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1. 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.

2. 发明专利

CZ2003765A3 Quinazoline derivatives functioning as kinase inhibitors 未知
公开(公告)号：CZ2003765A3
公开(公告)日：2004-08-18
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 , IRIE JUNKO , ODA SHOJI
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/541 , A61P9/08 , A61P9/10 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12 , C07D403/12 , A61K31/502
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 kinase and treating disese 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.

3. 发明专利

HU0302615A2 KINASE INHIBITOR QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE 未知
公开(公告)号：HU0302615A2
公开(公告)日：2003-12-29
申请号：HU0302615
申请日：2001-08-17
申请人： KYOWA HAKKO KOGYO KK , MILLENNIUM PHARMACEUTICALS
发明人： FUJIWARA SHIGEKI , ICHIMURA MICHIO , IDE SHINICHI , IRIE JUNKO , MATSUNO KENJI , NOMOTO YUJI , ODA SHOJI , PANDEY ANJALI , SCARBOROUGH ROBERT M , TSUKUDA EIJI
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/541 , A61P9/08 , A61P9/10 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12 , 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 kinase and treating disese 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.

5. 发明专利

CZ20030765A3 Quinazoline derivatives functioning as kinase inhibitors 未知
公开(公告)号：CZ20030765A3
公开(公告)日：2004-08-18
申请号：CZ20030765
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 , IRIE JUNKO , ODA SHOJI
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/541 , A61P9/08 , A61P9/10 , A61P13/12 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12 , C07D403/12 , A61K31/502
CPC分类号： C07D239/94 , A61K31/517 , C07D401/12 , C07D403/12

6. 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。

7. 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。

8. 发明公开

EP0603399A4 ENDOTHELIN-ANTAGONIZING PEPTIDE. 失效
标题翻译：内皮素拮抗肽。
公开(公告)号：EP0603399A4
公开(公告)日：1997-03-05
申请号：EP93900411
申请日：1992-12-28
申请人： KYOWA HAKKO KOGYO KK
发明人： TANAKA TAKEO , MORISHITA YOSHIKAZU , NOZAWA MIKA , CHIBA SHIGERU , KAWAMOTO ISAO , TSUKUDA EIJI , YOSHIDA MAYUMI , SHIMAZAKI CHIEKO , YAMAGUCHI KAZUO , MATSUDA YUZURU , KITAMURA SHIGETO , IKEMURA TOSHIHIDE , OGAWA TATSUHIRO , YANO KEIICHI , SUZAWA TOSHIYUKI , SHIBATA KENJI , YAMASAKI MOTOO
IPC分类号： A61K38/00 , C07K5/113 , C07K5/117 , C07K7/06 , C07K7/08 , C07K14/36 , C07K14/575 , C12P21/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1021 , C07K5/1024 , C07K7/08 , C07K14/36 , C07K14/57536
摘要： A novel peptide represented by the following general formula and a process for producing the same: X-A-Trp-B-Gly-Thr-E-G-Y wherein, A represents Asn or Asp; B represents His or Lys; E represents Ala or Ser; G represents Ala or Pro; X represents X -Gly or X -Cys-X ; and Y represents hydroxy, lower alkoxy, amino, Y -Asp-Z or Y -Cys-Z. The peptide is isolated from the product of culture of a streptomyces and has an endothelin antagonism and an activity of suppressing the rise of an intracellular calcium or cyclic guanosine-3,5-phosphate concentration caused by endothelin.

9. 发明公开

EP0679658A4 ENDOTHELIN-ANTAGONIZING PEPTIDE. 失效
标题翻译： ENDOTHELINANTAGONISIERENDES PEPTID。
公开(公告)号：EP0679658A4
公开(公告)日：1997-06-04
申请号：EP95904339
申请日：1994-06-23
申请人： KYOWA HAKKO KOGYO KK
发明人： SHIBATA KENJI , SUZAWA TOSHIYUKI , YAMASAKI MOTOO , TANAKA TAKEO , TSUKUDA EIJI , YAMADA KOJI , OHNO TETSUJI
IPC分类号： A61K38/00 , C07K7/06 , C07K14/575 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00 , C07K14/57536
摘要： An endothelin-antagonizing peptide compound represented by general formula (I) and a pharmacologically acceptable salt thereof: R -R -R -R -R -R -R -R -R -R -R -R -Phe-R -R -R -R -R -Ile-R -Z wherein R is X -Gly, X (a), X -SCH2CO or hydrogen; R is Asn, Asp, Phe, Tyr, Ser or a single bond; R is Trp, Ile, Pro, Ala or a single bond; R is His, Lys, Gly, Trp, Ala or a single bond; R is Gly, Thr, Trp, Val or a single bond; R is Gly, Thr, Asn, Tyr, Asp or a single bond; R is Ala, Ser, Asn, Asp, Tyr, Phe or a single bond; R is Pro, Ala, Arg or a single bond; R is (b), (c) or a single bond; R is Trp or Ala; R is Val, Pro or a single bond; R is Tyr or a single bond; R is Ala, MeAla, Ser or Cys; R is His or Trp; R is Leu or Nva; R is Asp, Thr, Asn, Ser, Gly or Glu; R is Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg or Nle; R is Trp, Phe or Tyr; and Z is hydroxy, lower alkoxy or amino.
摘要翻译：通式（I）所示的内皮缩血管肽拮抗肽化合物及其药理学上可接受的盐：R 1 -R 2 -R 3 -R 4 -R 5 -R 6 - [R <7> -R <8> -R <9> -R <10> -R <11> -R <12> -Phe-R <14> -R <15> -R <16> -R <17 R 18 -Ile-R 20 -Z其中R 1是X 1 -Gly，X 3（a），X 2 -SCH 2 CO或氢; R 2是Asn，Asp，Phe，Tyr，Ser或单键; R 3是Trp，Ile，Pro，Ala或单键; R 4是His，Lys，Gly，Trp，Ala或单键; R 5是Gly，Thr，Trp，Val或单键; R 6是Gly，Thr，Asn，Tyr，Asp或单键; R 7是Ala，Ser，Asn，Asp，Tyr，Phe或单键; R 8是Pro，Ala，Arg或单键; R 9是（b），（c）或单键; R 10是Trp或Ala; R 11是Val，Pro或单键; R 12是Tyr或单键; R 14是Ala，MeAla，Ser或Cys; R 15是His或Trp; R 16是Leu或Nva; R 17是Asp，Thr，Asn，Ser，Gly或Glu; R 18是Ile，Leu，Cha，Abu，Thi，Met，Tyr，MeLeu，MeIle，Phg或Nle; R 20是Trp，Phe或Tyr; Z是羟基，低级烷氧基或氨基。

10. 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.

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