公开(公告)号：EP1964839A2

公开(公告)日：2008-09-03

申请号：EP08075237.1

申请日：2001-08-17

申请人： MILLENNIUM PHARMACEUTICALS, INC. ,  KYOWA HAKKO KOGYO CO., LTD.

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： C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  A61P35/00 ,  A61K31/517

CPC分类号： C07D239/94 ,  A61K31/517 ,  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 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。

公开(公告)号：EP2277877A1

公开(公告)日：2011-01-26

申请号：EP10182322.7

申请日：2001-08-17

申请人： MILLENNIUM PHARMACEUTICALS, INC. ,  Kyowa Hakko Kogyo Co., Ltd

发明人： Pandey, Anjali ,  Scarborough, Carroll ,  Matsuno, Kenji ,  Ichimura, Michio ,  Nomoto, Yuji ,  Ide, Schinichi ,  Tsukuda, Eiji ,  Irie, Junko ,  Oda, Shoji

IPC分类号： C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  A61P35/00 ,  A61K31/517

CPC分类号： C07D239/94 ,  A61K31/517 ,  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.

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激素和治疗哺乳动物中的二恶烷状态的方法。 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，以及用于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。

公开(公告)号：EP1964839A3

公开(公告)日：2008-11-05

申请号：EP08075237.1

申请日：2001-08-17

申请人： MILLENNIUM PHARMACEUTICALS, INC. ,  KYOWA HAKKO KOGYO CO., LTD.

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： C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  A61P35/00 ,  A61K31/517

CPC分类号： C07D239/94 ,  A61K31/517 ,  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 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.

公开(公告)号：EP0092391A3

公开(公告)日：1984-09-26

申请号：EP83302123

申请日：1983-04-14

申请人： KYOWA HAKKO KOGYO CO., LTD

发明人： Teranishi, Masayuki ,  Obase, Hiroyuki ,  Nomoto, Yuji ,  Shuto, Katsuichi ,  Karasawa, Akira ,  Kasuya, Yutaka

IPC分类号： C07D401/06 ,  C07D401/04 ,  A61K31/445 ,  C07D211/58 ,  C07D211/26

CPC分类号： C07D401/04 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06

摘要： Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
ii) when Y = CH 3 , X represents
and when
X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.

摘要翻译： 公开了具有降血压活性的新型哌啶衍生物，以及含有它们的药物制剂。 该新化合物具有式CHEM，其中A为羟基，卤原子，C1-C5烷基，C1-C5烷氧基，C7-C5链烯氧基，C1-C5烷氧基， C1-C5烷硫基，羧基，C1-C5烷氧基羰基，硝基，氨基，C1-C5烷基氨基，C1-C5烷酰基氨基，氨磺酰基，一或二（ C1-C5烷基）氨基磺酰基，C1-C5烷基磺酰基，氨基甲酰基，氰基或三氟甲基; 当m为2以上时，A可以相同或不同，或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下：i）当Y = H时，X表示 ii）当Y = CH 3时，X表示，当Y = CHEM时，X表示氢原子及其药理学上可接受的酸加成盐 。

公开(公告)号：EP0092391A2

公开(公告)日：1983-10-26

申请号：EP83302123.1

申请日：1983-04-14

申请人： KYOWA HAKKO KOGYO CO., LTD

发明人： Teranishi, Masayuki ,  Obase, Hiroyuki ,  Nomoto, Yuji ,  Shuto, Katsuichi ,  Karasawa, Akira ,  Kasuya, Yutaka

IPC分类号： C07D401/06 ,  C07D401/04 ,  A61K31/445

CPC分类号： C07D401/04 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06

摘要： Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
ii) when Y = CH 3 , X represents
and when
X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.

摘要翻译： 公开了具有降血压活性的新型哌啶衍生物，以及含有它们的药物制剂。 该新化合物具有式CHEM，其中A为羟基，卤原子，C1-C5烷基，C1-C5烷氧基，C7-C5链烯氧基，C1-C5烷氧基， C1-C5烷硫基，羧基，C1-C5烷氧基羰基，硝基，氨基，C1-C5烷基氨基，C1-C5烷酰基氨基，氨磺酰基，一或二（ C1-C5烷基）氨基磺酰基，C1-C5烷基磺酰基，氨基甲酰基，氰基或三氟甲基; 当m为2以上时，A可以相同或不同，或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下：i）当Y = H时，X表示 ii）当Y = CH 3时，X表示，当Y = CHEM时，X表示氢原子及其药理学上可接受的酸加成盐 。