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1. 发明授权

US5420348A Urea derivatives and salts thereof 失效
标题翻译：尿素衍生物及其盐
公开(公告)号：US5420348A
公开(公告)日：1995-05-30
申请号：US086689
申请日：1993-07-02
申请人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka , Yuichi Iizumi
发明人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka , Yuichi Iizumi
IPC分类号： C07C275/28 , C07C275/26
CPC分类号： C07C275/28 , C07C2101/18 , C07C2103/18 , C07C2103/26
摘要： Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are-disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.
摘要翻译：通式（I）的脲衍生物（Ⅰ）及其盐，含有它们的药物组合物及其制备方法公开。通式（I）的脲衍生物及其盐是具有酰基-CoA胆固醇酰基转移酶（ACAT）抑制活性的新化合物。

2. 发明授权

US5258405A Urea derivatives and salts thereof in method for inhibiting the ACAT enzyme 失效
标题翻译：尿素衍生物及其盐在抑制ACAT酶的方法中
公开(公告)号：US5258405A
公开(公告)日：1993-11-02
申请号：US953755
申请日：1992-09-29
申请人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka
发明人： Noriki Ito , Koyo Matsuda , Kiyoshi Iwaoka
IPC分类号： C07C275/28 , A61K31/17
CPC分类号： C07C275/28 , C07C2101/18 , C07C2103/18 , C07C2103/26
摘要： Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are disclosed.The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.
摘要翻译：公开了通式（I）的脲衍生物及其盐，含有它们的药物组合物及其制备方法。通式（I）的脲衍生物及其盐是具有酰基-CoA胆固醇酰基转移酶（ACAT）抑制活性的新化合物。

3. 发明授权

US06300364B1 Medicinal compositions with cholesterol-lowering effect 有权
标题翻译：具有降胆固醇作用的药物组合物
公开(公告)号：US06300364B1
公开(公告)日：2001-10-09
申请号：US09463334
申请日：2000-01-24
申请人： Teruhiko Shimokawa , Satomi Nishijima , Koyo Matsuda , Yuichi Iizumi , Seiichi Hashimoto
发明人： Teruhiko Shimokawa , Satomi Nishijima , Koyo Matsuda , Yuichi Iizumi , Seiichi Hashimoto
IPC分类号： A01N4338
CPC分类号： A61K31/192 , C07K14/705
摘要： Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;. Also, a method for identifying a compound having an excellent cholesterol-lowering effect was found, wherein the desired compound can be quickly and efficiently screened from among a number of compounds by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect.
摘要翻译：包含具有降胆固醇作用的药物组合物，其包含具有PPAR（过氧化物酶体增殖物激活受体）δ激活作用或PPARδ和PPARγ活化作用的化合物或其药学上可接受的盐作为活性成分; 药物组合物，其中所述降胆固醇作用是降低LDL-胆固醇的作用; 以及用于鉴定具有胆固醇降低作用的化合物的方法，其特征在于测量PPARδ激活作用或其PPARδ和PPARγ活化作用。解决方法：发现对高等动物如人和猿具有优异的降低胆固醇的作用的化合物具有激活PPARdta或PPARδ和PPARγ的作用。另外，发现了鉴定具有优异的降胆固醇降低作用的化合物的方法，通过测量PPARδ激活效应或PPARδ和PPARγ活化效应，可以从多种化合物中快速有效地筛选所需化合物。

4. 发明授权

US06403588B1 Imidazopyridine derivatives 有权
公开(公告)号：US06403588B1
公开(公告)日：2002-06-11
申请号：US09843610
申请日：2001-04-26
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
IPC分类号： A61K31435
CPC分类号： C07D471/04 , A61K31/435 , C07D487/04
摘要： The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

5. 发明申请

US20100137585A1 FUSED HETEROARYL DERIVATIVES 审中-公开
公开(公告)号：US20100137585A1
公开(公告)日：2010-06-03
申请号：US12688273
申请日：2010-01-15
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号： C07D487/04 , C07D491/048 , C07D495/04
CPC分类号： C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

6. 发明授权

US5830902A Quinuclidine derivative having tricyclic hetero condensed ring 失效
标题翻译：具有三环杂环稠环的奎宁环衍生物
公开(公告)号：US5830902A
公开(公告)日：1998-11-03
申请号：US894549
申请日：1997-08-21
申请人： Masahiko Isaka , Tsukasa Ishihara , Koyo Matsuda , Hirotoshi Kakuta , Hiroshi Moritani
发明人： Masahiko Isaka , Tsukasa Ishihara , Koyo Matsuda , Hirotoshi Kakuta , Hiroshi Moritani
IPC分类号： C07D453/02 , A61K31/435 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D453/02
摘要： A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group, R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group, . . : a single bond or a double bond, with the proviso that R.sub.2 does not exist when . . . is a double bond, X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --, p: 0, 1 or 2, R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent, A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n -- or a group of the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n CR.sub.4 =, Z: an oxygen atom (--O--), a group of the formula --S(O).sub.q --, a carbonyl group (--CO--) or a group of the formula --NR.sub.5 --, R.sub.4 : a hydrogen atom, a halogen atom or a lower alkyl group, R.sub.5 : a hydrogen atom or a lower alkyl group, m and n: the same or different from each other and each is 0 or an integer of 1 to 5, m+n: an integer of 1 to 5 q: 0, 1 or 2, with the proviso that, when either one of X and Y is a bond, A is a group represented by the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n CR.sub.4 =.)
摘要翻译： PCT No.PCT / JP96 / 00491 Sec。 371日期1997年8月21日 102（e）日期1997年8月21日PCT 1996年3月1日PCT公布。 WO96 / 26938 PCT公开日期1996年9月6日由以下通式（I）表示的奎宁环衍生物，其药学上可接受的盐，其水合物或溶剂合物，具有强的角鲨烯合酶抑制活性，可用作胆固醇降低剂而不引起侧效果。（I）（式中的符号表示以下含义; R1：氢原子，卤素原子或低级烷基，R2：氢原子，羟基或低级烷氧基，+ E，ovs ... + EE：单键或双键，条件是当+ E，ovs ... EE是双键时，R2不存在，X和Y彼此相同或不同代表键，氧原子（-O-），羰基（-CO-），由式-S（O）p-表示的基团或由式-NR3-表示的基团，p：0， 1或2，R3：氢原子或可具有取代基的低级烷基，A：饱和或不饱和的低级亚烷基，式 - （CH2）mZ（CH2）n-的基团或式 - （CH 2）m Z（CH 2）n CR 4 =，Z：氧原子（-O-），式-S（O）q-的基团，羰基（-CO-）或式 -NR5-，R4：氢原子，卤素原子或低级烷基，R5：氢原子或低级烷基，m和n：相同或不同各自为0或1〜5的整数，m + n：1〜5的整数q：0,1或2，条件是当X和Y中的任一个为键时， A是由式 - （CH2）mZ（CH2）nCR4 =表示的基团。

7. 发明授权

US06608053B2 Fused heteroaryl derivatives 有权
公开(公告)号：US06608053B2
公开(公告)日：2003-08-19
申请号：US09843615
申请日：2001-04-26
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号： C07D41304
CPC分类号： C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

8. 发明申请

US20070037805A1 Fused heteroaryl derivatives 审中-公开
公开(公告)号：US20070037805A1
公开(公告)日：2007-02-15
申请号：US11544144
申请日：2006-10-06
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号： A61K31/5377
CPC分类号： C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

9. 发明授权

US07037915B2 Fused heteroaryl derivatives 有权
公开(公告)号：US07037915B2
公开(公告)日：2006-05-02
申请号：US10918094
申请日：2004-08-13
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

10. 发明授权

US06838457B2 Fused heteroaryl derivatives 有权
公开(公告)号：US06838457B2
公开(公告)日：2005-01-04
申请号：US10459002
申请日：2003-06-10
申请人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人： Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号： A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14 , C07D487/04 , A61K31/381
CPC分类号： C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

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