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1. 发明申请

US20040171618A1 Compounds as PDE IV and TNF-inhibitors 有权
标题翻译：化合物作为PDE IV和TNF-抑制剂
公开(公告)号：US20040171618A1
公开(公告)日：2004-09-02
申请号：US10792579
申请日：2004-03-03
申请人： AVENTIS PHARMA LIMITED
发明人： Garry Fenton , Tahir Nadeem Majid , Malcolm Norman Palfreyman
IPC分类号： A61K031/53 , A61K031/497 , A61K031/501 , C07D49/02
CPC分类号： C07D213/70 , C07C43/247 , C07C217/58 , C07C235/56 , C07C237/30 , C07C255/60 , C07C327/48 , C07C2601/08 , C07C2603/64 , C07C2603/66 , C07D213/65 , C07D213/69 , C07D213/75 , C07D213/79 , C07D213/81 , C07D213/82 , C07D213/89 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention is directed to a nulldi(ether or thioether)heteroaryl or fluoro substituted arylnull compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
摘要翻译：本发明涉及[二（醚或硫醚）杂芳基或氟取代的芳基]化合物或其N-氧化物或其药学上可接受的盐，其可用于抑制TNF在治疗中的产生或生理作用患有与生理上有害的肿瘤坏死因子（TNF）过量相关的疾病状态的患者。本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。

2. 发明申请

US20040122047A1 Substituted tetrahydroisoquinolines 失效
标题翻译：取代的四氢异喹啉
公开(公告)号：US20040122047A1
公开(公告)日：2004-06-24
申请号：US10715662
申请日：2003-11-18
申请人： Aventis Pharma Limited
发明人： Garry Fenton , Neil Victor Harris
IPC分类号： A61K031/4709 , A61K031/47 , C07D217/12
CPC分类号： C07D413/06 , C07D217/06 , C07D217/16 , C07D413/14
摘要： The invention is directed to physiologically active compounds of formula (I): 1 wherein: R1 represents optionally substituted aryl, optionally substituted heteroaryl, R3NHnullAr1nullL2null or R3nullNHnullC(nullO)nullNHnullAr2nullL2null; R3 represents aryl or heteroaryl; Ar1 represents a saturated, partially saturated or fully unsaturated 8- to 10-membered bicyclic ring systerm containing at least one heteroatom selected from O, S or N; Ar2 represents aryldiye or heteroaryldiyl; L1 represents a linkage, such as an alkylene linkage; L2 represents an alkylene chain linkage; R2 represents hydrogen, halogen, C1-4alkyl or C1-4alkoxy; and Y is carboxy or an acid bioisostere; but excluding compounds where an oxygen, nitrogen or sulfur atom is attached directly to a carbon carbon multiple bond of an alkenylene or alkynylene residue; and the corresponding N-oxides and ester prodrugs thereof, and the pharmaceutically acceptable salts and solvates of such compounds, and the N-oxides and ester prodrugs thereof. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (null4null1).
摘要翻译：本发明涉及式（I）的生理活性化合物：其中：R 1表示任选取代的芳基，任选取代的杂芳基，R 3 NH -Ar 1 -L 2 - 或R 3 -NH-C（= O）-NH-Ar 2 -L 2 - ; R 3表示芳基或杂芳基; Ar 1表示含有至少一个选自O，S或N的杂原子的饱和，部分饱和或完全不饱和的8至10元双环系统; Ar 2表示芳基二或杂芳基二; L 1表示连接，例如亚烷基键; L 2表示亚烷基链键; R 2表示氢，卤素，C 1-4烷基或C 1-4烷氧基; Y为羧基或酸式生物电子等排体; 但不包括其中氧，氮或硫原子直接连接到亚烯基或亚炔基残基的碳碳多重键上的化合物; 和其相应的N-氧化物和酯前体药物，以及这些化合物的药学上可接受的盐和溶剂化物，及其N-氧化物和酯前体药物。这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

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