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1. 发明申请

WO2005123731A3 PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS CRTH2 ANTAGONISTS 审中-公开
标题翻译：吡咯并吡啶衍生物及其作为CRTH2拮抗剂的用途
公开(公告)号：WO2005123731A3
公开(公告)日：2006-05-04
申请号：PCT/EP2005006493
申请日：2005-06-16
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BALA KAMLESH , LEBLANC CATHERINE , SANDHAM DAVID ANDREW , TURNER KATHARINE LOUISE , WATSON SIMON JAMES , BROWN LYNDON NIGEL , COX BRIAN
发明人： BALA KAMLESH , LEBLANC CATHERINE , SANDHAM DAVID ANDREW , TURNER KATHARINE LOUISE , WATSON SIMON JAMES , BROWN LYNDON NIGEL , COX BRIAN
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06
摘要： There are provided according to the invention compounds of formula (I), in free or salt form, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.
摘要翻译：根据本发明，提供游离或盐形式的式（I）化合物，其中R 1，R 2，R 3， R 4，R 5，R 6，Q，W，X，m，n和p如说明书中所述，方法准备他们，并用作药物。

2. 发明申请

WO2004096800A3 QUINUCLIDINE DERIVATIVES BINDING TO MUCARINIC M3 RECEPTORS 审中-公开
标题翻译：喹诺酮衍生物与MUCARINIC M3受体结合
公开(公告)号：WO2004096800A3
公开(公告)日：2005-01-06
申请号：PCT/EP2004004605
申请日：2004-04-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , COLLINGWOOD STEPHEN PAUL , COX BRIAN , BAETTIG URS , BHALAY GURDIP , DEVEREUX NICHOLAS JAMES
发明人： COLLINGWOOD STEPHEN PAUL , COX BRIAN , BAETTIG URS , BHALAY GURDIP , DEVEREUX NICHOLAS JAMES
IPC分类号： A61P11/06 , C07D453/02 , C07D519/00 , A61K31/5365
CPC分类号： C07D453/02
摘要： Compounds of formula (I), in salt or zwitterionic form wherein, wherein R , R , R , and R have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：式（I）化合物，其盐或两性离子形式，其中R 1，R 2，R 3和R 4具有说明书中所示的含义，可用于处理是由毒蕈碱M3受体介导的。还描述了含有化合物的药物组合物和制备该化合物的方法。

3. 发明申请

WO2007121920A3 PURINE DERIVATIVES FOR USE AS ADENOSIN A2A RECEPTOR AGONISTS 审中-公开
标题翻译：用作腺苷A2A受体激动剂的嘌呤衍生物
公开(公告)号：WO2007121920A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007003435
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN , COX BRIAN
发明人： FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN , COX BRIAN
IPC分类号： C07D473/16 , A61K31/52 , A61K31/7076 , A61P29/00 , C07D473/18 , C07D473/34 , C07H19/167
CPC分类号： C07D473/16 , C07D473/34
摘要： Purine derivatives of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are as defined herein. The compounds are useful for the treatment of a condition mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions comprising a purine derivative as active ingredient and a process for the preparation of these compounds.
摘要翻译：式（I）的嘌呤衍生物或其立体异构体或其药学上可接受的盐，其中R 1，R 2和R 3如本文所定义。该化合物可用于治疗由腺苷A2A受体的活化介导的病症，特别是炎性或阻塞性气道疾病。包含嘌呤衍生物作为活性成分的药物组合物和这些化合物的制备方法。

4. 发明申请

WO2007134827A8 5-PHENYL-THIAZ0L-2-YL-UREA DERIVATIVES AND USE AS PI3 KINASE INHIBITORS 审中-公开
标题翻译： 5-PHENYL-THIAZ0L-2-YL-UREA衍生物和用作PI3激酶抑制剂
公开(公告)号：WO2007134827A8
公开(公告)日：2009-01-08
申请号：PCT/EP2007004500
申请日：2007-05-21
申请人： NOVARTIS AG , BUDD EMMA , HAYLER JUDY FOX , BRUCE IAN , LEGRAND DARREN MARK , COX BRIAN
发明人： BUDD EMMA , HAYLER JUDY FOX , BRUCE IAN , LEGRAND DARREN MARK , COX BRIAN
IPC分类号： C07D277/48 , A61K31/427 , A61P11/00 , C07D417/12
CPC分类号： C07D277/48 , C07D417/12
摘要： The present invention concerns a compound of formula Ia wherein: Ra * is hydrogen or C1-C4-alkyl; Rb* is -(C1-C4-alkylene)-Y-C1-C4-haloalkyl or -(C1-C4-alkylene)-Y-C1-C4-hydroxyalkyl; Y represents -CONH- or a five membered heteroaryl group. R2* is C1-C4-alkyl or halogen; R3* is halo, -SO2-CH3, -SO2-CF3, carboxy, -CO-NH2, -CO-di(C1-C8-alkyl)amino, or a 5- or 6- membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, that ring being optionally substituted by halo, cyano, oxo, hydroxy, carboxy, nitro, C3-C8-cycloalkyl, C1-C8-alkylcarbonyl, C1-C8-alkoxy optionally substituted by aminocarbonyl, or C1-C8-alkyl optionally substituted by hydroxy, C1- C8-alkoxy, C1- C8-alkylamino or di(C1- C8-alkyl)amino; R4* is hydrogen, halo, -SO2-CH3, nitrile, C1- C8-haloalkyl, imidazolyl, C1- C8-alkyl, -NR8*R9*, or -SO2-NR8*R9*; and R5* is hydrogen, halogen or C1- C8-alkyl; R8* and R9* are independently hydrogen, amino, C1- C8-alkylamino, di(C1- C8-alkyl)amino, or CC1- C8-alkyl optionally substituted by hydroxyl; or a pharmaceutically acceptable salt, or solvate thereof, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译：本发明涉及式Ia化合物，其中：Ra *是氢或C 1 -C 4 - 烷基; Rb *是 - （C1-C4-亚烷基）-Y-C1-C4-卤代烷基或 - （C1-C4-亚烷基）-Y-C1-C4-羟基烷基; Y表示-CONH-或五元杂芳基。 R2 *是C1-C4-烷基或卤素; R3 *是卤素，-SO2-CH3，-SO2-CF3，羧基，-CO-NH2，-CO-二（C1-C8-烷基）氨基或具有一个或多个环的5-或6-元杂环氰基，氧代，羟基，羧基，硝基，C 3 -C 8 - 环烷基，C 1 -C 8 - 烷基羰基，C 1 -C 8 - 烷氧基任选地被选自氧，氮和硫的杂原子被氨基羰基取代，或任选被羟基取代的C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基氨基或二（C 1 -C 8 - 烷基）氨基; R4 *是氢，卤素，-SO2-CH3，腈，C1-8-卤代烷基，咪唑基，C1-8-烷基，-NR8 * R9 *或-SO2-NR8 * R9 *; 和R5 *是氢，卤素或C 1 -C 8 - 烷基; R 8 *和R 9 *独立地为氢，氨基，C 1 -C 8 - 烷基氨基，二（C 1 -C 8 - 烷基）氨基或任选被羟基取代的C 1 -C 8烷基; 或其药学上可接受的盐或溶剂合物，用于治疗通过抑制磷脂酰肌醇3-激酶而变质的疾病的组合物和用途。

5. 发明专利

ES2353142T3 DERIVADOS DE QUINUCLIDINA Y SU USO COMO ANTAGONISTAS DEL RECPTOR DEL M3 MUSCARINICO. 未知
公开(公告)号：ES2353142T3
公开(公告)日：2011-02-25
申请号：ES05798470
申请日：2005-10-31
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： GARAD SUDHAKAR , WATSON SIMON , PRESS NEIL , COLLINGWOOD STEPHEN , BAETTIG URS , COX BRIAN , KIM HYUNGCHUL , PAPOUTSAKIS DIMITRIS
IPC分类号： A61P29/00 , A61K31/439 , C07D453/02
摘要： Un compuesto de formula I **(Ver fórmula)**en forma de sal o zwitteriónica donde R1 y R2son cada uno independientementefenilo,uno o ambos de R1 y R2sustituidos en una, dos o tres posiciones por halo, C1-C8-alquilo o C1-C8alcoxi, y R3 es hidrógeno, hidroxi, C1-C8-alquilo, C1-C8alcoxi o C1-C8-alquiltio; o R1 y R2son cada uno fenilo no sustituido, y R3 es hidrógeno, C1-C8-alquilo, C1-C8-alcoxi o C1-C8alquiltio; o R1 es C3-C8-cicloalquiloo un grupo heterocíclico de 4 a 6 miembrosque contiene al menos un heteroátomo de anillo seleccionado entrenitrógeno, oxígeno y azufre, R2 es fenilo opcionalmente sustituido en una, dos o tres posiciones por halo, C1-C8-alquilo o C1-C8-alcoxi, o R2es un grupo heterocíclico de 4 a 6 miembrosque contiene al menos un heteroátomo de anillo seleccionado entrenitrógeno, oxígeno y azufre, y R3 es hidrógeno, hidroxi, C1C8-alquilo, C1-C8-alcoxi o C1-C8-alquiltio; o -CR1R2R3denota 9H-fluoren-9-ilo, 9, 10,-dihidroantracenil-9-ilo, 9-hidroxi-9,10-dihidroantracenil-9ilo, 9-hidroxi-9H-fluoren-9-ilo, 9H-xanten-9-ilo, 9-hidroxi-9H-xanten-9-ilo, 5Hdibenzo[a,d]ciclohepten-5-ilo o 5-hidroxi-5Hdibenzo[a,d]ciclohepten-5-ilo; y R4 es C1-C8-alquilo sustituido en una, dos o tres posiciones por -CO-N(R5)R6donde R5 es hidrógeno o C1-C8-alquilo y R6es un grupo heterocíclico de 4 a 6 miembrosque contiene al menos un heteroátomo de anillo seleccionado entrenitrógeno, oxígeno y azufre; o R1 y R2son cada uno fenilo no sustituido, R3 es hidroxi, y R4 es C1-C8-alquilo sustituido en una, dos o tres posiciones por -CO-N(R5)R6donde R5 es hidrógeno o C1-C4-alquilo y R6 es 5-metil-3-isoxazolilo; o R1 y R2son cada uno fenilo no sustituido, R3 es hidroxi, y R4 es 1-etilo sustituido en una, dos o tres posiciones por -CO-N(R5)R6donde R5 es hidrógeno o C1C4-alquilo y R6es un grupo heterocíclico de 4 a 6 miembrosque contiene al menos un heteroátomo de anillo seleccionado entrenitrógeno, oxígeno y azufre; con la condición de que el compuesto de fórmula I no sea (R)-3-(2-Hidroxi-2,2-di-tiofen-2-il-acetoxi) -1-(pirazin-2-ilcarbamoil-metil) -1-azonia-biciclo[

6. 发明专利

RS50552B DERIVATI PIROLOPIRIDINA I NJIHOVA UPOTREBA KAO ANTAGONISTA CRTH2 未知
公开(公告)号：RS50552B
公开(公告)日：2010-05-07
申请号：RSP20070507
申请日：2005-06-16
申请人： NOVARTIS PHARMA GMBH , NOVARTIS AG
发明人： BALA KAMLESH , LEBLANC CATHERINE , SANDHAM DAVID ANDREW , TURNER KATHARINE L , WATSON SIMON JAMES , BROWN LYNDON NIGEL , COX BRIAN
IPC分类号： C07D471/04 , A61K31/437
摘要： Jedinjenje formule (I) u slobodnom obliku ili u obliku soli, gdeQ predstavlja vezu ili C1-C10-alkilensku grupu po slobodnom izboru supstituisanu sa halogenom;gde R1 i R2 svaki za sebe nezavisno predstavalju H, halogen, ili C1-C8-alkil, ili gde R1 i R2 zajedno sa atomom ugljenika za koji su vezani, grade dvovalentnu C3-C8-cikloalifatičnu grupu;gde R3 predstavlja H, C1-C8-alkil, C3-C15-karbocikličnu grupu, C1-C8-haloalkil, alkoksi C1-C8 alkil, C1-C8-hidroksialkil; gde R4 i R5 svaki za sebe nezavisno, predstavljaju halogen, C1-C8-alkil, C1-C8-haloalkil, C3-C15-karbocikličnu grupu, nitro, cijano, C1-C8-alkilsulfonil, C1-C8-alkilsulfinil, C1-C8-alkilkarbonil, C1-C8-alkoksikarbonil,C1-C8C1-C8-alkoksi, C1-C8-haloalkoksi, karboksi, karboksi-C1-C8-alkil, amino, C1-C8-alkilamino, di(C1-C8-alkil)amino, SO2NH2, (C1-C8-alkilamino)sulfonil, di(C1-C8-alkil)aminosulfonil, aminokarbonil, C1-C8-alkilaminokarbonil, di(C1-C8-alkil)aminokarbonil ili 4-očlanu do 10-očlanu heterocikličnu grupu sa jednim ili više heteroatoma odabranim iz grupe koju čine kiseonik, azot i sumpor; gde R6 predstavlja H ili C1-C8-alkil; W je C6-C15 aromatična karbociklična grupa ili 4-očlana do 10-očlana heterociklična grupa koja sadrži najmanje jedan prsten sa heteroatomom koji je odabran iz grupe koju čine azot, kiseonik i sumpor; X je -SO2, -CH2-, -CON(C1-C8-alkil)-, -CH(C1-C8-alkil)- ili veza; gde m i n svaki za sebe predstavljaju srednji broj od 0-3, i gde je p 1. Prijava sadrži još 9 patentnih zahteva.

7. 发明专利

DE602004022805D1 未知
公开(公告)号：DE602004022805D1
公开(公告)日：2009-10-08
申请号：DE602004022805
申请日：2004-04-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： COLLINGWOOD STEPHEN PAUL , COX BRIAN , BAETTIG URS , BHALAY GURDIP , DEVEREUX NICHOLAS JAMES
IPC分类号： C07D453/02 , A61K31/5365 , A61P11/06 , C07D519/00
摘要： Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

8. 发明专利

PT1761529E DERIVADOS DE PIRROLOPIRIDINA E SUA UTILIZAÇÃO COMO ANTAGONISTAS DE CRTH2 未知
公开(公告)号：PT1761529E
公开(公告)日：2008-02-11
申请号：PT05751627
申请日：2005-06-16
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： WATSON SIMON JAMES , BALA KAMLESH , LEBLANC CATHERINE , SANDHAM DAVID ANDREW , TURNER KATHARINE L , BROWN LYNDON NIGEL , COX BRIAN
IPC分类号： C07D471/04 , A61K31/437

9. 发明申请

WO9938877A3 2-(PURIN-9-yl)-TETRAHYDROFURAN-3,4-DIOL DERIVATIVES 审中-公开
标题翻译： 2-（嘌呤-9-基） - 四氢呋喃-3,4-二醇衍生物
公开(公告)号：WO9938877A3
公开(公告)日：1999-09-30
申请号：PCT/EP9900503
申请日：1999-01-29
申请人： GLAXO GROUP LTD , CHAN CHUEN , COUSINS RICHARD PETER CHARLES , COX BRIAN
发明人： CHAN CHUEN , COUSINS RICHARD PETER CHARLES , COX BRIAN
IPC分类号： A61K20060101 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P11/00 , A61P11/06 , A61P29/00 , C07D20060101 , C07H17/00 , C07H19/16 , A61K31/70
CPC分类号： C07H19/16 , C07H17/00 , Y10S514/851 , Y10S514/885 , Y10S514/925
摘要： There are provided according to the invention, novel compounds of formula (I) wherein R , R and R are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要翻译：根据本发明提供了新的式（I）化合物，其中R 1，R 2和R 3如说明书中所述，其制备方法，含有它们的制剂及其在治疗中的用途用于治疗炎性疾病。

10. 发明申请

WO2013058889A3 BRAIDING MECHANISM AND METHODS OF USE 审中-公开
标题翻译：制动机制及使用方法
公开(公告)号：WO2013058889A3
公开(公告)日：2014-05-08
申请号：PCT/US2012054517
申请日：2012-09-10
申请人： SEQUENT MEDICAL INC , MARCHAND PHILIPPE , NOLTING JOHN , KENT DARRIN , DINH TAN , TRAN HUNG , MILBURN JAMES , THOMPSON JAMES , COX BRIAN , ROSENBLUTH ROBERT
发明人： MARCHAND PHILIPPE , NOLTING JOHN , KENT DARRIN , DINH TAN , TRAN HUNG , MILBURN JAMES , THOMPSON JAMES , COX BRIAN , ROSENBLUTH ROBERT
IPC分类号： D04C3/40
CPC分类号： D04C3/40 , D04C1/00 , D04C1/02 , D04C1/06 , D04C1/12 , D04C3/42 , D04C3/48 , D10B2509/04
摘要： Devices and methods for forming a tubular braid comprising a plurality of filaments are described. In one embodiment, the braiding machine includes a disc with a mandrel extending from the center in a perpendicular direction and a plurality of catch mechanisms arranged circumferentially around the edge of the disc. A plurality of filaments are temporarily affixed to the mandrel, each filament extending from the mandrel toward the edge of the disc and engaging the edge of the disc at a discrete point of engagement. The plurality of catch mechanisms are attached to actuators adapted to move the catch mechanisms in a generally radial direction relative to the edge of the disc to allow the catch mechanism to engage a subset of the filaments and move the engaged filaments beyond the circumferential edge of the disc.
摘要翻译：描述了用于形成包括多根细丝的管状编织物的装置和方法。在一个实施例中，编织机包括具有在垂直方向上从中心延伸的心轴的盘和围绕盘的边缘周向布置的多个捕获机构。许多细丝临时固定在心轴上，每根细丝从心轴向盘的边缘延伸并且在离散的接合点处与盘的边缘接合。多个捕捉机构附接到致动器，其适于相对于盘的边缘在大致径向方向上移动捕获机构，以允许捕获机构接合细丝的一部分并且将所接合的细丝移动超过所述纤维的圆周边缘光盘。

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