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1. 发明申请

WO2007025709A3 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007025709A3
公开(公告)日：2007-05-10
申请号：PCT/EP2006008426
申请日：2006-08-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FLOR PETER JOSEF , MARZINZIK ANDREAS , NOZULAK JOACHIM , OFNER SILVIO , ROY BERNARD , SPANKA CARSTEN
发明人： FLOR PETER JOSEF , MARZINZIK ANDREAS , NOZULAK JOACHIM , OFNER SILVIO , ROY BERNARD , SPANKA CARSTEN
IPC分类号： C07C237/04 , C07C211/29 , C07C217/58 , C07C237/06 , C07C237/22 , C07D209/16 , C07D209/40 , C07D209/42 , C07D209/86 , C07D211/58 , C07D213/38 , C07D213/85 , C07D215/08 , C07D217/04 , C07D217/06 , C07D223/26 , C07D223/28 , C07D233/22 , C07D263/58 , C07D265/38 , C07D307/68 , C07D307/79 , C07D311/68 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/12 , C07D451/14 , C07D495/04
CPC分类号： C07D209/42 , C07C211/29 , C07C217/58 , C07C237/04 , C07C237/06 , C07C237/22 , C07C2601/02 , C07C2602/10 , C07C2603/20 , C07D209/16 , C07D209/86 , C07D211/58 , C07D213/38 , C07D213/85 , C07D215/08 , C07D217/04 , C07D217/06 , C07D223/26 , C07D223/28 , C07D263/58 , C07D265/38 , C07D307/79 , C07D311/68 , C07D401/06 , C07D401/14 , C07D405/12 , C07D495/04
摘要： The invention relates to novel diamines of the formula (I) in which all variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及新的式（I）二胺，其中所有变量如说明书中所定义，游离碱形式或酸加成盐形式，它们的制备，它们作为药物的用途和包含它们的药物。

2. 发明申请

WO2006010591A3 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2006010591A3
公开(公告)日：2006-10-12
申请号：PCT/EP2005008113
申请日：2005-07-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ALLGEIER HANS , FROESTL WOLFGANG , KOLLER MANUEL , MATTES HENRI , NOZULAK JOACHIM , OFNER SILVIO , ORAIN DAVID , RASETTI VITTORIO , RENAUD JOHANNE , SOLDERMANN NICOLAS , FLOERSHEIM PHILIPP
发明人： ALLGEIER HANS , FROESTL WOLFGANG , KOLLER MANUEL , MATTES HENRI , NOZULAK JOACHIM , OFNER SILVIO , ORAIN DAVID , RASETTI VITTORIO , RENAUD JOHANNE , SOLDERMANN NICOLAS , FLOERSHEIM PHILIPP
IPC分类号： C07D239/96 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28 , C07D401/12 , C07D403/04 , C07D409/12
CPC分类号： C07D409/12 , C07D239/96 , C07D401/12 , C07D403/04
摘要： The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula (I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的1H-喹唑啉-2,4-二酮衍生物，其中取代基如说明书中所定义，它们的制备，它们作为药物的用途以及含有它们的药物组合物。

3. 发明专利

ES2398662T3 Derivados de quinazolina 未知
公开(公告)号：ES2398662T3
公开(公告)日：2013-03-20
申请号：ES05768294
申请日：2005-07-26
申请人： NOVARTIS PHARMA GMBH , NOVARTIS AG
发明人： FLOERSHEIM PHILIPP , ALLGEIER HANS , FROESTL WOLFGANG , KOLLER MANUEL , MATTES HENRI , NOZULAK JOACHIM , OFNER SILVIO , ORAIN DAVID , RASETTI VITTORIO , RENAUD JOHANNE , SOLDERMANN NICOLAS
IPC分类号： C07D239/96 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28 , C07D401/12 , C07D403/04 , C07D409/12
摘要： Compuestos de la fórmula (I) en donde G está en la posición 6 y R1 está en la posición 7 de la benzipirimidin-diona; G es NR3R4; R3 y R4, junto con el átomo de nitrógeno adyacente forman un residuo heteroarilo mono o policíclico aromático de 5a 10 miembros que está unido a través del átomo de nitrógeno al anillo y que contiene uno o más heteroátomos enel anillo; en donde dicho residuo está sustituido o no sustituido por sustituyentes seleccionados de entrehalógeno, nitro, ciano, formilo, carboxamido, hidroxilo, amino, alquilamino de 1 a 4 átomos de carbono, dialquilaminode 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos de carbono, alcoxi de 1 a 4 átomos de carbono, alcoxicarbonilo de 1 a 4 átomos de carbono, alcanosulfonilo de 1 a 4 átomos de carbono, alquilcarbonilo de 1 a 4átomos de carbono, alcoxicarbonilamino de 1 a 4 átomos de carbono, alquilcarbonilamino de 1 a 4 átomos decarbono, arilo, alquilo de 1 a 8 átomos de carbono sustituido por arilo, ariloxi-alquilo de 1 a 8 átomos de carbono,aminocarbonil-alquilo de 1 a 8 átomos de carbono, mono-alquilaminocarbonilo de 1 a 8 átomos de carbono-alquilode 1 a 8 átomos de carbono, di- alquilaminocarbonilo de 1 a 8 átomos de carbono-alquilo de 1 a 8 átomos decarbono y morfolinocarbonil-alquilo de 1 a 8 átomos de carbono, en donde los grupos arilo se seleccionan entre fenilo, naftilo y un heteroarilo mono o policíclico aromático de 5 a 10miembros que contiene uno o más heteroátomos en el anillo, y en donde los mismos grupos arilo están sustituidos ono sustituidos por sustituyentes seleccionados entre halógeno, nitro, ciano, formilo, carboxamido, hidroxilo, amino,alquilamino de 1 a 4 átomos de carbono, di-alquilamino de 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos decarbono, alcoxi de 1 a 4 átomos de carbono, alcoxicarbonilo de 1 a 4 átomos de carbono, alcanosulfonilo de 1 a 4átomos de carbono, alquilcarbonilo de 1 a 4 átomos de carbono, alcoxicarbonilamino de 1 a 4 átomos de carbono yalquilcarbonilamino de 1 a 4 átomos de carbono; o R3 y R4 junto con el átomo de nitrógeno adyacente forman un residuo heterocíclico mono o policíclico saturado oparcialmente insaturado que contiene de tres a diez átomos en el anillo que están unidos a través de este átomo denitrógeno al anillo y en donde uno o más de los átomos del anillo son heteroátomos; en donde dicho residuo estásustituido o no sustituido por sustituyentes seleccionados de entre halógeno, nitro, ciano, formilo, carboxamido,hidroxilo, amino, alquilamino de 1 a 4 átomos de carbono, di-alquilamino de 1 a 4 átomos de carbono, alquilo de 1 a4 átomos de carbono, alcoxi de 1 a 4 átomos de carbono, alcoxicarbonilo de 1 a 4 átomos de carbono,alcanosulfonilo de 1 a 4 átomos de carbono, alquilcarbonilo de 1 a 4 átomos de carbono, alcoxicarbonilamino de 1 a4 átomos de carbono, alquilcarbonilamino de 1 a 4 átomos de carbono, arilo, alquilo de 1 a 8 átomos de carbonosustituido por arilo, ariloxi-alquilo de 1 a 8 átomos de carbono, aminocarbonil-alquilo de 1 a 8 átomos de carbono,mono-alquil-aminocarbonilo de 1 a 8 átomos de carbono-alquilo de 1 a 8 átomos de carbono, di-alquilaminocarbonilode 1 a 8 átomos de carbono-alquilo de 1 a 8 átomos de carbono y morfolinocarbonil-alquilo de 1 a 8átomos de carbono, en donde los grupos arilo se seleccionan entre fenilo, naftilo y un heteroarilo mono o policíclico aromático de 5 a 10miembros que contiene uno o más heteroátomos en el anillo, y en donde los mismos grupos arilo están sustituidos ono sustituidos por sustituyentes seleccionados entre halógeno, nitro, ciano, formilo, carboxamido, hidroxilo, amino,alquilamino de 1 a 4 átomos de carbono, di-alquilamino de 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos decarbono, alcoxi de 1 a 4 átomos de carbono, alcoxicarbonilo de 1 a 4 átomos de carbono, alcanosulfonilo de 1 a 4átomos de carbono, alquilcarbonilo de 1 a 4 átomos de carbono, alcoxicarbonilamino de 1 a 4 átomos de carbono yalquilcarbonilamino de 1 a 4 átomos de carbono; R1 es nitro o trifluorometilo; R2 es alquilo de 1 a 8 átomos de carbono, arilo o alquilo de 1 a 8 átomos de carbono sustituido por arilo,en donde los grupos arilo se seleccionan entre fenilo, naftilo y un heteroarilo mono o policíclico aromático de 5 a 10miembros que contiene uno o más heteroátomos en el anillo, y en donde los mismos grupos arilo están sustituidos ono sustituidos por sustituyentes seleccionados entre halógeno, nitro, ciano, formilo, carboxamido, hidroxilo, amino,alquilamino de 1 a 4 átomos de carbono, di-alquilamino de 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos decarbono, alcoxi de 1 a 4 átomos de carbono, alcoxicarbonilo de 1 a 4 átomos de carbono, alcanosulfonilo de 1 a 4átomos de carbono, alquilcarbonilo de 1 a 4 átomos de carbono, alcoxicarbonilamino de 1 a 4 átomos de carbono yalquilcarbonilamino de 1 a 4 átomos de carbono; y sus sales fisiológicamente aceptables.

4. 发明专利

JP2008303226A Acetylene derivatives having mglur5 antagonistic activity 有权
标题翻译：具有MGLUR5拮抗活性的乙酰衍生物
公开(公告)号：JP2008303226A
公开(公告)日：2008-12-18
申请号：JP2008179005
申请日：2008-07-09
申请人： Novartis Ag , ノバルティスアクチエンゲゼルシャフト
发明人： GASPARINI FABRIZIO , AUBERSON YVES , OFNER SILVIO , ZIMMERMANN KASPAR , HART TERANCE W
IPC分类号： C07D209/08 , C07D215/26 , A61K31/27 , A61K31/32 , A61K31/4035 , A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00 , C07C231/12 , C07C233/18 , C07C269/06 , C07C271/16 , C07D209/36 , C07D209/38 , C07D209/44 , C07D215/06 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12
CPC分类号： C07C271/16 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To provide compounds useful in treatment of disorders associated with irregularities of glutamatergic signal transmission and of nervous system disorders mediated full or in part by mGluR5.
SOLUTION: The invention provides the compounds of formula (I) and method for producing them. The compounds of formula (I) are useful as pharmaceuticals e.g. in treatment of nervous system disorders.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗与谷氨酸能信号传递不规则性有关的疾病和由mGluR5全部或部分介导的神经系统疾病的化合物。解决方案：本发明提供了式（I）的化合物及其制备方法。式（I）化合物可用作药物例如治疗神经系统疾病。版权所有（C）2009，JPO＆INPIT

5. 发明专利

AT325128T 未知
公开(公告)号：AT325128T
公开(公告)日：2006-06-15
申请号：AT97946755
申请日：1997-10-22
申请人： NOVARTIS PHARMA GMBH
发明人： ACKLIN PIERRE , ALLGEIER HANS , AUBERSON YVES , OFNER SILVIO , VEENSTRA SIEM JACOB
IPC分类号： A61K31/675 , A61P9/00 , A61P25/00 , A61P25/08 , A61P43/00 , C07F9/6509
摘要： PCT No. PCT/EP97/05843 Sec. 371 Date Apr. 23, 1999 Sec. 102(e) Date Apr. 23, 1999 PCT Filed Oct. 22, 1997 PCT Pub. No. WO98/17672 PCT Pub. Date Apr. 30, 1998Compounds of the formula I in which R1 is hydroxyl or an aliphatic, araliphatic or aromatic radical, X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical, R2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene and R3, R4 and R5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.

6. 发明专利

AT260902T 未知
公开(公告)号：AT260902T
公开(公告)日：2004-03-15
申请号：AT96929275
申请日：1996-08-19
申请人： NOVARTIS PHARMA GMBH
发明人： ACKLIN PIERRE , ALLGEIER HANS , AUBERSON YVES , BIOLLAZ MICHEL , MORETTI ROBERT , OFNER SILVIO , VEENSTRA SIEM JACOB
IPC分类号： A61K20060101 , A61K31/00 , A61K31/495 , A61K31/498 , A61K31/502 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61K31/662 , A61P25/28 , A61P43/00 , C07D20060101 , C07D241/44 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/12 , C07D491/113 , C07F9/6509
摘要： PCT No. PCT/EP96/03644 Sec. 371 Date Feb. 27, 1998 Sec. 102(e) Date Feb. 27, 1998 PCT Filed Aug. 19, 1996 PCT Pub. No. WO97/08155 PCT Pub. Date Mar. 6, 19972,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

8. 发明专利

CA2466560C ACETYLENE DERIVATIVES HAVING MGLUR5 ANTAGONISTIC ACTIVITY 未知
公开(公告)号：CA2466560C
公开(公告)日：2010-07-27
申请号：CA2466560
申请日：2002-12-03
申请人： NOVARTIS AG
发明人： GASPARINI FABRIZIO , AUBERSON YVES , OFNER SILVIO , ZIMMERMAN KASPAR , HART TERENCE W
IPC分类号： C07D215/26 , C07D405/12 , A61K31/32 , A61K31/4035 , A61K31/404 , A61K31/405 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/5377 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00 , C07C231/12 , C07C233/18 , C07C233/23 , C07C269/06 , C07C271/16 , C07C271/24 , C07D209/08 , C07D209/32 , C07D209/36 , C07D209/38 , C07D209/44 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06
摘要： The invention provides compounds of formula (I) wherein m, n, A, R, R', R", Ro, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g. nervous system disorders.

9. 发明专利

AU2005266490B2 Quinazoline derivatives 未知
公开(公告)号：AU2005266490B2
公开(公告)日：2009-12-24
申请号：AU2005266490
申请日：2005-07-26
申请人： NOVARTIS AG
发明人： NOZULAK JOACHIM , RASETTI VITTORIO , ALLGEIER HANS , RENAUD JOHANNE , MATTES HENRI , FLOERSHEIM PHILIPP , SOLDERMANN NICOLAS , KOLLER MANUEL , OFNER SILVIO , ORAIN DAVID , FROESTL WOLFGANG
IPC分类号： C07D239/96 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28 , C07D401/12 , C07D403/04 , C07D409/12
摘要： The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula(I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.

10. 发明专利

HU226562B1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AS NEUROKININ, ESPECIALLY NEUROKININ-1 ANTAGONISTS, AND MEDICAMENTS CONTAINING THE SAID COMPOUNDS. 未知
公开(公告)号：HU226562B1
公开(公告)日：2009-04-28
申请号：HU9800051
申请日：1996-02-09
申请人： NOVARTIS AG
发明人： AUBERSON YVES , BETSCHART CLAUDIA , GERSPACHER MARC , MAH ROBERT , OFNER SILVIO , ROGGO SILVIO , SCHILLING WALTER , VEENSTRA SIEM JACOB , VON SPRECHER ANDREAS
IPC分类号： C07C237/22 , C07D249/08 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/454 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C231/02 , C07C231/12 , C07C255/29 , C07C311/51 , C07D207/27 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/18 , C07D209/20 , C07D211/16 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D211/62 , C07D213/40 , C07D213/70 , C07D213/81 , C07D215/46 , C07D223/12 , C07D223/16 , C07D231/38 , C07D233/60 , C07D235/16 , C07D235/28 , C07D239/28 , C07D239/42 , C07D241/14 , C07D241/20 , C07D295/13 , C07D295/135 , C07D295/14 , C07D295/18 , C07D295/185 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/10 , C07D521/00
摘要： PCT No. PCT/EP96/00555 Sec. 371 Date Aug. 21, 1997 Sec. 102(e) Date Aug. 21, 1997 PCT Filed Feb. 9, 1996 PCT Pub. No. WO96/26183 PCT Pub. Date Aug. 29, 19961-Aryl-2-acylaminoethane compounds of formula I wherein R1-R4, X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1 antagonists.

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