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1. 发明申请

WO02057223A3 COMPOUNDS AZEPANE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译：化合物AZEPANE，其制备方法及含有化合物的药物组合物
公开(公告)号：WO02057223A3
公开(公告)日：2002-11-28
申请号：PCT/FR0200147
申请日：2002-01-16
申请人： SERVIER LAB , CASARA PATRICK , LE DIGUARHER THIERRY , DOREY GILBERT , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , GUILBAUD NICOLAS , ORTUNO JEAN-CLAUDE , FAUCHERE JEAN-LUC
发明人： CASARA PATRICK , LE DIGUARHER THIERRY , DOREY GILBERT , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , GUILBAUD NICOLAS , ORTUNO JEAN-CLAUDE , FAUCHERE JEAN-LUC
IPC分类号： A61P35/00 , C07D401/14 , C07D403/12 , C07D413/12 , A61K31/415 , C07D401/12
CPC分类号： C07D401/14 , C07D403/12 , C07D413/12
摘要： A compound having formula (I), wherein X denotes an alkylene group or chain, CO, S(O)n, -S(O)n-A1-, -CO-A1-, -A1-S(O)n-A'1, or A1-CO-A'1-; Y denotes a substituted or non-substituted aryl, heteroaryl, cycloalkyl or heterocyclalkyl group; W denotes a CO or CH2 group; T denotes a N(R1)- or N(R1)CO- group; V denotes a hydrogen atom or a substituted or non-substituted aryl or heteroaryl group; A2 denotes a [C(R2)(R'2)]p group; R1 and R2 are as defined in the description. Medicaments.
摘要翻译：具有式（I）的化合物，其中X表示亚烷基或链，CO，S（O）n，-S（O）n -A1，-CO-A1-，-A1-S（O） A'1或A1-CO-A'1-; Y表示取代或未取代的芳基，杂芳基，环烷基或杂环烷基; W表示CO或CH 2基团; T表示N（R1） - 或N（R1）CO-基团; V表示氢原子或取代或未取代的芳基或杂芳基; A2表示[C（R2）（R'2）] p基团; R1和R2如说明书中所定义。药物。

2. 发明申请

WO8800950A3 PRODUCTION OF COVALENT-LINKED CONJUGATES FROM AN ANTIBIOTIC AND A NON-TOXIC DERIVATIVE OF POLYMYXINE B 审中-公开
标题翻译：生产聚氨基甲酸乙酯的抗生素和非毒性衍生物的共价连接体
公开(公告)号：WO8800950A3
公开(公告)日：1988-03-24
申请号：PCT/CH8700095
申请日：1987-08-03
申请人： FAUCHERE JEAN LUC , MOSBACH KLAUS
发明人： FAUCHERE JEAN-LUC , MOSBACH KLAUS
IPC分类号： C07K7/62 , A61K37/02 , C07D498/08
CPC分类号： C07K7/62
摘要： The invention concerns the known resistance of Gram-negative bacteria to hydrophobic antibiotics. It makes use of the property of the cyclic heptapeptide part of polymyxine B to act in a membrane-permeabilizing manner, without being toxic. It demonstrates, using the example of rifamycin B, that conjugates of hydrophobic antibiotics with the cyclic heptapeptide part of polymyxine B have a bacteriostatic effect and that this effect can be increased if a suitable spacer molecule is inserted between the two associated substances. A description is also given of a synthetic strategy for producing these conjugates in a chemically specific manner.

3. 发明专利

NO20031219A 未知
公开(公告)号：NO20031219A
公开(公告)日：2003-09-19
申请号：NO20031219
申请日：2003-03-17
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/06

4. 发明专利

CA2423259A1 NOUVEAUX COMPOSES DERIVES DE LA QUINAZOLINE, LEUR PROCEDE DEPREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：CA2423259A1
公开(公告)日：2003-09-18
申请号：CA2423259
申请日：2003-03-18
申请人： SERVIER LAB
发明人： DHAINAUT ALAIN , GOLDSTEIN SOLO , FAUCHERE JEAN-LUC , TUCKER GORDON , TIZOT ANDRE , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00 , C07D403/10
摘要： Composés de formule (I): (voir formule I) dans laquelle A, B, D, x, R1, R2, m et n sont tels que définis dans la description, leurs stéréoisomères ainsi que leurs sels d'addition à un acide ou à une base pharmaceutiquement acceptable. Médicaments.

5. 发明专利

NO20031643A 未知
公开(公告)号：NO20031643A
公开(公告)日：2003-04-10
申请号：NO20031643
申请日：2003-04-10
申请人： SERVIER LAB
发明人： FAUCHERE JEAN-LUC , ORTUNO JEAN-CLAUDE , LEVENS NIGEL , CHAMORRO SUSANA , BOUTIN JEAN-ALBERT
IPC分类号： C07D249/14 , A61K31/4196 , A61K31/422 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/55 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/12 , A61P15/10 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , A61D9/12
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12

6. 发明专利

AU1266097A New pseudopeptides derived from neurokinins, process for preparing them and pharmaceutical compositions containing them 未知
公开(公告)号：AU1266097A
公开(公告)日：1997-08-21
申请号：AU1266097
申请日：1997-02-13
申请人： SERVIER LAB
发明人： FAUCHERE JEAN-LUC , KUCHARCZYK-GENTRIC NATHALIE , CANAT EMMANUEL , LONCHAMPT MICHEL
IPC分类号： C07D403/14 , A61K31/41 , A61K38/00 , A61P1/08 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D409/14 , C07K5/02 , C07K5/023 , A61K38/06
摘要： Pseudopeptide neurokinin derivatives of formula (I), their enantiomers, diastereomers, epimers and acid or base addition salts are new. R1 = indolyl, naphthyl, tetrahydronaphthyl, thienyl, Ph (optionally substituted by one or more halo, 1-6C alkyl, 1-6C alkoxy, OH or trihalomethyl) or 3-7C cycloalkyl; n = 1-8; m = 1-4; and R2 = benzyl or Ph (both optionally substituted by one or more halo, 1-6C alkyl, 1-6C alkoxy, OH or trihalomethyl) or 1-6C alkyl.

7. 发明专利

DE60213106D1 未知
公开(公告)号：DE60213106D1
公开(公告)日：2006-08-24
申请号：DE60213106
申请日：2002-09-09
申请人： CENTRE NAT RECH SCIENT , SERVIER LAB
发明人： NEIMARK JEAN , HENLIN JEAN-MICHEL , FAUCHERE JEAN-LUC
IPC分类号： B01J19/00 , C40B40/10 , C40B60/14

8. 发明专利

BR0300698A 未知
公开(公告)号：BR0300698A
公开(公告)日：2004-09-08
申请号：BR0300698
申请日：2003-03-18
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00 , C07D403/10
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

9. 发明专利

ZA200302159B New compounds derived from quinazoline, a process for their preparation and pharmaceutical compositions containing them. 未知
公开(公告)号：ZA200302159B
公开(公告)日：2003-09-23
申请号：ZA200302159
申请日：2003-03-18
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00 , C07D , A61K , A61P
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

10. 发明专利

NO20031219L 未知
公开(公告)号：NO20031219L
公开(公告)日：2003-09-19
申请号：NO20031219
申请日：2003-03-17
申请人： SERVIER LAB
发明人： GOLDSTEIN SOLO , DHAINAUT ALAIN , TIZOT ANDRE , FAUCHERE JEAN-LUC , KUCHARCZYK NATHALIE , HICKMAN JOHN , PIERRE ALAIN , TUCKER GORDON , KRAUS-BERTHIER LAURENCE
IPC分类号： C07D401/06 , A61K31/517 , A61P9/00 , A61P25/00 , A61P35/00 , C07D401/14 , C07D403/06 , C07D407/14 , C07D409/14 , C07D521/00
摘要： Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I).

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