公开(公告)号：EP0907731A1

公开(公告)日：1999-04-14

申请号：EP97908260.0

申请日：1997-03-19

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： KAUPMANN, Klemens ,  BETTLER, Bernhard ,  BITTIGER, Helmut ,  FRÖSTL, Wolfgang ,  MICKEL, Stuart, John

IPC分类号： A01K67 ,  C07F9 ,  C07K14 ,  C07K16 ,  C12N1 ,  C12N5 ,  C12N15 ,  C12P21 ,  C12Q1 ,  G01N33 ,  A61K38

CPC分类号： C07K14/70571 ,  A01K2217/05 ,  A61K38/00 ,  C07F9/301

摘要： The present invention provides purified GABAB receptors and receptor proteins derived from rat and human sources, as well as nucleic acids which encode such proteins. The proteins and nucleic acids of the invention share significant homology with the GABAB receptor and the DNA encoding it as specifically disclosed herein. The invention moreover provides methods for isolating other members of the GABAB receptor family using DNA cloning technology and probes derived from the sequences provided herein, as well as novel members of the GABAB receptor family isolated by such methods. Furthermore, the invention relates to the use of GABAB receptors and receptor proteins and cells transformed with a gene encoding a GABAB receptor protein in a method for identifying and characterising compounds which modulate the activity of the GABAB receptor, such as GABAB receptor agonists and antagonists, which may be useful as pharmacological agents for the treatment of disorders associated with the central and peripheral nervous systems.

公开(公告)号：EP0853626A1

公开(公告)日：1998-07-22

申请号：EP96928599.0

申请日：1996-08-30

申请人： Novartis AG

发明人： FRÖSTL, Wolfgang ,  MICKEL, Stuart, John ,  COOKE, Nigel, Graham ,  BENNETT, Stuart, Norman, Lile ,  WILLIAMS, Anne, Rachel, Burton

IPC分类号： A61K31 ,  A61P25 ,  A61P29 ,  A61P43 ,  C07C213 ,  C07C215 ,  C07C229 ,  C07C255 ,  C07C271 ,  C07F9

CPC分类号： C07F9/65583 ,  C07C215/28 ,  C07C229/36 ,  C07C229/38 ,  C07C255/41 ,  C07C255/42 ,  C07C271/16 ,  C07C271/22 ,  C07F9/301 ,  C07F9/302 ,  C07F9/3211 ,  C07F9/3217 ,  C07F9/48 ,  C07F9/5728 ,  C07F9/6533 ,  Y02P20/55

摘要： A compound which is a substituted phosphinic acid of formula (I), or a salt or ester thereof, where R1 is a monovalent aromatic or araliphatic group connected through a carbon atom thereof to the indicated carbon atom, R2 is an unsubstituted or substituted hydrocarbyl group, Rx is hydrogen or an unsubstituted or substituted hydrocarbyl group, Ry is hydrogen, Rya or a NH-protecting group and Rya is an unsubstituted or substituted hydrocarbyl group.

公开(公告)号：EP0907731B1

公开(公告)日：2005-03-02

申请号：EP97908260.9

申请日：1997-03-19

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： KAUPMANN, Klemens ,  BETTLER, Bernhard ,  BITTIGER, Helmut ,  FRÖSTL, Wolfgang ,  MICKEL, Stuart, John

IPC分类号： C12N15/12 ,  C07K14/705 ,  C07K16/28 ,  G01N33/68 ,  C07F9/30 ,  C12N15/11 ,  A01K67/027

CPC分类号： C07K14/70571 ,  A01K2217/05 ,  A61K38/00 ,  C07F9/301

摘要： The present invention provides purified GABAB receptors and receptor proteins derived from rat and human sources, as well as nucleic acids which encode such proteins. The proteins and nucleic acids of the invention share significant homology with the GABAB receptor and the DNA encoding it as specifically disclosed herein. The invention moreover provides methods for isolating other members of the GABAB receptor family using DNA cloning technology and probes derived from the sequences provided herein, as well as novel members of the GABAB receptor family isolated by such methods. Furthermore, the invention relates to the use of GABAB receptors and receptor proteins and cells transformed with a gene encoding a GABAB receptor protein in a method for identifying and characterising compounds which modulate the activity of the GABAB receptor, such as GABAB receptor agonists and antagonists, which may be useful as pharmacological agents for the treatment of disorders associated with the central and peripheral nervous systems.

公开(公告)号：EP1896411A2

公开(公告)日：2008-03-12

申请号：EP06754143.3

申请日：2006-06-06

申请人： Novartis AG

发明人： MICKEL, Stuart, John ,  SEDELMEIER, Gottfried ,  HIRT, Hans ,  SCHÄFER, Frank ,  FOULKES, Michael ,  PRIKOSZOVICH, Walter

IPC分类号： C07D207/08 ,  C07D207/16 ,  C07D407/04

CPC分类号： C07D405/04 ,  C07C237/22 ,  C07D207/08 ,  C07D307/32 ,  C07D307/33 ,  Y02P20/55

摘要： The invention related to a novel process, novel process Steps and novel intermediates useful in the synthesis of pharmaceutically active Compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a Compound of the formula (III), wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof, said manufacture comprising (preferably consisting in) reacting a Compound of the formula (I) with a reagent able to transform hydroxy into X where X is for example a leaving group.

公开(公告)号：EP1789377A1

公开(公告)日：2007-05-30

申请号：EP05775930.0

申请日：2005-08-30

申请人： Novartis AG ,  NOVARTIS-PHARMA GMBH

发明人： SEDELMEIER, Gottfried ,  MICKEL, Stuart, John ,  RUEEGER, Heinrich

IPC分类号： C07C53/128 ,  C07D413/04 ,  C07D207/38 ,  C07C271/10 ,  C07D307/32 ,  C07D211/76

CPC分类号： C07D207/26 ,  C07C271/16 ,  C07C271/22 ,  C07D211/76 ,  C07D307/33

摘要： The present invention relates to synthetic routes to prepare a compound of the formula (A); wherein R1 is halogen, C1-6halogenalkyl, C1-6 alkoxy-C1-6 alcoxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, Cl-6alkoxy-C 1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, Cl-6dialkylamino-C1-6alkyl, C1-6alkanoylamino­ C1-6alkyl, HO(O)C-Cl-6alkyl, C1-6alkyl-O-(O)C-C1-6alkyl, H2N-C(O)-Cl-6alkyl, C1-6alkyl-HN­C(O)-C1-6alkyl or (C1-6alkyl)2N-C(O)-C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

公开(公告)号：EP1931629B1

公开(公告)日：2010-12-22

申请号：EP06805861.9

申请日：2006-09-26

申请人： Novartis AG

发明人： MICKEL, Stuart, John ,  MARTERER, Wolfgang

IPC分类号： C07D207/16 ,  C07C251/24 ,  C07C237/22

CPC分类号： C07C251/24 ,  C07C231/12 ,  C07D207/08 ,  C07D207/16 ,  C07C237/22

摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula (III), wherein R, R1, and R' are as defined in the specification, or a salt thereof, and a compound of formula (IV) wherein R, R1, R2 and R' are as defined in the specification, and processes of manufacturing these.

公开(公告)号：EP1789377B1

公开(公告)日：2010-10-20

申请号：EP05775930.0

申请日：2005-08-30

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： SEDELMEIER, Gottfried ,  MICKEL, Stuart, John ,  RUEEGER, Heinrich

IPC分类号： C07C53/128 ,  C07D413/04 ,  C07D207/38 ,  C07C271/10 ,  C07D307/32 ,  C07D211/76

CPC分类号： C07D207/26 ,  C07C271/16 ,  C07C271/22 ,  C07D211/76 ,  C07D307/33

摘要： The present invention relates to synthetic routes to prepare a compound of the formula (A); wherein R1 is halogen, C1-6halogenalkyl, C1-6 alkoxy-C1-6 alcoxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, Cl-6alkoxy-C 1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, Cl-6dialkylamino-C1-6alkyl, C1-6alkanoylamino­ C1-6alkyl, HO(O)C-Cl-6alkyl, C1-6alkyl-O-(O)C-C1-6alkyl, H2N-C(O)-Cl-6alkyl, C1-6alkyl-HN­C(O)-C1-6alkyl or (C1-6alkyl)2N-C(O)-C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

公开(公告)号：EP1931629A1

公开(公告)日：2008-06-18

申请号：EP06805861.9

申请日：2006-09-26

申请人： Novartis AG

发明人： MICKEL, Stuart, John ,  MARTERER, Wolfgang

IPC分类号： C07D207/16 ,  C07C251/24 ,  C07C237/22

CPC分类号： C07C251/24 ,  C07C231/12 ,  C07D207/08 ,  C07D207/16 ,  C07C237/22

摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula (III), wherein R, R1, and R' are as defined in the specification, or a salt thereof, and a compound of formula (IV) wherein R, R1, R2 and R' are as defined in the specification, and processes of manufacturing these.