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1. 发明公开

EP2111406A1 SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 有权转让
标题翻译：取代SPIROCHROMANON衍生物作为ACC抑制剂
公开(公告)号：EP2111406A1
公开(公告)日：2009-10-28
申请号：EP08713050.6
申请日：2008-01-08
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： C07D491/10 , A61K31/438 , A61P3/00 , C07D495/04
CPC分类号： C07D519/00 , C07D491/10
摘要： The invention relates to a compound of a general formula (I): (I) wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of -N(Re)Rf; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

2. 发明公开

EP2120569A2 SPIROCHROMANON DERIVATIVES 有权
标题翻译：螺旋色素衍生物
公开(公告)号：EP2120569A2
公开(公告)日：2009-11-25
申请号：EP08705516.6
申请日：2008-01-08
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： IINO, Tomoharu , JONA, Hideki , KURIHARA, Hideki , NAKAMURA, Masayuki , NIIYAMA, Kenji , SHIBATA, Jun , SHIMAMURA, Tadashi , WATANABE, Hitomi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： A01N43/16 , A61K31/35
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[2,1- 1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-b]吡啶，其具有Ar 2，并且任选地具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C1-C6烷氧基，羧基-C2-C6链烯基或-Q1-N（Ra）-Q2-Rb的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基团; 或具有芳基或杂环基的C1-C6烷基或C2-C6烯基; T和U各自独立地表示氮原子或次甲基; V代表氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

3. 发明公开

EP1754706A1 SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON 审中-公开
标题翻译： SELEKTIVE INHIBITOREN GEGEN CDK4 UND CDK6 MIT AMINOTHIAZOLSKELETT
公开(公告)号：EP1754706A1
公开(公告)日：2007-02-21
申请号：EP05743671.9
申请日：2005-05-19
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： IWASAWA, Yoshikazu , SHIBATA, Jun , SHIMAMURA, Tadashi , KURIHARA, Hideki , MITA, Takashi , KAWANISHI, Nobuhiko , HASHIHAYATA, Takashi , KAWAMURA, Mikako , SAGARA, Takeshi , ARAI, Sachie , HIRAI, Hiroshi
IPC分类号： C07D417/12 , C07D417/14 , C07D491/08 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P43/00
CPC分类号： C07D417/14 , C07D417/12 , C07D491/08
摘要： The present invention relates to a compound represented by Formula [I]:

wherein
X is O, S, NH or CH 2 ;
Y 1 , Y 2 , Y 3 , Y 4 and Y 5 , which may be identical or different, are each CH or N; however, at least one of Y 1 , Y 2 , Y 3 , Y 4 and Y 5 is N;
Z 1 and Z 2 , which may be identical or different, are each CH or N;
n is an integer from 1 to 3;
R 1 is a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group;
R 2 and R 3 , which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aromatic heterocyclic ring, or the like; and
R 4 is a hydrogen atom, a lower alkyl group, a C 3 -C 6 cycloalkyl group or the like,
or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及由式[I]表示的化合物：其中X是O，S，NH或CH 2; Y 1，Y 2，Y 3，Y 4和Y 5可以相同或不同，分别为CH或N; 然而，Y 1，Y 2，Y 3，Y 4和Y 5中的至少一个为N; Z 1和Z 2可以相同或不同，各自为CH或N; n为1〜3的整数， R 1为C 3〜C 8环烷基，C 6〜C 10芳基，脂肪族杂环或芳香族杂环，双环脂肪族饱和烃基， R 2和R 3可以相同或不同，分别为氢原子，低级烷基，低级烯基，C 3〜C 8环烷基，C 6〜C 10芳基，芳香族杂环环等; R 4为氢原子，低级烷基，C 3〜C 6环烷基等，或其药学上可接受的盐或酯，以及对Cdk4和/或Cdk6的选择性抑制剂或含有化合物或其药学上可接受的盐或酯。

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