公开(公告)号：EP1330240A2

公开(公告)日：2003-07-30

申请号：EP01968558.5

申请日：2001-09-06

申请人： MCW Research Foundation ,  Taisho Pharmaceutical Co. Ltd.

发明人： ROMAN, Richard, J. ,  HARDER, David, R. ,  MIYATA, Noriyuki ,  SATO, Masakazu ,  KAMEO, Kazuya ,  OKUYAMA, Shigeru

IPC分类号： A61K31/00 ,  A61K31/155 ,  A61K31/145 ,  A61K31/20 ,  A61K31/4192 ,  A61K31/4174 ,  A61K39/395 ,  A61K48/00 ,  A61P9/10 ,  A61P31/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/28

CPC分类号： A61K31/15 ,  A61K31/20 ,  A61K31/4164 ,  A61K31/4192 ,  A61K48/00

摘要： A method for treating cerebral vascular diseases in a human or non-human animal is disclosed. The method involves inhibiting 20-HETE synthesizing enzyme activity sufficiently to increase or prevent a decrease in cerebral blood flow in the human or non-human animal. This can be obtained by treating the animal with inhibitors of CYP4A or CYP4F family of enzymes, such as HET0016, 17-ODYA (17-octadecynoic acid), DDMS (dibromododecenyl methylsulfimide), 1-ABT (1-aminobenzotriazole) and miconazole, or with an antibody to 20-HETE synthetizing enzyme or with an antisense oligo-nucleotide directed against 5' end of CYP4A1, CYP4A2, CYP4A11, CYP4F2 or CYP4F3.

公开(公告)号：EP1389611B1

公开(公告)日：2012-06-27

申请号：EP02722849.3

申请日：2002-04-26

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： SATO, Masakazu ,  MIYATA, Noriyuki ,  ISHII, Takaaki ,  MATSUNAGA, Yuko ,  AMADA, Hideaki

IPC分类号： A61K31/4418 ,  A61K31/4525 ,  A61K31/47 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  A61P3/10 ,  C07C259/14 ,  C07D207/20 ,  C07D211/70 ,  C07D213/74 ,  C07D215/06 ,  C07D241/04 ,  C07D265/30 ,  C07D491/113 ,  C07D217/04 ,  C07D213/75 ,  C07D401/04 ,  C07D491/10 ,  C07D295/15

CPC分类号： C07D213/75 ,  A61K31/136 ,  A61K31/402 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/4525 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  C07C259/14 ,  C07D207/20 ,  C07D211/22 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D217/04 ,  C07D295/13 ,  C07D295/135 ,  C07D295/15 ,  C07D401/04 ,  C07D491/10

摘要： Hydroxyformamidine compounds represented by the following general formula or pharmaceutically acceptable salts thereof: wherein R1 represents substituted morpholino, substituted piperidino, piperazin-1-yl, substituted piperazin-1-yl, thiomorpholin-1-yl, perhydroazepin-1-yl, perhydroazocin-1-yl, tetrahydropyridin-1-yl, pyrrolin-1-yl, etc.; X represents nitrogen or CR5; and R2 to R5 are the same or different and each represents hydrogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or halogeno. Drugs inhibiting 20-HETE synthase relating to contraction/dilation of microvessels, induction of cell proliferation, etc. in main organs such as kidney and cerebral vessels.

公开(公告)号：EP2891499A1

公开(公告)日：2015-07-08

申请号：EP13832429.8

申请日：2013-08-30

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： KOJIMA, Naoki ,  ROMAN, J., Richard ,  MIYATA, Noriyuki ,  TAKAHASHI, Teisuke ,  TOMOIKE, Hideki ,  TAKEDA, Takuya

IPC分类号： A61K45/06 ,  A61K31/382 ,  A61K31/401 ,  A61K31/41 ,  A61P9/12 ,  A61P31/10

CPC分类号： A61K31/382 ,  A61K31/40 ,  A61K31/401 ,  A61K31/41 ,  A61K45/06 ,  A61K2300/00

摘要： Medicaments that depend on a combination of SGLT 2 inhibitors and antihypertensive drugs and which are useful in the treatment of diseases involving at least hypertension or diabetes mellitus as a risk factor of cardiovascular events, as well as methods of treating the diseases are provided. Since the present invention exhibits a superior hypotensive action that cannot be attained by any single antihypertensive drugs, the conventional problems associated with the use of two or more antihypertensive drugs in order to lower the blood pressure to the desired level can be solved. In addition, the present invention shows a marked therapeutic efficacy in diabetes mellitus, a disease associated with diabetes mellitus, or complications of diabetes mellitus, in particular, diabetic nephropathy. As a further advantage, the present invention is also useful for the treatment of diseases involving lowered renal function.

摘要翻译： 提供依赖于SGLT 2抑制剂和抗高血压药物组合的药物，其可用于治疗涉及至少高血压或糖尿病的疾病作为心血管事件的危险因素，以及治疗疾病的方法。 由于本发明显示出通过任何单一抗高血压药物无法获得的优异的降血压作用，因此可以解决与使用两种或更多种抗高血压药物相关联以将血压降低到所需水平的常规问题。 此外，本发明显示出在糖尿病，与糖尿病相关的疾病或糖尿病并发症，特别是糖尿病性肾病中的显着治疗功效。 作为另外的优点，本发明也可用于治疗涉及肾功能降低的疾病。

公开(公告)号：EP1475102A1

公开(公告)日：2004-11-10

申请号：EP03705219.8

申请日：2003-02-17

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： MIYATA, Noriyuki ,  OKUYAMA, Shigeru ,  TAKAHASHI, Teisuke ,  TAKAHASHI, Kenzo

IPC分类号： A61K45/00 ,  A61K31/136 ,  A61P9/12 ,  A61P43/00

CPC分类号： A61K31/136

摘要： A therapeutic agent for hypertension, which comprises as an active ingredient a compound capable of inhibiting Na + /Ca 2+ exchanger 1.

摘要翻译： 高血压治疗剂，其含有能够抑制Na + / Ca 2+交换体1的化合物作为活性成分。

公开(公告)号：EP1291343B1

公开(公告)日：2006-12-06

申请号：EP01941061.2

申请日：2001-06-15

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： SATO, Masakazu ,  MIYATA, Noriyuki ,  ISHII, Takaaki ,  KOBAYASHI, Yuko ,  AMADA, Hideaki

IPC分类号： C07D213/74 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D409/12 ,  C07D473/08 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/522 ,  A61P13/12 ,  A61P9/00 ,  A61P9/10

CPC分类号： C07D213/74

摘要： Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula: wherein R represents a group represented by the formula: R -(CH2)m- (wherein R represents a C3-8 cycloalkyl group, a C2-6 alkoxycarbonyl group, a C2-10 alkenyl group, a C2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R -A- (wherein R represents a hydrogen atom, a C1-6 alkoxy group, a C3-8 cycloalkoxy group, or the like, and A represents a straight-chain C2-10 alkylene group which may be substituted with a C1-6 alkyl group or a trifluoromethyl group), or a C3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom, or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.

公开(公告)号：EP1425258A2

公开(公告)日：2004-06-09

申请号：EP02761383.5

申请日：2002-09-09

申请人： TAISHO PHARMACEUTICAL CO., LTD ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

发明人： FALCK, John R. ,  MIYATA, Noriyuki ,  ONO, Naoya ,  CHONAN, Tomomichi ,  HIRANO, Hitomi ,  TODA, Yoshihisa ,  TANAMI, Tohru ,  OKUYAMA, Shigeru

IPC分类号： C07C59/00 ,  C07C255/00 ,  A61K31/42 ,  A61K31/425 ,  C07D277/00

CPC分类号： C07D257/04 ,  C07C33/044 ,  C07C33/423 ,  C07C33/426 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/34

摘要： A hydroxyeicosenoic acid analog represented by the following Formula (I), the bond represents a cis-vinylene group or an ethynylene group; Y represents CH2, O or S(O)p wherein p is 0, 1 or 2; m represents an integer of 1 to 4 inclusive; n represents an integer of 0 to 3 inclusive; the sum of m and n is an integer of 3 to 7 inclusive; R1 represents a C1-4 alkyl group or a C3-8 cycloalkyl group; R2 represents a hydrogen atom or a methyl group; R3 represents COR4, a nitrile group, a halogen atom, a tetrazole group or a thiazolidinedione group; R4 represents OR6, NHR6, N(OH)R?6, NHSO2R5¿, glycerol or functionalized glycerols; R5 represents a C¿1-15? alkyl group, a C6-10 aryl group or a C7-14 aryl group substituted with alkyl groups, halogens or amino groups; R?6¿ represents a hydrogen, a C¿1-10? alkyl group or a C1-10 alkyl group substituted with a hydroxyl group, or a pharmaceutically acceptable salt or hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.

摘要翻译： 由下式（I）表示的羟基二十碳烯酸类似物，该键代表顺式亚乙烯基或亚乙炔基; Y代表CH 2，O或S（O）p，其中p是0,1或2; m表示1〜4的整数， n表示0〜3的整数， m和n的总和是3〜7的整数， R1代表C1-4烷基或C3-8环烷基; R2代表氢原子或甲基; R3代表COR4，腈基，卤素原子，四唑基或噻唑烷二酮基; R4代表OR6，NHR6，N（OH）R6 6，NHSO2R5，甘油或官能化甘油; R5代表C 1-15？ 烷基，被烷基，卤素或氨基取代的C 6-10芳基或C 7-14芳基; R 6表示氢，C 1-10 - 烷基或被羟基取代的C1-10烷基，或其药学上可接受的盐或水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。

公开(公告)号：EP1291343A1

公开(公告)日：2003-03-12

申请号：EP01941061.2

申请日：2001-06-15

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： SATO, Masakazu ,  MIYATA, Noriyuki ,  ISHII, Takaaki ,  KOBAYASHI, Yuko ,  AMADA, Hideaki

IPC分类号： C07D213/74 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D409/12 ,  C07D473/08 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/522 ,  A61P13/12 ,  A61P9/00 ,  A61P9/10

CPC分类号： C07D213/74

摘要： Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula:
wherein R 1 represents a group represented by the formula: R 2 -(CH 2 ) m - (wherein R 2 represents a C 3-8 cycloalkyl group, a C 2-6 alkoxycarbonyl group, a C 2-10 alkenyl group, a C 2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R 3 -A- (wherein R 3 represents a hydrogen atom, a C 1-6 alkoxy group, a C 3-8 cycloalkoxy group, or the like, and A represents a straight-chain C 2-10 alkylene group which may be substituted with a C 1-6 alkyl group or a trifluoromethyl group), or a C 3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom,
or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.

摘要翻译： 提供了用于抑制参与诸如肾脏和脑血管等主要器官的微血管收缩或扩张的20-HETE的生产的药剂，或参与引起细胞增殖。 本发明涉及由下式表示的羟基脒化合物：其中R 1表示由下式表示的基团：R 2 - （CH 2）m - （其中R 2表示C 3-8环烷基 基团，C 2-6烷氧基羰基，C 2-10烯基，C 2-6炔基，取代或未取代的芳基等，m为1〜8的整数）表示的基团 通式为R 3 -A（其中R 3表示氢原子，C 1-6烷氧基，C 3-8环烷氧基等，A表示直链C 2-10 可以被C 1-6烷基或三氟甲基取代的亚烷基）或C 3-8环烷基，X表示氧原子或硫原子，或其药学上可接受的盐，涉及包括 与活性成分一样。