专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5654449A Taxoids, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5654449A
公开(公告)日：1997-08-05
申请号：US607854
申请日：1996-02-27
申请人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon , Jean-Pierre Pulicani
发明人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon , Jean-Pierre Pulicani
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： This invention relates to a process for preparing taxoid derivatives of formulae II and XI: ##STR1## in which Ar represents an aryl radical; R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, or saturated or unsaturated heterocyclic radical; R.sub.3 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, saturated or unsaturated heterocyclic, or aryl radial, but not a phenyl radical; R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydroxyl-protecting group or R.sub.4 and R.sub.5 together form a heterocyclic group; G.sub.1 represents a hydroxyl-protecting group; and G.sub.2 represents an acetyl radical or hydroxyl-protecting group;by electrolytically reducing a protected taxoid compound in an electrolyte comprising a quaternary ammonium salt which is soluble in an organic solvent or in an aqueous/organic mixture at a controlled potential.
摘要翻译：本发明涉及制备式II和XI的类固醇衍生物的方法：其中Ar表示芳基;其中Ar表示芳基; R 1表示苯甲酰基或基团R 2 -O-CO-，其中R 2表示未取代或取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或饱和或不饱和杂环基; R 3表示未取代或取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，饱和或不饱和杂环，或芳基，但不是苯基; R4表示氢原子，R5表示羟基保护基，或R4和R5一起形成杂环基; G1表示羟基保护基; G 2代表乙酰基或羟基保护基; 通过在包含可溶于有机溶剂的季铵盐或在受控电位的水/有机混合物中的电解质中电解还原受保护的紫杉烷化合物。

2. 发明授权

US5606083A Process for the preparation of taxane derivatives, new derivatives thus obtained and the compositions which contain them 失效
标题翻译：制备紫杉烷衍生物的方法，由此获得的新衍生物和含有它们的组合物
公开(公告)号：US5606083A
公开(公告)日：1997-02-25
申请号：US424512
申请日：1995-05-23
申请人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D305/14 , A61K31/335 , A61K31/337 , A61K31/34 , A61K31/41 , A61K31/415 , A61K31/425 , A61P35/00 , A61P35/02 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D407/12 , C07D409/12
摘要： This invention relates to a method for the preparation of taxane derivatives having the formula (I) and pharmaceutical compositions which contain the derivatives thus obtained. In formula (I), R is hydrogen or acetyl, R.sub.1 is benzoyl or R.sub.2 --O--CO wherein R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The products of formula (I) have remarkable antitumor and antileukemia properties. ##STR1##
摘要翻译： PCT No.PCT / FR93 / 01145 Sec。 371日期：1995年5月23日 102（e）日期1995年5月23日PCT提交1993年11月22日PCT公布。出版物WO94 / 12484 日期1994年6月9日本发明涉及制备具有式（I）的紫杉烷衍生物的方法和含有所得衍生物的药物组合物。在式（I）中，R为氢或乙酰基，R 1为苯甲酰基或R 2 -O-CO，其中R 2为烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基，Het为5元任选取代的芳族杂环（噻吩，噻唑，呋喃，吡咯，咪唑，恶唑，异恶唑，吡唑）。式（I）的产物具有显着的抗肿瘤和抗白血病特性。（一）

3. 发明授权

US5814658A Taxoids, their preparation and pharmaceutical compositions containing them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5814658A
公开(公告)日：1998-09-29
申请号：US477518
申请日：1995-06-07
申请人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D305/14 , A61K31/335
CPC分类号： C07D305/14
摘要： New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. ##STR1## In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.
摘要翻译：通式（I）的新紫杉烷类，其制备方法和含有它们的药物化合物，Ar表示芳基，R表示烷氧基乙酰基，R1表示苯甲酰基或式R2-O-CO-基团，其中 R 2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。通式（I）的新产品具有显着的抗肿瘤活性。

4. 发明授权

US5532388A Taxoids, their preparation and pharmaceutical compositions containing them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5532388A
公开(公告)日：1996-07-02
申请号：US475621
申请日：1995-06-07
申请人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Herve Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： A61K31/335 , A61K31/337 , A61K31/42 , A61P35/00 , C07D305/14 , C07D405/12 , C07D413/12
CPC分类号： C07D305/14 , Y02P20/55
摘要： New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radicalR represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radicalThe new products of general formula (I) have a remarkable antitumour activity. ##STR1##
摘要翻译：通式（I）的新紫杉烷类，其制备方法和含有它们的药物组合物。在通式（I）中，Ar表示芳基R表示氢原子或乙酰基，烷氧基乙酰基或烷基，R1表示苯甲酰基或式R2-O-CO-基团，其中R2表示任选取代的烷基基团，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基通式（I）的新产物具有显着的抗肿瘤活性。（一）

5. 发明授权

US5556877A Taxoids, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5556877A
公开(公告)日：1996-09-17
申请号：US204128
申请日：1994-03-02
申请人： Herv e Bouchard , Jean-Dominique Bourzat , Alain Commer.cedilla.on , Jean-Pierre Pulicani
发明人： Herv e Bouchard , Jean-Dominique Bourzat , Alain Commer.cedilla.on , Jean-Pierre Pulicani
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： This invention relates to taxoids of general formula (I), their preparation and the pharmaceutical compositions which contain them. The products of general formula (I) have notable antitumoral properties. In the general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl or alkoxyacetyl radical,R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, andR.sub.3 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted aryl (with the exception of unsubstituted phenyl) or heterocyclyl radical. ##STR1##
摘要翻译：本发明涉及通式（I）的紫杉烷类，其制备方法和含有它们的药物组合物。通式（I）的产物具有显着的抗肿瘤特性。在通式（I）中，Ar表示芳基，R表示氢原子或乙酰基或烷氧基乙酰基，R 1表示苯甲酰基或基团R 2 -O-CO-，其中R 2表示烷基，烯基，环烷基，环烯基，双环烷基，苯基或杂环基，R 3表示烷基，烯基，环烷基，环烯基，双环烷基，任选取代的芳基（除未取代的苯基）或杂环基。（一）

6. 发明授权

US06194582B1 Taxoids, their preparation and pharmaceutical compositions containing them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US06194582B1
公开(公告)日：2001-02-27
申请号：US09126590
申请日：1998-07-31
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D26304
CPC分类号： C07D305/14
摘要： New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.
摘要翻译：通式（I）的新紫杉烷类，其制备方法和含有它们的药物化合物。在通式（I）中，例如，Ar表示芳基，R表示烷氧基乙酰基，R 1表示苯甲酰基或式 R2-O-CO-，其中R2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。通式（I）的新产品具有显着的抗肿瘤活性。

7. 发明授权

US5763628A Process for the preparation of .beta.-phenylisoserine and its analogues 失效
标题翻译：制备β-苯基异丝氨酸及其类似物的方法
公开(公告)号：US5763628A
公开(公告)日：1998-06-09
申请号：US697420
申请日：1996-08-23
申请人： Jean-Dominique Bourzat , Alain Commercon
发明人： Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07C227/18 , C07C227/22 , C07C229/34 , C07D205/08 , C07D305/14
CPC分类号： C07D305/14 , C07C227/18 , C07C227/22 , C07D205/08 , Y02P20/55
摘要： The present invention relates to new process for the preparation of .beta.-phenylisoserine and its analogues of general formula: ##STR1## which are particularly useful for preparing taxane derivatives which have remarkable antitumour and antileukaemic activities.
摘要翻译：本发明涉及制备β-苯代异丝氨酸及其类似物的新方法，其通式如下：特别适用于制备具有显着抗肿瘤和抗白血病活性的紫杉烷衍生物。

8. 发明授权

US5550261A Taxoids, their preparation and pharmaceutical compositions containing them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US5550261A
公开(公告)日：1996-08-27
申请号：US483693
申请日：1995-06-07
申请人： Herv e Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Herv e Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： A61K31/335 , A61K31/337 , A61K31/42 , A61P35/00 , C07D305/14 , C07D405/12 , C07D413/12
CPC分类号： C07D305/14 , Y02P20/55
摘要： New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical.The new products of general formula (I) have a remarkable antitumor activity. ##STR1##
摘要翻译：通式（I）的新紫杉烷类，其制备方法和含有它们的药物组合物。在通式（I）中，Ar表示芳基，R表示氢原子或乙酰基，烷氧基乙酰基或烷基，R1表示苯甲酰基或式R2-O-CO-基团，其中R2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。通式（I）的新产品具有显着的抗肿瘤活性。（一）

9. 发明授权

US07074821B1 Taxoids, their preparation and pharmaceutical composition containing them 失效
标题翻译：紫杉烷，它们的制备和含有它们的药物组合物
公开(公告)号：US07074821B1
公开(公告)日：2006-07-11
申请号：US08162984
申请日：1993-12-08
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commercon
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D305/00 , A61K31/335
CPC分类号： C07D305/14 , Y02P20/55
摘要： New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I), Ar represents an aryl radical, R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.
摘要翻译：通式（I）的新紫杉烷类，其制备方法和含有它们的药物组合物。在通式（I）中，Ar表示芳基，R表示氢原子或乙酰基，烷氧基乙酰基或烷基，R 1表示苯甲酰基或式R 2的基团其中R 2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。通式（I）的新产品具有显着的抗肿瘤活性。

10. 发明授权

US06632814B1 Dihydro-benzo(1,4)oxazines 失效
公开(公告)号：US06632814B1
公开(公告)日：2003-10-14
申请号：US09644308
申请日：2000-08-23
申请人： Jean-Dominique Bourzat , Alain Commercon , Bruno Jacques Christophe Filoche , Neil Victor Harris , Thomas David Pallin , Keith Alfred James Stuttle
发明人： Jean-Dominique Bourzat , Alain Commercon , Bruno Jacques Christophe Filoche , Neil Victor Harris , Thomas David Pallin , Keith Alfred James Stuttle
IPC分类号： C07D24138
CPC分类号： C07D241/38 , C07D265/36
摘要： The invention is directed to physiologically active compounds of formula (I): wherein R1 represents R3—Z3—, R3—L2—R4—Z3—, R3—L3—Ar1—L4—Z3— or R3—L3—Ar1—L2—R4—Z3—; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; A1 represents a straight chain C2-3alkylene linkage optionally substituted by one or more groups chosen from alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, imino, oxo, thioxo, or alkyl substituted by —ZR6, —NY1Y2, —CO2R6 or —C(═O)—NY1Y2; L1 represents a direct bond; an alkenylene, alkylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage each optionally substituted by (a) an acidic functional group, cyano, oxo, —S(O)mR9, R3, —C(═O)—R3, —C(═O)—OR3, —N(R8)—C(═O)—R9, —N(R8)—C(═O)—OR9, —N(R8)—SO2—R9, —NY4Y5 or —[C(═O)—N(R10)—C(R5)(R11)]p—C(═O)—NY4Y5, or by (b) alkyl substituted by an acidic functional group, or by S(O)mR9, —C(═O)—NY4Y5 or —NY4Y5; a —[C(═O)—N(R10)—C(R5)(R11)]p— linkage; a —Z2—R12— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R 12—Z2—R12— linkage; a —C(R4)(R13)—[C(═O)—N(R10)—C(R5)(R11)]p— linkage; or a —L5—L6—L7— linkage; Z1 is NR17 or O; Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式