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.

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。

公开(公告)号：EP1910375A1

公开(公告)日：2008-04-16

申请号：EP06787451.1

申请日：2006-07-14

申请人： Merck & Co., Inc. ,  BANYU PHARMACEUTICAL CO., LTD.

发明人： YAMAKAWA, Takeru ,  JONA, Hideki ,  NIIYAMA, Kenji ,  YAMADA, Koji ,  IINO, Tomoharu ,  OHKUBO, Mitsuru ,  IMAMURA, Hideaki ,  SHIBATA, Jun ,  KUSUNOKI, Jun ,  YANG, Lihu

IPC分类号： C07D491/10 ,  C07D497/10 ,  A61K31/438 ,  A61P3/00 ,  A61P35/00 ,  A61P31/00

CPC分类号： C07D491/10 ,  C07D495/10

摘要： The invention relates to a compound of a formula (I): , or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.

公开(公告)号：EP1515722A2

公开(公告)日：2005-03-23

申请号：EP03739192.7

申请日：2003-06-17

申请人： Merck & Co., Inc. ,  BANYU PHARMACEUTICAL CO., LTD.

发明人： OGIDIGBEN, Miller, J. ,  YAMAKAWA, Takeru ,  SAGARA, Yufu

IPC分类号： A61K31/4545 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D409/14

CPC分类号： C07D271/107 ,  C07D235/26 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D495/04

摘要： This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. In addition, the present invention relates to the use of the compounds in the treatment of dementia such as Alzheimer's disease and vascular dementia, depression, attention deficit disorder, sleep disorder, schizophrenia, pain, ischemia, atrophic gastritis, and atony of gastrointestinal tract.

公开(公告)号：EP2307422A1

公开(公告)日：2011-04-13

申请号：EP09773588.0

申请日：2009-06-29

申请人： Banyu Pharmaceutical Co., Ltd.

发明人： JONA, Hideki ,  SHIBATA, Yoshihiro ,  YAMAKAWA, Takeru

IPC分类号： C07D491/107 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P31/00 ,  A61P35/00

CPC分类号： C07D491/107 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709

摘要： The invention relates to a compound of a general formula (I): wherein A represents a linking group; Ar
1 represents a group formed from an aromatic ring; R
1 and R
2 each independently 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 -Q
1 -N(R
a )-Q
2 -R
b ; a C1-C6 alkyl group optionally having substituent(s); an aryl or heterocyclic group optionally having substituent(s); 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, a sulfur atom or an imino group. 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A表示连接基团; Ar 1表示由芳香环形成的基团; 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，卤代C 1 -C 6烷氧基，环C 3 -C 6烷氧基 C2-C7烷酰基，C2-C7烷氧基羰基，卤代C2-C7烷氧基羰基，环C3-C6烷氧基羰基，芳烷氧基羰基，氨基甲酰基 - C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a）-Q 2 -R b的基团; 任选具有取代基的C1-C6烷基; 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，硫原子或亚氨基。 本发明的化合物可用作各种ACC相关疾病的治疗剂。