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81. 发明授权

US06337332B1 Neuropeptide Y receptor antagonists 失效
标题翻译：神经肽Y受体拮抗剂
公开(公告)号：US06337332B1
公开(公告)日：2002-01-08
申请号：US09382418
申请日：1999-08-24
申请人： Philip A. Carpino
发明人： Philip A. Carpino
IPC分类号： A01N4354
CPC分类号： C07D401/04 , C07D239/88 , C07D239/94
摘要： Compounds of the structures are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.
摘要翻译：该结构的化合物可用于治疗与过量神经肽Y相关的病症，包括肥胖症和循环系统疾病。

82. 发明授权

US06310071B1 2-(0-(Pyrimidin-4-yl)methyleneoxy)phenylacetic acid derivatives and their use for controlling harmful fungi and animal pests 失效
标题翻译： 2-（O-（嘧啶-4-基）亚甲氧基）苯乙酸衍生物及其用于控制有害真菌和动物害虫
公开(公告)号：US06310071B1
公开(公告)日：2001-10-30
申请号：US09604111
申请日：2000-06-26
申请人： Klaus Oberdorf , Wassilios Grammenos , Hubert Sauter , Thomas Grote , Reinhard Kirstgen , Ruth Müller , Bernd Müller , Franz Röhl , Michael Rack , Herbert Bayer , Gisela Lorenz , Eberhard Ammermann , Siegfried Strathmann , Volker Harries
发明人： Klaus Oberdorf , Wassilios Grammenos , Hubert Sauter , Thomas Grote , Reinhard Kirstgen , Ruth Müller , Bernd Müller , Franz Röhl , Michael Rack , Herbert Bayer , Gisela Lorenz , Eberhard Ammermann , Siegfried Strathmann , Volker Harries
IPC分类号： A01N4354
CPC分类号： C07D239/34 , A01N43/54
摘要： 2-(O-[pyrimidin-4-yl]methylenoxy)phenylacetic acid derivatives of the general formula I and the salts and N-oxides thereof where the radicals R1 to R4 and Q have the following meanings: R1 is hydrogen or alkyl; R2 is halogen, alkyl or haloalkyl; R3 is hydrogen; amino; hydroxyl; mercapto; halogen; unsubstituted or phenyl-substituted alkyl; haloalkyl; alkoxyalkyl; alkoxy; monoalkylamino; dialkylamino; alkylthio; alkylsulfoxyl; alkylsulfonyl; cycloalkyl; trialkylsilyloxy, or: phenyl, phenoxy, phenoxymethyl, benzyloxy or hetaryl, unsubstituted or substituted in the aromatic ring; R4 is hydrogen; cyano; halogen; alkyl; haloalkyl or alkoxy; Q is C(═NOCH3)—CONHCH3, C(═NOCH3)—COOCH3 or N(OCH3)—COOCH3, the salts and N-oxides thereof, and their use for controlling harmful fungi and animal pests.
摘要翻译： 2-（O- [嘧啶-4-基]亚甲基氧基）苯基乙酸衍生物及其盐和N-氧化物，其中基团R 1至R 4和Q具有以下含义：R 1为氢或烷基; R 2为卤素，烷基或卤代烷基; R 3是氢; 氨基; 羟; 巯基卤素; 未取代或苯基取代的烷基; 卤代烷基烷氧基烷基烷氧基单烷基氨基; 二烷基氨基; 烷硫基烷基磺酰基; 烷基磺酰基; 环烷基三烷基甲硅烷氧基，或苯基，苯氧基，苯氧基甲基，苄氧基或杂芳基，未取代或取代在芳香环中; R4为氢; 氰基; 卤素; 烷基; 卤代烷基或烷氧基; Q是C（= NOCH 3）-CONHCH 3，C（= NOCH 3）-COOCH 3或N（OCH 3）-COOCH 3，其盐和N-氧化物及其用于控制有害真菌和动物害虫的用途。

83. 发明授权

US06294517B1 Compositions and kits comprising alpha-adrenergic receptor antagonists and nitric oxide donors and methods of use 失效
标题翻译：包含α-肾上腺素能受体拮抗剂和一氧化氮供体的组合物和试剂盒及使用方法
公开(公告)号：US06294517B1
公开(公告)日：2001-09-25
申请号：US09145143
申请日：1998-09-01
申请人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
发明人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
IPC分类号： A01N4354
CPC分类号： C07D459/00 , A61K45/06 , C07C381/00 , C07D211/62 , C07D233/24 , C07D239/95 , C07D401/04 , C07D405/12 , Y10S514/929 , Y10S514/968
摘要： The present invention describes novel compositions and kits comprising alpha-adrenergic receptor antagonists and compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, or stimulate nitric oxide synthesis. In preferred embodiments, the alpha-adrenergic receptor antagonist is an alkaloid selected from the group consisting of rauwolscine, corynanthine, yohimbine, apoyohimbine, beta-yohimbine, yohimbol, pseudoyohimbine and epi-3&agr;-yohimbine, and the compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, or stimulates nitric oxide synthesis is selected from the group consisting of L-arginine, S-nitroso-N-acetylcysteine, S-nitroso-captopril, S-nitroso-homocysteine, S-nitroso-cysteine and S-nitroso-glutathione. In other embodiments, the present invention describes novel compositions comprising yohimbine and L-arginine. In still other embodiments, the invention describes novel compositions comprising yohimbine and L-arginine where the yohimbine is derived from yohimbe bark or Rauwolfia root. The novel compositions of the invention are useful for treating impotence in males and females.
摘要翻译：本发明描述了包含α-肾上腺素能受体拮抗剂和捐赠，转移或释放一氧化氮，提高内源性松弛因子的内源水平或刺激一氧化氮合成的化合物的新型组合物和试剂盒。在优选的实施方案中，α-肾上腺素能受体拮抗剂是选自以下的生物碱：羊尿苷，色氨酸，育亨宾，去氨嘌呤，β-育亨宾，育亨宾，假蛋黄嘌呤和epi-3α-育亨宾，以及捐赠，转移或释放的化合物一氧化氮提高内源性舒张因子的内源水平，或刺激一氧化氮合成选自L-精氨酸，S-亚硝基-N-乙酰半胱氨酸，S-亚硝基卡托普利，S-亚硝基高半胱氨酸，S 亚硝基半胱氨酸和S-亚硝基 - 谷胱甘肽。在其它实施方案中，本发明描述了包含育亨宾和L-精氨酸的新型组合物。在其它实施方案中，本发明描述了包含育亨宾和L-精氨酸的新型组合物，其中育亨宾衍生自yohimbe树皮或Rauwolfia根。本发明的新型组合物可用于治疗男性和女性的阳。。

84. 发明授权

US06288070B1 Triazolopurine derivatives, medicinal composition containing the derivatives, adenosine A3 receptor compatibilizing agent, and asthmatic remedy 有权
标题翻译：三唑嘌呤衍生物，含有衍生物的药物组合物，腺苷A3受体相容剂和哮喘补救剂
公开(公告)号：US06288070B1
公开(公告)日：2001-09-11
申请号：US09647613
申请日：2000-10-03
申请人： Takashi Okamura , Yasuhisa Kurogi , Hiroshi Nishikawa
发明人： Takashi Okamura , Yasuhisa Kurogi , Hiroshi Nishikawa
IPC分类号： A01N4354
CPC分类号： C07D487/14 , C07F9/6561
摘要： Disclosed is a triazolopurine derivative represented by the general formula: wherein R1 and R2 represent the same groups as those described in the specification; and A represents a group: wherein R3 represents the same groups as those described in the specification. This compound is incorporated in a pharmaceutical composition because of its affinity to an adenosine A3 receptor, and is used as an adenosine A3 receptor antagonist or a remedy for asthma.
摘要翻译：公开了由以下通式表示的三唑并嘌呤衍生物：其中R1和R2表示与说明书中所述相同的基团; A表示基团：其中R3表示与说明书中所述相同的基团。该化合物由于其对腺苷A 3受体的亲和力而被并入药物组合物中，并且用作腺苷A 3受体拮抗剂或哮喘药。

85. 发明授权

US06284766B1 9H-pyrimido [4,5-b] indole derivatives: CRF1 specific ligands 失效
标题翻译： 9H-嘧啶并[4,5-b]吲哚衍生物：CRF1特异性配体
公开(公告)号：US06284766B1
公开(公告)日：2001-09-04
申请号：US09561569
申请日：2000-04-28
申请人： Raymond F. Horvath
发明人： Raymond F. Horvath
IPC分类号： A01N4354
CPC分类号： C07D487/04 , G01N2333/5751 , G01N2333/726
摘要： Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, R4 and R5 are defined herein, which compounds are selective antagonists at CRF1 receptors and are therefore useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache, anxiety, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
摘要翻译：公开了下式的化合物：其中Ar，R 1，R 2，R 3，R 4和R 5在本文中定义，这些化合物是CRF1受体的选择性拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁，头痛，焦虑，心血管疾病和饮食失调。还公开了治疗这种病症以及包装的药物组合物的方法。

86. 发明授权

US06281219B1 Acaricidal and insecticidal substituted pyrimidines and a process for the preparation thereof 失效
标题翻译：杀螨和杀虫剂的取代嘧啶及其制备方法
公开(公告)号：US06281219B1
公开(公告)日：2001-08-28
申请号：US09351547
申请日：1999-07-12
申请人： Salvatore John Cuccia , William Wakefield Wood , Brian Lee Buckwalter , John Francis Chiarello , Linda Barbara Fleming
发明人： Salvatore John Cuccia , William Wakefield Wood , Brian Lee Buckwalter , John Francis Chiarello , Linda Barbara Fleming
IPC分类号： A01N4354
CPC分类号： C07D239/42 , A01N43/54 , C07D239/28
摘要： The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.
摘要翻译：本发明提供式Ⅰ化合物的制备方法及其作为杀螨剂和杀虫剂的用途。

87. 发明授权

US06274586B1 Combatting parasitic fungi with a combination of an active agent inhibiting respiration in the cytochrome complex III and of fenazaquine 失效
标题翻译：用寄生真菌与抑制细胞色素复合物III中呼吸作用的活性剂和芬达喹
公开(公告)号：US06274586B1
公开(公告)日：2001-08-14
申请号：US09571402
申请日：2000-05-15
申请人： Herbert Bayer , Hubert Sauter , Eberhard Ammermann , Gisela Lorenz , Siegfried Strathmann , Harald Köhle , Günter Retzlaf
发明人： Herbert Bayer , Hubert Sauter , Eberhard Ammermann , Gisela Lorenz , Siegfried Strathmann , Harald Köhle , Günter Retzlaf
IPC分类号： A01N4354
CPC分类号： A01N43/54 , A01N61/00 , A01N43/56 , A01N37/50 , A01N2300/00
摘要： The present nvention relates to compositions for controlling harmful fungi which comprise, as active ingredients, at least one compound which inhibits respiration on the cytochrome complex III and fenazaquin. The compositions according to the invention are useful in particular for controlling botrytis.
摘要翻译：本发明涉及用于控制有害真菌的组合物，其包含作为活性成分的至少一种抑制细胞色素复合物III和fenazaquin上的呼吸的化合物。根据本发明的组合物特别用于防治葡萄孢菌。

88. 发明授权

US06258819B1 Substituted 2(4-piperidyl)-4(3H)-quinazolinones and 2-(4-piperidyl)-4(3H)-azaquinazolinones 失效
标题翻译：取代的2（4-哌啶基）-4（3H） - 喹唑啉酮和2-（4-哌啶基）-4（3H） - 氮杂喹唑啉酮
公开(公告)号：US06258819B1
公开(公告)日：2001-07-10
申请号：US09626806
申请日：2000-07-27
申请人： Robin Douglas Clark , Counde O'Yang
发明人： Robin Douglas Clark , Counde O'Yang
IPC分类号： A01N4354
CPC分类号： C07D401/14 , C07D471/04
摘要： This invention relates to compounds which are generally alpha1A/B-receptor antagonists and which are represented by Formula I: wherein the substituents are as defined in the specification; or pharmaceutically acceptable salts, hydrates, or N-oxides thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and a process for their preparation.
摘要翻译：本发明涉及通常为α1A/ B-受体拮抗剂并由式I表示的化合物：其中取代基如说明书中所定义; 或其药学上可接受的盐，水合物或N-氧化物。本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

89. 发明授权

US06245772B1 Fungicidal active compound combinations 失效
标题翻译：杀真菌活性化合物组合
公开(公告)号：US06245772B1
公开(公告)日：2001-06-12
申请号：US09541922
申请日：2000-04-03
申请人： Heinz-Wilhelm Dehne , Wilhelm Brandes , Karl-Heinz Kuck , Thomas Seitz
发明人： Heinz-Wilhelm Dehne , Wilhelm Brandes , Karl-Heinz Kuck , Thomas Seitz
IPC分类号： A01N4354
CPC分类号： A01N47/12 , A01N47/04 , A01N37/34 , A01N47/14 , A01N47/26 , A01N43/66 , A01N59/20 , A01N37/38 , A01N43/32 , A01N47/34 , A01N57/12 , A01N37/46 , A01N43/76 , A01N43/40 , A01N43/54 , A01N37/50 , A01N43/653 , A01N43/82 , A01N47/32 , A01N2300/00
摘要： New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.
摘要翻译：描述了式（I）的缬氨酰胺衍生物（其中R 1和R 2具有说明书中给出的含义，已知的杀真菌活性物质）及其用于防治植物病原真菌的新活性化合物组合。

90. 发明授权

US06194417B1 Fungicide mixtures 失效
标题翻译：杀菌剂混合物
公开(公告)号：US06194417B1
公开(公告)日：2001-02-27
申请号：US09155089
申请日：1998-09-21
申请人： Ruth Müller , Herbert Bayer , Hubert Sauter , Eberhard Ammermann , Gisela Lorenz , Siegfried Strathmann , Klaus Schelberger , Dietrich Mappes , Joachim Leyendecker , Bernd Müller
发明人： Ruth Müller , Herbert Bayer , Hubert Sauter , Eberhard Ammermann , Gisela Lorenz , Siegfried Strathmann , Klaus Schelberger , Dietrich Mappes , Joachim Leyendecker , Bernd Müller
IPC分类号： A01N4354
CPC分类号： A01N37/52 , A01N47/24 , A01N43/54 , A01N2300/00
摘要： Fungicidal mixtures, comprising a) oxime ether of the formula I where the substituents have the following meanings: X is oxygen or amino (NH); Y is CH or N; Z is oxygen, sulfur, amino (NH) or C1-C4-alkylamino (N—C1-C4-alkyl); R′ is C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-alkenyl, C2-C6-haloalkenyl, C3-C6-alkynyl, C3-C6-haloalkynyl, C3-C6-cycloalkylmethyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-halo-alkoxy and C1-C4-alkylthio; and/or b) a carbamate of the formula I, where T is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different when n is 2, and c) (±)-(2-chlorophenyl)(4-chlorophenyl)(pyrimidin-5-yl)methanol in a synergistically active amount.
摘要翻译：杀真菌混合物，包含a）式I的肟醚，其中取代基具有以下含义：X是氧或氨基（NH）; Y是CH或N; Z是氧，硫，氨基（NH）或C 1 -C 4 - 烷基氨基（N-C 1 -C 4 - 烷基）; R'是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 3 -C 6烯基，C 2 -C 6卤代链烯基，C 3 -C 6炔基，C 3 -C 6卤代炔基，C 3 -C 1-6 - 烷基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷基，C 1 -C 4环烷基，或者可以部分或完全卤化和/或可以与其相连的苄基，，C 1 -C 4卤代烷氧基和C 1 -C 4 - 烷硫基; 和/ orb）式I的氨基甲酸酯，其中T是CH或N，n是0,1或2，R是卤素，C 1 -C 4烷基或C 1 -C 4卤代烷基，基团R 当n为2时，并且c）（±） - （2-氯苯基）（4-氯苯基）（嘧啶-5-基）甲醇具有协同活性量。

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