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    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    52.
    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：US07202278B2

    公开(公告)日：2007-04-10

    申请号：US10920395

    申请日：2004-08-18

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

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

    IPC分类号： A61K31/165 ,  A61K31/495 ,  A61K31/44 ,  A61K31/195

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： A 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. 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.

    摘要翻译： 一种刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括给予生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺，

    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    53.
    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：US06812253B2

    公开(公告)日：2004-11-02

    申请号：US10623775

    申请日：2003-07-22

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

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

    IPC分类号： A61K31165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： 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. 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.

    摘要翻译： 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性心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化， PTCA后的再狭窄，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，以及降低绝经后妇女心血管危险或摄入避孕药后，治疗和预防糖尿病和糖尿病并发症 （肾病，视网膜病变），血管发生，支气管哮喘，慢性肾功能衰竭，肝硬化，受限的记忆力或受限的学习能力。

    Pyrimido-2-benzazepines
    57.
    发明授权
    Pyrimido-2-benzazepines 失效
    嘧啶-2-苯并吖庚因

    公开(公告)号：US4546183A

    公开(公告)日：1985-10-08

    申请号：US643509

    申请日：1984-08-23

    申请人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

    发明人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

    IPC分类号： C07C45/63 ,  C07C45/71 ,  C07C65/34 ,  C07D209/48 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04 ,  C07D211/70

    CPC分类号： C07D209/48 ,  C07C45/63 ,  C07C45/71 ,  C07C65/34 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04

    摘要： There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.9 are hydrogen or lower alkyl; n is 0 or 1 and m is 1 to 7 with the limitations that (1) at least one of R.sub.1 and R.sub.2 are hydrogen, (2) when R.sub.3 is lower acyloxy or hydroxy, A is the group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl, (3) when A is group (d) and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 then R.sub.8 and R.sub.9 are lower alkyl and (4) when n is 1, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group --CH.sub.2 --CO--R.sub.7 with R.sub.7 as above then A is the group (a) or (b)and the pharmaceutically acceptable salts thereof.The compounds exhibit pharmacological activity as anxiolytics and sedatives.Also presented are various novel intermediates and processes to produce the above end products.

    摘要翻译： 提供式IMA的化合物，其中A选自由下列组成的组：R 1选自氢，氯，溴，低级烷基，基团NR 4 R 5，基团-CH 2 -CO-R7，基团-NH（CH2）mNR8R9，羟基，低级烷氧基，巯基和低级烷基巯基; R2选自氢，氨基和二低级烷基氨基; R3选自氢，低级酰氧基和羟基; X选自氢，卤素，三氟甲基，乙基，α-羟基乙基和乙酰基; Y是氢或卤素; R4和R5是氢或低级烷基，或与它们的共键键合的氮原子一起形成5至7元杂环基; R7选自羟基低级烷氧基和NR8R9; R8和R9是氢或低级烷基; n为0或1，m为1至7，限制为（1）R 1和R 2中的至少一个为氢，（2）当R3为酰氧基或羟基时，A为（a），X为氢 ，卤素，三氟甲基，乙基或乙酰基，R 1为基团-NH（CH 2）m NR 8 R 9，则R 8和R 9为低级烷基，（3）当A为基团（d）且R 1为基团-NH（CH 2）m NR 8 R 9时 R8和R9为低级烷基，（4）当n为1时，R1为氢，低级烷基，低级烷氧基，氯，溴，或基团为-CH2-CO-R7，R7为上述，则A为（a）或 （b）及其药学上可接受的盐。 该化合物显示出作为抗焦虑药和镇静剂的药理活性。 还提出了生产上述最终产品的各种新型中间体和方法。

    1H-Pyrrole-3-carbonitrile-4(2-benzoyl)phenyl derivatives as intermediates for pyrrolo[3,4-D][2]benzazepines
    58.
    发明授权
    1H-Pyrrole-3-carbonitrile-4(2-benzoyl)phenyl derivatives as intermediates for pyrrolo[3,4-D][2]benzazepines 失效
    1H-吡咯-3-甲腈-4（2-苯甲酰基）苯基衍生物作为吡咯并[3,4-D] [2]苯并氮杂的中间体

    公开(公告)号：US4431823A

    公开(公告)日：1984-02-14

    申请号：US404788

    申请日：1982-08-03

    申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

    发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

    IPC分类号： C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

    CPC分类号： C07D207/335 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C63/72 ,  C07D207/34 ,  C07D487/04

    摘要： The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 C.sub.7 alkynyl, and R.sub.2 is the ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and the pharmaceutically acceptable salts thereof.Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

    摘要翻译： 本发明涉及式IMA的化合物，其为下式化合物的中间体：其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基， 其中R 11是氢，羟基，烷氧基，氨基和一或二低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单或二低级 烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R6是卤素，条件是如果R1或R3中的一个是羟甲基或其中R11如上所述，则剩余的取代基选自氢，低级烷基和C 3至C 7烯基或炔基，R 2 另外条件是（A）当R 4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7烯基或C 3 -C 7炔基，R 2为当R 4为羟基时R 1和 R3为氢，低级烷基，C3至C7烯基或C3至C7炔基，R2为氢或（C）当R4为烷氧基时，R1和R3为氢，低级烷基，C3至C7烯基或C3至C7炔基，以及 其药学上可接受的盐。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

    Pyrrolo[3,4-d] [2] benzazepines
    59.
    发明授权
    Pyrrolo[3,4-d] [2] benzazepines 失效
    吡咯并[3,4-d] [2]苯并吖庚因

    公开(公告)号：US4405518A

    公开(公告)日：1983-09-20

    申请号：US404936

    申请日：1982-08-02

    申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

    发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

    IPC分类号： C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

    CPC分类号： C07D207/335 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C63/72 ,  C07D207/34 ,  C07D487/04

    摘要： The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the group ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the group - ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is the group ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl,and the pharmaceutically acceptable salts thereof.Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

    摘要翻译： 本发明涉及式IMA的化合物，其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基，其中R 11为氢，羟基，烷氧基，氨基 和单 - 或二 - 低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，基团C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单 - 或二 - 低级烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R 6是卤素，条件是如果R 1或R 3中的一个是羟甲基或基团 - 其中R 11如上所述，则剩余取代基选自氢，低级烷基和C 3至C 7烯基或炔基， 另外条件是（A）当R 4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7烯基或C 3至C 7炔基，R 2为当R 4为 羟基，则R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7炔基，且R 2为氢或（C）当R 4为烷氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至 C7炔基及其药学上可接受的盐。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

    Imidazodiazepines and processes therefor
    60.
    发明授权
    Imidazodiazepines and processes therefor 失效
    咪唑二氮类及其制备方法

    公开(公告)号：US4401597A

    公开(公告)日：1983-08-30

    申请号：US242852

    申请日：1981-03-12

    申请人： Armin Walser ,  Rodney I. Fryer

    发明人： Armin Walser ,  Rodney I. Fryer

    IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  A61K31/55 ,  C07D487/22

    CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

    摘要： Novel immidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included with the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro or halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof; R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety; and R.sub.2 is hydrogen and lower alkyl.

    摘要翻译： 新型的咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢和低级烷基，优选甲基; R3和R5是氢; R4是氢，硝基或卤素，最优选氯，而在最优选的实施方式中，当位于咪唑并二氮杂的稠合的苯并部分位于其8-位时; R6是苯基或卤素，硝基或低级烷基取代的苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位; 并且R 2是氢和低级烷基。