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91. 发明授权

US09168251B2 High dose buprenorphine compositions and use as analgesic 有权
标题翻译：高剂量丁丙诺啡组合物，用作镇痛药
公开(公告)号：US09168251B2
公开(公告)日：2015-10-27
申请号：US13818013
申请日：2011-09-02
申请人： Rachel A. Richardson , Carmela H. Luangdilok , Luk Chiu Li
发明人： Rachel A. Richardson , Carmela H. Luangdilok , Luk Chiu Li
IPC分类号： A61K31/44 , A01N43/42 , A61K31/485 , A61K9/00 , A61K47/14
CPC分类号： A61K31/485 , A61K9/0019 , A61K47/14
摘要： The present disclosure relates to a method of providing prolonged analgesia to a mammal in need thereof. Specifically, the current disclosure is directed to a method of treating pain in a mammal for a prolonged period of time using a single high dose of a buprenorphine formulation.
摘要翻译：本公开涉及对有需要的哺乳动物提供长时间镇痛的方法。具体地，本公开涉及使用单次高剂量的丁丙诺啡制剂治疗哺乳动物疼痛的方法长时间。

92. 发明申请

US20150216181A1 PESTICIDE HAVING AN INSECTICIDE, ACARICIDE AND NEMATICIDE ACTION BASED ON ISOQUINOLINE ALKALOIDS AND FLAVONOIDS 审中-公开
标题翻译：具有杀虫剂，杀虫剂和杀虫剂作用的杀虫剂，基于异喹啉碱和氟虫腈
公开(公告)号：US20150216181A1
公开(公告)日：2015-08-06
申请号：US13636330
申请日：2012-03-21
申请人： Yanet Micahela HERNANDEZ ROMERO , Cristina Margarita NARVAEZ , Mario SAAVEDRA AGUILAR
发明人： Yanet Micahela Hernandez Romero , Cristina Margarita Rodriguez Narvaez , Mario Saavedra Aguilar
IPC分类号： A01N65/12 , A01N43/42
CPC分类号： A01N65/12 , A01N43/42 , A01N65/00 , A01N65/08 , A01N65/32 , A01N2300/00
摘要： The present invention relates to a pesticide having an insecticide, acaricide and nematicide action obtained from plant extracts that have important synergic interactions in their pesticide activity, the characteristics of which are efficient control of insects, mites and nematodes; low toxicity for mammals and low persistence in the environment. This pesticide is a composition based on plant extracts which is characterized because it is constituted by: Isoquinoline alkaloids and their derivatives (0.1-20%) and Flavonoids and their glycosylated derivatives (0.001-10%). Therefore, the scope of the invention is aligned in general with organic pesticides and in particular to obtaining an organic pesticide which contains as active ingredient a mixture of isoquinoline alkaloids and flavonoids to be used to control agricultural pest.
摘要翻译：本发明涉及一种具有杀虫剂，杀螨剂和杀线虫剂作用的农药，其特征是昆虫，螨虫和线虫的有效控制，其植物提取物在农药活性中具有重要的协同作用，对哺乳动物毒性低，环境持续低。该农药是基于植物提取物的组合物，其特征在于其由以下物质组成：异喹啉生物碱及其衍生物（0.1-20％）和类黄酮及其糖基化衍生物（0.001-10％）。因此，本发明的范围一般与有机农药一致，特别是获得含有作为活性成分的异喹啉生物碱和类黄酮混合物用于防治农业害虫的有机农药。

93. 发明申请

US20150216174A1 POTENTIATING AGENTS FOR PROTECTING PLANTS FROM FUNGAL INFECTIONS 审中-公开
标题翻译：用于保护植物免受真菌感染的潜在药剂
公开(公告)号：US20150216174A1
公开(公告)日：2015-08-06
申请号：US14414788
申请日：2013-06-27
申请人： UNIVERSITE D'ANGERS
发明人： Philippe Simoneau , Thomas Guillemette , Pascal Richomme , Jean-Jacques Helesbeux
IPC分类号： A01N43/90 , A01N43/42
CPC分类号： A01N43/90 , A01N25/00 , A01N31/06 , A01N43/16 , A01N43/38 , A01N43/42 , A01N31/16 , A01N43/78 , A01N47/14 , A01N2300/00
摘要： A method for preventing, controlling or treating a fungal infection on a plant organ includes applying to the plant organ a non-fungicidal amount or a potentiating amount of a composition including a potentiating agent of a plant defense molecule, in association with a phytopharmaceutical vehicle.
摘要翻译：用于预防，控制或治疗植物器官真菌感染的方法包括向植物器官施用非杀真菌量或增强量的包含植物防御分子的增效剂的组合物，其与植物药物载体相结合。

94. 发明授权

US09089139B2 Agri-horticultural pest control compositions comprising 4-(3-butynyl)aminopyrimidine derivatives 有权
标题翻译：包含4-（3-丁炔基）氨基嘧啶衍生物的农业园艺害虫防治组合物
公开(公告)号：US09089139B2
公开(公告)日：2015-07-28
申请号：US13979306
申请日：2011-12-27
申请人： Masaaki Sakai , Tomoaki Matsumura , Satohiro Midorikawa , Takashi Nomoto , Tomoko Muraki , Ryutaro Katsuki
发明人： Masaaki Sakai , Tomoaki Matsumura , Satohiro Midorikawa , Takashi Nomoto , Tomoko Muraki , Ryutaro Katsuki
IPC分类号： A61K31/517 , A01N55/00 , A01N37/34 , A01N37/50 , A01N37/52 , A01N43/42 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/653 , A01N43/78 , A01N43/84 , A01N43/90 , A01N47/24 , A01N47/34 , A01N47/44 , A01N43/82 , A01N53/00 , A01N57/26 , A01N59/16
CPC分类号： A01N55/00 , A01N37/34 , A01N37/50 , A01N37/52 , A01N43/42 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/653 , A01N43/78 , A01N43/82 , A01N43/84 , A01N43/90 , A01N47/24 , A01N47/34 , A01N47/44 , A01N53/00 , A01N57/26 , A01N59/16 , A01N37/36 , A01N37/38 , A01N37/46 , A01N43/40 , A01N47/12 , A01N47/14 , A01N51/00 , A01N57/28 , A01N2300/00
摘要： Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compounds, nucleic acids synthesis inhibitory active compounds, mitosis and cell division inhibitory active compounds, and/or agri-horticultural insecticidal, miticidal or nematicidal compounds, say, acetylcholinesterase inhibitors, GABA-gated chloride antagonists, and sodium channel modulators. Since the 4-(3-butynyl)aminopyrimidine derivatives and the existing antimicrobial active compounds and/or insecticidal active compounds are used in admixture, the 4-(3-butynyl)aminopyrimidine derivatives which are useful as pest control agents, particularly as agri-horticultural pest control agents, need be used in smaller amounts and yet their antimicrobial or insecticidal activity can be improved.
摘要翻译：具有对害虫，特别是农业园艺害虫具有突出防治效果的农业园艺害虫防治组合物，其包含作为活性成分的一种或多种由通式[I]表示的4-（3-丁炔基）氨基嘧啶衍生物，即其中 R1通常选自：a）苯基c）-SiR 5 R 6 R 7（可以相同或不同的R 5，R 6和R 7表示具有1-6个碳原子的直链或支链烷基，具有1-3个直链或支链烷基的直链或支链烷基）被一个卤素原子取代的碳原子，被一个氰基取代的具有1-3个碳原子的直链或支链氰基烷基和苯基）; d）氢原子; R2通常表示氢原子; R3通常表示氢原子; R4表示氢原子和一种或多种选自农业园艺抗微生物化合物，例如多位点接触活性化合物，核酸合成抑制活性化合物，有丝分裂和细胞分裂抑制活性化合物的农业园艺害虫控制化合物和/ 或农业园艺杀虫，杀螨或杀线虫化合物，例如乙酰胆碱酯酶抑制剂，GABA门控氯化物拮抗剂和钠通道调节剂。由于4-（3-丁炔基）氨基嘧啶衍生物和现有的抗微生物活性化合物和/或杀虫活性化合物混合使用，可用作害虫防治剂的4-（3-丁炔基）氨基嘧啶衍生物，特别是农业 - 园艺害虫防治剂需要较少量使用，但可以提高其抗微生物或杀虫活性。

95. 发明授权

US09084790B2 Compositions and methods for treating skin cancer associated diseases 有权
标题翻译：用于治疗皮肤癌相关疾病的组合物和方法
公开(公告)号：US09084790B2
公开(公告)日：2015-07-21
申请号：US13786926
申请日：2013-03-06
申请人： The Trustees of the Unversity of Pennsylvania
发明人： John T. Seykora
IPC分类号： A01N43/42 , A61K31/44 , A61K31/519 , A61K31/4745 , A61K31/506 , A61K31/277 , A61K31/4184 , A61K31/517 , A61K45/06 , A61K9/00 , A61K47/10 , A61K47/20
CPC分类号： A61K31/519 , A61K9/0014 , A61K31/277 , A61K31/33 , A61K31/4184 , A61K31/4709 , A61K31/4745 , A61K31/506 , A61K31/517 , A61K45/06 , A61K47/10 , A61K47/20 , A61K2300/00
摘要： The invention provides compositions and methods for treating skin cancer associated diseases. Specifically, the invention relates to topically administering a signaling pathway inhibitor or a related compound to treat pre-cancerous skin lesions, skin tumors, and their associated diseases or disorders.
摘要翻译：本发明提供了治疗皮肤癌相关疾病的组合物和方法。具体地，本发明涉及局部施用信号通路抑制剂或相关化合物以治疗癌前皮肤病变，皮肤肿瘤及其相关疾病或病症。

96. 发明授权

US09078889B2 Lower dosage strength imiquimod formulations and short dosing regimens for treating genital and perianal warts 有权
标题翻译：较低的剂量强度咪喹莫特配方和用于治疗生殖器和肛周疣的短剂量方案
公开(公告)号：US09078889B2
公开(公告)日：2015-07-14
申请号：US14091965
申请日：2013-11-27
申请人： Medicis Pharmaceutical Corporation
发明人： Michael T. Nordsiek , Jefferson J. Gregory
IPC分类号： A01N43/42 , A61K31/44 , A61K31/4745
CPC分类号： A61K31/4745 , A61K9/0014 , A61K9/06 , A61K31/44 , A61K47/10 , A61K47/12
摘要： Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.
摘要翻译：用于局部或透皮递送1异丁基-1H-咪唑并[4,5-c] - 喹啉-4-胺或1-（2-甲基丙基）-1H-咪唑并[4,5-c]喹啉-2-酮的药物制剂和方法， 4-胺，即咪喹莫特，以现在由美国食品和药物管理局（FDA）批准的5％咪喹莫特乳膏市售的治疗时间短于治疗的生殖器/肛周疣，被公开和描述。更具体地说，低剂量强度的咪喹莫特制剂，以递送有效剂量的咪喹莫特，用于治疗生殖器/肛周疣，具有可接受的安全性和对于患者使用而言比目前由美国食品和药物当前批准的给药方案更短和更方便的给药方案还公开和描述了用于治疗生殖器/肛周疣的Aldara 5％咪喹莫特乳膏的给药（“FDA”）。

97. 发明授权

US09073851B2 Compositions and methods for treating cancer 有权
标题翻译：用于治疗癌症的组合物和方法
公开(公告)号：US09073851B2
公开(公告)日：2015-07-07
申请号：US13662135
申请日：2012-10-26
申请人： Board of Regents, The University of Texas System
发明人： Bulent Ozpolat , Gabriel Lopez-Berestein , Kevin N. Dalby , Jiney Jose
IPC分类号： A61K9/127 , A01N43/42 , A61K31/44 , C07D209/14 , C07D471/04 , C07D403/12 , C07D209/18 , C07D471/14 , C07D209/20
CPC分类号： A61K31/437 , A61K31/404 , A61K45/06 , C07D209/14 , C07D209/18 , C07D209/20 , C07D403/12 , C07D471/04 , C07D471/14
摘要： Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression.
摘要翻译：本文提供的方法和组合物尤其用于治疗疾病，包括过度增生性疾病，偏头痛和抑郁症。

98. 发明授权

US09073825B2 Methods and intermediates for preparing macrolactams 有权
标题翻译：制备大环内酯的方法和中间体
公开(公告)号：US09073825B2
公开(公告)日：2015-07-07
申请号：US14239391
申请日：2012-08-16
申请人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
发明人： Nobuyoshi Yasuda , Jeffrey T. Kuethe , Guy Humphrey , Gregory L. Beutner , Yong-Li Zhong , Edward Cleator , Carl Baxter
IPC分类号： A01N43/04 , A01N43/42 , C07C35/04 , C07K5/083 , C07D403/12 , C07D498/16 , C07K5/12 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , A61K38/00
CPC分类号： C07C35/04 , A61K38/00 , C07C67/14 , C07C69/013 , C07C69/12 , C07C269/04 , C07C271/34 , C07D403/12 , C07D498/16 , C07K5/0808 , C07K5/126
摘要： A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound A
摘要翻译：本发明的第一方面描述了选自下组的化合物：其中R是H，C（O）RA或C（O）NHCH（X）COOH; 条件是X是C 2 -C 6烷基或C 3 -C 8环烷基，RA是C 1-6烷基或芳基; 这些化合物用于制备化合物A.

99. 发明授权

US09062048B2 Cyclohexyl-azetidinyl antagonists of CCR2 有权
标题翻译： CCR2的环己基 - 氮杂环丁烷基拮抗剂
公开(公告)号：US09062048B2
公开(公告)日：2015-06-23
申请号：US13947340
申请日：2013-07-22
申请人： Janssen Pharmaceutica NV
发明人： James C. Lanter , Thomas P. Markotan , Nalin Subasinghe , Zhihua Sui
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00 , C07D471/04 , A61K31/4709 , A61K31/4725 , A61K31/502 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D471/04 , A61K31/4709 , A61K31/4725 , A61K31/502 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
摘要翻译：本发明包括式I化合物，其中：R1，R2，R4，J，Q和A如说明书中所定义。本发明还包括预防，治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是II型糖尿病，肥胖症和哮喘。本发明还包括通过施用治疗有效量的至少一种式I化合物来抑制哺乳动物CCR2活性的方法。

100. 发明授权

US09034899B2 Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof 有权
标题翻译：芳基，杂芳基和杂环取代的四氢异喹啉及其用途
公开(公告)号：US09034899B2
公开(公告)日：2015-05-19
申请号：US12777728
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A01N43/42 , A61K31/47 , C07D217/02 , C07D217/12 , C07D401/04 , C07D413/04 , C07D471/04
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译：本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。这些化合物用于治疗各种神经和生理疾病。制备这些化合物的方法也在本发明中描述。

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