公开(公告)号：WO2003066636A1

公开(公告)日：2003-08-14

申请号：PCT/US2003/003449

申请日：2003-02-06

Applicant: TANABE SEIYAKU CO., LTD. ,  SIRCAR, Ila ,  MORNINGSTAR, Marshall ,  KAKUSHIMA, Masatoshi ,  KAJI, Hidefumi ,  KAWAGUCHI, Takayuki ,  KUME, Toshiyuki

Inventor： SIRCAR, Ila ,  MORNINGSTAR, Marshall ,  KAKUSHIMA, Masatoshi ,  KAJI, Hidefumi ,  KAWAGUCHI, Takayuki ,  KUME, Toshiyuki

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to a compound of formula (I): wherein R is hydrogen atom, hydroxyl group or carbamoyl group, and n is 1 or 2, or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中R是氢原子，羟基或氨基甲酰基，n是1或2。

公开(公告)号：WO1998018763A1

公开(公告)日：1998-05-07

申请号：PCT/JP1997003804

申请日：1997-10-22

Applicant: TANABE SEIYAKU CO., LTD. ,  SUGITA, Takahisa ,  OHNUKI, Tetsuo ,  YAMADA, Masaki ,  TANAKA, Sumiko ,  NONAKA, Nobuaki ,  ASAI, Yasuyuki

Inventor： TANABE SEIYAKU CO., LTD.

IPC: C07D217/26

CPC classification number: A61K31/472 ,  A61K31/4725 ,  A61K38/00 ,  C07D217/26 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06139 ,  C07K5/06156 ,  C07K5/0821 ,  Y02P20/55

Abstract: Medicinal compositions containing as the active ingredient compounds having an inhibitory effect on dipeptidyl-peptidase IV and having the tetrahydroisoquinoline skeleton, for example, tetrahydroisoquinoline derivatives represented by general formula (I) and the tetrahydroisoquinoline derivatives, wherein R represents (1) a group having the structure of an amino acid with optionally substituted amino from which the hydroxy atomic group in the carboxy atomic group has been eliminated, or (2) an amino protective group; R represents (1) optionally protected hydroxy, (2) having the structure of an amino acid with an optionally protected carboxy atomic group from which a hydrogen atom in the amino atomic group has been eliminated, or (3) a group having the stuctures of a primary or secondary amine or ammonia from which a hydrogen atom on the nitrogen atom has been eliminated; and R , R , R and R are the same or different and each represents hydrogen hydroxy or lower alkoxy.

Abstract translation: 含有对二肽基肽酶IV具有抑制作用并具有四氢异喹啉骨架的活性成分化合物的药物组合物，例如由通式（I）表示的四氢异喹啉衍生物和四氢异喹啉衍生物，其中R 1表示（1）a 具有氨基酸结构的基团，其具有任选取代的氨基，羧基原子团中的羟基原子团已被除去，或（2）氨基保护基; R 2表示（1）任选被保护的羟基，（2）具有氨基酸结构的具有任选保护的羧基原子团的结构，氨基原子团中的氢原子从该氨基酸被除去，或（3）具有 原子或仲胺或氮原子上的氢原子已被除去的结构; R 3，R 4，R 5和R 6相同或不同，各自表示氢羟基或低级烷氧基。

公开(公告)号：WO1997036864A1

公开(公告)日：1997-10-09

申请号：PCT/JP1997001017

申请日：1997-03-26

Applicant: TANABE SEIYAKU CO., LTD. ,  OHMIZU, Hiroshi ,  OHTANI, Akio ,  OHGIKU, Tsuyoshi ,  SAI, Hiroshi ,  MURAKAMI, Jun

Inventor： TANABE SEIYAKU CO., LTD.

IPC: C07D207/02

CPC classification number: C07D207/02 ,  C07C69/734 ,  C07C235/34 ,  C07C2601/08 ,  C07D211/58 ,  C07D213/40 ,  C07D213/55 ,  C07D213/56 ,  C07D213/75 ,  C07D213/89 ,  C07D231/12 ,  C07D231/38 ,  C07D231/40 ,  C07D233/56 ,  C07D239/42 ,  C07D249/08 ,  C07D261/14 ,  C07D317/60 ,  C07D401/06 ,  C07D405/12

Abstract: A novel butadiene derivative of formula (1-a) wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R and R are each H or lower alkyl, one of -COR and -COR is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof. Said compounds show excellent PAI-1 inhibitory activity and are useful in the prophylaxis or treatment of various thromboses such as myocardial infarction, intra-atrial thrombus in atrial fibrillation, cerebral infarction, angina pectoris, stroke, pulmonary infarction, deep venous thrombus (DVT), disseminated intravascular coagulation syndrome (DIC), diabetic complications, restenosis after percutaneous transluminal coronary angioplasty (PTCA), etc.

Abstract translation: 式（1-a）的新型丁二烯衍生物，其中环A为杂环，或苯任选被低级烷基，烷氧基，硝基，羟基，取代或未取代的氨基或卤素取代的苯，环B为杂环或任选被 低级烷氧基，低级亚烷基二氧基或二低级烷基氨基，R 1和R 2各自为H或低级烷基，-COR 32和-COR 42之一为羧基，另一个为任选的羧基 酯化或相应的酰胺或吡咯烷衍生物或其药学上可接受的盐。 所述化合物显示优异的PAI-1抑制活性，可用于预防或治疗心肌梗死，心房颤动，脑梗死，心绞痛，中风，肺梗死，深静脉血栓（DVT）等心血管栓塞， ，弥漫性血管内凝血综合征（DIC），糖尿病并发症，经皮腔内冠状动脉成形术（PTCA）后再狭窄等。

公开(公告)号：WO1993007488A1

公开(公告)日：1993-04-15

申请号：PCT/JP1992001276

申请日：1992-10-02

Applicant: TANABE SEIYAKU CO., LTD. ,  EIKEN KAGAKU KABUSHIKI KAISHA ,  THE RESEARCH FOUNDATION FOR MICROBIAL DISEASES OF ,  ISHIBASHI, Kaichiro ,  ITO, Masao ,  YOSHIDA, Iwao; ,  TAKAMIZAWA, Akihisa; ,  SHIBATANI, Takeji

Inventor： TANABE SEIYAKU CO., LTD. ,  EIKEN KAGAKU KABUSHIKI KAISHA ,  THE RESEARCH FOUNDATION FOR MICROBIAL DISEASES OF

IPC: G01N33/576

CPC classification number: C07K14/005 ,  C12N2770/24222

Abstract: A reagent for testing an antibody of hepatitis C by using as an antigen a peptide containing an essential peptide comprising a specified sequence having an epitope of an HCV structural region, Arg Xaa Gly Pro Arg Leu Gly Arg Arg Pro, wherein Xaa represents preferably Leu, Lys or Arg. The reagent serves to detect an antibody against the HCV structural region specifically at a high detection rate, whereby HCV infection can be tested accurately in an early stage. The necessary peptide can be chemically synthesized readily.

Abstract translation: 通过使用含有包含具有HCV结构域的表位的特定序列的必需肽的肽作为抗原来测试丙型肝炎抗体的试剂Arg Xaa Gly Pro Arg Leu Gly Arg Arg Pro，其中Xaa优选为Leu， Lys或Arg。 该试剂用于以高检测率特异性地检测针对HCV结构区的抗体，由此可以在早期准确地检测HCV感染。 所需的肽可以容易化学合成。

公开(公告)号：WO1992020326A1

公开(公告)日：1992-11-26

申请号：PCT/US1992004267

申请日：1992-05-20

Applicant: MARION LABORATORIES, INC. ,  TANABE SEIYAKU CO., LTD.

Inventor： MARION LABORATORIES, INC. ,  TANABE SEIYAKU CO., LTD. ,  NODA, Kazuo ,  YOSHINO, Hiroyuki ,  HIRAKAWA, Yoshiyuki ,  MACLAREN, David, D. ,  SKULTETY, Paul, F. ,  LEFLER, John, R. ,  BECK, Greg, M.

IPC: A61K09/54

CPC classification number: A61K9/5078

Abstract: Controlled release pharmaceutical beads are provided having a multi-layered core and a multi-layered periphery. The core contains at least (A) an inner portion having a suitable organic acid and (B) a sustainably-acid-releasing coating thereover. The periphery contains at least (A) an inner portion having a mixture of at least (i) a pharmaceutical compound and (ii) a surface-active agent, and (B) a sustainably-drug-releasing exterior coating.

Abstract translation: 提供具有多层芯和多层外围的控释药物珠粒。 核心至少包含（A）具有合适的有机酸的内部部分和（B）其上可持续发酸的涂层。 外围至少包含（A）具有至少（i）药物化合物和（ii）表面活性剂的混合物的内部部分，和（B）可持续释放药物的外部涂层。

公开(公告)号：WO2007089034A1

公开(公告)日：2007-08-09

申请号：PCT/JP2007/052165

申请日：2007-02-01

Applicant: TANABE SEIYAKU CO., LTD. ,  IIJIMA, Toru ,  YAMAMOTO, Yasuo ,  AKATSUKA, Hidenori ,  KAWAGUCHI, Takayuki

Inventor： IIJIMA, Toru ,  YAMAMOTO, Yasuo ,  AKATSUKA, Hidenori ,  KAWAGUCHI, Takayuki

IPC: C07D265/36 ,  C07D279/16 ,  C07D413/04 ,  A61K31/538 ,  A61K31/5415 ,  A61P9/12

CPC classification number: C07D265/36 ,  C07D279/16 ,  C07D413/04

Abstract: The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R 1 etc, R 1 is a group of the formula: R a SO?2#191NH- etc, R a is an alkyl group etc, R 2 and R 3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: -C(=O)- etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及用作下式[I]的盐皮质激素受体调节剂的化合物：其中环A是任选具有除R 1以外的取代基的苯环， 等等，R 1是下式的基团：R a，SO 2，R 3，NH 3等，R a是烷基等， R 2和R 3各自为氢原子，苯基，任选取代的烷基等，X为氧原子等，Y为式 ：-C（= O） - 等，Ar为任选取代的芳基或任选取代的杂芳基，Q为单键，亚烷基等，或其药学上可接受的盐。

公开(公告)号：WO2007088996A1

公开(公告)日：2007-08-09

申请号：PCT/JP2007/051861

申请日：2007-01-30

Applicant: TANABE SEIYAKU CO., LTD. ,  NAKAMURA, Yoshinori ,  HAYASHI, Norimitsu ,  HIGASHIJIMA, Takanori ,  KUBOTA, Hitoshi ,  OKA, Kozo

Inventor： NAKAMURA, Yoshinori ,  HAYASHI, Norimitsu ,  HIGASHIJIMA, Takanori ,  KUBOTA, Hitoshi ,  OKA, Kozo

IPC: C07D239/46 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/505 ,  A61P3/06

CPC classification number: C07D239/47 ,  C07D239/42 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D257/06 ,  C07D401/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: The present invention relates to a compound of the general formula (1): (1)wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R 1 is an optionally substituted alkyl group, and the like; and R 2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

Abstract translation: 本发明涉及通式（1）的化合物：（1）其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的苯基等; R 1是任选取代的烷基等; 和R 2是任选取代的氨基，等等; 或其药学上可接受的衍生物，其具有对胆固醇酯转移蛋白（CETP）的抑制活性，从而可用于预防和/或治疗动脉硬化性疾病，高脂血症或血脂异常等。

公开(公告)号：WO2007026966A1

公开(公告)日：2007-03-08

申请号：PCT/JP2006/317798

申请日：2006-09-01

Applicant: TANABE SEIYAKU CO., LTD. ,  TAKAHASHI, Masami ,  YAMANAKA, Takeshi ,  MIYAKE, Tsutomu

Inventor： TAKAHASHI, Masami ,  YAMANAKA, Takeshi ,  MIYAKE, Tsutomu

IPC: C07D211/58 ,  A61K31/541 ,  A61P1/04 ,  A61P1/06 ,  A61P1/08 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/10 ,  A61P11/14 ,  A61P13/02 ,  A61P13/10 ,  A61P17/00 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/22 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00

CPC classification number: C07D211/58

Abstract: The present invention discloses a thiomorpholine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring; Ring B represents an optionally substituted benzene ring; R 1 represents hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom; R 2 represents hydrogen atom or an optionally substituted alkyl group; and R 3a and R 3b may be the same or different from each other, and each represent hydrogen atom or an optionally substituted alkyl group, or combined to each other at the both ends thereof to form an alkylene group, and n is an integer of 1 or 2, or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明公开了由式[I]表示的硫代吗啉化合物：其中环A表示任选取代的苯环; 环B表示任选取代的苯环; R 1表示氢原子，任选取代的羟基，任选取代的氨基，任选取代的烷基，取代的羰基或卤素原子; R 2表示氢原子或任选取代的烷基; 并且R 3a和R 3b可以彼此相同或不同，并且各自表示氢原子或任选取代的烷基，或者两者彼此组合 或其药学上可接受的盐，其中n为1或2的整数。

公开(公告)号：WO2006030984A1

公开(公告)日：2006-03-23

申请号：PCT/JP2005/017555

申请日：2005-09-16

Applicant: TANABE SEIYAKU CO., LTD. ,  MIYAKE, Tsutomu ,  YAMANAKA, Takeshi ,  KINO, Rie ,  ASAI, Hidetoshi

Inventor： MIYAKE, Tsutomu ,  YAMANAKA, Takeshi ,  KINO, Rie ,  ASAI, Hidetoshi

IPC: C07D211/58 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  A61P43/00 ,  C07D401/04 ,  C07D401/06 ,  A61K31/4468 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06

CPC classification number: C07D211/58 ,  C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D257/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06

Abstract: The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R 1 is hydrogen atom or a substituent for amino group, R 2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or -N(R 3 )-, R 3 is hydrogen atom or an optionally substituted alkyl group, R 4a and R 4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.

Abstract translation: 本发明提供由式[I]表示的哌啶化合物：其中环A是任选取代的苯环，环B是任选取代的苯环，R 1， R 2是氢原子或氨基的取代基，R 2是氢原子，任选取代的羟基，任选取代的氨基，任选取代的烷基，取代的羰基或 卤素原子，Z为氧原子或-N（R 3） - ，R 3为氢原子或任选取代的烷基，R 4a为 和R 4b可以相同或不同，并且各自是氢原子或任选取代的烷基，或其药学上可接受的盐，其具有优异的速激肽受体拮抗作用。

公开(公告)号：WO2006004195A1

公开(公告)日：2006-01-12

申请号：PCT/JP2005/012630

申请日：2005-07-01

Applicant: TANABE SEIYAKU CO., LTD. ,  MIYAKE, Tsutomu ,  YAMANAKA, Takeshi ,  ASAI, Hidetoshi ,  TERAKAWA, Yoshihiro

Inventor： MIYAKE, Tsutomu ,  YAMANAKA, Takeshi ,  ASAI, Hidetoshi ,  TERAKAWA, Yoshihiro

IPC: C07D211/62

CPC classification number: C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06

Abstract: The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R 1 is hydrogen atom or a substituent for amino group, R 2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or -N (R 3 )-, R 3 is hydrogen atom or an optionally substituted alkyl group, R 4a and R 4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or may be bonded to each other at the both ends to form an alkylene group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.

Abstract translation: 本发明提供由式[I]表示的哌啶化合物：其中环A是任选取代的苯环，环B是任选取代的苯环，R sup