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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

WO1998014431A1 NITROGENOUS HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：硝基杂环化合物
公开(公告)号：WO1998014431A1
公开(公告)日：1998-04-09
申请号：PCT/JP1997003510
申请日：1997-10-01
申请人： KYOWA HAKKO KOGYO CO., LTD. , MATSUNO, Kenji , ICHIMURA, Michio , NOMOTO, Yuji , FUJIWARA, Shigeki , IDE, Shinichi , TSUKUDA, Eiji , IRIE, Junko , ODA, Shoji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D215/46
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-R , Y is nitrogen or C-R and Z is nitrogen or C-R , with at least one of X, Y and Z being nitrogen; R is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like; R is substituted alkyl, substituted or unsubstituted cycloalkyl or the like; R , R , R and R are each independently hydrogen, halogeno, substituted or unsubstituted alkyl, nitro, cyano, -OR , -NR R or the like; R is halogeno or the like; R is the same as defined above for R ; and R is hydrogen or -COR .
摘要翻译：通式（I）的氮杂环化合物及其药理学上可接受的盐阻碍PDGF受体的磷酸化和细胞的异常增殖或迁移等，有效预防或治疗细胞增殖性疾病如动脉硬化，血管再闭塞疾病，癌症和肾小球硬化，其中V是氧或硫; W是可以在环上被未取代的烷基取代的1,4-哌嗪二基或1,4-高哌嗪二基; X是氮或C-R 9，Y是氮或C-R 8，Z是氮或C-R 7，X，Y和Z中的至少一个是氮; R 1是氢，取代或未取代的烷基，取代或未取代的环烷基等; R 2是取代的烷基，取代或未取代的环烷基等; R 3，R 4，R 5和R 6各自独立地为氢，卤素，取代或未取代的烷基，硝基，氰基，-OR 12，-NR 15 R 16，或类似物; R 7是卤代等; R 8与上述R 7相同; R 9为氢或-COR 41。

3. 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。

4. 发明申请

WO1995000546A1 ENDOTHELIN-ANTAGONIZING PEPTIDE 审中-公开
标题翻译：内皮素 - 拮抗肽
公开(公告)号：WO1995000546A1
公开(公告)日：1995-01-05
申请号：PCT/JP1994001011
申请日：1994-06-23
申请人： KYOWA HAKKO KOGYO CO., LTD. , SHIBATA, Kenji , SUZAWA, Toshiyuki , YAMASAKI, Motoo , TANAKA, Takeo , TSUKUDA, Eiji , YAMADA, Koji , OHNO, Tetsuji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07K07/08
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：由通式（I）表示的内皮素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 其中R 1为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; Pro，Ala，Arg或单键; R 9为（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为羟基，低级烷氧基或氨基。

5. 发明申请

WO1995026960A1 PHYSIOLOGICALLY ACTIVE SUBSTANCE EI-1507 审中-公开
标题翻译：生理活性物质EI-1507
公开(公告)号：WO1995026960A1
公开(公告)日：1995-10-12
申请号：PCT/JP1995000625
申请日：1995-03-31
申请人： KYOWA HAKKO KOGYO CO., LTD. , TSUKUDA, Eiji , TANAKA, Takeo , OCHIAI, Keiko , ANDO, Katsuhiko , KONDO, Hidemasa , TESHIBA, Sadao , AGATSUMA, Tsutomu , YOSHIDA, Mayumi , MATSUDA, Yuzuru
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D303/32
CPC分类号： C12P17/02 , C07D303/32
摘要： A physiologically active substance EI-1507 represented by general formula (I), wherein X and Y are combined together to represent oxygen, or each independently represents hydrogen or hydroxyl.
摘要翻译：由通式（I）表示的生理活性物质EI-1507，其中X和Y组合在一起代表氧，或各自独立地表示氢或羟基。

6. 发明申请

WO1994022806A1 PHYSIOLOGICALY ACTIVE SUBSTANCE RES-1149-1 AND DERIVATIVE THEREOF 审中-公开
标题翻译：生理活性物质RES-1149-1及其衍生物
公开(公告)号：WO1994022806A1
公开(公告)日：1994-10-13
申请号：PCT/JP1994000506
申请日：1994-03-29
申请人： KYOWA HAKKO KOGYO CO., LTD. , OGAWA, Tatsuhiro , TANAKA, Takeo , TSUKUDA, Eiji , UOSAKI, Youichi , YOSHIDA, Mayumi , ANDO, Katsuhiko , IWASAKI, Toshiaki , KITA, Katsunori , MATSUDA, Yuzuru
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07C69/013
CPC分类号： A61K31/215 , C07C69/013 , C12P7/62
摘要： A physiologically active substance RES-1149-1 having excellent effects of antagonizing endoserine and suppressing the rise of the intracellular calcium level and represented by general formula (I) and a derivative thereof, wherein R represents C2 - C22 alkyl or alkenyl, (un)substituted aryl or (un)substituted heterocyclic group.
摘要翻译：具有优异的拮抗内啡肽的效果的生理活性物质RES-1149-1，抑制由通式（I）表示的细胞内钙水平升高及其衍生物，其中R表示C2-C22烷基或链烯基，（un）取代的芳基或（未）取代的杂环基。

7. 发明申请

WO1993013218A1 ENDOTHELIN-ANTAGONIZING PEPTIDE 审中-公开
标题翻译：内皮素拮抗肽
公开(公告)号：WO1993013218A1
公开(公告)日：1993-07-08
申请号：PCT/JP1992001731
申请日：1992-12-28
申请人： KYOWA HAKKO KOGYO CO., LTD. , 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
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： 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.
摘要翻译：由以下通式表示的新肽及其制备方法：X-A-Trp-B-Gly-Thr-E-G-Y其中A表示Asn或Asp; B代表His或Lys; E表示Ala或Ser; G代表Ala或Pro; X表示X 1 -Gly或X 3 -Cys-X 2; Y表示羟基，低级烷氧基，氨基，Y 1 -Asp-Z或Y 2 -Cys-Z。从链霉菌培养物的产物中分离肽，具有内皮素拮抗作用和抑制由内皮素引起的细胞内钙或环鸟苷-3磷酸盐浓度升高的活性。

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