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    Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them
    64.
    发明授权
    Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them 有权
    取代的4-氨基-2-芳基环戊基[d]嘧啶，其制备方法及其用途和包含它们的药物制剂

    公开(公告)号：US07138398B2

    公开(公告)日：2006-11-21

    申请号：US10660489

    申请日：2003-09-12

    Applicant: Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

    IPC: C07D239/70 ,  A61K31/517 ,  C07D401/12

    CPC classification number: C07D401/12 ,  C07D239/70

    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).

    Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3具有权利要求中给出的含义。 所述化合物是药物中有价值的活性剂，用于治疗和预防疾病，例如高血压，心绞痛，心力衰竭，血栓形成和动脉粥样硬化等心血管疾病。 式（I）化合物能够调节人体自身产生的环鸟苷酸（cGMP），并且通常适用于与受损的cGMP平衡相关的疾病的治疗和预防。 本发明还涉及制备式（I）化合物的方法，用于治疗和预防上述疾病以及用于制备这些疾病的药物，以及含有式（I）化合物的药物制剂。

    Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical preparations comprising them
    66.
    发明授权
    Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical preparations comprising them 有权
    取代的4-氨基-2-芳基 - 四氢喹唑啉，其制备方法及其用途和包含它们的药物制剂

    公开(公告)号：US07045526B2

    公开(公告)日：2006-05-16

    申请号：US10674350

    申请日：2003-10-01

    Applicant: Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    IPC: A61K31/55 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/517 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC classification number: C07D239/94

    Abstract: The present invention relates to compounds of formula I: wherein R1, R2, and R3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases such as cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses, or atherosclerosis. Compounds of formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for the preparation of compounds of formula I, methods of therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, and pharmaceutical compositions which comprise at least one compound of formula I.

    Abstract translation: 本发明涉及式I化合物：其中R 1，R 2和R 3具有说明书中所示的含义，其中 是用于治疗和预防心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化等疾病的有价值的药物活性化合物。 式I的化合物具有调节环鸟苷酸（cGMP）的内源性产生的能力，并且通常适用于治疗和预防与扰动的cGMP平衡相关的疾病状态。 本发明还涉及制备式I化合物的方法，治疗和预防指定疾病状态及其制备方法，以及包含至少一种式I化合物的药物组合物。

    Substituted 4-amino-2-aryl-tetrahydoquinazolines, their preparation, their use and pharmaceutical preparations comprising them
    68.
    发明授权
    Substituted 4-amino-2-aryl-tetrahydoquinazolines, their preparation, their use and pharmaceutical preparations comprising them 有权
    取代的4-氨基-2-芳基 - 四氢喹唑啉，其制备方法及其用途和包含它们的药物制剂

    公开(公告)号：US06660746B1

    公开(公告)日：2003-12-09

    申请号：US09497723

    申请日：2000-02-04

    Applicant: Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    Inventor： Ursula Schindler ,  Karl Schönafinger ,  Hartmut Strobel

    IPC: A61K31517

    CPC classification number: C07D239/94

    Abstract: The present invention relates to compounds of formula I: wherein R1, R2, and R3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases such as cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses, or atherosclerosis. Compounds of formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for the preparation of compounds formula I, methods of therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, and pharmaceutical compositions which comprise at least one compound of formula I.

    Abstract translation: 本发明涉及式I化合物：其中R 1，R 2和R 3具有说明书中所述的含义，其是用于治疗和预防诸如心血管疾病的有价值的药物活性化合物 疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物具有调节环鸟苷酸（cGMP）的内源性产生的能力，并且通常适用于治疗和预防与扰动的cGMP平衡相关的疾病状态。 本发明还涉及制备式I化合物的方法，治疗和预防指定疾病状态及其制备方法，以及包含至少一种式I化合物的药物组合物。

    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    69.
    发明授权
    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US06617359B2

    公开(公告)日：2003-09-09

    申请号：US10073330

    申请日：2002-02-13

    Applicant: Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    Inventor： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC: A61K3165

    CPC classification number: C07C233/65 ,  A61K31/166 ,  C07C2602/08

    Abstract: The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    Abstract translation: 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化 ，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防 并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

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