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1. 发明专利

IL196585D0 FUSED RING SPIROKETAL DERIVATIVE AND USE THEREOF AS ANTI-DIABETIC DRUG 未知
公开(公告)号：IL196585D0
公开(公告)日：2009-11-18
申请号：IL19658509
申请日：2009-01-19
申请人： CHUGAI PHARMACEUTICAL CO LTD , NISHIMOTO MASAHIRO , EMURA TAKASHI , KOBAYASHI TAKAMITSU , SATO TSUTOMU , OHTAKE YOSHIHITO , YAMAGUCHI MARINA , TAKAMI KYOUKO
IPC分类号： C07H20100101
摘要： Provided are a compound represented by Formula (I): wherein R 1 , R 2 , R 3 , and R 4 are each independently selected from a hydrogen atom, a C 1-6 alkyl group which may be substituted, a C 7-14 aralkyl group which may be substituted and -C(=O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). , or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.

2. 发明专利

IL180916D0 NOVEL CYCLOHEXANE DERIVATIVE, PRODRUG THEREOF AND SALT THEREOF, AND THERAPEUTIC AGENT CONTAINING THE SAME FOR DIABETES 未知
公开(公告)号：IL180916D0
公开(公告)日：2007-07-04
申请号：IL18091607
申请日：2007-01-23
申请人： CHUGAI PHARMACEUTICAL CO LTD , MATSUOKA HIROHARU , SATO TSUTOMU , NISHIMOTO MASAHIRO , SHIMMA NOBUO
IPC分类号： C07C20100101
摘要： A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein A is -O-, -CH 2 -, or -NH-; n is an integer selected between 0 and 1; R 6 and R 7 each independently is hydrogen or C 1-6 alkyl; m is an integer selected among 1-3; Q is selected among the following formulae Q 1 to Q 5 ; Ar 1 is optionally substituted arylene or optionally substituted heteroarylene, provided that the heteroarylene may be bonded to an aromatic carbocycle or aromatic heterocycle to form a fused ring; and Ar 2 is optionally substituted aryl or optionally substituted heteroaryl), a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, or the like each containing the compound.

3. 发明专利

IL184838A SPIROKETAL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND THEIR USE IN THE PREPARATION OF DIABETIC MEDICINES 未知
公开(公告)号：IL184838A
公开(公告)日：2012-02-29
申请号：IL18483807
申请日：2007-07-25
申请人： CHUGAI PHARMACEUTICAL CO LTD , NISHIMOTO MASAHIRO , KOBAYASHI TAKAMITSU , SATO TSUTOMU
发明人： NISHIMOTO MASAHIRO , KOBAYASHI TAKAMITSU , SATO TSUTOMU
摘要： The present invention provides a compound of Formula (I): wherein R 1 , R 2 , R 3 and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and -C(=O)Rx; Rx represents an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents -(CH 2 ) m -(L) p - or -(L) p -(CH 2 ) m -; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents -O-, -S- or -NR 5 -; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.

4. 发明专利

IL184838D0 SPIROKETAL DERIVATIVE AND USE THEREOF AS DIABETIC MEDICINE 未知
公开(公告)号：IL184838D0
公开(公告)日：2007-12-03
申请号：IL18483807
申请日：2007-07-25
申请人： CHUGAI PHARMACEUTICAL CO LTD , NISHIMOTO MASAHIRO , KOBAYASHI TAKAMITSU , SATO TSUTOMU
IPC分类号： C07H20100101
摘要： The present invention provides a compound of Formula (I): wherein R 1 , R 2 , R 3 and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and -C(=O)Rx; Rx represents an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents -(CH 2 ) m -(L) p - or -(L) p -(CH 2 ) m -; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents -O-, -S- or -NR 5 -; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.

5. 发明申请

WO2002064136A3 MALONYL-COA DECARBOXYLASE INHIBITORS USEFUL AS METABOLIC MODULATORS 审中-公开
公开(公告)号：WO2002064136A3
公开(公告)日：2002-08-22
申请号：PCT/US2002/002179
申请日：2002-01-22
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA , ARRHENIUS, Thomas , CHEN, Mi , CHENG, Jie Fei , HUANG, Yujin , NADZAN, Alex , TITH, Sovouthy , WALLACE, David , LIU, Bin , NISHIMOTO, Masahiro
发明人： ARRHENIUS, Thomas , CHEN, Mi , CHENG, Jie Fei , HUANG, Yujin , NADZAN, Alex , TITH, Sovouthy , WALLACE, David , LIU, Bin , NISHIMOTO, Masahiro
IPC分类号： A61K31/42
摘要： The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

6. 发明申请

WO2002066034A1 METHODS FOR TREATING METABOLIC DISEASES USING MALONYL-COA DECARBOXYLASE INHIBITORS 审中-公开
标题翻译：使用MALONYL-COA脱羧酶抑制剂治疗代谢性疾病的方法
公开(公告)号：WO2002066034A1
公开(公告)日：2002-08-29
申请号：PCT/US2002/004729
申请日：2002-02-19
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA , ARRHENIUS, Thomas , CHENG, Jie Fei , WILSON, Mark , SERAFIMOV, Rossy , NISHIMOTO, Masahiro , WALLACE, David , TITH, Sovouthy , HARMON, Charles , BROWN, Steve
发明人： ARRHENIUS, Thomas , CHENG, Jie Fei , WILSON, Mark , SERAFIMOV, Rossy , NISHIMOTO, Masahiro , WALLACE, David , TITH, Sovouthy , HARMON, Charles , BROWN, Steve
IPC分类号： A61K31/425
CPC分类号： A61K31/423 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541
摘要： The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R 1 , R 2 , R 6 , and R 7 are defined herein.
摘要翻译：本发明涉及治疗某些代谢疾病的方法，以及使用化合物及其前药，和/或药学上可接受的盐，含有可用于治疗这些疾病的化合物的药物组合物。特别地，本发明涉及通过抑制丙二酰辅酶A脱羧酶（MCD）来治疗心血管疾病，糖尿病，癌症，酸中毒和肥胖的化合物和组合物的用途。这些化合物具有下式：（I）和（II）其中Y，C，R 1，R 2，R 6和R 7在本文中定义。

7. 发明申请

WO2002064136A2 MALONYL-COA DECARBOXYLASE INHIBITORS USEFUL AS METABOLIC MODULATORS 审中-公开
标题翻译：可用作代谢调节剂的MALONYL-COA脱羧酶抑制剂
公开(公告)号：WO2002064136A2
公开(公告)日：2002-08-22
申请号：PCT/US2002/002179
申请日：2002-01-22
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA , ARRHENIUS, Thomas , CHEN, Mi , CHENG, Jie Fei , HUANG, Yujin , NADZAN, Alex , TITH, Sovouthy , WALLACE, David , LIU, Bin , NISHIMOTO, Masahiro
发明人： ARRHENIUS, Thomas , CHEN, Mi , CHENG, Jie Fei , HUANG, Yujin , NADZAN, Alex , TITH, Sovouthy , WALLACE, David , LIU, Bin , NISHIMOTO, Masahiro
IPC分类号： A61K31/42
CPC分类号： C07D231/06 , A61K31/16 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/44 , A61K31/5375 , C07C33/46 , C07C257/22 , C07C279/18 , C07C307/10 , C07C335/18 , C07D231/14 , C07D233/64 , C07D233/90 , C07D261/04 , C07D261/08 , C07D261/14 , C07D261/18 , C07D295/13 , C07D295/194 , C07D295/21 , C07D295/215 , C07D295/32 , C07D307/52 , C07D401/12 , C07F9/247 , C07F9/4021
摘要： The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
摘要翻译：本发明涉及新型化合物（I），其前药和药学上可接受的盐以及含有这些化合物的药物组合物，所述化合物用于治疗某些代谢疾病和通过抑制酶调节的疾病丙二酰辅酶A脱羧酶（丙二酰辅酶A脱羧酶，MCD）。具体而言，本发明涉及通过抑制丙二酰辅酶A脱羧酶来预防，控制和治疗心血管疾病，糖尿病，酸中毒，癌症和肥胖症的化合物和组合物以及方法。

8. 发明申请

WO1998025916A1 NOVEL BENZOPYRAN DERIVATIVES 审中-公开
标题翻译：新的BENZOPYRAN衍生物
公开(公告)号：WO1998025916A1
公开(公告)日：1998-06-18
申请号：PCT/KR1997000265
申请日：1997-12-13
申请人： C & C RESEARCH LABORATORIES , JO, Jae, Chon , PARK, Sung, Dae , LIM, Hyun, Suk , KIM, Ju, Su , KIM, Sung, Jin , MORIKAWA, Kazumi , KANBE, Yoshitake , NISHIMOTO, Masahiro , KIM, Myung-Hwa
发明人： C & C RESEARCH LABORATORIES
IPC分类号： C07D311/30
CPC分类号： C07D335/06 , C07D311/38 , C07D311/58
摘要： The present invention relates to a novel benzopyran derivative having anti-estrogenic activity. More specifically, the present invention relates to a novel benzopyran derivative represented by formula (I) and pharmaceutically acceptable salt thereof, in which ----- represents a single bond or a double bond; R1 and R2 independently of one another represent hydrogen, hydroxy or OR group, wherein R represents acyl or alkyl; R3 represents hydrogen, lower alkyl or halogeno lower alkyl, provided that when ----- represents a double bond, R3 is not present; R4 represents hydrogen or lower alkyl; A represents a group of formula (a), (b), (c) or (d); R5, R6 and R7 independently of one another represent hydrogen, alkyl, halogenoalkyl, alkenyl or halogenoalkenyl, or R6 and R7 together with nitrogen atom to which they are bound can form a 4- to 8-membered heterocyclic ring which can be substituted with R5; X represents O, S or NR8, wherein R8 represents hydrogen or lower alkyl; m denotes an integer of 2 to 15; n denotes an integer of 0 to 2; and p denotes an integer of 0 to 4, and to a process for preparation thereof and a pharmaceutical composition having anti-estrogenic activity which contains the compound (I) as an active component.
摘要翻译：本发明涉及具有抗雌激素活性的新型苯并吡喃衍生物。更具体地说，本发明涉及式（I）表示的新的苯并吡喃衍生物及其药学上可接受的盐，其中代表单键或双键; R 1和R 2彼此独立地表示氢，羟基或OR基，其中R表示酰基或烷基; R 3表示氢，低级烷基或卤代低级烷基，条件是当o-表示双键时，R 3不存在; R4代表氢或低级烷基; A表示式（a），（b），（c）或（d）的基团; R 5，R 6和R 7彼此独立地表示氢，烷基，卤代烷基，烯基或卤代烯基，或者R 6和R 7与它们所连接的氮原子一起可以形成可被R 5取代的4至8元杂环 ; X表示O，S或NR8，其中R8表示氢或低级烷基; m表示2〜15的整数， n表示0〜2的整数，和p表示0〜4的整数，以及其制备方法和含有化合物（I）作为活性成分的具有抗雌激素活性的药物组合物。

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