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1. 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。

2. 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。

3. 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）

4. 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。

5. 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).

6. 发明授权

US06608084B1 Aza-bicycles which modulate the inhibition of cell adhesion 有权
标题翻译：调节细胞粘附抑制的Aza-自行车
公开(公告)号：US06608084B1
公开(公告)日：2003-08-19
申请号：US09856106
申请日：2001-10-17
申请人： Jean-Dominique Bourzat , Alain Commercon , Bruno Jacques Christophe Filoche , Neil Victor Harris , Clive McCarthy
发明人： Jean-Dominique Bourzat , Alain Commercon , Bruno Jacques Christophe Filoche , Neil Victor Harris , Clive McCarthy
IPC分类号： A61K3147
CPC分类号： C07D401/12 , C07D209/12 , C07D215/08 , C07D215/14 , C07D405/04 , C07D413/06 , C07D413/12
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 C1-3alkylene 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)—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 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 —R12—Z2—R12— linkage; a —C(R4)(R13)—[C(═O)—N(R10)—C(R5)(R11)]p— linkage; or a —L5—L6—L7— linkage; Z1 is C(R7)(R7a), C(═O) or CH(OH); 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).
摘要翻译：本发明涉及式（I）的生理活性化合物，其中R1表示R3-Z3-，R3-L2-R4-Z3-，R3-L3-Ar1-L4-Z3-或R3-L3-Ar1-L2-R4 -Z3-; R2代表氢，卤素，低级烷基或低级烷氧基; A1表示任选被一个或多个选自烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，亚氨基，氧代，硫代或被-ZR 6，-NY 1 Y 2，-CO 2 R 6或-C（ = O）-NY1Y2; L1表示直接键; 各自任选被（a）酸性官能团氰基，氧代，-S（O）m R 9，R 3，-C（= O）-R 3中的一个取代的亚烯基，亚烷基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，亚杂环基或亚芳基，-C（= O）-OR3，-N（R8）-C（= O）R9，-N（R8）-SO2-R9，-NY4Y5或 - [C（= O）-N（R10）-C （R 5）（R 11）] p C（= O）-NY 4 Y 5或（b）被酸性官能团取代的烷基或S（O）m R 9，-C（= O）-NY 4 Y 5或-NY 4 Y 5; a - [C（= O）-N（R 10）-C（R 5）（R 11）] p-键; a -Z2-R12-键; 一个-C（= O）-CH 2

7. 发明授权

US6043375A Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids 失效
标题翻译：可用于制备治疗活性紫杉烷的恶唑烷羧酸的制备方法
公开(公告)号：US6043375A
公开(公告)日：2000-03-28
申请号：US53486
申请日：1998-04-02
申请人： Jean-Dominique Bourzat , Alain Commercon
发明人： Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D263/04 , C07D263/06 , C07D305/14
CPC分类号： C07D263/04 , C07D305/14
摘要： A method of preparing a taxoid of formula III by esterifying protected baccatin III or deacetylbaccatin III using an oxazolidinecarboxylic acid, or an acid halide, or an acid anhydride thereof.
摘要翻译：通过使用恶唑烷羧酸或其酰基酸或其酸酐酯化保护的浆果赤霉素III或脱乙酰基浆果赤霉素III来制备式III的紫杉烷的方法。

8. 发明授权

US5939561A Process for the preparation of .beta.-phenylisoserine and .beta.-lactam and their analogues 失效
标题翻译：制备β-苯基异丝氨酸和β-内酰胺及其类似物的方法
公开(公告)号：US5939561A
公开(公告)日：1999-08-17
申请号：US852611
申请日：1997-05-07
申请人： Jean-Dominique Bourzat , Alain Commercon
发明人： Jean-Dominique Bourzat , Alain Commercon
IPC分类号： C07D205/08 , C07D205/00
CPC分类号： C07D205/08
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-苯基异丝氨酸及其类似物的新方法，其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。

9. 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。

10. 发明授权

US5580997A Baccatin III derivatives 失效
标题翻译：浆果赤霉素Ⅲ衍生物
公开(公告)号：US5580997A
公开(公告)日：1996-12-03
申请号：US479198
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 Baccatin III derivatives are disclosed for use in making taxoid compounds having formula (I) illustrated herein that exhibit antitumor activity.
摘要翻译：公开了新的浆果赤霉素Ⅲ衍生物用于制备具有本文所示的具有抗肿瘤活性的式（I）的紫杉烷类化合物。

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