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1. 发明申请

WO2011037771A1 DIARYLMETHYLAMIDE DERIVATIVE HAVING MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISM 审中-公开
标题翻译：含有茂金属浓度的HORMONE受体拮抗剂的二甲基甲酰胺衍生物
公开(公告)号：WO2011037771A1
公开(公告)日：2011-03-31
申请号：PCT/US2010/048563
申请日：2010-09-13
申请人： MERCK SHARP & DOHME CORP. , MSD K.K. , LIN, Linus, S. , SUZUKI, Takao
发明人： LIN, Linus, S. , SUZUKI, Takao
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D491/20
摘要： The present invention is directed to diarylmethylamide derivatives represented of structural formula I which are melanin-concentrating hormone receptor antagonists, and are useful as an agent for the prevention, treatment, or remedy of various circulatory diseases, neurological diseases, metabolic diseases, reproductive system diseases, respiratory diseases, digestive diseases, and the like. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the melanin-concentrating hormone is involved. I
摘要翻译：本发明涉及作为黑色素浓缩激素受体拮抗剂的结构式I表示的二芳基甲基酰胺衍生物，可用作预防，治疗或补救各种循环系统疾病，神经系统疾病，代谢疾病，生殖系统疾病呼吸系统疾病，消化系统疾病等。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及黑色素浓缩激素的疾病中的用途。一世

2. 发明申请

US20130085156A1 NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES 有权
标题翻译：新型2-吡啶甲酰胺衍生物
公开(公告)号：US20130085156A1
公开(公告)日：2013-04-04
申请号：US13685775
申请日：2012-11-27
申请人： MSD K.K.
发明人： MORIHIRO MITSUYA , MAKOTO BAMBA , FUMIKO SAKAI , HITOMI WATANABE , YASUHIRO SASAKI , TERUYUKI NISHIMURA , JUN-ICHI EIKI
IPC分类号： C07D471/04 , C07D417/14
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，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。

3. 发明授权

US08367708B2 Phenyl-isoxazol-3-ol derivative 有权
标题翻译：苯基异恶唑-3-醇衍生物
公开(公告)号：US08367708B2
公开(公告)日：2013-02-05
申请号：US12516025
申请日：2007-11-29
申请人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
发明人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
IPC分类号： A01N43/76 , A01N43/64 , A01N43/18 , A01N43/06 , A01N43/16 , A01N43/08 , A61K31/42 , A61K31/41 , A61K31/54 , A61K31/38 , A61K31/35 , A61K31/34
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其具有GPR120激动剂作用，因此可用于治疗糖尿病或高脂血症或其药学上可接受的盐。式中，（AA）表示可以被低级烷氧基等取代的苯基等，（BB）表示通过从可以被卤素原子等取代的苯中除去两个氢原子得到的二价基团等; X表示具有由1-8个碳原子构成的主链的间隔基，其中主链中的1-3个碳原子可以被氧原子等取代; Y表示氢原子等。

4. 发明授权

US08367698B2 3-substituted sulfonyl piperidine derivative 有权
标题翻译： 3-取代的磺酰哌啶衍生物
公开(公告)号：US08367698B2
公开(公告)日：2013-02-05
申请号：US13478680
申请日：2012-05-23
申请人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
发明人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/454 , C07D471/08 , C07D401/12 , C07D211/96
CPC分类号： C07D211/26 , C07D401/04 , C07D401/14 , C07D453/06
摘要： [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease.[Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
摘要翻译： [问题]提供了用作心血管疾病，神经疾病，代谢疾病，生殖疾病和消化疾病的预防或补救的化合物。 [解决方法]由下式（I）表示的化合物或其药学上可接受的盐，其中Z表示其中n1，n2和n3分别为0,1或2; R 1表示C 1-6烷基，C 3-8环烷基等; R2表示芳基或杂芳基; R3表示氢原子，C1-6烷基等; 并且M1，M2，M3和M4独立地表示氢原子，C1-6烷基等，或M1与M2，M3或M4一起形成-CH 2 - 等。

5. 发明授权

US08263632B2 Aminopyridine derivatives having Aurora A selective inhibitory action 有权
标题翻译：具有极光A的氨基吡啶衍生物选择性抑制作用
公开(公告)号：US08263632B2
公开(公告)日：2012-09-11
申请号：US13258782
申请日：2010-03-15
申请人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： C07D401/04 , A61K31/535
CPC分类号： C07D471/04 , C07D498/04
摘要： The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof
摘要翻译：本发明涉及式（I）的化合物：其中：n为0或1; X为0或CH2; R1是H或C1-2烷基; R2是H或C1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中烷基可以被一至三个相同或不同的选自R 10的取代基取代; R5是H或OCH3; R10为F或Cl; 或其药学上可接受的盐或酯

6. 发明授权

US08207169B2 Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D 有权
标题翻译：取代的[1,2,4]三唑并[4'，3'：1,6]吡啶并[2,3-b]
公开(公告)号：US08207169B2
公开(公告)日：2012-06-26
申请号：US12995832
申请日：2009-05-28
申请人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
发明人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/495
CPC分类号： C07D471/14
摘要： The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer
摘要翻译：式D的化合物是三唑并 - 吡啶并吡嗪类，其是可用于治疗癌症的AKT抑制剂

7. 发明申请

US20120035155A1 INDOLE-2-CARBOXAMIDE DEIVATIVE 审中-公开
标题翻译：吲哚-2-羧酰胺衍生物
公开(公告)号：US20120035155A1
公开(公告)日：2012-02-09
申请号：US13263801
申请日：2010-04-17
申请人： Yuji Haga , Sayaka Mizutani , Nagaaki Sato
发明人： Yuji Haga , Sayaka Mizutani , Nagaaki Sato
IPC分类号： A61K31/4725 , C07D401/14 , A61P9/12 , A61P9/10 , A61P13/12 , A61P9/00 , A61P3/04 , A61P3/10 , A61P5/00 , A61P3/06 , A61P19/06 , A61P1/16 , A61P29/00 , A61P1/04 , C07D401/12
CPC分类号： C07D403/06 , C07D403/12 , C07D403/14
摘要： To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R1 represents a hydrogen atom, a halogen, a C1-6 alkyl, etc,; R2 represents a C1-6 alkyl, or a halo-C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl, etc.; R4 represents a hydrogen atom, a C1-6 alkyl, a halo-C1-6 alkyl, etc.; or R3 and R4, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R3 and Y3, taken together, form —CH2—CH2—; Y1 and Y2 are both hydrogen atoms; or Y1 and Y2, taken together, form —CH2—CH2—; and Y3 represents a hydrogen atom; or Y3 and R3, taken together, form —CH2—CH2—].
摘要翻译：提供具有人QRFP受体拮抗活性的吲哚化合物，并且可用作各种疾病的预防或补救。提供式（I）化合物或其药学上可接受的盐：[其中，R 1表示氢原子，卤素，C 1-6烷基等; R 2表示C 1-6烷基或卤代C 1-6烷基; R3代表氢原子，C1-6烷基等; R 4表示氢原子，C 1-6烷基，卤代C 1-6烷基等; 或R 3和R 4与它们键合的氮原子一起形成3至6元脂族含氮杂环; 或R 3和Y 3一起形成-CH 2 -CH 2 - ; Y1和Y2都是氢原子; 或Y1和Y2一起形成-CH 2 -CH 2 - ; Y 3表示氢原子; 或Y 3和R 3一起形成-CH 2 -CH 2 - ]。

8. 发明授权

US08101621B2 Aminopyridine derivatives having aurora a selective inhibitory action 有权
标题翻译：具有极光选择性抑制作用的氨基吡啶衍生物
公开(公告)号：US08101621B2
公开(公告)日：2012-01-24
申请号：US12226639
申请日：2007-04-25
申请人： Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Keita Nagai , Katsumasa Nonoshita , Mitsuru Ohkubo
发明人： Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Keita Nagai , Katsumasa Nonoshita , Mitsuru Ohkubo
IPC分类号： C07D239/42 , C07D239/02 , C07D403/14
CPC分类号： C07D487/08
摘要： The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及通式I的化合物：其中：n1和n2相同或不同，为0或1; R是芳基，杂芳基等; Re为氢原子或低级烷基; 选自由（i）Ra1和Ra1'中的任一个组成的四组中的两个基团，（ii）Ra2和Ra2'中的任一个，（iii）Rb1和Rb1'中的任一个，以及（iv）Rb2和 Rb2'组合形成 - （CH 2）n - ，其中n为1,2或3; 在Ra1，Ra1'，Ra2，Ra2'，Rb1，Rb1'，Rb2和Rb2'之间，不形成 - （CH2）n-的基团各自独立地为氢原子等; X1，X2，X3和X4各自独立地为CH，N等; Y1，Y2，Y3和Y4相同或不同，为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

9. 发明授权

US08101618B2 1,4-substituted piperazine derivatives 失效
标题翻译： 1,4-取代的哌嗪衍生物
公开(公告)号：US08101618B2
公开(公告)日：2012-01-24
申请号：US11887671
申请日：2006-04-05
申请人： Hiroshi Kawamoto , Toshifumi Kimura , Hisashi Ohta , Akio Sato , Atsushi Satoh , Gentaroh Suzuki
发明人： Hiroshi Kawamoto , Toshifumi Kimura , Hisashi Ohta , Akio Sato , Atsushi Satoh , Gentaroh Suzuki
IPC分类号： A61K31/496 , C07D401/04 , C07D413/04 , C07D413/14 , A61K31/501 , A61K31/506 , C07D213/74 , C07D263/58 , C07D277/42 , C07D403/04
CPC分类号： C07D413/14 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2059 , A61K9/485 , A61K9/4858 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14
摘要： A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐，其中：R 1表示具有3至9个碳原子的支链低级烷基等; R2表示具有1或2个氮原子等的6元杂芳基; R3表示氢原子，烷酰氨基等; R4表示氢原子，低级烷基等; X1表示氧原子或硫原子; X2表示氧原子或单键; m表示0〜4的整数。该化合物具有代谢型谷氨酸受体1抑制作用，因此可用于治疗脑部疾病如惊厥，急性疼痛，炎性疼痛，慢性疼痛，脑梗死或瞬时脑缺血发作，精神功能障碍如精神分裂症，以及焦虑和药物添加等疾病。

10. 发明授权

US08093389B2 Substituted spirochromanone derivatives 有权
标题翻译：取代的螺二氢茚酮衍生物
公开(公告)号：US08093389B2
公开(公告)日：2012-01-10
申请号：US12007000
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
IPC分类号： C07D413/06 , C07D405/04 , A61K31/438
CPC分类号： C07D519/00 , C07D491/10
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 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.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1表示由选自吲哚，1H-吲唑，2H-吲唑，1H-噻吩并[2,3-c]所示的芳环形成的基团，吡唑，1H-吡唑并[3,4-b]吡啶，苯并[b]呋喃，苯并咪唑，苯并恶唑，1,2-苯并异恶唑和咪唑并[1,2-a] R 1和R 2各自表示氢原子，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，卤代-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-C1-C6 烷氧基，羧基-C2-C6烯基或-Q1-N（Ra）-Q2-Rb的基团; 任选取代的C 1 -C 6烷基，芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; R 3和R 4各自表示氢原子，卤素原子，硝基，环-C 3 -C 6烷基，任选被C 1 -C 6烷基或环-C 3 -C 6烷基取代的氨基甲酰基，或者 -N（R f）R f; 任选取代的C 2 -C 7烷酰基，C 1 -C 6烷氧基，C 2 -C 7烷氧基羰基，环C 3 -C 6烷氧基羰基，C 1 -C 6烷基磺酰基，C 1 -C 6烷硫基，环C 3 -C 6烷氧基，环C 3 -C 6烷基 - C 1 -C 6烷氧基，环-C 3 -C 6烷基磺酰基，环-C 3 -C 6烷硫基或环-C 3 -C 6烷基-C 1 -C 6烷硫基; 或任选取代的C 1 -C 6烷基; T和U各自表示氮原子或次甲基; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

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