利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

18 条记录 (耗时 0.034 秒)

    Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists
    2.
    发明授权
    Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists 失效
    氨基亚甲基取代的非芳族杂环并用作物质P拮抗剂

    公开(公告)号：US06369074B1

    公开(公告)日：2002-04-09

    申请号：US09410809

    申请日：1999-10-01

    申请人： Harry R. Howard ,  Brian T O'Neill

    发明人： Harry R. Howard ,  Brian T O'Neill

    IPC分类号： C07D40112

    CPC分类号： C07D401/12 ,  C07D417/12

    摘要： The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

    摘要翻译： 本发明涉及新的氨基亚甲基取代的非芳族杂环，具体地说，涉及式（Ⅳ）的化合物，其中W，R 1，R 2，R 3，A，X'，Y'和Z'如本说明书中所定义， 在这种化合物的合成中。 式Ia和Ib的新化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。

    Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists
    3.
    发明授权
    Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists 失效
    氨基亚甲基取代的非芳族杂环并用作物质P拮抗剂

    公开(公告)号：US5854262A

    公开(公告)日：1998-12-29

    申请号：US522230

    申请日：1995-05-25

    申请人： Harry R. Howard ,  Brian T. O'Neill

    发明人： Harry R. Howard ,  Brian T. O'Neill

    IPC分类号： C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  A61K31/445 ,  C07D211/36 ,  C07D211/56

    CPC分类号： C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

    摘要： A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof; W is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with from one to three fluorine atoms, --S(O).sub.v --(C.sub.1 -C.sub.6) alkyl wherein v is zero, one or two, halo, benzyloxy or (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three fluorine atoms; R.sup.1 is a 4, 5 or 6 membered heterocyclic ring containing from one to three heteroatoms selected from oxygen, nitrogen and sulfur, wherein said heterocyclic ring contains from zero to three double bonds and is optionally substituted with one or two substituents independently selected from (C.sub.1 -C.sub.6) alkyl optionally substituted with from one to three fluorine atoms and (C.sub.1 -C.sub.6) alkoxy optionally substituted with from one to three fluorine atoms; R.sup.2 is hydrogen or --CO.sub.2 (C.sub.1 -C.sub.10)alkyl; R.sup.3 is ##STR2##

    摘要翻译： PCT No.PCT / US93 / 09407 Sec。 371日期：1995年5月25日 102（e）日期1995年5月25日PCT提交1993年10月7日PCT公布。 公开号WO94 / 13663 日期：1994年6月23日一种式[IMAGE]的化合物或其药学上可接受的盐; W是氢，任选地被一至三个氟原子取代的（C 1 -C 6）烷基，其中v是0的一个或多个，（C 1 -C 6）烷基，卤素，苄氧基或（C 1 -C 6） ）烷氧基，其任选被1至3个氟原子取代; R1是含有1至3个选自氧，氮和硫的杂原子的4,5或6元杂环，其中所述杂环含有0至3个双键，并且任选地被一个或两个独立地选自（C1 任选被一至三个氟原子取代的C 1-6烷基和任选被一至三个氟原子取代的（C 1 -C 6）烷氧基; R2是氢或-CO2（C1-C10）烷基; R3是 VII

    Articles having reduced pigment swirling
    5.
    发明授权
    Articles having reduced pigment swirling 失效
    减少颜料旋转的物品

    公开(公告)号：US6051641A

    公开(公告)日：2000-04-18

    申请号：US72600

    申请日：1998-05-05

    申请人： Harry R. Howard

    发明人： Harry R. Howard

    IPC分类号： C08K3/22 ,  C08K5/00 ,  C08K3/18

    CPC分类号： C08K5/0075 ,  C08K3/22 ,  C08K5/0041

    摘要： Articles having reduced pigment swirling are disclosed. The articles can include a resin, one or more pigments and less than about 1 percent by weight of a non-hygroscopic anti-static agent.

    摘要翻译： 公开了具有减少颜料旋转的制品。 制品可以包括树脂，一种或多种颜料和小于约1重量％的非吸湿性抗静电剂。

    N-acyl and N-aroyl aralkylamides
    6.
    发明授权
    N-acyl and N-aroyl aralkylamides 失效
    N-酰基和N-芳酰基芳烷基酰胺

    公开(公告)号：US06323229B1

    公开(公告)日：2001-11-27

    申请号：US09291454

    申请日：1999-04-14

    申请人： Harry R. Howard

    发明人： Harry R. Howard

    IPC分类号： A61K31496

    CPC分类号： C07D295/135 ,  C07D295/13 ,  C07D333/38

    摘要： A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

    摘要翻译： 式中的化合物m，R 1，R 2，R 3，R 4，R 5和X如上所定义，可用于治疗或预防偏头痛，抑郁症和其他指示5-HT1激动剂或拮抗剂的疾病。

    Heterocyclic carboxamides
    8.
    发明授权
    Heterocyclic carboxamides 失效
    杂环羧酰胺

    公开(公告)号：US06537995B2

    公开(公告)日：2003-03-25

    申请号：US09862691

    申请日：2001-05-22

    申请人： Harry R. Howard

    发明人： Harry R. Howard

    IPC分类号： C07D40310

    CPC分类号： C07D207/416 ,  C07D207/34 ,  C07D307/68 ,  C07D333/38

    摘要： A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I) or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.

    摘要翻译： 提供一种用于治疗或预防选自高血压，抑郁症，广泛性焦虑症，恐惧症，创伤后应激综合征，避孕人格障碍，早泄，进食障碍，肥胖，丛集性头痛，偏头痛，疼痛，强迫症 紊乱，恐慌症，内分泌紊乱，血管痉挛，小脑共济失调，胃肠道疾病，经前期综合征，纤维肌痛综合征，压力性尿失禁，哺乳动物慢性阵发性高血压和头痛，包括向需要这种治疗或预​​防的哺乳动物施用量 式（I）的化合物或其药学上可接受的盐; 其中X，Y，Z，R 2和R 3如本文所定义。

    Piperazinyl 5-HT1 agonists and antagonists
    9.
    发明授权
    Piperazinyl 5-HT1 agonists and antagonists 失效
    哌嗪基5-HT1激动剂和拮抗剂

    公开(公告)号：US06277852B1

    公开(公告)日：2001-08-21

    申请号：US09291352

    申请日：1999-04-14

    申请人： Harry R. Howard

    发明人： Harry R. Howard

    IPC分类号： C07D40314

    CPC分类号： C07D207/416 ,  C07D207/34 ,  C07D307/68 ,  C07D333/38

    摘要： A compound of the formula or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted; Y is wherein M is oxygen or sulfur; X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2; R1 is selected from wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and R3 is —(CH2)tB, wherein t is 0-3 and B is hydrogen, phenyl, naphthyl or a 5 or 6 membered heteroaryl group. These compounds are useful in treating and preventing a variety of central nervous system diseases, disorders and conditions for which a 5-HT1, agonist or antagonist is indicated.

    摘要翻译： 式的化合物或其药学上可接受的盐，其中Z是氧，S（O）m，其中m是0,1或2; 或其中Q是氢，（C 1 -C 6）烷基或苯基的NQ; X是氢，氯，氟，溴，碘，羟基，硝基，氰基，（C 1 -C 6）烷基，三氟甲基，（C 1 -C 6）烷氧基， （C 1 -C 6）烷基S（O）a，其中a是0,1或2; 或苯基，其中苯基任选被取代; Y是其中M是氧或硫; X 2是氢，氟，氯，三氟甲基，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基或（C 1 -C 6）烷基S O）c其中c是0,1或2; R 1选自其中R 6选自氢，任选取代的（C 1 -C 6）烷基; 并且其中G 5中的R 6与R 7一起形成2个碳链; 并且R 9和R 10独立地为氢或（C 1 -C 6）烷基; R 2为氢，（C 1 -C 4）烷基，苯基或萘基，其中所述苯基或萘基可任意取代; 和R 3为 - （CH 2）t B，其中t为0-3，B为氢，苯基，萘基或5或6元杂芳基。 这些化合物可用于治疗和预防指示5-HT1，激动剂或拮抗剂的各种中枢神经系统疾病，病症和病症。

    Compositions containing sertraline and a 5-HT.sub.1D receptor agonist or antagonist
    10.
    发明授权
    Compositions containing sertraline and a 5-HT.sub.1D receptor agonist or antagonist 失效
    含有舍曲林和5-HT1D受体激动剂或拮抗剂的组合物

    公开(公告)号：US5597826A

    公开(公告)日：1997-01-28

    申请号：US306230

    申请日：1994-09-14

    申请人： Harry R. Howard ,  John E. Macor ,  Bertrand L. Chenard ,  Jeffrey S. Sprouse ,  David W. Schulz

    发明人： Harry R. Howard ,  John E. Macor ,  Bertrand L. Chenard ,  Jeffrey S. Sprouse ,  David W. Schulz

    IPC分类号： C07D295/12 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K45/06 ,  A61P1/00 ,  A61P3/04 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D207/09 ,  C07D211/08 ,  C07D235/06 ,  C07D239/26 ,  C07D401/10 ,  C07D471/04 ,  A01N43/60

    CPC分类号： A61K45/06 ,  Y10S514/811

    摘要： The present invention relates to novel compositions containing the serotonin selective re-uptake inhibitor (SSRI), preferably (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine, and an agonist or antagonist of the serotonin 1 (5-HT.sub.1) receptor and to the use of such compositions for treating or preventing a condition selected from mood disorders, including depression, seasonal affective disorders and dysthmia, anxiety disorders including generalized anxiety disorder and panic disorder; agoraphobia, avoidant personality disorder; social phobia; obsessive compulsive disorder; post-traumatic stress disorder; memory disorders including dementia, amnestic disorders and age-associated memory impairment; disorders of eating behavior, including anorexia nervosa and bulimia nervosa; obesity; cluster headache; migraine; pain; Alzheimer's disease; chronic paroxysmal hemicrania; headache associated with vascular disorders; Parkinson's disease, including dementia in Parkinson's disease, neuroleptic-induced parkinsonism and tardive dyskinesias; endocrine disorders such as hyperprolactinaemia; vasospasm (particularly in the cerebral vasculature); hypertension; disorders in the gastrointestinal tract where changes in motility and secretion are involved; sexual dysfunction, including premature ejaculation; and chemical dependencies.

    摘要翻译： 本发明涉及含有5-羟色胺选择性再摄取抑制剂（SSRI），优选（1S-顺式）-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基 - 以及5-羟色胺1（5-HT1）受体的激动剂或拮抗剂，以及这些组合物用于治疗或预防选自情绪障碍，包括抑郁症，季节性情感障碍和心律不适的病症的用途，焦虑症包括广泛性 焦虑症和恐慌症; 广场恐惧症，避孕人格障碍; 社交恐惧症 强迫症 创伤后应激障碍; 记忆障碍包括痴呆，遗忘性障碍和年龄相关记忆障碍; 饮食行为障碍，包括神经性厌食症和神经性贪食症; 肥胖; 簇头痛; 偏头痛 疼痛; 阿尔茨海默氏病; 慢性阵发性黑血病 与血管疾病相关的头痛; 帕金森病，包括帕金森病中的痴呆，精神安定药物引起的帕金森综合征和迟发性运动障碍; 内分泌紊乱如高泌乳素血症; 血管痉挛（特别是脑血管系统）; 高血压; 涉及运动和分泌变化的胃肠道疾病; 性功能障碍，包括早泄; 和化学依赖性。