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1. 发明申请

WO0216362A3 NITROGENOUS HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：非活性杂环化合物
公开(公告)号：WO0216362A3
公开(公告)日：2002-06-13
申请号：PCT/US0141751
申请日：2001-08-17
申请人： COR THERAPEUTICS INC , KYOWA HAKKO KOGYO KK , PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , FUJIWARA SHIGEKI , IDE SHINICHI , TSUKUDA EIJI , IRIE JUNKO , ODA SHOJI
发明人： PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , FUJIWARA SHIGEKI , IDE SHINICHI , TSUKUDA EIJI , IRIE JUNKO , ODA SHOJI
IPC分类号： A61P35/00 , C07D239/94 , C07D401/12 , C07D403/12 , A61K31/517
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
摘要翻译：本发明涉及对激酶的磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐，其抑制这些激酶的活性。本发明还涉及抑制激酶并通过抑制激酶的磷酸化来治疗哺乳动物的疾病状态的方法。本发明的一个特定方面提供了抑制PDGF受体的磷酸化以阻碍异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管性重建，癌症和肾小球硬化。

2. 发明申请

WO0216360A3 NITROGENOUS HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：硝基杂环化合物
公开(公告)号：WO0216360A3
公开(公告)日：2002-06-13
申请号：PCT/US0141749
申请日：2001-08-17
申请人： COR THERAPEUTICS INC , KYOWA HAKKO KOGYO KK , PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , FUJIWARA SHIGEKI , IDE SHINICHI , TSUKUDA EIJI , IRIE JUNKO , ODA SHOJI
发明人： PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , FUJIWARA SHIGEKI , IDE SHINICHI , TSUKUDA EIJI , IRIE JUNKO , ODA SHOJI
IPC分类号： A61P35/00 , C07D239/94 , C07D401/12 , C07D403/12 , A61K31/517 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
摘要翻译：本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管重建，癌症和肾小球硬化症。

3. 发明公开

EP0668280A4 IMIDAZOQUINAZOLINE DERIVATIVE. 失效
标题翻译：咪唑并CHINAZOLIN衍生物。
公开(公告)号：EP0668280A4
公开(公告)日：1995-07-04
申请号：EP94925621
申请日：1994-09-02
申请人： KYOWA HAKKO KOGYO KK
发明人： MACHII DAISUKE , MATSUNO KENJI , KINOSHITA IWAO , NOMOTO YUJI , TAKAI HARUKI , OHNO TETSUJI , NAGASHIMA KEN , ISHIKAWA TOMOKO , YAMADA KOJI , ICHIMURA MICHIO , KASE HIROSHI
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R1 andR2 may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R3 represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.

4. 发明公开

EP1251130A4 FUSED PURINE DERIVATIVES 有权
标题翻译：简明的嘌呤衍生物
公开(公告)号：EP1251130A4
公开(公告)日：2003-05-02
申请号：EP00985847
申请日：2000-12-22
申请人： KYOWA HAKKO KOGYO KK
发明人： UENO KIMIHISA , OGAWA AKIRA , OHTA YOSHIHISA , NOMOTO YUJI , TAKASAKI KOTARO , KUSAKA HIDEAKI , YANO HIROSHI , SUZUKI CHIHARU , NAKANISHI SATOSHI
IPC分类号： A61P3/10 , C07D487/14 , A61K31/505 , A61K31/519 , A61K31/522 , A61K31/5377
CPC分类号： C07D487/14
摘要： Fused purine derivatives represented by the general formula (I) or pharmacologically acceptable salts thereof, wherein X--Y--Z represents R1N-C=O (wherein R1 is hydrogen, lower alkyl, or the like) or N=C-W (wherein W is halogeno, an aromatic heterocyclic group, an aliphatic heterocyclic group, or the like); R2 is hydrogen, lower alkyl, aralkyl, aryl, an aromatic heterocyclic group, an aliphatic heterocyclic group, or the like; R3 is hydrogen, lower alkyl, aralkyl, or the like; n is an integer of 0 to 3; V1 is hydrogen, lower alkyl, aralkyl, aryl, or an aromatic heterocyclic group; and V2 is substituted lower alkyl or an aromatic heterocyclic group, with the proviso that V2 may represent lower alkyl, aralkyl, or aryl in, e.g., cases wherein V1 is hydrogen, lower alkyl, aralkyl, or aryl; X--Y--Z is R1aN-C=O (wherein R1a is the same as defined for R1, except substituted lower alkyl); and R2 is substituted lower alkyl, aralkyl, or an aliphatic heterocyclic group.

5. 发明公开

EP1067123A4 NITROGENOUS HETEROCYCLIC COMPOUNDS 有权
标题翻译：。。。。。。。。。。。。。。。。。
公开(公告)号：EP1067123A4
公开(公告)日：2002-04-03
申请号：EP99912061
申请日：1999-03-31
申请人： KYOWA HAKKO KOGYO KK
发明人： MATSUNO KENJI , NOMOTO YUJI , ICHIMURA MICHIO , IDE SHIN-ICH , ODA SHOJI
IPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D473/34 , C07D487/04 , A61K31/52 , C07D473/32 , C07D495/04
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D405/12 , C07D471/04 , C07D473/34 , C07D487/04
摘要： Nitrogenous heterocyclic compounds represented by general formula (I) or pharmacologically acceptable salts thereof, wherein W reprsents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents hydrogen, optionally substituted alkyl, etc. and R2 represents hydrogen, etc.), OR?4, or SR5¿; V represents oxygen, sulfur, N-R?6, or CR7R8¿; at least one of X, Y, and Z represents nitrogen and the remainder are the same or different and each represents nitrogen or C-R?A; and D1, D2, D3, and D4¿ each independently represents C-RB, nitrogen, oxygen, sulfur, etc. or any adjacent two of D1 to D4 in combination represent nitrogen, N-R2A, oxygen, sulfur, etc., or any adjacent two of D1 to D4 represent C-RB'' (wherein two RB''s in combination represent optionally substituted alicyclic alkene, optionally substituted pyrrole, optionally substituted pyrazole, etc.), etc.
摘要翻译：本发明涉及由式（I）表示的含氮杂环化合物：其中W代表1,4-哌嗪二基等; U表示NR 1 R 2（其中R 1表示氢原子，取代或未取代的烷基等; R 2表示氢原子等），OR 4，或SR <5>; V表示氧原子，硫原子，NR 6或CR 7 R 8，X，Y和Z中的至少一个表示氮原子，其它相同或不同，各自相同或不同，表示氮原子或CR ; 和D 1，D 2，D 3和D 4各自独立地表示CR B，氮原子，氧原子，硫原子等，D <1中任意相邻的两个 > D <4>组合以表示氮原子，NR 2A，氧原子，硫原子等，或选自D 1至D 4中的任选相邻的两个表示CR

6. 发明公开

EP0882717A4 NITROGENOUS HETEROCYCLIC COMPOUNDS 失效
标题翻译：含氮化合物HYDROCYCLISCHE
公开(公告)号：EP0882717A4
公开(公告)日：2002-06-19
申请号：EP97943133
申请日：1997-10-01
申请人： KYOWA HAKKO KOGYO KK
发明人： MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , FUJIWARA SHIGEKI , IDE SHINICHI , TSUKUDA EIJI , IRIE JUNKO , ODA SHOJI
IPC分类号： A61K31/496 , A61K31/502 , A61K31/517 , C07D215/46 , C07D217/22 , C07D237/34 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/04 , A61K31/495 , A61K31/50 , C07D491/04
CPC分类号： C07D401/12 , A61K31/496 , A61K31/502 , A61K31/517 , C07D215/46 , C07D217/22 , C07D237/34 , C07D239/94 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/04
摘要： Nitrogenous heterocyclic compounds of general formula (I) and pharmacologically acceptable salts thereof, which hinder the phosphorylation of PDGF acceptors and the abnormal proliferation or migration of cells and so are effective in preventing or treating cell proliferative diseases such as arterial sclerosis, vascular reocclusion diseases, cancer and glomerulosclerosis, wherein V is oxygen or sulfur; W is 1,4-piperazinediyl or 1,4-homopiperazinediyl which may be substituted with unsubstituted alkyl on the ring; X is nitrogen or C-R9, Y is nitrogen or C-R8 and Z is nitrogen or C-R7, with at least one of X, Y and Z being nitrogen; R1 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like; R2 is substituted alkyl, substituted or unsubstituted cycloalkyl or the like; R?3, R4, R5 and R6¿ are each independently hydrogen, halogeno, substituted or unsubstituted alkyl, nitro, cyano, -OR?12, -NR15R16¿ or the like; R7 is halogeno or the like; R8 is the same as defined above for R?7; and R9¿ is hydrogen or -COR41.

7. 发明公开

EP0863144A4 IMIDAZOQUINAZOLINE DERIVATIVES 失效
标题翻译： IMIDAZOCHINAZOLINE
公开(公告)号：EP0863144A4
公开(公告)日：2001-04-11
申请号：EP97937841
申请日：1997-08-29
申请人： KYOWA HAKKO KOGYO KK
发明人： ONODA YASUO , NOMOTO YUJI , OHNO TETSUJI , YAMADA KOJI , ICHIMURA MICHIO
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, which have potent and selective inhibitory effects on cyclic guanosine-3',5'-monophosphate (cGMP)-specific phosphodiesterase and are useful in, for example, treating or relieving cardiovascular diseases such as thrombosis, angina pectoris, hypertension, cardiac insufficiency and arteriosclerosis, asthma, etc. and treating sexual impotence. In said formula, R1 represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, etc.; R2 represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicyclaolkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc.; R3 represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc., or R?2 and R3¿ may form together with N an optionally substituted heterocyclic group; and X represents O or S.
摘要翻译：由通式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其对环鸟苷-3'，5'-单磷酸（cGMP）特异性磷酸二酯酶具有有效和选择性的抑制作用，并且可用于例如治疗或缓解心血管疾病如血栓形成，心绞痛，高血压，心功能不全和动脉硬化，哮喘等，并治疗性无能。在所述式中，R 1表示氢，任选取代的低级烷基，任选取代的环烷基，任选取代的二环烷基，任选取代的三环烷基等; R2代表氢，任选取代的低级烷基，任选取代的环烷基，任选取代的二环烷基，任选取代的三环烷基，任选取代的低级烯基，任选取代的芳烷基等; R 3代表氢，任选取代的低级烷基，任选取代的环烷基，任选取代的双环烷基，任选取代的三环烷基，任选取代的低级烯基，任选取代的芳烷基等，或者R 2和R 3可与N一起形成任选取代的杂环基 ; X代表O或S.

8. 发明专利

CZ304061B6 Derivát chinazolinu, farmaceutická kompozice a lécivo s jeho obsahem 未知
公开(公告)号：CZ304061B6
公开(公告)日：2013-09-11
申请号：CZ2003765
申请日：2001-08-17
申请人： MILLENNIUM PHARMACEUTICALS , KYOWA HAKKO KOGYO KK
发明人： PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , IDE SHINICHI , TSUKUDA EIJI , SASAKI JUNKO , ODA SHOJI
IPC分类号： C07D403/14 , A61K31/517 , A61K31/5377 , A61K31/541 , A61P9/08 , A61P9/10 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/14 , C07D417/14
摘要： Derivát chinazolinu obecného vzorce I(g) nebo I(h), kde R.sup.1.n. je clen vybraný ze souboru sestávajícího ze skupin -CN, -O-methyl, -O-ethyl, -O-propyl, -O-1-methylethyl, -O-butyl, -O-1,1-dimethylethyl, -O-3-methylbutyl, 1-naftyloxy, 2-naftyloxy, 4-indolyloxy, 5-indolyloxy, a 5-isochinolyloxy, R.sup.3.n. je clen vybraný ze souboru sestávajícího ze skupin -OH, -O-CH.sub.3.n., -O-CH.sub.2.n.-CH.sub.3.n., -NH.sub.2.n., -N(-CH.sub.3.n.).sub.2.n., -NH(CH.sub.3.n.-fenyl), -NH(fenyl), -CN, -C(=NH)NH.sub.2.n., -HNC(=NH)NH.sub.2.n. a hererocyklických zbytku definovaných v nároku 1 a n je císlo 2 nebo 3; a jeho farmaceuticky vhodné soli. Farmaceutická kompozice obsahující tento derivát chinazolinu a farmaceuticky vhodné redidlo nebo nosic. Lécivo pro inhibici fosforylace receptoru rustového faktoru pocházejícího z krevních desticek, PDGF receptoru u pacienta a lécivo pro prevenci a lécení choroby spojené s bunecnou proliferací, jako arteriosklerózy, vaskulární reobstrukce, restenózy, rakoviny a glomerulosklerózy.

9. 发明专利

CA2426440C QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS 未知
公开(公告)号：CA2426440C
公开(公告)日：2011-03-15
申请号：CA2426440
申请日：2001-08-17
申请人： MILLENNIUM PHARM INC , KYOWA HAKKO KOGYO KK
发明人： PANDEY ANJALI , SCARBOROUGH ROBERT M , MATSUNO KENJI , ICHIMURA MICHIO , NOMOTO YUJI , IDE SHINICHI , TSUKUDA EIJI , SASAKI JUNKO , ODA SHOJI
IPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/541 , A61P9/08 , A61P9/10 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

10. 发明专利

CA2326324C NITROGEN-CONTAINING HETEROCYCLIC COMPOUND 未知
公开(公告)号：CA2326324C
公开(公告)日：2010-05-11
申请号：CA2326324
申请日：1999-03-31
申请人： KYOWA HAKKO KOGYO KK
发明人： MATSUNO KENJI , NOMOTO YUJI , ICHIMURA MICHIO , IDE SHIN-ICHI , ODA SHOJI
IPC分类号： C07D239/94 , A61K31/435 , A61K31/505 , A61K31/52 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D473/32 , C07D473/34 , C07D487/04 , C07D495/04
摘要： The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): (see formula I) wherein W represents 1, 4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc.), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N-R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C-R A; and D1, D2, D3 and D4 each independently represent C-R B, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N-R2A, an oxygen atom, a sulfur atom, etc., or optional adjoining two selected from D1 to D4 represent C-R B" (wherein two R B"s are combined to represent substituted or unsubstituted alicyclic alkene, substituted or unsubstituted pyrrole, substituted or unsubstituted pyrazole, etc.; or pharmaceutically acceptable salts thereof.

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