公开(公告)号：EP1539768A2

公开(公告)日：2005-06-15

申请号：EP03748015.9

申请日：2003-09-12

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： KOCH, Guido ,  LOISELEUR, Olivier

IPC分类号： C07D493/04 ,  C07D303/14 ,  C07D303/16 ,  C07D275/06 ,  A61P35/00

CPC分类号： C07D275/06 ,  C07D303/16 ,  C07D303/18 ,  C07D493/04 ,  Y02P20/55

摘要： The present invention provides a synthesis for the preparation of epothilone derivatives of formula (9) wherein R1 is methyl, and R2 has the meaning of an unsubstituted or substituted aryl, an unsubstituted or substituted heteroaryl or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus, and salts thereof, and intermediates for the synthesis of a compound of formula (9).

公开(公告)号：EP2069333A1

公开(公告)日：2009-06-17

申请号：EP07818248.2

申请日：2007-09-19

申请人： Novartis AG

发明人： HENG, Richard ,  KOCH, Guido ,  SCHLAPBACH, Achim ,  SEILER, Max, Peter

IPC分类号： C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  C07D401/04 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4439 ,  A61P37/00

CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

摘要： A compound of Formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R1-R6 and A are as defined in the specification.

公开(公告)号：EP1368334A2

公开(公告)日：2003-12-10

申请号：EP02710021.3

申请日：2002-01-21

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： KOCH, Guido ,  LOISELEUR, Olivier ,  SEDELMEIER, Gottfried.

IPC分类号： C07D319/12

CPC分类号： C07D263/26 ,  C07D309/30 ,  C07D319/06 ,  Y02P20/55

摘要： The invention relates to a process for the preparation of a substituted alkene of formula (I) wherein R1, R2 and R3 are independently of each other a protecting group for a hydroxy group or hydrogen and R4 is phenyl which is unsubstituted or mono- or disubstituted by alkoxy, which alkene constitutes an intermediate for the preparation of discodermolide and discodermolide analogues.

公开(公告)号：EP2178874A1

公开(公告)日：2010-04-28

申请号：EP08786115.9

申请日：2008-07-14

申请人： Novartis AG

发明人： SCHLAPBACH, Achim ,  RÉVÉSZ, Lászlo ,  KOCH, Guido

IPC分类号： C07D471/14 ,  C07D471/20 ,  C07D471/22 ,  C07D487/22 ,  C07D491/22 ,  A61K31/4375 ,  A61K31/437 ,  A61P9/00 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D471/14 ,  C07D471/20 ,  C07D471/22 ,  C07D487/22 ,  C07D491/22

摘要： The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.

公开(公告)号：EP1539768B1

公开(公告)日：2007-09-19

申请号：EP03748015.9

申请日：2003-09-12

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： KOCH, Guido ,  LOISELEUR, Olivier

IPC分类号： C07D493/04 ,  C07D303/14 ,  C07D303/16 ,  C07D275/06 ,  A61P35/00

CPC分类号： C07D275/06 ,  C07D303/16 ,  C07D303/18 ,  C07D493/04 ,  Y02P20/55

摘要： The present invention provides a synthesis for the preparation of epothilone derivatives of formula (9) wherein R1 is methyl, and R2 has the meaning of an unsubstituted or substituted aryl, an unsubstituted or substituted heteroaryl or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus, and salts thereof, and intermediates for the synthesis of a compound of formula (9).

公开(公告)号：EP3698796A1

公开(公告)日：2020-08-26

申请号：EP20165564.4

申请日：2017-09-28

申请人： Novartis AG

发明人： CASAREZ, Anthony ,  FUREGATI, Markus ,  KOCH, Guido ,  LIN, Xiaodong ,  OSSOLA, Flavio ,  RECK, Folkert ,  SIMMONS, Robert Lowell ,  ZHU, Qingming

IPC分类号： A61K31/535 ,  A61P31/04

摘要： This invention pertains generally to compounds of Formula (A),

as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.

公开(公告)号：EP2729466B1

公开(公告)日：2015-08-19

申请号：EP12761655.5

申请日：2012-07-07

申请人： Novartis AG

发明人： HENG, Richard ,  HOEGENAUER, Elizabeth, Kate ,  KOCH, Guido ,  PULZ, Robert, Alexander ,  VULPETTI, Anna ,  WAELCHLI, Rudolf

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00

CPC分类号： A61K31/519 ,  C07D487/04

公开(公告)号：EP2729466A1

公开(公告)日：2014-05-14

申请号：EP12761655.5

申请日：2012-07-07

申请人： Novartis AG

发明人： HENG, Richard ,  HOEGENAUER, Elizabeth, Kate ,  KOCH, Guido ,  PULZ, Robert, Alexander ,  VULPETTI, Anna ,  WAELCHLI, Rudolf

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.

摘要翻译： 本发明描述了似乎与布鲁顿酪氨酸激酶（Btk）相互作用的新的吡咯并嘧啶衍生物及其药学上可接受的盐。 因此，新型吡咯并嘧啶可有效治疗自身免疫性疾病，炎性疾病，过敏性疾病，气道疾病如哮喘和慢性阻塞性肺病（COPD），移植排斥，癌症例如癌症。 造血起源或实体瘤。

公开(公告)号：EP1368334B1

公开(公告)日：2007-09-05

申请号：EP02710021.3

申请日：2002-01-21

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： KOCH, Guido ,  LOISELEUR, Olivier ,  SEDELMEIER, Gottfried.

IPC分类号： C07D319/12

CPC分类号： C07D263/26 ,  C07D309/30 ,  C07D319/06 ,  Y02P20/55

摘要： The invention relates to a process for the preparation of a substituted alkene of formula (I) wherein R1, R2 and R3 are independently of each other a protecting group for a hydroxy group or hydrogen and R4 is phenyl which is unsubstituted or mono- or disubstituted by alkoxy, which alkene constitutes an intermediate for the preparation of discodermolide and discodermolide analogues.

公开(公告)号：EP3519419B1

公开(公告)日：2020-05-27

申请号：EP17791737.4

申请日：2017-09-28

申请人： Novartis AG

发明人： CASAREZ, Anthony ,  FUREGATI, Markus ,  KOCH, Guido ,  LIN, Xiaodong ,  OSSOLA, Flavio ,  RECK, Folkert ,  SIMMONS, Robert Lowell ,  ZHU, Qingming

IPC分类号： C07D471/18 ,  A61K31/496 ,  A61K45/06 ,  A61K31/5025 ,  A61K31/551 ,  A61K31/546 ,  A61K31/407 ,  A61P31/04 ,  A61K31/427 ,  A61K31/431 ,  A61K31/4545