公开(公告)号：EP1406878B1

公开(公告)日：2006-06-07

申请号：EP02751042.9

申请日：2002-06-19

申请人： Merck Patent GmbH

发明人： EGGENWEILER, Hans-Michael ,  WOLF, Michael ,  BEIER, Norbert ,  LEIBROCK, Joachim ,  SCHELLING, Pierre ,  GASSEN, Michael ,  EHRING, Thomas

IPC分类号： C07D253/06 ,  A61K31/53 ,  A61P9/10 ,  A61P37/08 ,  C07D401/12

CPC分类号： C07D253/075 ,  C07D401/12

摘要： The invention relates to triazine derivatives of formula (I), and the physiologically compatible salts and solvates thereof, wherein R1, R2, A and R5 have the designations cited in claim 1. Said derivatives exhibit a phosphodiesterase IV-inhibiting action and can be used for the treatment of allergic diseases, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, auto-immune diseases such as rheumatoid arthritis, multiple sclerosis, Crohn's disease, pancreatic diabetes or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumour growth or tumour metastases, sepsis, memory defects, arteriosclerosis and AIDS. Said derivatives can also be used to inhibit the formation of TNF α.

公开(公告)号：EP1351962B1

公开(公告)日：2005-03-16

申请号：EP01974106.5

申请日：2001-08-03

申请人： MERCK PATENT GmbH

发明人： JONAS, Rochus ,  EGGENWEILER, Hans-Michael ,  SCHELLING, Pierre ,  CHRISTADLER, Maria ,  BEIER, Norbert

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidines of formula (I) and the physiologically tolerable salts thereof, wherein R1, R2 and X have the designation cited in patent claim 1. Said compounds exhibit a phosphodiesterase V inhibition and can be used to treat illnesses of the cardiovascular system. They can also be used for treating, and/or as therapy for, potency problems.

公开(公告)号：EP1357915A2

公开(公告)日：2003-11-05

申请号：EP02702259.9

申请日：2002-01-14

申请人： MERCK PATENT GmbH

发明人： EGGENWEILER, Hans-Michael ,  EIERMANN, Volker ,  SCHELLING, Pierre

IPC分类号： A61K31/505 ,  A61K31/27 ,  A61P25/22

CPC分类号： A61K45/06 ,  A61K31/519 ,  A61K2300/00

摘要： Pharmaceutical preparation comprising at least one phosphodiesterase V inhibitor have, and/or physiologically acceptable salts and/or solvates thereof and at least one endothelin receptor antagonist for the preparation of a medicament for the treatment of angina, high blood pressure, high pulmonary pressure, congestive heart failure (CHF), chronic obstructive pulmonary disease (COPD), cor pulmonale, dextrocardiac insufficiency, atherosclerosis, conditions of reduced patency of the heart vessels, peripheral vascular diseases, strokes, bronchitis, allergic asthma, chronic asthma, allergic rhinitis, glaucoma, irritable bowel syndrome, tumours, renal insufficiency, liver cirrhosis, erectile dysfunction and for the treatment of female sexual disorders.

公开(公告)号：EP0934321A1

公开(公告)日：1999-08-11

申请号：EP97912139.0

申请日：1997-10-08

申请人： MERCK PATENT GmbH

发明人： JONAS, Rochus ,  SCHELLING, Pierre ,  CHRISTADLER, Maria ,  KLUXEN, Franz-Werner

IPC分类号： A61K31 ,  A61P9 ,  A61P15 ,  A61P43 ,  C07D495 ,  C07D239 ,  C07D333

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidine of the formula (I) as well as to their physiologically acceptable salts, wherein R?1, R2, R3, R4¿, X and n have the meaning cited in Claim 1. Said compounds exhibit a phosphodiesterase V inhibition and can be used in the treatment of cardiovascular diseases and for the treatment and/or therapy potency disorders.

公开(公告)号：EP0920431A1

公开(公告)日：1999-06-09

申请号：EP97940047.0

申请日：1997-07-30

申请人： MERCK PATENT GmbH

发明人： ROCHUS, Jonas ,  SCHELLING, Pierre ,  KLUXEN, Franz-Werner ,  CHRISTADLER, Maria

IPC分类号： A61K31 ,  A61P9 ,  A61P15 ,  A61P43 ,  C07D495 ,  C07D239 ,  C07D333

CPC分类号： C07D495/04

摘要： Thienopyrimidines of formula (I) and their physiologically harmless salts, in which R?1, R2, R3, R4¿, X and n have the meaning indicated in claim 1, present a phosphodiesterase V-Inhibition activity and can be used in the treatment of cardio-vascular disorders and in impotence therapy.

公开(公告)号：EP1511737B1

公开(公告)日：2010-02-17

申请号：EP03732395.3

申请日：2003-05-16

申请人： Merck Patent GmbH

发明人： EGGENWEILER, Hans-Michael ,  BEIER, Norbert ,  SCHELLING, Pierre ,  WOLF, Michael

IPC分类号： C07D237/04 ,  C07D401/12 ,  A61K31/50 ,  A61P37/00

CPC分类号： C07D401/12 ,  C07D237/04 ,  C07D403/12

摘要： The invention relates to aryloximes of formula (I), wherein R , R , R , X and B have the meanings as cited in Claim No. 1. These aryloximes act as phosphodiesterase IV inhibitors and can be used for treating osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.

公开(公告)号：EP1432715B1

公开(公告)日：2008-03-19

申请号：EP02800556.9

申请日：2002-09-05

申请人： Merck Patent GmbH

发明人： EGGENWEILER, Hans-Michael ,  BAUMGARTH, Manfred ,  SCHELLING, Pierre ,  BEIER, Norbert ,  CHRISTADLER, Maria

IPC分类号： C07D487/04 ,  C07D495/04 ,  A61K31/505 ,  A61P9/08

CPC分类号： C07D487/04 ,  C07D491/04

摘要： Pyrimidine derivatives of formula (I) and the physiologically acceptable salts thereof, where R?1, R2, R3, R4¿, W, X, Y and Z have the meanings given in claim 1, display a phosphodiesterase V inhibition and can be used for treatment of diseases of the coronary circulatory system and for treatment and/or therapy of potency disorders.

摘要翻译： 式（I）的嘧啶衍生物及其生理上可接受的盐，其中R 1，R 2，R 3，R 4，W，X，Y和Z具有权利要求1中给出的含义，显示磷酸二酯酶V抑制作用， 用于治疗冠状动脉循环系统疾病和用于治疗和/或治疗效力失调。

公开(公告)号：EP1084125B1

公开(公告)日：2005-12-28

申请号：EP99919263.6

申请日：1999-04-23

申请人： Merck Patent GmbH

发明人： JONAS, Rochus ,  SCHELLING, Pierre ,  KLUXEN, Franz-Werner ,  CHRISTADLER, Maria

IPC分类号： C07D495/04 ,  A61K31/505 ,  A61K31/38

CPC分类号： C07D495/04

摘要： The invention relates to thienopyrimidines of the formula (I) and their physiologically compatible salts, where R1, R2 and X have the meanings given in claim 1. These thienopyrimidines have a phosphodiesterase-V inhibiting action and can be used for the treatment of cardiovascular diseases and for the preventive and/or curative treatment of impotence.

公开(公告)号：EP1368035A1

公开(公告)日：2003-12-10

申请号：EP02710008.0

申请日：2002-01-15

申请人： MERCK PATENT GmbH

发明人： SUTTER, Arne ,  EHRING, Thomas ,  WELGE, Thomas ,  MINCK, Klaus ,  WILM, Claudia ,  GASSEN, Michael ,  EGGENWEILER, Hans-Michael ,  WOLF, Michael ,  SCHELLING, Pierre ,  BEIER, Norbert ,  LEIBROCK, Joachim

IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/50 ,  A61P9/00

CPC分类号： A61K31/50 ,  A61K31/5395 ,  A61K31/549

摘要： The invention relates to the use of type 4 phosphodiesterase inhibitors to treat myocardial diseases.

公开(公告)号：EP1353927A2

公开(公告)日：2003-10-22

申请号：EP01271992.8

申请日：2001-12-03

申请人： MERCK PATENT GmbH

发明人： EGGENWEILER, Hans-Michael ,  SCHWARTZ, Harry ,  SCHELLING, Pierre ,  BEIER, Norbert ,  CHRISTADLER, Maria

IPC分类号： C07D495/00

CPC分类号： C07D495/04

摘要： The invention relates to compounds of formula (I) wherein R1, E2 and X have the designation cited in the description. Said compounds have phosphodiesterase V inhibiting properties and can be used for treating diseases of the cardiovascular system and potency disorders.

摘要翻译： 本发明涉及式（I）的化合物，其中R 1，E 2和X具有在说明书中引用的名称。 所述化合物具有磷酸二酯酶V抑制性质，并可用于治疗心血管系统疾病和功效紊乱。