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1. 发明授权

US07112593B2 N-aryl-substituted cyclic amine derivative and medicine containing the same as active ingredient 失效
标题翻译： N-芳基取代环胺衍生物和含有活性成分的药物
公开(公告)号：US07112593B2
公开(公告)日：2006-09-26
申请号：US10470675
申请日：2002-03-27
申请人： Toshimi Okada , Nobuyuki Kurusu , Keigo Tanaka , Seiji Yoshikawa , Daisuke Shinmyo , Nobuhisa Watanabe , Hironori Ikuta , Hironobu Hiyoshi , Takao Saeki , Mamoru Yanagimachi , Masashi Ito
发明人： Toshimi Okada , Nobuyuki Kurusu , Keigo Tanaka , Seiji Yoshikawa , Daisuke Shinmyo , Nobuhisa Watanabe , Hironori Ikuta , Hironobu Hiyoshi , Takao Saeki , Mamoru Yanagimachi , Masashi Ito
IPC分类号： A61K31/44 , C07D453/02
CPC分类号： C07D401/04 , A61K31/435 , A61K31/439 , A61K31/4545 , C07D401/14 , C07D453/04 , C07D491/10
摘要： An excellent squalene synthase inhibitor is provided. Specifically, what is provided is a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In formula (I), R1 represents an optionally substituted vinyl group or an aromatic ring which may be substituted. Also, n is an integer of 0 to 2. Further, X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring. Also in the formula, CyA represents a 5- to 14 membered non-aromatic cyclic amino group or non-aromatic cyclic amido group which may be substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom. Finally, W represents a chain
摘要翻译：提供了极好的角鲨烯合酶抑制剂。具体地，提供由下式表示的化合物（I），其盐或它们的水合物。在式（I）中，R 1表示任选取代的乙烯基或可被取代的芳环。此外，n是0〜2的整数。此外，X，Y和Z彼此相同或不同，各自表示任选取代的碳原子，或任选取代的氮原子，硫原子或氧原子，以及 Y任选表示单键，当Y表示单键时，X，Y和Z所属的环为5元环。式中，CyA表示可以被取代的5〜14元非芳香族环状氨基或非芳香族环状酰胺基，非芳香族环状氨基或非芳香族环状酰胺基任选具有氧原子或硫原子。最后，W代表一个链

2. 发明授权

US06599917B1 Quinuclidine compounds and drugs containing the same as the active ingredient 失效
标题翻译：奎宁环化合物和含有与活性成分相同的药物
公开(公告)号：US06599917B1
公开(公告)日：2003-07-29
申请号：US10088554
申请日：2002-03-19
申请人： Toshimi Okada , Nobuyuki Kurusu , Keigo Tanaka , Kazuki Miyazaki , Daisuke Shinmyo , Hiroyuki Sugumi , Hironori Ikuta , Hironobu Hiyoshi , Takao Saeki , Mamoru Yanagimachi , Masashi Ito
发明人： Toshimi Okada , Nobuyuki Kurusu , Keigo Tanaka , Kazuki Miyazaki , Daisuke Shinmyo , Hiroyuki Sugumi , Hironori Ikuta , Hironobu Hiyoshi , Takao Saeki , Mamoru Yanagimachi , Masashi Ito
IPC分类号： A61K31439
CPC分类号： C07D453/02
摘要： The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In which R1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) —CH2—CH2— which may be substituted, (2) —CH═CH— which may be substituted, (3) —C≡C—, (4) —NH—CO—, (5) —CO—NH—, (6) —NH—CH2—, (7) —CH2—NH—, (8) —CH2—CO—, (9) —CO—CH2—, (10) —NH—S(O)l—, (11) —S(O)l—NH—, (12) —CH2—S(O)— or (13) —S(O)l—CH2— (l denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C1-6 alkylene chain, (3) an optionally substituted C2-6 alkenylene chain, (4) an optionally substituted C2-6 alkynylene chain, (5) a formula —Q— (wherein Q represents oxygen atom, sulfur atom, CO or N(R2) (wherein R2 represents a C1-6 alkyl group or a C1-6 alkoxy group)), (6) —NH—CO—, (7) —CO—NH—, (8) —NH—CH2—, (9) —CH2—NH—, (10) —CH2—CO—, (11) —CO—CH2—, (12) —NH—S(O)m—, (13) —S(O)m—NH—, (14) —CH2—S(O)m—, (15) —S(O)m—CH2— (wherein m denotes 0, 1 or 2) or (16) —(CH2)n—O— (wherein n denotes an integer from 1 to 6).
摘要翻译：本发明提供优良的角鲨烯合成酶抑制剂。具体地说，它提供由下式表示的化合物（I），其盐或它们的水合物。其中R1表示（1）氢原子或（2）羟基; HAr表示可被1〜3个基团取代的芳香族杂环; Ar表示任选取代的芳环; W表示可被取代的（1）-CH 2 -CH 2 - 表示的链，（2）可以被取代的-CH = CH-，（3）-C = C-，（4）-NH-CO-，（5）-CO-NH-，（6）-NH-CH2-，（7）-CH2-NH-，（8）-CH2-CO-，（9）-CO-CH2-，（10）-NH -S（O）1 - ，（11）-S（O）1 -NH-，（12）-CH 2 -S（O） - 或（13）-S（O） 1或2）; 并且X表示由（1）单键表示的链，（2）任选取代的C 1-6亚烷基链，（3）任选取代的C 2-6亚烯基链，（4）任选取代的C 2-6亚炔基链，（5）式-Q-（其中Q表示氧原子，硫原子，CO或N（R2）（其中R2表示C1-6烷基或C1-6烷氧基）），（6）-NH- CO-，（7）-CO-NH-，（8）-NH-CH2-，（9）-CH2-NH-，（10）-CH2-CO-，（11）-CO-CH2-，）-NH-S（O）m - ，（13）-S（O）m -NH-，（14）-CH 2 -S（O）m - ，（15）-S（O）m -CH 2 - 其中m表示0,1或2）或（16） - （CH2）nO-（其中n表示1至6的整数）。

3. 发明授权

US5801180A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US5801180A
公开(公告)日：1998-09-01
申请号：US904260
申请日：1997-07-31
申请人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
发明人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04
CPC分类号： C07D235/06 , C07D215/42 , C07D231/12 , C07D233/56 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , C07D491/04
摘要： The present invention provides a nitrogenous heterocyclic compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof which is useful for various ischemic heart diseases and the like: ##STR1## �in formula (1), ring A represents a benzene ring, a pyridine ring or a cyclohexane ring; ring B represents a pyridine ring, a pyrimidine ring or an imidazole ring, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent each a hydrogen atom, a halogen atom or a group such as a lower alkoxy group; R.sup.5 represents a group represented by the formula --NR.sup.11 R.sup.12 (wherein R.sup.11 and R.sup.12 represent each a hydrogen atom or a group such as a lower alkyl group) or the like; and R.sup.6 represents a group represented by the formula ##STR2## (wherein R.sup.19 represents a hydrogen atom, a lower alkyl group or the like; R.sup.20, R.sup.21 and R.sup.22 represent each a hydrogen atom, a halogen atom, a hydroxyl group or the like; and r represents 0 or an integer of 1 to 8)!.
摘要翻译：本发明提供由以下通式（1）表示的含氮杂环化合物或其药理学上可接受的盐，其可用于各种缺血性心脏病等：（1）[式（1）中，环A 表示苯环，吡啶环或环己烷环; 环B表示吡啶环，嘧啶环或咪唑环，R1，R2，R3和R4分别表示氢原子，卤素原子或低级烷氧基等基团。 R5表示由式-NR11R12表示的基团（其中R11和R12各自表示氢原子或低级烷基等基团）等; R 6表示氢原子，低级烷基等，R 20，R 21，R 22分别表示氢原子，卤素原子，羟基等。和r表示0或1〜8的整数）]。

4. 发明授权

US5668136A Trisubstituted benzene derivatives, composition and methods of treatment 失效
标题翻译：三取代苯衍生物，组成及处理方法
公开(公告)号：US5668136A
公开(公告)日：1997-09-16
申请号：US757908
申请日：1991-09-11
申请人： Teiji Kimura , Nobuhisa Watanabe , Yasutaka Takase , Kenji Hayashi , Makoto Matsui , Hironori Ikuta , Youji Yamagishi , Kozo Akasaka , Hiroshi Tanaka , Issei Ohtsuka , Takao Saeki , Motoji Kogushi , Tohru Fujimori , Isao Saito
发明人： Teiji Kimura , Nobuhisa Watanabe , Yasutaka Takase , Kenji Hayashi , Makoto Matsui , Hironori Ikuta , Youji Yamagishi , Kozo Akasaka , Hiroshi Tanaka , Issei Ohtsuka , Takao Saeki , Motoji Kogushi , Tohru Fujimori , Isao Saito
IPC分类号： A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/27 , A61K31/275 , A61K31/415 , A61K31/505 , A61P3/06 , A61P9/10 , C07C233/18 , C07C255/58 , C07C255/59 , C07C255/60 , C07C275/34 , C07C275/40 , C07D211/14 , C07D213/02 , C07D233/54 , C07D233/60 , C07D233/68 , C07D233/90 , C07D233/96 , C07D235/02 , C07D235/06 , C07D235/12 , C07D235/14 , C07D249/04 , C07D249/06 , C07D249/18 , C07D253/08 , C07D257/04 , C07D295/08 , C07D295/092 , C07D401/04 , C07D401/12 , C07D403/12 , C07D521/00 , A61K31/495 , C07D241/04
CPC分类号： C07D233/64 , C07C275/40 , C07D211/14 , C07D231/12 , C07D233/56 , C07D233/68 , C07D233/90 , C07D235/02 , C07D235/06 , C07D235/12 , C07D235/14 , C07D249/06 , C07D249/08 , C07D249/18 , C07D257/04 , C07D295/088 , C07D401/12 , C07D403/12
摘要： A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.
摘要翻译：具有下式所示的苯，吡啶或嘧啶衍生物是新颖的，可用作抗动脉硬化剂。（I）其中R1代表低级烷基，可被取代的氨基等; R2代表由下式表示的基团：其中R16表示碳原子数1〜6的烷基等）等。 R3表示由下式表示的基团：-O-（CH 2）m -Y（Y表示咪唑基或哌嗪基等，m为1至6）等; R5代表氢原子，低级烷基等; A表示由下式表示的基团：其中R6表示氢原子，低级烷基等，-N =等; B代表由下式表示的基团：其中R4代表氢等，-N =等。

5. 发明授权

US5576322A Anti-ischemic 2,4-diaminoquinazolines 失效
标题翻译：抗缺血性2,4-二氨基喹唑啉
公开(公告)号：US5576322A
公开(公告)日：1996-11-19
申请号：US196110
申请日：1994-02-18
申请人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
发明人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04
CPC分类号： C07D235/06 , C07D215/42 , C07D231/12 , C07D233/56 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , C07D491/04
摘要： The invention is directed to certain 2,4-diaminoquinazoline compounds, their pharmaceutically acceptable salts, the pharmaceutical compositions comprising those compounds and their therapeutic methods of use. The compounds possess anti-ischemic activity.
摘要翻译： PCT No.PCT / JP92 / 01258 Sec。 371日期1994年2月18日 102（e）日期1994年2月18日PCT提交1992年9月30日PCT公布。出版物WO93 / 07124 日期1994年4月15日本发明涉及某些2,4-二氨基喹唑啉化合物，其药学上可接受的盐，包含那些化合物的药物组合物及其治疗方法。该化合物具有抗缺血活性。

6. 发明授权

US5693652A Benzimidazoles for ischemic heart conditions 失效
标题翻译：苯并咪唑用于缺血性心脏病
公开(公告)号：US5693652A
公开(公告)日：1997-12-02
申请号：US408867
申请日：1995-03-23
申请人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
发明人： Yasutaka Takase , Nobuhisa Watanabe , Makoto Matsui , Hironori Ikuta , Teiji Kimura , Takao Saeki , Hideyuki Adachi , Tadakazu Tokumura , Hisatoshi Mochida , Yasunori Akita , Shigeru Souda
IPC分类号： C07D215/42 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P37/00 , A61P43/00 , B60S1/16 , B60S1/24 , C07D215/48 , C07D235/06 , C07D235/08 , C07D239/78 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/90 , C07D239/94 , C07D239/95 , C07D239/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/056 , C07D521/00 , F16C7/02 , F16C11/04 , C07D235/04
CPC分类号： C07D235/06 , C07D215/42 , C07D231/12 , C07D233/56 , C07D239/84 , C07D239/86 , C07D239/88 , C07D239/94 , C07D239/95 , C07D239/96 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/12 , C07D471/04 , C07D491/04
摘要： The present invention provides a nitrogenous heterocyclic compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof which is useful for various ischemic heart diseases and the like: ##STR1## �in formula (1), ring A represents a benzene ring, a pyridine ring or a cyclohexane ring: ring B represents a pyridine ring, a pyrimidine ring or an imidazole ring, R.sup.1, R.sup.2, R.sup.3 R.sup.4, R.sup.5 and R.sup.6 are described herein.
摘要翻译：本发明提供由以下通式（1）表示的含氮杂环化合物或其药理学上可接受的盐，其可用于各种缺血性心脏病等：（1）[式（1）中，环A 表示苯环，吡啶环或环己烷环：环B表示吡啶环，嘧啶环或咪唑环，R1，R2，R3，R4，R5和R6如本文所述。

7. 发明授权

US07238720B2 Pharmaceutical use of N-carbamoylazole derivatives 失效
标题翻译： N-氨基甲酰唑衍生物的药用
公开(公告)号：US07238720B2
公开(公告)日：2007-07-03
申请号：US10766388
申请日：2004-01-27
申请人： Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Seiji Yoshikawa , Toshimi Okada , Hironori Ikuta , Mika Koyanagi
发明人： Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Seiji Yoshikawa , Toshimi Okada , Hironori Ikuta , Mika Koyanagi
IPC分类号： A61K31/4196 , A61K31/416 , C07D43/02
CPC分类号： C07D451/02 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects. The present invention provides a dipeptidyl peptidase IV inhibiting agent comprising a compound represented by the general formula (I):
摘要翻译：本发明涉及1-氨基甲酰唑衍生物作为药物的用途，以及含有1-氨基甲酰唑衍生物作为活性成分的药物组合物，基于其DPPIV抑制作用。本发明提供了包含通式（I）表示的化合物的二肽基肽酶IV抑制剂：

8. 发明授权

US5453524A Phosphorus-containing isoprenoid derivatives 失效
标题翻译：含磷类异戊二烯衍生物
公开(公告)号：US5453524A
公开(公告)日：1995-09-26
申请号：US199231
申请日：1994-02-22
申请人： Katsuya Tagami , Ichirou Yoshida , Naoki Kobayashi , Yoshio Fukuda , Yoshihito Eguchi , Makoto Nakagawa , Hironobu Hiyoshi , Hironori Ikuta , Makoto Kaino , Kenji Hayashi , Issei Ohtsuka , Shinya Abe , Shigeru Souda
发明人： Katsuya Tagami , Ichirou Yoshida , Naoki Kobayashi , Yoshio Fukuda , Yoshihito Eguchi , Makoto Nakagawa , Hironobu Hiyoshi , Hironori Ikuta , Makoto Kaino , Kenji Hayashi , Issei Ohtsuka , Shinya Abe , Shigeru Souda
IPC分类号： A61K31/66 , A61P3/06 , C07C211/21 , C07C233/03 , C07F9/38 , C07F9/40 , C07F9/02
CPC分类号： C07F9/405 , C07C211/21 , C07C233/03 , C07F9/3808 , C07F9/3826 , C07F9/3843 , C07F9/3873 , C07F9/4006 , C07F9/4015 , C07F9/4025
摘要： The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.sub.2).sub.m -- (wherein m is an integer of 0 to 3), a group represented by the formula: --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.q -- (wherein p is 0 or 1 and q is 1 or 2) or a group represented by the Formula: ##STR3## (wherein R.sup.8 represents a hydrogen atom or a lower alkyl group; A represents an alkylene chain which has 1 to 5 carbon atoms and which may have a substituent on each carbon atom; and r is zero or an integer of 1 to 5); and n is zero or an integer of 1 to 5.
摘要翻译： PCT No.PCT / JP92 / 01082 Sec。 371日期：1994年2月22日 102（e）日期1994年2月22日PCT提交1992年8月27日PCT公布。公开号WO93 / 04073 日本1993年3月4日。本发明提供由以下通式（I）表示的含磷类异戊二烯衍生物或其药理学上可接受的盐，其可用作抑制角鲨烯合成酶的疾病的预防和治疗剂作用有效：其中R 1和R 2各自表示氢原子，低级烷基，环烷基，烯基或炔基，可被取代的芳基，芳基可以被取代的芳基烷基或杂芳基或杂芳基烷基：R 3和R 4各自表示氢原子，低级烷基或碱金属; Y表示由下式表示的基团：其中R 5和R 6各自表示氢原子，低级烷基或碱金属或由下式表示的基团：-CO 2 R 7（其中R 7表示氢原子，低级烷基或碱金属）; Z表示由下式表示的基团： - （CH 2）m - （其中m为0至3的整数），由下式表示的基团： - （CH 2）p-CH = CH-（CH 2）q - （其中p为0或1，q为1或2）或由下式表示的基团：其中R8表示氢原子或低级烷基; A表示亚烷基具有1至5个碳原子并且在每个碳原子上可以具有取代基的链;并且r为0或1至5的整数）; n为0或1至5的整数。

9. 发明授权

US5719303A Phosphonic acid derivatives 失效
标题翻译：膦酸衍生物
公开(公告)号：US5719303A
公开(公告)日：1998-02-17
申请号：US530311
申请日：1995-09-06
申请人： Ichirou Yoshida , Hironori Ikuta , Yoshio Fukuda , Yoshihito Eguchi , Makoto Kaino , Katsuya Tagami , Naoki Kobayashi , Kenji Hayashi , Hironobu Hiyoshi , Issei Ohtsuka , Makoto Nakagawa , Shinya Abe , Shigeru Souda
发明人： Ichirou Yoshida , Hironori Ikuta , Yoshio Fukuda , Yoshihito Eguchi , Makoto Kaino , Katsuya Tagami , Naoki Kobayashi , Kenji Hayashi , Hironobu Hiyoshi , Issei Ohtsuka , Makoto Nakagawa , Shinya Abe , Shigeru Souda
IPC分类号： A61K31/66 , A61K31/675 , A61P3/06 , A61P9/12 , C07F9/38 , C07F9/40 , C07F9/547 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/62 , C07F9/6503 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6541 , C07F9/655 , C07F9/6553 , C07F9/6558 , C07F9/6574
CPC分类号： C07F9/65746 , C07F9/3808 , C07F9/3826 , C07F9/3839 , C07F9/386 , C07F9/3873 , C07F9/4006 , C07F9/4015 , C07F9/4025 , C07F9/404 , C07F9/405 , C07F9/4056 , C07F9/4075 , C07F9/5721 , C07F9/5727 , C07F9/5728 , C07F9/582 , C07F9/588 , C07F9/591 , C07F9/592 , C07F9/598 , C07F9/60 , C07F9/62 , C07F9/65038 , C07F9/65061 , C07F9/65068 , C07F9/650958 , C07F9/650994 , C07F9/65127 , C07F9/653 , C07F9/65324 , C07F9/6533 , C07F9/6539 , C07F9/6541 , C07F9/65505 , C07F9/65515 , C07F9/65517 , C07F9/6552 , C07F9/65522 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/65742
摘要： A phosphonic acid derivative which is useful for medically treating hyperlipemia, represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## Representative example of the compound according to the present invention is one represented by the following formula: ##STR2##
摘要翻译： PCT No.PCT / JP94 / 00354 Sec。 371日期：1995年9月6日 102（e）日期1995年9月6日PCT 1994年3月4日PCT公布。 WO94 / 20508 PCT公开号日期：1994年9月15日由以下通式（I）表示的用于医疗治疗高脂血症的膦酸衍生物或其药理学上可接受的盐：（I）本发明化合物的代表性实例是一个由以下公式表示：

10. 发明申请

US20090018331A1 CONDENSED IMIDAZOLE DERIVATIVES 失效
标题翻译：稠密咪唑衍生物
公开(公告)号：US20090018331A1
公开(公告)日：2009-01-15
申请号：US12199982
申请日：2008-08-28
申请人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号： C07D498/14 , C07D473/04 , C07D487/04
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译：本发明涉及由下式表示的化合物或其盐或水合物，其中，T1表示在环中含有一个或两个氮原子的4至12元杂环基，其为单环或双环结构，其可以是具有一个或多个取代基; X表示可以具有一个或多个取代基的C 1-6烷基; Z 1和Z 2各自独立地表示氮原子或由式-CR 2表示的基团; R1和R2独立地表示氢原子，可以具有一个或多个取代基的C 1-6烷基或可以具有一个或多个取代基的C 1-6烷氧基等。这些是表现出优异的DPPIV抑制活性的新型化合物。

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