公开(公告)号：US07060823B2

公开(公告)日：2006-06-13

申请号：US10312766

申请日：2001-06-28

Applicant: Rochus Jonas ,  Pierre Schelling ,  Maria Christadler ,  Norbert Beier

Inventor： Rochus Jonas ,  Pierre Schelling ,  Maria Christadler ,  Norbert Beier

IPC: C07D487/04 ,  A61P31/5025

CPC classification number: C07D487/04

Abstract: The present invention relates to 5-aminomethylpyrazolo[4,3-d]pyrimidines of the general formula (I) in which the radicals R1 to R6 have the meaning indicated in the text. The compounds show phosphodiesterase V inhibition and can be employed for the treatment of conditions of the cardiovascular system and for the treatment of potency disorders.

Abstract translation: 本发明涉及通式（I）的5-氨基甲基吡唑并[4,3-d]嘧啶，其中基团R 1至R 6具有所述含义 在文中。 化合物显示磷酸二酯酶V抑制，并且可用于治疗心血管系统的病症和治疗效力障碍。

公开(公告)号：US20050070529A1

公开(公告)日：2005-03-31

申请号：US10467793

申请日：2002-01-15

Applicant: Arne Sutter ,  Thomas Ehring ,  Thomas Welge ,  Klause Minck ,  Claudia Wilm ,  Michael Gassen ,  Hans-Michael Eggenweiler ,  Michael Wolf ,  Pierre Schelling ,  Norbert Beier ,  Joachim Leibrock

Inventor： Arne Sutter ,  Thomas Ehring ,  Thomas Welge ,  Klause Minck ,  Claudia Wilm ,  Michael Gassen ,  Hans-Michael Eggenweiler ,  Michael Wolf ,  Pierre Schelling ,  Norbert Beier ,  Joachim Leibrock

IPC: A61K31/50 ,  A61K31/501 ,  A61K31/535 ,  A61K31/5395 ,  A61K31/54 ,  A61K31/549 ,  A61P9/00 ,  A61P29/00 ,  A61P37/02

CPC classification number: A61K31/50 ,  A61K31/5395 ,  A61K31/549

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

Abstract translation: 本发明涉及使用4型磷酸二酯酶抑制剂来治疗心肌疾病。

公开(公告)号：US06777419B1

公开(公告)日：2004-08-17

申请号：US10070305

申请日：2002-07-29

Applicant: Rochus Jonas ,  Hans-Michael Eggenweiler ,  Pierre Schelling ,  Maria Christadler ,  Norbert Beier

Inventor： Rochus Jonas ,  Hans-Michael Eggenweiler ,  Pierre Schelling ,  Maria Christadler ,  Norbert Beier

IPC: C07D48704

CPC classification number: C07D487/04

Abstract: Pyrazolo[4,3-d]pyrimidines of the formula I and their physiologically acceptable salts, in which R1, R2, R3, R4 and X have the meanings indicated in Claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of disorders of the cardiovascular system and for the treatment and/or therapy of potency disorders.

Abstract translation: 式I的吡唑并[4,3-d]嘧啶及其生理上可接受的盐，其中R 1，R 2，R 3，R 4和X具有权利要求1所示的含义，表示磷酸二酯酶 V抑制，可用于治疗心血管系统疾病和治疗和/或治疗效力障碍。

公开(公告)号：US06495557B1

公开(公告)日：2002-12-17

申请号：US09674269

申请日：2001-03-23

Applicant: Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

Inventor： Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

IPC: A61K31505

CPC classification number: C07D495/04

Abstract: Thienopyrimidines of the formula I and their physiologically acceptable salts, in which R1, R2 and X have the meanings given in claim 1, inhibit phosphodiesterase V and can be employed for the treatment of illnesses of the cardiovascular system and for the treatment and/or therapy of impaired potency.

Abstract translation: 式I的噻吩并嘧啶及其生理上可接受的盐，其中R 1，R 2和X具有权利要求1中给出的含义，抑制磷酸二酯酶V，并且可用于治疗心血管系统的疾病和治疗和/或治疗受损的 效力

公开(公告)号：US06495554B2

公开(公告)日：2002-12-17

申请号：US10146028

申请日：2002-05-16

Applicant: Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

Inventor： Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

IPC: A61K315025

CPC classification number: C07D495/04

Abstract: The thienopyrimidines of the formula (I) and their physiologically compatible salts display a phosphodiesterase V inhibiting activity and can be used for treating diseases of the cardiovascular system and for treatment and/or therapy of erectile dysfunction.

公开(公告)号：US06420368B1

公开(公告)日：2002-07-16

申请号：US09555210

申请日：2000-05-26

Applicant: Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

Inventor： Rochus Jonas ,  Pierre Schelling ,  Franz-Werner Kluxen ,  Maria Christadler

IPC: A61K31519

CPC classification number: C07D495/04

Abstract: The thienopyrimidines of the formula (I) and their physiologically compatible salts display a phosphodiesterase V inhibiting activity and can be used for treating diseases of the cardiovascular system and for treatment and/or therapy of erectile dysfunction.

公开(公告)号：US5684015A

公开(公告)日：1997-11-04

申请号：US528305

申请日：1995-09-14

Applicant: Werner Mederski ,  Matthias Osswald ,  Pierre Schelling ,  Klaus-Otto Minck ,  Dieter Dorsch ,  Norbert Beier ,  Ingeborg Lues

Inventor： Werner Mederski ,  Matthias Osswald ,  Pierre Schelling ,  Klaus-Otto Minck ,  Dieter Dorsch ,  Norbert Beier ,  Ingeborg Lues

IPC: A61K31/4164 ,  A61K31/435 ,  A61K31/437 ,  A61K31/495 ,  A61K31/535 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00 ,  C07D213/00 ,  C07D221/00 ,  C07D231/00 ,  C07D235/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Described herein are novel imidazopyridine derivatives of the formula I ##STR1## wherein R is ##STR2## and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in Patent Claim 1, and their salts, which exhibit antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and increased intraocular pressure, and of disorders of the central nervous system.

Abstract translation: 本文描述的是式I的新咪唑并吡啶衍生物，其中R是R 1，R 1，R 2，R 3和R 4如权利要求1中所定义，并且它们的盐对血管紧张素II表现出拮抗作用，可以是 用于治疗高血压，醛固酮增多症，心功能不全和眼内压升高以及中枢神经系统疾病。

公开(公告)号：US07485639B2

公开(公告)日：2009-02-03

申请号：US10484172

申请日：2002-06-19

Applicant: Hans-Michael Eggenweiler ,  Michael Wolf ,  Norbert Beier ,  Joachim Leibrock ,  Pierre Schelling ,  Michael Gassen ,  Thomas Ehring

Inventor： Hans-Michael Eggenweiler ,  Michael Wolf ,  Norbert Beier ,  Joachim Leibrock ,  Pierre Schelling ,  Michael Gassen ,  Thomas Ehring

IPC: A01N43/64 ,  A61K31/53 ,  C07D253/00

CPC classification number: C07D253/075 ,  C07D401/12

Abstract: Triazine derivatives of the formula (I) and physiologically acceptable salts and solvates thereof, in which R1, R2, A and R5 are as defined in Claim 1, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of allergic diseases, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, autoimmune diseases, such as, for example, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumour growth or tumour metastases, sepsis, memory disorders, atherosclerosis and AIDS, furthermore for inhibiting the formation of TNFα.

Abstract translation: 式（I）的三嗪衍生物及其生理上可接受的盐和溶剂化物，其中R1，R2，A和R5如权利要求1所定义，表现出磷酸二酯酶IV抑制作用，可用于治疗过敏性疾病，哮喘，慢性 支气管炎，特应性皮炎，牛皮癣和其他皮肤疾病，炎性疾病，自身免疫疾病，例如类风湿性关节炎，多发性硬化，克罗恩病，糖尿病或溃疡性结肠炎，骨质疏松症，移植排斥反应，恶病质，肿瘤生长或肿瘤 转移，败血症，记忆障碍，动脉粥样硬化和AIDS，此外用于抑制TNFα的形成。

公开(公告)号：US07141572B2

公开(公告)日：2006-11-28

申请号：US10494631

申请日：2002-10-10

Applicant: Hans-Michael Eggenweiler ,  Michael Wolf ,  Norbert Beier ,  Pierre Schelling ,  Thomas Ehring

Inventor： Hans-Michael Eggenweiler ,  Michael Wolf ,  Norbert Beier ,  Pierre Schelling ,  Thomas Ehring

IPC: C07D403/12 ,  C07D237/04 ,  A61K31/501 ,  A61K31/50 ,  A61P11/06

CPC classification number: C07D403/12 ,  C07D237/04

Abstract: Hydrazono-malonitrile derivatives of the formula (I) in which R1, R2, R3, R3′ and R4 have the meanings given in Claim 1 act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS

Abstract translation: 式（I）的肼 - 丙腈衍生物其中R 1，R 2，R 3，R 3， SUP>和R 4具有权利要求1中给出的含义作为磷酸二酯酶IV抑制剂，并且可用于治疗骨质疏松症，肿瘤，恶病质，动脉粥样硬化，类风湿性关节炎，多发性硬化，糖尿病，炎性 过程，过敏，哮喘，自身免疫性疾病，心肌疾病和艾滋病

公开(公告)号：US20060205708A1

公开(公告)日：2006-09-14

申请号：US11429181

申请日：2006-05-08

Applicant: Hans-Michael Eggenweiler ,  Norbert Beier ,  Pierre Schelling ,  Michael Wolf

Inventor： Hans-Michael Eggenweiler ,  Norbert Beier ,  Pierre Schelling ,  Michael Wolf

IPC: A61K31/501 ,  A61K31/53 ,  C07D403/02

CPC classification number: C07D401/12 ,  C07D237/04 ,  C07D403/12

Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in Claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.

Abstract translation: 式（I）的芳基肟衍生物，其中R 1，R 2，R 3，X和B如权利要求中所定义， 1，作为磷酸二酯酶IV抑制剂，可用于治疗骨质疏松症，肿瘤，恶病质，动脉粥样硬化，类风湿性关节炎，多发性硬化，糖尿病，炎症过程，过敏，哮喘，自身免疫性疾病，心肌疾病和艾滋病。