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1. 发明申请

WO2004043956A8 PYRIDOPYRIMIDINONE COMPOUNDS, METHOD FOR PRODUCTION THEREOF AND MEDICAMENTS COMPRISING THE SAME 审中-公开
标题翻译：吡咯烷酮化合物，其生产方法和包含其的药物
公开(公告)号：WO2004043956A8
公开(公告)日：2005-06-09
申请号：PCT/FR0303274
申请日：2003-11-04
申请人： SERVIER LAB , RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/02 , A61P35/00 , C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： Compounds of formula (I), where: R1, R2, R3, R4 are as defined in the description, the enantiomers, diastereomers, tautomers and addition salts thereof with a pharmaceutically-acceptable acid or base. Said compounds have kinase modulating properties and are useful in the treatment of cancer, diabetes, obesity etc.
摘要翻译：式（I）化合物，其中：R 1，R 2，R 3，R 4如说明书中所定义，其对映异构体，非对映异构体，互变异构体及其药学上可接受的酸或碱的加成盐。所述化合物具有激酶调节性质，可用于治疗癌症，糖尿病，肥胖等。

2. 发明专利

MY140164A PYRIDOPYRIMIDINONE COMPOUNDS, METHOD FOR PRODUCTION THEREOF AND MEDICAMENTS COMPRISING THE SAME 未知
公开(公告)号：MY140164A
公开(公告)日：2009-11-30
申请号：MYPI20033854
申请日：2003-10-09
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： C07D471/04 , A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/02 , A61P35/00
摘要： COMPOUNDS OF FORMULA (I):@WHEREIN: @> R( ), R( ), R( ), R( ) ARE DEFINED IN THE DESCRIPTION, THEIR ENANTIOMERS, DIASTEREOISOMERS, TAUTOMERS AND ALSO ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID OR BASE.

3. 发明专利

EA009043B1 НОВЫЕ СОЕДИНЕНИЯ ПИРИДОПИРИМИДИНОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ИХ СОДЕРЖАТ 未知
公开(公告)号：EA009043B1
公开(公告)日：2007-10-26
申请号：EA200500690
申请日：2003-11-04
申请人： SERVIER LAB
发明人： RAULT SYLVIAN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： C07D471/04 , A61K31/505 , A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/02 , A61P35/00
摘要： Соединенияформулы (I)вкоторой R, R, R, Rимеютзначения, указанныев описании, ихэнантиомеры, диастереоизомеры, таутомеры, атакжеихсолиприсоединенияс фармацевтическиприемлемойкислотойилиоснованием. Лекарственныесредства.

4. 发明专利

SI1558612T1 DERIVATI IMIDAZOPIRIDINA, POSTOPEK ZA NJIHOVO PRIPRAVO IN FARMACEVTSKI SESTAVKI, KI JIH VSEBUJEJO 未知
公开(公告)号：SI1558612T1
公开(公告)日：2006-10-31
申请号：SI200330428
申请日：2003-11-04
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE , BIZOT-ESPIARD JEAN-GUY
IPC分类号： C07D471/00 , A61K31/00

5. 发明专利

DE60307875D1 未知
公开(公告)号：DE60307875D1
公开(公告)日：2006-10-05
申请号：DE60307875
申请日：2003-11-04
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE , BIZOT-ESPIARD JEAN-GUY
IPC分类号： C07D471/04 , A61K31/44 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07D221/00 , C07D235/00
摘要： Imidazopyridine derivatives (I) are new. Imidazopyridine derivatives of formula (I), their enantiomers, diastereoisomers, and their salts with acids and bases are new. R1 = H, halogen, alkyl, polyhaloalkyl, CN, NO2, hydroxycarbonyl, alkoxycarbonyl, aminocarbonyl, or dialkylaminocarbonyl; R2 = H, alkyl, aryl (optionally substituted), heteroaryl (optionally substituted) or a group of formula R20-C(X)-; R20 = alkyl, alkoxy, amino, alkylamino, dialkylamino, aryl (optionally substituted), or heteroaryl (optionally substituted); X = O, S, or NR21; R21, R3 = H or alkyl; n = 1-6; and N = pyrido ring with the N atom in the 1, 2, 3, or 4 positions. Alkyl and alkoxy groups have 1-6 C atoms, aryl is phenyl or naphthyl, polyhaloalkyl groups having 1-3 C atoms and 1-7 halogen atoms, heteroaryl groups may be mono or bicyclic of 5 - 11 ring atoms, at least one ring being aromatic, and having 2 or 3 heteroatoms (O, N, S) and may be substituted by 1-3 alkyl groups. Optional substituents on aryl groups may be 1 or 2 substituents selected from halogens, alkyl, alkoxy, polyhaloalkyl, hydroxy, CN, NO2, amino, alkylamino, dialkylamino, carboxyl, amido, and -COO-alkyl groups, and heteroaryl groups having a non-aromatic ring may be further substituted on this non-aromatic ring by oxo.

6. 发明专利

HK1081965A1 Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same 未知
公开(公告)号：HK1081965A1
公开(公告)日：2006-05-26
申请号：HK06102331
申请日：2006-02-22
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101 , A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/02 , A61P35/00 , C07D471/04
摘要： Pyridopyrimidone derivatives (I), their enantiomers, diastereoisomers, tautomers, and their salts with acids and bases are new. Pyridopyrimidone derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and their salts with acids and bases are new. R1, R2 = H or alkyl; R3 = halogen, alkoxy, aryl (optionally substituted by 1-3 R33), or NR'1R'2; R'1, R'2 = H, alkyl, or R'1-N-R'2 is a heterocycle; R4 = H or NR''1R''2; R''1, R''2 = H or alkyl; R1+R2, R'1+R'2, R''1+R''2 = mono or bicyclic of 5 - 11 C heterocycle optionally containing a further 1 or 2 heteroatoms (O, N, S), optionally substituted by 1-3 alkyl groups; R33 = halogens, alkyl, alkoxy, polyhaloalkyl (containing 1 - 3 C atoms and 1 - 7 halogen atoms) and hydroxy; provided that: (1) alkyl and alkoxy groups have 1 - 8 C atoms, aryl is phenyl or naphthyl; and An Independent claim is also included for the preparation of (I).

7. 发明专利

NO20052710L 未知
公开(公告)号：NO20052710L
公开(公告)日：2005-06-06
申请号：NO20052710
申请日：2005-06-06
申请人： SERVIER LAB
发明人： BIZOT-ESPIARD JEAN-GUY , RAULT SYLVAIN , LANCELOT JEAN-CHARLES , RENARD PIERRE , CAIGNARD DANIEL-HENRI , KOPP MARINA , PFEIFFER BUNO
IPC分类号： A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07D471/04 , A61K31/44
摘要： Imidazopyridine derivatives (I) are new. Imidazopyridine derivatives of formula (I), their enantiomers, diastereoisomers, and their salts with acids and bases are new. R1 = H, halogen, alkyl, polyhaloalkyl, CN, NO2, hydroxycarbonyl, alkoxycarbonyl, aminocarbonyl, or dialkylaminocarbonyl; R2 = H, alkyl, aryl (optionally substituted), heteroaryl (optionally substituted) or a group of formula R20-C(X)-; R20 = alkyl, alkoxy, amino, alkylamino, dialkylamino, aryl (optionally substituted), or heteroaryl (optionally substituted); X = O, S, or NR21; R21, R3 = H or alkyl; n = 1-6; and N = pyrido ring with the N atom in the 1, 2, 3, or 4 positions. Alkyl and alkoxy groups have 1-6 C atoms, aryl is phenyl or naphthyl, polyhaloalkyl groups having 1-3 C atoms and 1-7 halogen atoms, heteroaryl groups may be mono or bicyclic of 5 - 11 ring atoms, at least one ring being aromatic, and having 2 or 3 heteroatoms (O, N, S) and may be substituted by 1-3 alkyl groups. Optional substituents on aryl groups may be 1 or 2 substituents selected from halogens, alkyl, alkoxy, polyhaloalkyl, hydroxy, CN, NO2, amino, alkylamino, dialkylamino, carboxyl, amido, and -COO-alkyl groups, and heteroaryl groups having a non-aromatic ring may be further substituted on this non-aromatic ring by oxo.

8. 发明专利

MA27410A1 NOUVEAUX COMPOSES PYRIDOPYRIMIDINONE LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：MA27410A1
公开(公告)日：2005-06-01
申请号：MA28232
申请日：2005-04-19
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE
IPC分类号： A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P19/02 , A61P35/00 , C07D471/04 , A61K31/505

9. 发明专利

AR041882A1 COMPUESTOS DE IMIDAZOPIRIDINA, UN PROCEDIMIENTO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：AR041882A1
公开(公告)日：2005-06-01
申请号：ARP030104024
申请日：2003-11-04
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , LANCELOT JEAN-CHARLES , KOPP MARINA , CAIGNARD DANIEL-HENRI , PFEIFFER BRUNO , RENARD PIERRE , BIZOT-ESPIARD JEAN-GUY
IPC分类号： A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , C07D471/04 , A61K31/437 , A61P3/00 , A61P9/00 , C07D235/00 , C07D213/00
摘要： Reivindicación 1: Compuestos fórmula (1), en la cual: R1 representa un átomo de hidrógeno, un átomo de halógeno o un grupo alquilo, polihaloalquilo, ciano, nitro, hidroxicarbonilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, o dialquilaminocarbonilo; R2 representa un átomo de hidrógeno, un grupo alquilo, un grupo arilo opcionalmente sustituido, un grupo heteroarilo opcionalmente sustituido o un grupo R20 -C(X)- en el cual: R20 representa un grupo alquilo, un grupo alcoxi, un grupo amino, un grupo alquilamino, un grupo dialquilamino, un grupo arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido; X representa un átomo de oxígeno, un átomo de azufre, o un grupo NR21 donde R21 representa un átomo de hidrógeno o un grupo alquilo; R3 representa un átomo de hidrógeno, o un grupo alquilo; n representa un entero comprendido entre 1 y 6 inclusive; la representación del resto de un grupo de fórmula (2), donde, sus enantiómeros, diastereoisómeros, y también las sales de adición de los mismos con un ácido o con una base farmacéuticamente aceptable, y se entiende que: el término "alquilo" designa una cadena hidrocarbonada, lineal o ramificada C1-6; el término "alcoxi" designa un grupo alquilo-oxi en el cual la cadena alquilo, que es lineal o ramificada C1-6; el término "arilo" designa un grupo fenilo o bifenilo; el término "polihaloalquilo" designa una cadena carbonada, lineal o ramificada C1-3 y de 1 a 7 átomos de halógeno; el término "heteroarilo" designa un grupo de 5 a 11 miembros en el anillo que monocíclico o bicíclico, en el cual al menos uno de los anillos es aromático, y que contiene en el sistema de anillo monocíclico o en el sistema de anillo bicíclico 1, 2 ó 3 heteroátomos, seleccionados entre nitrógeno, oxígeno y azufre; y el término "opcionalmente sustituido" asociado a las expresiones arilo y heteroarilo significa que los grupos en cuestión están sustituidos por uno o dos sustituyentes, idénticos o diferentes, seleccionados entre átomos de halógeno y los grupos alquilo, alcoxi, polihaloalquilo, hidroxi, ciano, nitro, amino (opcionalmente sustituido por uno o dos grupos alquilo) y -C(O)Rd en la cual Rd representa un grupo seleccionado entre hidroxi, alcoxi y amino, y se entiende que el grupo heteroarilo puede ser además sustituido por un grupo oxo en la parte no aromático del heteroarilo. Reivindicación 15: Composición farmacéutica de acuerdo con la reivindicación 13 caracterizada porque comprende al menos un ingrediente activo de acuerdo con alguna de las reivindicaciones 1 a 11, para emplear en la fabricación de medicamentos para tratar la diabetes de tipo II no insulinodependiente, la obesidad, la diabetes de tipo I, la hiperlipidemia, la hipercolesterolemia y sus complicaciones cardiovasculares.

10. 发明专利

NZ529084A New imidazoline compounds, a process for their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：NZ529084A
公开(公告)日：2005-04-29
申请号：NZ52908403
申请日：2003-10-22
申请人： SERVIER LAB
发明人： RAULT SYLVAIN , KOPP MARINA , LANCELOT JEAN-CHARLES , LEMAITRE STEPHANE , CAIGNARD DANIEL-HENRI , BIZOT-ESPIARD JEAN-GUY , RENARD PIERRE
IPC分类号： A61K31/381 , A61K31/402 , A61K31/417 , A61K31/4178 , A61K31/44 , A61K31/4439 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , C07D401/06 , C07D403/06 , C07D409/06
摘要： Compounds of formula (I), wherein: R1 represents an optionally substituted heteroaryl group R2 represents an optionally substituted cycloalkyl group R3 represents a hydrogen atom or an alkyl group, and R4 and R5, which may be identical or different, each represents a hydrogen atom, a halogen atom or an alkyl, polyhaloalkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R10-C(X)-Y-R11-, R10-Y-R11- or R10-S(O)n-R11 group, in which: R10 represents a hydrogen atom or an alkyl group, R11 represents a bond, or an alkylene, alkenylene or alkynylene group, X represents an oxygen atom, a sulphur atom, or an NR12 group in which R12 represents a hydrogen atom or an alkyl group, Y represents an oxygen atom, a sulphur atom, or an amino or alkylamino group, and n represents an integer of form 1 to 2 inclusive, pharmaceutical compositions comprising compounds of formula (I) and a process for their preparation are disclosed. The compounds disclosed are useful in the treatment of non-insulin-dependent type II diabetes, obesity, type I diabetes, hyperlipidaemia, hypercholesterolaemia and cardiovascular complications thereof.

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