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71. 发明申请

WO1992016205A2 NOVEL DERIVATIVES OF 2-CARBOXYNDOLES HAVING PHARMACEUTICAL ACTIVITY 审中-公开
标题翻译：具有药物活性的2-羧基嘌呤衍生物的新颖衍生物
公开(公告)号：WO1992016205A2
公开(公告)日：1992-10-01
申请号：PCT/US1992001699
申请日：1992-03-04
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BIGGE, Christopher, Franklin , JOHNSON, Graham , YUEN, Po-wai
IPC分类号： A61K31/40
CPC分类号： C07D209/42
摘要： The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic acids or ester amides, or 2-acylsulfon amides thereof; and including also as 3-substituents unsaturated acids and their further ester and amide derivatives. These 2-carboxyindoles are useful as pharmaceutical agents, therefore, the present invention is also pharmaceutical compositions and pharmaceutical methods of treatment therefor. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.
摘要翻译：本发明涉及在3-位取代的新颖的2-羧基吲哚化合物，其包含异羟肟酸酰胺和这些酸的衍生物或脲和羰基，羧基或膦酸或酯酰胺或它们的2-酰基砜酰胺，并且其在3位不饱和酸及其其他酯和酰胺衍生物中也含有取代基。这些2-羧基吲哚可用作药物，因此本发明还涉及使用这些组合物的药物组合物和治疗方法。所公开的化合物可用于治疗神经变性疾病，例如脑血管疾病。

72. 发明申请

WO1992015198A1 ORAL AND PERSONAL HYGIENE ARTICLES CONTAINING ACTIVE AGENTS BONDED TO THE SURFACE THEREOF 审中-公开
标题翻译：含有活性剂的口腔和个人卫生用品与其表面粘合
公开(公告)号：WO1992015198A1
公开(公告)日：1992-09-17
申请号：PCT/US1991009116
申请日：1991-12-05
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , BOOTH, Anthony, R.
IPC分类号： A01N25/34
CPC分类号： A01N25/34 , A01N55/00 , A01N2300/00
摘要： An article suitable for oral or personal hygiene use, such as a toothbrush, toothpick, dental floss, denture, razor, eye glasses, contact lens, hair brush or comb, and comprised of polymeric material, has one or more chemically or biologically active agent(s) bonded to the surface thereof.
摘要翻译：适用于口腔或个人卫生用途的物品，例如牙刷，牙签，牙线，义齿，剃刀，眼镜，隐形眼镜，毛刷或梳子，并且由聚合物材料组成，具有一种或多种化学或生物活性剂（s）结合到其表面。

73. 发明申请

WO1992011245A1 2-ACYLAMIDO DERIVATIVES OF 3,4-DIHYDRO-3-OXO-QUINOXALINE HAVING PHARMACEUTICAL ACTIVITY 审中-公开
标题翻译：具有药物活性的3,4-二羟基-3-氧代喹啉的2-亚氨基衍生物
公开(公告)号：WO1992011245A1
公开(公告)日：1992-07-09
申请号：PCT/US1991008586
申请日：1991-11-22
申请人： WARNER-LAMBERT COMPANY , HAYS, Sheryl, Jeanne , JOHNSON, Graham , LESCOSKY, Leonard, Joseph , MALONE, Thomas, Charles , NOVAK, Perry, Michael
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D241/44
CPC分类号： C07D409/12 , C07C233/15 , C07C251/38 , C07D241/44 , C07D409/14 , C07D413/10
摘要： The present invention relates to novel 2-acylamide derivatives of 3,4-dihydro-3-oxo-quinoxaline useful as pharmaceutical agents, to methods for their production, to pharmaceutical compositions and methods of treatment therefor. The compounds of the present invention have activity as excitatory amino acid receptor mediators and, thus, are useful in the treatment of a wide range of neurodegenerative disorders including cerebrovascular disorders such as stroke.
摘要翻译：本发明涉及可用作药物的3,4-二氢-3-氧代喹喔啉的新型2-酰基酰胺衍生物，其生产方法，药物组合物及其治疗方法。本发明的化合物具有作为兴奋性氨基酸受体介质的活性，因此可用于治疗广泛范围的神经变性疾病，包括脑血管疾病如中风。

74. 发明申请

WO1992009596A1 INDIVIDUAL STEREOISOMERS OF 7-[3-(1-AMINOALKYL)-1-PYRROLIDINYL]-QUINOLONES AND NAPHTHYRIDONES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7- [3-（1-氨基环戊基）-1-吡咯烷基] - 苯并噻唑类作为抗菌剂的单独立体异构体
公开(公告)号：WO1992009596A1
公开(公告)日：1992-06-11
申请号：PCT/US1991008419
申请日：1991-11-12
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , DOMAGALA, John, Michael , KIELY, John, Steven , SCHROEDER, Mel, Conrad
IPC分类号： C07D401/04
CPC分类号： C07D207/26 , C07D207/09 , C07D401/04 , C07D471/04
摘要： Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.
摘要翻译：描述了7- [3-（1-氨基烷基）-1-吡咯烷基] - 喹诺酮和萘啶酮的单个立体异构体，它们作为抗菌剂的治疗优点，以及制备和分离这些立体异构体的新方法。

75. 发明申请

WO1992007831A1 SUBSTITUTED TETRAHYDROPYRIDINES AND HYDROXYPIPERIDINES AS CENTRAL NERVOUS SYSTEM AGENTS 审中-公开
标题翻译：作为中枢神经系统药物的替代四氢吡啶类和羟脯氨酸
公开(公告)号：WO1992007831A1
公开(公告)日：1992-05-14
申请号：PCT/US1991008017
申请日：1991-10-29
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , GLASE, Shelly , JAEN, Juan Carlos , SMITH, Sarah, Jane , WISE, Lawrence, David
IPC分类号： C07D211/70
CPC分类号： C07D401/06 , C07D211/70 , C07D409/14
摘要： Substituted tetrahydropyridines and hydroxypiperidines of formula (I) and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

76. 发明申请

WO1992007549A1 IMPROVED ANTI-PLAQUE COMPOSITIONS COMPRISING A COMBINATION OF MORPHOLINOAMINO ALCOHOL AND ANTIBIOTIC 审中-公开
标题翻译：包含莫尔林氨基醇和抗生素组合的抗结构组合物
公开(公告)号：WO1992007549A1
公开(公告)日：1992-05-14
申请号：PCT/US1991007077
申请日：1991-09-26
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , PAN, Pauline, H. , STURDIVANT, Linda, D.
IPC分类号： A61K07/16
CPC分类号： A61Q11/00 , A61K8/49 , A61K31/535 , A61K2800/59 , Y02A50/406 , A61K2300/00
摘要： Compositions having improved anti-plaque and anti-gingivitis activity comprises a synergistic combination of a) a morpholinoamino alcohol, such as 3-(4-propylheptyl)-4-(2-hydroxyethyl)morpholine and b) and antibiotic, such as the aminoglycosides, amphenicols, ansamycins, carbapenems, cephalosporins, cephamycins, monobactams, oxacephems, penicillins, lincosamides, macrolides, polypeptides and tetracyclines.

77. 发明申请

WO1992007487A1 TOOTHBRUSH WITH SEMI-PERMEABLE HOLLOW FIBERS 审中-公开
标题翻译：具有半透明中空纤维的牙刷
公开(公告)号：WO1992007487A1
公开(公告)日：1992-05-14
申请号：PCT/US1991007432
申请日：1991-10-08
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , PAN, Pauline, H. , VAN DONGEN, David, B.
IPC分类号： A46B11/00
CPC分类号： A46B11/00 , A46B2200/1066
摘要： A toothbrush (10) has a handle (12) and a head (16) which is formed on the handle (12). A plurality of semi-permeable hollow fibers (82) are grouped on the head (16) in outwardly-projecting tufts (86). A diffusible medium (24) that contains appropriate dental agents is held within the lumens (96) of the repective fibers (82). Further, a reservoir (34) may be formed in the handle (32) of the toothbrush (10) to hold the medium (24) and to pass the medium (24) from the reservoir (34) to the lumens (54) of the respective fibers (68). When the hollow fibers (82) are wetted during the brushing process, the agents diffuse through the wall of the semi-permeable hollow fibers (82) onto the teeth and gums. Additionally, standard toothbrush monofilament bristles (74) may also be grouped on the head (76) of the toothbrush (10) in tufts (72) which are interspersed among the tufts (86) of hollow fibers (82). The tufts (86) of hollow fibers (82) and tufts (72) of bristles (74) can be arranged in various patterns on the head (70) of the toothbrush (10) to efficaciously cleanse the teeth and gums and to directly apply the dental agents to the teeth and gums.
摘要翻译：牙刷（10）具有手柄（12）和形成在手柄（12）上的头部。多个半透空心纤维（82）以向外突出的簇（86）分组在头部（16）上。包含适当的牙科剂的可扩散介质（24）被保持在指向纤维（82）的腔（96）内。此外，储存器（34）可以形成在牙刷（10）的手柄（32）中以保持介质（24）并使介质（24）从储存器（34）传递到腔（54）的内腔相应的纤维（68）。当中空纤维（82）在刷洗过程中被润湿时，试剂通过半渗透性中空纤维（82）的壁扩散到牙齿和牙龈上。此外，标准牙刷单丝刷毛（74）也可以分组在牙刷（10）的头部（76）上，所述刷毛簇（72）分散在中空纤维（82）的簇（86）之间。中空纤维（82）的毛簇（86）和刷毛（74）的刷毛簇（72）可以以各种图案布置在牙刷（10）的头部（70）上，以有效地清洁牙齿和牙龈并直接施加牙齿剂对牙齿和牙龈。

78. 发明申请

WO1992004025A1 AMINO ACID ANALOGS AS CCK ANTAGONISTS 审中-公开
标题翻译：氨基酸类似物作为CCK拮抗剂
公开(公告)号：WO1992004025A1
公开(公告)日：1992-03-19
申请号：PCT/US1991006181
申请日：1991-08-29
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , HORWELL, David, Christopher , ARANDA, Julian , AUGELLI-SZAFRAN, Corinne, Elizabeth , BETCHE, Hans-Jurgen , HOLMES, Ann , MULLICAN, Michael, David , PRITCHARD, Martyn, Clive , RICHARDSON, Reginald, Stewart , ROTH, Bruce, David , ROBERTS, Edward , TAIT, Bradley, Dean , TRIVEDI, Bharat, Kalidas , TROSTMANN, Uwe , UNANGST, Paul, Charles
IPC分类号： A61K31/395
CPC分类号： C07D243/16 , C07C271/34 , C07C2603/74 , C07D207/327 , C07D213/56 , C07D213/89 , C07D215/12 , C07D231/56 , C07D233/26 , C07D235/16 , C07D243/24 , C07D249/18 , C07D261/08 , C07D277/46 , C07D285/06 , C07D307/79 , C07D307/81 , C07D307/82 , C07D333/60 , C07D403/12 , C07D471/04
摘要： Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.
摘要翻译：公开了用作治疗肥胖症，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药物的新型非天然罂粟脂。此外，化合物是抗焦虑剂和抗溃疡剂。这些化合物是可用于预防慢性治疗或使用尼古丁，地西泮，酒精，可卡因，咖啡因和阿片样物质的戒断反应的药剂。这些化合物也可用于治疗和/或预防恐慌发作。还公开了药物组合物和使用二趾甲的治疗方法以及制备它们的方法和可用于其制备的新型中间体。本发明的另一个特征是本发明化合物用于制备诊断组合物的用途。

79. 发明申请

WO1992002219A1 TETRACYCLIC AMINES USEFUL AS CEREBROVASCULAR AGENTS 审中-公开
标题翻译：四环胺可用作微囊剂
公开(公告)号：WO1992002219A1
公开(公告)日：1992-02-20
申请号：PCT/US1991005853
申请日：1991-08-08
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , MALONE, Thomas, Charles
IPC分类号： A61K31/395
CPC分类号： C07D209/58 , C07D221/18
摘要： A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.

80. 发明申请

WO1991010679A2 RENIN INHIBITING PEPTIDES HAVING AN 'alpha'-HETEROATOM AMINO ACID AT THE P3 POSITION 审中-公开
标题翻译：在P3位置上具有α-异源氨基酸的RENIN抑制肽
公开(公告)号：WO1991010679A2
公开(公告)日：1991-07-25
申请号：PCT/US1991000308
申请日：1991-01-15
申请人： WARNER-LAMBERT COMPANY
发明人： WARNER-LAMBERT COMPANY , KALTENBRONN, James, Stanley , REPINE, Joseph, Thomas
IPC分类号： C07K05/02
CPC分类号： C07K5/081 , A61K38/00 , C07K5/0205 , C07K5/0606 , C07K5/06078 , Y10S530/80
摘要： Nouveaux composés inhibiteurs de la rénine, utiles dans le traitement de l'hypertension, de l'insuffisance cardiaque, de l'hyperaldostéronisme, du glaucome associés à la rénine, ainsi que d'autres maladies provoquées par des rétrovirus comprenant HTLV-I, -II, -III. L'invention concerne également des procédés de préparation des composés, des nouveaux intermédiaires utiles dans la préparation de ces derniers, des compositions les contenant, ainsi que leurs procédés d'utilisation. En outre, l'invention concerne un procédé de diagnostic utilisant les composés afin de déterminer la présence d'hypertension, d'insuffisance cardiaque, ou d'hyperaldostéronisme associés à la rénine.

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