07148224B2
公开(公告)日：2006-12-12
申请号：US11105534
申请日：2005-04-14
申请人： Takashi Hayama , Nobuhiko Kawanishi , Tooru Takaki
发明人： Takashi Hayama , Nobuhiko Kawanishi , Tooru Takaki
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00
CPC分类号： C07D213/75 , C07D277/48 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/04
摘要： The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1, is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.
摘要翻译：本发明涉及通式（I）的化合物：[Ar 1]在第5和6位与相邻的吡嗪酮环稠合的芳基等，X是CO等， Y是CH等，Z是CH等，V是CH等，W n是 - （CH 2）n

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