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49 条记录 (耗时 0.027 秒)

    4-Phenylpiperidine derivatives as renin inhibitors
    23.
    发明申请
    4-Phenylpiperidine derivatives as renin inhibitors 审中-公开
    4-苯基哌啶衍生物作为肾素抑制剂

    公开(公告)号：US20070078164A1

    公开(公告)日：2007-04-05

    申请号：US10580296

    申请日：2004-11-25

    申请人： Richard Sedrani ,  Juergen-Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    发明人： Richard Sedrani ,  Juergen-Klaus Maibaum ,  Werner Breitenstein ,  Holger Sellner ,  Claus Ehrhardt ,  Nils Ostermann

    IPC分类号： A61K31/454 ,  C07D401/02

    CPC分类号： C07D401/10 ,  C07D211/42 ,  C07D405/04 ,  C07D409/10

    摘要： Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

    摘要翻译： 具有下式的本发明化合物对天然酶肾素表现出抑制活性。 因此，式（I）化合物可用于治疗高血压，动脉粥样硬化，不稳定冠状动脉综合征，充血性心力衰竭，心脏肥大，心脏纤维化，心肌梗塞后梗死，冠状动脉综合征不稳定，舒张功能障碍，慢性肾脏疾病，肝纤维化， 糖尿病引起的并发症如肾病，血管病变和神经病变，冠状血管疾病，血管成形术后再狭窄，眼内压升高，青光眼，异常血管生长，醛固酮增多症，认知障碍，阿尔茨海默病，痴呆，焦虑状态和认知障碍。

    Novel pyrimidineamide derivatives and the use thereof
    26.
    发明申请
    Novel pyrimidineamide derivatives and the use thereof 失效
    新型嘧啶酰胺衍生物及其用途

    公开(公告)号：US20060142577A1

    公开(公告)日：2006-06-29

    申请号：US10528913

    申请日：2003-09-26

    申请人： Paul Manley ,  Werner Breitenstein ,  Sandra Jacob ,  Pascal Furet

    发明人： Paul Manley ,  Werner Breitenstein ,  Sandra Jacob ,  Pascal Furet

    IPC分类号： A61K31/506 ,  C07D403/14

    CPC分类号： C07D401/04

    摘要： The invention relates to novel substituted N-(3-benzoylaminophenyl)-4-pyridyl-2-pyrimidinamine derivatives, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, and a method for the treatment of such a disease.

    摘要翻译： 本发明涉及新的取代的N-（3-苯甲酰氨基苯基）-4-吡啶基-2-嘧啶胺衍生物，其制备方法，含有它们的药物组合物，其用途任选与一种或多种其它药物活性化合物组合用于 治疗对抑制蛋白激酶活性，特别是肿瘤性疾病作出反应的疾病，以及治疗这种疾病的方法。

    .alpha.-Hydroxy thioethers
    27.
    发明授权
    .alpha.-Hydroxy thioethers 失效
    α-羟基硫醚

    公开(公告)号：US4808572A

    公开(公告)日：1989-02-28

    申请号：US936671

    申请日：1986-12-01

    申请人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/23 ,  A61K38/00 ,  A61K45/00 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07C321/18 ,  C07C323/00 ,  C07C323/52 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07C149/243

    CPC分类号： C07K5/0606 ,  A61K31/19 ,  A61K31/215 ,  C07C323/00 ,  A61K38/00

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.1-7 -alkoxy or an optionally substituted amino group, and--X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新型不对称硫醚，其中通式具有以下含义：a为1至7的整数，R 4表示氢或C 1-7 - 烷酰基，R 1表示C 1-3 - 烷基， 可以在末端碳原子上被游离或酰化的羟基，原子数至多为17的卤素原子或甲氧基取代，或表示C1-3-全氟烷基，R2表示任选不饱和的脂肪族基，其具有 5至15个碳原子，A代表乙烯，或者，如果R1代表卤代基，和/或B代表亚苯基或亚乙基，则单键或亚乙烯基，B代表单键，亚乙炔基或亚苯基，R3代表羟基，C1-7 - 烷氧基或任选取代的氨基，-X-表示单键，任选N-酰化的伯氨基亚甲基的亚甲基，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除平滑肌的收缩b 由白细胞三烯生成，因此适用于治疗过敏性疾病，特别是哮喘病症。

    Aromatic thioethers
    28.
    发明授权
    Aromatic thioethers 失效
    芳香硫醚

    公开(公告)号：US4785004A

    公开(公告)日：1988-11-15

    申请号：US941676

    申请日：1986-12-15

    申请人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： C07D215/54 ,  C07D311/24 ,  C07C149/40 ,  A61K31/235

    CPC分类号： C07D311/24 ,  C07D215/54

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有 原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基 ，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则 单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于 治疗过敏，特别是哮喘，病情。