公开(公告)号：EP1965792A2

公开(公告)日：2008-09-10

申请号：EP06818678.2

申请日：2006-11-20

申请人： Novartis AG

发明人： COLLINGWOOD, Stephen, Paul ,  HAEBERLIN, Barbara

IPC分类号： A61K31/40 ,  A61K31/4704 ,  A61K31/56 ,  A61K31/58 ,  A61P11/00 ,  A61P29/00

CPC分类号： A61K31/4704 ,  A61K31/40 ,  A61K31/56 ,  A61K31/58 ,  A61K2300/00

摘要： A medicament comprising, separately or together (A) a compound of formula (I) in free or salt or solvate form, a glycopyrronium salt; and (Q a compound of formula (II) for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.

公开(公告)号：EP1831208B1

公开(公告)日：2011-08-24

申请号：EP05820639.2

申请日：2005-12-22

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： PRESS, Neil, John ,  COLLINGWOOD, Stephen, Paul

IPC分类号： C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/53 ,  A61K31/42 ,  A61K31/454 ,  A61K31/497 ,  A61P11/08

CPC分类号： C07D413/12 ,  C07D211/14 ,  C07D401/12 ,  C07D413/14

摘要： Compounds of formula (I), in salt or zwitterionic form, wherein J, L, M, R1, R2, R3, R4 and R5 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.

公开(公告)号：EP0906327A2

公开(公告)日：1999-04-07

申请号：EP97924155.0

申请日：1997-06-03

申请人： Novartis AG

发明人： COLLINGWOOD, Stephen, Paul ,  MOSER, Heinz, Ernst ,  ALTMANN, Karl-Heinz ,  DOUGLAS, Mark, Edward

IPC分类号： C07H19 ,  C07H21

CPC分类号： C07H19/04 ,  Y02P20/55

摘要： A compound of formula (I) where B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2' nucleoside-modifying atom or group, R3 is an unsubstituted or substituted C¿1? to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R?4 and R5¿ are each independently an unsubstituted or substituted C¿1? to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R?4¿ is said group and R5 is hydrogen, or R?4 and R5¿ together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-¿O?-, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5'-hydroxyl group therefrom attached through a 5' methylene thereof to the indicated oxygen atom.

公开(公告)号：EP2755967A1

公开(公告)日：2014-07-23

申请号：EP12783308.5

申请日：2012-09-14

申请人： Novartis AG

发明人： BALA, Kamlesh, Jagdis ,  BUTLER, Rebecca ,  COLLINGWOOD, Stephen, Paul ,  HALL, Edward, Charles ,  EDWARDS, Lee ,  LEGRAND, Darren, Mark ,  SPIEGEL, Katrin

IPC分类号： C07D413/04 ,  C07D417/04 ,  A61K31/4439 ,  A61K31/497 ,  A61P11/00

CPC分类号： A61K31/497 ,  A61K31/4439 ,  A61K45/06 ,  C07D413/04 ,  C07D417/04

摘要： The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：EP1954267A1

公开(公告)日：2008-08-13

申请号：EP06818680.8

申请日：2006-11-20

申请人： Novartis AG

发明人： COLLINGWOOD, Stephen, Paul ,  HAEBERLIN, Barbara

IPC分类号： A61K31/40 ,  A61K31/58 ,  A61K9/00 ,  A61P11/06 ,  A61P11/08

CPC分类号： A61K9/0075 ,  A61K9/0078 ,  A61K9/008 ,  A61K31/40 ,  A61K31/58 ,  A61K2300/00

摘要： Medicaments comprising (A) an antimuscarinic agent and (B) a corticosteroid for the treatment of inflammatory or obstructive airways diseases.

摘要翻译： 包含（A）抗毒蕈碱剂和（B）皮质类固醇的药物，用于治疗炎性或阻塞性气道疾病。

公开(公告)号：EP1831208A1

公开(公告)日：2007-09-12

申请号：EP05820639.2

申请日：2005-12-22

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： PRESS, Neil, John ,  COLLINGWOOD, Stephen, Paul

IPC分类号： C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/53 ,  A61K31/42 ,  A61K31/454 ,  A61K31/497 ,  A61P11/08

CPC分类号： C07D413/12 ,  C07D211/14 ,  C07D401/12 ,  C07D413/14

摘要： Compounds of formula (I), in salt or zwitterionic form, wherein J, L, M, R1, R2, R3, R4 and R5 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.

公开(公告)号：EP2755967B1

公开(公告)日：2015-10-21

申请号：EP12783308.5

申请日：2012-09-14

申请人： Novartis AG

发明人： BALA, Kamlesh, Jagdis ,  BUTLER, Rebecca ,  COLLINGWOOD, Stephen, Paul ,  HALL, Edward, Charles ,  EDWARDS, Lee ,  LEGRAND, Darren, Mark ,  SPIEGEL, Katrin

IPC分类号： C07D413/04 ,  C07D417/04 ,  A61K31/4439 ,  A61K31/497 ,  A61P11/00 ,  A61K45/06

CPC分类号： A61K31/497 ,  A61K31/4439 ,  A61K45/06 ,  C07D413/04 ,  C07D417/04

公开(公告)号：EP0778843A1

公开(公告)日：1997-06-18

申请号：EP95928582.0

申请日：1995-08-17

申请人： Novartis AG

发明人： BAXTER, Anthony, David ,  TAYLOR, Roger, John ,  COLLINGWOOD, Stephen, Paul

IPC分类号： A61K31 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D405 ,  C07F9 ,  C07F19 ,  C07H9 ,  C07H13 ,  C07H19 ,  C07H21 ,  C07H23

CPC分类号： C07H9/04 ,  C07H13/04 ,  C07H13/08 ,  C07H19/04 ,  C07H21/00 ,  Y02P20/55

摘要： A compound of formula (I) or salts thereof, where Ro is hydrogen or together with R7O denotes a C¿1?-C15 hydrocarbylidenedioxy group, R?1¿ is hydrogen, R1a or a group of formula (II), R1a is R1b or a protecting group Q, R1b is C1-C20 alkyl, C2-C20 alkenyl, C3-C10 cycloalkyl, C6-C15 aryl, C7-C16 aralkyl or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R2 is R2a or -OR15 or together with R5 denotes an oxy group -O-, provided that R?2 is -OR15 when R1¿ is a group of formula (II), R2a is a C1-C20 aliphatic group, a C3-C10 cycloaliphatic group, a C6-C15 aromatic group, a C7-C16 araliphatic group, or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R3 is R3a or Z, R3a is hydrogen, halogen, hydroxy, R?16, -OR16, OCOR16¿, -OSO¿2R?16, or tri(C¿1?-C15 hydrocarbyl)silyloxy, R?4¿ is hydrogen, halogen or R?17, R5 is R5¿a or Z or together with R2 denotes an oxy group -O-, R5a is hydrogen, halogen, hydroxy, R?18, -OR18, -OCOR18¿, -OSO¿2R?18, or tri(C¿1?-C15 hydrocarbyl)silyloxy, or together with R?6¿ denotes a C¿1?-C15 hydrocarbylidenedioxy group, R?6¿ is halogen, hydroxy, -OR?19, -OCOR19¿, -OSO¿2?R?19 or B1¿, or together with R5 denotes a C¿1?-C15 hydrocarbylidenedioxy group, provided that R?6¿ is not B?1 when R1¿ is a group of formula (II) in which R?14 is B2, R7¿ is hydrogen or R7a, R7a is R?20, -COR20, -SO¿2R20 or tri(C¿1?-C15 hydrocarbyl)silyl, or together with the attached oxygen atom and R?o¿ denotes a C¿1?-C15 hydrocarbylidenedioxy group, R?8¿ is hydrogen, halogen, hydroxy, R?21, -OR21, -OCOR21¿, -OSO¿2R?21 or together with R10 denotes a valence bond, R9 is hydrogen, halogen or R22, R10 is hydrogen, halogen, hydroxy, R?23, -OR23, -OCOR23¿ or -OSO¿2R?23, or together with R8 denotes a valence bond, R11 is hydrogen, halogen or R24, R12 is hydrogen or R12a, or R12O- together with R13 denotes a C¿1?-C15 hydrocarbylidenedioxy group, R?12¿a is R?25, -COR25, -SO¿2R25 or tri(C¿1?-C15 hydrocarbyl)silyl, R?13 is R13¿a or Z, R13a is hydrogen, halogen, hydroxy, R?26, -OR26, -OCOR26¿, -OSO¿2R?26 or tri(C¿1?-C15 hydrocarbyl)silyloxy, or together with R?14¿ denotes a C¿1?-C15 hydrocarbylidenedioxy group, or together with R?12¿O- denotes a C¿1?-C15 hydrocarbylidenedioxy group, R?14¿ is halogen, hydroxy, -OR?27, -OCOR27¿, -OSO¿2?R?27 or B2¿ or together with R13 denotes a C¿1?-C15 hydrocarbylidenedioxy group, provided that R?14¿ is not B?2 when R6 is B1, R15¿ is hydrogen or R15a, R15a is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C16 araliphatic group, R?16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26 and R27¿ are independently a C¿1? to C10 aliphatic group, a C3 to C10 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C30 araliphatic group, B?1 and B2¿ are independently each a monovalent nucleoside base radical, and Z is substituted or unsubstituted C¿6? to C10 aryloxythiocarbonyloxy.

公开(公告)号：EP2037915A2

公开(公告)日：2009-03-25

申请号：EP07726173.3

申请日：2007-06-28

申请人： NOVARTIS AG

发明人： COLLINGWOOD, Stephen, Paul ,  FAIRHURST, Robin, Alec ,  PRESS, Neil, John

IPC分类号： A61K31/428 ,  A61K31/4375 ,  A61K31/45 ,  C07D417/12 ,  C07D471/02 ,  A61P11/00

CPC分类号： C07D471/04 ,  C07D277/68 ,  C07D417/14

摘要： Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X1, L and Q have the meanings as indicated in the specification, are useful for treating obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

公开(公告)号：EP1968969A2

公开(公告)日：2008-09-17

申请号：EP06841060.4

申请日：2006-12-20

申请人： Novartis AG

发明人： COLLINGWOOD, Stephen, Paul ,  SMITH, Nicola

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/70 ,  A61P11/12

CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M1, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.

摘要翻译： 其中M 1，M 1，L 1，L 2，W 1，W 2，X 1，X 2，Y 1，Y 2，A，R 5和R 5a如上所定义的式（I）化合物或其互变异构体，立体异构体或溶剂合物或药学上可接受的盐为 本文定义为用于治疗由阻断上皮钠通道介导的病症，特别是炎性或过敏性病症。