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1. 发明申请

WO2006072589A3 DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的消除性尿路炎
公开(公告)号：WO2006072589A3
公开(公告)日：2006-10-12
申请号：PCT/EP2006000098
申请日：2006-01-09
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FURET PASCAL , MARTINY-BARON GEORG , MCCARTHY CLIVE , RASETTI VITTORIO , VAUPEL ANDREA
发明人： FURET PASCAL , MARTINY-BARON GEORG , MCCARTHY CLIVE , RASETTI VITTORIO , VAUPEL ANDREA
IPC分类号： C07D403/12 , A61K31/496 , A61P35/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及式（I）化合物，其作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗温血动物，特别是人的所述化合物，其用于治疗疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂，包括将所述化合物施用于温血动物，特别是人的治疗方法，以及所述化合物的制备方法。

2. 发明申请

WO2005000815A3 PIPERIDINIUM AND PYRROLIDINIUM DERIVATIVES AS LIGANDS FOR THE MUSCARINIC M3 RECEPTOR 审中-公开
标题翻译：作为MUSCARINIC M3受体配体的哌啶和吡咯烷酮衍生物
公开(公告)号：WO2005000815A3
公开(公告)日：2005-04-14
申请号：PCT/EP2004006795
申请日：2004-06-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , COLLINGWOOD STEPHEN PAUL , BAETTIG URS , MCCARTHY CLIVE
发明人： COLLINGWOOD STEPHEN PAUL , BAETTIG URS , MCCARTHY CLIVE
IPC分类号： A61P11/00 , C07D207/08 , C07D211/22 , C07D211/46 , C07D409/14 , A61K31/40 , A61K31/4025 , A61K31/452
CPC分类号： C07D207/08 , C07D211/22 , C07D211/46 , C07D409/14
摘要： Compounds of formula (I) in salt or zwitterionic form wherein, wherein R , R , R , R , R , J, L and M 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）的盐或两性离子形式的化合物，其中R 1，R 2，R 3，R 4，R 5，J，L和M具有如该说明书可用于治疗由毒蕈碱M3受体介导的病症。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

WO2006015860A3 PYRAZOLE DERIVATIVES FOR TREATING CONDITIONS MEDIATED BY ACTIVATION OF THE ADENOSINE A2B OR A3 RECEPTOR 审中-公开
标题翻译：通过激活腺苷A2B或A3受体介导的治疗条件的吡唑衍生物
公开(公告)号：WO2006015860A3
公开(公告)日：2006-06-15
申请号：PCT/EP2005008696
申请日：2005-08-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BLOOMFIELD GRAHAM CHARLES , LEBLANC CATHERINE , MCCARTHY CLIVE , PRESS NEIL JOHN
发明人： BLOOMFIELD GRAHAM CHARLES , LEBLANC CATHERINE , MCCARTHY CLIVE , PRESS NEIL JOHN
IPC分类号： A61K31/415 , A61P29/00 , A61P37/00 , C07D231/12 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/04
CPC分类号： C07D231/12 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04
摘要： Compounds of formula (I) in free or salt form, wherein R 1 , R 2 , R 3 and R 4 have the meanings as indicated in the specification, are useful for treating a condition mediated by activation of the adenosine Alb receptor or the adenosine A3 receptor, particularly an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：游离或盐形式的式（I）化合物，其中R 1，R 2，R 3和R 4， SUP>具有说明书中指出的含义，可用于治疗由腺苷Alb受体或腺苷A3受体的激活介导的病症，特别是炎性或阻塞性气道疾病。还描述了含有化合物的药物组合物和用于制备化合物的方法。

4. 发明申请

WO2005075420A3 PYRROLIDINE DERIVATIVES ACTING AS CCR3-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CCR3受体拮抗剂的吡咯烷衍生物
公开(公告)号：WO2005075420A3
公开(公告)日：2005-10-06
申请号：PCT/EP2005000874
申请日：2005-01-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BHALAY GURDIP , DUNSTAN ANDREW , GLEN ANGELA , HOWE TREVOR JOHN , MCCARTHY CLIVE
发明人： BHALAY GURDIP , DUNSTAN ANDREW , GLEN ANGELA , HOWE TREVOR JOHN , MCCARTHY CLIVE
IPC分类号： A61K31/4015 , C07D207/12 , C07D211/26 , A61P11/06
CPC分类号： C07D207/12 , C07D211/26
摘要： Compounds of formula (I) in free or salt form, wherein T, X, Y, U, R , R , m, n and p have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：游离或盐形式的式（I）化合物，其中T，X，Y，U，R 1，R 2，m，n和p具有说明书中所示的含义，可用于治疗由CCR3介导的病症。还描述了含有化合物的药物组合物和用于制备化合物的方法。

5. 发明申请

WO2005021519A3 5-PHENYL-4-METHYL-THIAZOL-2-YL-AMINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3 KINASE ENZYMES (PI3) FOR THE TREATMENT OF INFLAMMATORY AIRWAY DISEASES 审中-公开
标题翻译： 5-苯基-4-甲基 - 噻唑-2-基胺衍生物作为磷酸胆碱酯酶3激酶（PI3）的抑制剂用于治疗炎症性气道疾病
公开(公告)号：WO2005021519A3
公开(公告)日：2005-05-12
申请号：PCT/EP2004009586
申请日：2004-08-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BLOOMFIELD GRAHAM CHARLES , BRUCE IAN , HAYLER JUDY FOX , LEBLANC CATHERINE , LE GRAND DARREN MARK , MCCARTHY CLIVE
发明人： BLOOMFIELD GRAHAM CHARLES , BRUCE IAN , HAYLER JUDY FOX , LEBLANC CATHERINE , LE GRAND DARREN MARK , MCCARTHY CLIVE
IPC分类号： C07D277/48 , C07D417/12 , C07D451/04 , C07D471/04 , A61K31/427 , A61P11/06 , C07C275/26
CPC分类号： C07D451/04 , C07D277/48 , C07D417/12 , C07D471/04
摘要： Compounds of Formula (I) in free or salt form, wherein R , R , R , R , R and R have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase such as inflammatory airway diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的式（I）化合物，其中R a，R b，R 2，R 3，R 4和R 5具有如说明书中所示的含义可用于治疗由磷脂酰肌醇3-激酶介导的病症，例如炎性气道疾病。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。

6. 发明专利

ES2351602T3 DERIVADOS DE PIRROLIDINIO COMO LIGANDOS PARA EL RECEPTOR M3 MUSCARINICO. 未知
公开(公告)号：ES2351602T3
公开(公告)日：2011-02-08
申请号：ES04740214
申请日：2004-06-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： COLLINGWOOD STEPHEN PAUL , MCCARTHY CLIVE , BAETTIG URS
IPC分类号： C07D211/46 , A61K31/40 , A61K31/4025 , A61K31/452 , A61P11/00 , C07D207/08 , C07D211/22 , C07D409/14
摘要： Un compuesto de la fórmula I **(Ver fórmula)** en forma de sal o de ión bipolar en donde R1 y R3 son cada uno independientemente un grupo carbocíclico C3-C15 o un grupo heterocíclico de 5 a 12 miembros que tiene por lo menos un heteroátomo en el anillo seleccionado de nitrógeno, oxígeno y azufre; R2 es hidrógeno, hidroxi, o alquilo C1-C4 opcionalmente sustituido por hidroxi; J es alquileno C1-C2; R4 es alquilo C1-C4; R5 es alquilo C1 sustituido por -SO-R6, -S(=O)2-R6, -CO-R6, -CO-O-R6, -CO-NH-R6 o -R7, o R5 es alquilo C2-C10 sustituido por -O-R6, -S-R6, -SO-R6, -S(=O)2-R6, -CO-R6, -O-CO-R6, -CO-O-R6, -NH-CO-R6, -CO-NH-R6, -R7 o -R8, o R5 es alquenilo C2-C10 o alquinilo C2-C10 opcionalmente sustituido por -R7 o -R8; R6 es un grupo carbocíclico C3-C15 o un grupo heterocíclico de 5 a 12 miembros que tiene por lo menos un heteroátomo en el anillo seleccionado de nitrógeno, oxígeno y azufre, o R6 es alquilo C1-C10 opcionalmente sustituido por alcoxi C1-C10, -O-R7, un grupo carbocíclico C3-C15 o un grupo heterocíclico de 5 a 12 miembros que tiene por lo menos un heteroátomo en el anillo seleccionado de nitrógeno, oxígeno y azufre; R7 es un grupo heterocíclico de 5 a 12 miembros que tiene por lo menos un heteroátomo en el anillo seleccionado de nitrógeno, oxígeno y azufre; y R8 es un grupo carbocíclico C3-C15.

7. 发明专利

ES2362907T3 FENILACETAMINAS ADECUADAS COMO INHIBIDORES DE QUINASA PROTEINICA. 未知
公开(公告)号：ES2362907T3
公开(公告)日：2011-07-14
申请号：ES06724286
申请日：2006-04-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BOLD GUIDO , FURET PASCAL , GUAGNANO VITO , MCCARTHY CLIVE , VAUPEL ANDREA
IPC分类号： A61K31/4184 , C07D471/04 , A61K31/4188 , A61P35/00 , A61P35/02 , C07D235/04 , C07D235/06 , C07D401/12 , C07D403/12 , C07D473/00
摘要： Un compuesto de la formula I, donde cada uno de R1 y R2, independientemente uno de otro, se selecciona del grupo consistente de hidrogeno, halo y C1-C7- alquilo; R3 esta ausente si Z es nitrogeno o, si Z es C (carbono), es hidrogeno, arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido; X es N (nitrogeno) o CH (carbono sustituido con hidrogeno), Y es CH o N, Z es C o N, y Q es una unidad estructural de la formula (A) donde R4 es hidrogeno, halo, hidrogeno no sustituido o sustituido, arilo no sustituido o sustituido, heterociclilo no sustituido o sustituido enlazado a traves de un atomo de anillo diferente a nitrogeno, cicloalquilo no sustituido o sustituido, alquilo no sustituido o sustituido, alquenilo no sustituido o sustituido o alquinilo no sustituido o sustituido; R5 es hidrogeno, alquilo no sustituido o sustituido, hidrogeno no sustituido o sustituido, arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido; y R6 es hidrogeno, cicloalquilo no sustituido o sustituido o alquilo no sustituido o (preferiblemente) sustituido; o una unidad estructural de la formula (B) donde R7 es arilo no sustituido o sustituido o heterociclilo no sustituido o sustituido y R8 es alquilo o cicloalquilo; donde el asterisco * en las formulas (A) y (B) marca el enlace a traves del cual la unidad estructural esta enlazada al NH del grupo amida en la formula I; y (a) cada uno de R9 y R10, independientemente del otro, se selecciona del grupo consistente de hidrogeno, hidroxilo y C1-C7-alquilo; o (b) R9 y R10 representan juntos oxo; o R1 y R9 forman juntos un grupo -C(O)-CH2- o -CH2-CH2-, R2 se selecciona del grupo consistente de hidrogeno, halo y C1-C7-alquilo, y R10 representa hidrogeno; o una sal farmaceuticamente aceptable de los mismos.

8. 发明申请

WO0164659A3 INDANE DERIVATIVES AND THEIR USE AS CELL ADHESION INHIBITORS 审中-公开
标题翻译： INDANE衍生物及其作为细胞粘附抑制剂的用途
公开(公告)号：WO0164659A3
公开(公告)日：2001-12-27
申请号：PCT/GB0100844
申请日：2001-02-28
申请人： AVENTIS PHARMA LTD , FENTON GARRY , MCCARTHY CLIVE , MACKENZIE ROBERT EDWARD , MORLEY ANDREW DAVID
发明人： FENTON GARRY , MCCARTHY CLIVE , MACKENZIE ROBERT EDWARD , MORLEY ANDREW DAVID
IPC分类号： A61K31/423 , A61P11/06 , A61P29/00 , C07D235/30 , C07D263/58 , A61K31/4184
CPC分类号： C07D263/58 , C07D235/30
摘要： The invention is directed to physiologically active compounds of general formula (I) wherein: R represents aryl, heteroaryl or a group R -L -Ar -L -; R represents hydrogen or lower alkyl; R represents aryl or heteroaryl; and Ar represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or 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( alpha 4 beta 1).
摘要翻译：本发明涉及通式（I）的生理活性化合物，其中：R 1表示芳基，杂芳基或基团R 3 -L 2 -Ar 1 -L 3 - ; R 2表示氢或低级烷基; R 3表示芳基或杂芳基; 并且Ar 1表示含有至少一个选自O，S或N的杂原子的任选取代的饱和，部分饱和或完全不饱和的8至10元双环体系; Y是羧基或酸性生物电子等排体; 及其相应的N-氧化物或前体药物，以及这些化合物及其相应的N-氧化物或前药的药学上可接受的盐和溶剂合物。这些化合物具有有价值的药物特性，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

9. 发明专利

GB2488981A Adjustable laundry basket 未知
公开(公告)号：GB2488981A
公开(公告)日：2012-09-19
申请号：GB201103832
申请日：2011-03-07
申请人： CARRICK DEAN , MCCARTHY CLIVE
发明人： CARRICK DEAN , MCCARTHY CLIVE
IPC分类号： D06F95/00
摘要： The laundry basket 1 includes a telescopic leg 2 and a latch 7 to retain the leg in a retracted or extended position. The leg has multiple members 2A, 2B, 2C, 2D which are nested when the leg is retracted. The leg also has a biasing mass (14, Figure 5) which is sufficient to overcome the resistance between the nested members so that when the latch is opened, the telescopic leg can be extended. The basket may have a frame 3 supporting a collapsible bag 4. The telescopic leg may be pivotally mounted to the frame.

10. 发明专利

JP2009298799A 5-phenylthiazole derivative, and use as pi3 kinase inhibitor 审中-公开
标题翻译： 5-苯并噻唑衍生物，用作PI3激酶抑制剂
公开(公告)号：JP2009298799A
公开(公告)日：2009-12-24
申请号：JP2009187248
申请日：2009-08-12
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： BRUCE IAN , FINAN PETER , LEBLANC CATHERINE , MCCARTHY CLIVE , WHITEHEAD LEWIS , PRESS NICOLA , BLOOMFIELD GRAHAM CHARLES , HAYLER JUDY , KIRMAN LOUISE , OZA MRINALINI SACHIN , SHUKLA LENA
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P1/12 , A61P1/16 , A61P3/04 , A61P3/10 , A61P7/06 , A61P7/08 , A61P9/00 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/04 , A61P11/06 , A61P11/08 , A61P11/16 , A61P13/12 , A61P17/02 , A61P17/04 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P31/22 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/12
CPC分类号： C07D277/40 , C07D277/46 , C07D277/48 , C07D417/04 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a compound useful in the treatment of diseases mediated by phosphatidylinositol 3-kinase, useful in the treatment of inflammatory or obstructive airways diseases, and resulting, for example, in reduction of tissue damage, airways inflammation, bronchial hyperactivity, remodeling or disease progression. SOLUTION: A 5-phenylthiazole derivative in a free or a salt form is represented by formula I, and a pharmaceutically acceptable salt thereof. Furthermore, a method for producing the compound is provided. COPYRIGHT: (C)2010,JPO&INPIT

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