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1. 发明申请

WO2010065877A2 METHODS OF TREATING AN OVERWEIGHT OR OBESE SUBJECT 审中-公开
标题翻译：治疗过度或成瘾症的方法
公开(公告)号：WO2010065877A2
公开(公告)日：2010-06-10
申请号：PCT/US2009/066809
申请日：2009-12-04
申请人： ZAFGEN CORPORATION , VATH, James, E.
发明人： VATH, James, E.
IPC分类号： C07D303/06 , C07D303/10 , C07D405/12
CPC分类号： C07D303/22 , A61K31/336 , A61K31/4025 , A61K31/439 , C07D303/06 , C07D303/10 , C07D405/12 , C07D453/02 , Y10S514/909
摘要： The disclosure herein generally relates to methods of treating an overweight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
摘要翻译：本文的公开内容通常涉及治疗超重或肥胖状况以及超重或肥胖相关病症的方法。在一个实施方案中，本公开提供了治疗超重或肥胖病症的方法，包括向有需要的受试者施用一定量的包含MetAP-2抑制化合物或其盐，酯或前药的药物组合物，其有效导致受试者体重减轻。

2. 发明申请

WO2010065877A9 METHODS OF TREATING AN OVERWEIGHT OR OBESE SUBJECT 审中-公开
标题翻译：治疗过度或成瘾症的方法
公开(公告)号：WO2010065877A9
公开(公告)日：2010-10-21
申请号：PCT/US2009066809
申请日：2009-12-04
申请人： ZAFGEN CORP , VATH JAMES E
发明人： VATH JAMES E
IPC分类号： C07D303/06 , C07D303/10 , C07D405/12
CPC分类号： C07D303/22 , A61K31/336 , A61K31/4025 , A61K31/439 , C07D303/06 , C07D303/10 , C07D405/12 , C07D453/02 , Y10S514/909
摘要： The disclosure herein generally relates to methods of treating an over eight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MctAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
摘要翻译：本文的公开内容通常涉及治疗超重或肥胖状况以及超重或肥胖相关病症的方法。在一个实施方案中，本公开提供了治疗超重或肥胖病症的方法，包括向有需要的受试者施用一定量的包含MetAp-2抑制化合物或其盐，酯或前药的药物组合物，其有效导致受试者体重减轻。

3. 发明申请

WO1990004921A1 NON-BIOACCUMULABLE PESTICIDES 审中-公开
标题翻译：非生物可吸收的农药
公开(公告)号：WO1990004921A1
公开(公告)日：1990-05-17
申请号：PCT/US1989004929
申请日：1989-11-02
申请人： COULSTON, Frederick , KORTE, Friedhelm , KORTE, Stephan, W. , COULSTON, Craig, W.
IPC分类号： A01N29/04
CPC分类号： C07C69/00 , A01N29/08 , A01N31/06 , A01N37/08 , A01N37/34 , A01N37/36 , A01N43/20 , C07C23/28 , C07C23/38 , C07C35/37 , C07C43/192 , C07C61/15 , C07C61/40 , C07C62/06 , C07C62/12 , C07C62/32 , C07C62/34 , C07C255/47 , C07C2602/42 , C07C2603/00 , C07C2603/68 , C07D303/08 , C07D303/10
摘要： Novel pesticidal compositions, which are characterized by biodegradability and do not bioaccumulate to an unacceptable level in fats and tissues of animals, fowl and fish, containing active compounds and optionally a carrier suitable for administering said compounds to a pest by contact, ingestion or inhalation, are disclosed. Such compositions comprise in addition to the carrier compounds of formula (I), where R is H, Cl or other Hal, hydroxyl, lower alkoxyl, lower alkyl, cyano, CONR2 or NR2, where R2 is H or lower alkyl; X and Y may be R, and when taken together may be -0- or a saturated or unsaturated monocyclic or bicyclic group which may be substituted with R, epoxide, carboxy or carboxymethyl group; and the unsaturated analogs thereof wherein the unsaturation occurs at at least one of the 2 or the 5 positions, and wherein unsaturation may occur optionally in the ring formed by X and Y taken together; with the further proviso that said compound has between 4 and 6 halogens; and a carrier for said compound. Methods of using such pesticides to kill or disable pests are disclosed. Certain novel compounds within the group and novel methods of making said compounds are disclosed.
摘要翻译：新型杀虫组合物，其特征在于生物降解性，并且不含有活性化合物和任选的适合于通过接触，摄取或吸入将所述化合物施用于有害生物的动物，家禽和鱼的脂肪和组织中的生物累积水平达到不可接受的水平，被披露。除了式（I）的载体化合物外，其中R是H，Cl或其它Hal，羟基，低级烷氧基，低级烷基，氰基，CONR2或NR2，其中R2是H或低级烷基; X和Y可以是R，并且一起可以是-O-或可以被R，环氧化物，羧基或羧甲基取代的饱和或不饱和的单环或双环基团; 和其不饱和类似物，其中不饱和键在2或5个位置中的至少一个上发生，并且其中不饱和可任选地在由X和Y形成的环中一起发生; 进一步的条件是所述化合物具有4至6个卤素; 和所述化合物的载体。公开了使用这种杀虫剂杀死或禁用害虫的方法。公开了该组内的某些新化合物和制备所述化合物的新方法。

4. 发明申请

WO2012083408A1 COMPOSIÇÕES FARMACÊUTICAS ANTIMALÁRICAS CONTENDO DERIVADOS DE DITERPENOS CAURÂNICOS 审中-公开
标题翻译：含茉莉酸衍生物的抗疟药物组合物
公开(公告)号：WO2012083408A1
公开(公告)日：2012-06-28
申请号：PCT/BR2011/000513
申请日：2011-12-23
申请人： UNIVERSIDADE FEDERAL DE MINAS GERAIS - UFMG , OLIVEIRA, Alaíde Braga de , VAROTTI, Fernando de Pilla , BATISTA, Ronan
发明人： OLIVEIRA, Alaíde Braga de , VAROTTI, Fernando de Pilla , BATISTA, Ronan
IPC分类号： A61K31/215 , A61K31/336 , A61K31/395 , A61P33/06
CPC分类号： A61K31/215 , A61K31/336 , A61K31/505 , C07D303/10 , C07D493/10 , Y02A50/411
摘要： A presente invenção descreve composições farmacêuticas contendo derivados caurânicos produzidos a partir do ácido caurenoico e de outros diterpenos, bem como a sua atividade antimalárica. Os mesmos podem ser utilizados isoladamente ou em combinação para o tratamento de malária.
摘要翻译：本发明描述了含有由耐热酸和其它二萜产生的山梨醇衍生物的药物组合物，以及可以分离或组合用于治疗疟疾的这些山梨醇衍生物的抗疟疾活性。

5. 发明申请

WO2006000555A3 NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES 审中-公开
标题翻译：新型不饱和四氢呋喃衍生物衍生物
公开(公告)号：WO2006000555A3
公开(公告)日：2006-08-17
申请号：PCT/EP2005052891
申请日：2005-06-21
申请人： JANSSEN PHARMACEUTICA NV , CID-NUNEZ JOSE MARIA , MEGENS ANTONIUS ADRIANUS HENDR , TRABANCO-SUAREZ ANDRES AVELINO
发明人： CID-NUNEZ JOSE MARIA , MEGENS ANTONIUS ADRIANUS HENDR , TRABANCO-SUAREZ ANDRES AVELINO
IPC分类号： C07D493/04 , A61K31/34 , C07D491/04 , C07D495/04 , C07D495/16
CPC分类号： C07D307/935 , C07D303/10 , C07D317/26 , C07D333/80 , C07D335/04 , C07D405/06 , C07D405/12 , C07D491/04 , C07D491/10 , C07D493/04 , C07D495/04 , C07D495/14
摘要： This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT 2A and 5-HT 2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I), and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及对5-羟色胺受体，特别是5-HT 2A和5-HT 2C受体具有结合亲和力的新型取代的不饱和四环四氢呋喃衍生物，特别是多巴胺受体多巴胺D2受体和去甲肾上腺素再摄取抑制性质，包含根据本发明的化合物的药物组合物，其作为药物的用途，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产过程。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式和其前药，其中所有取代基被定义如权利要求1所述。

6. 发明申请

WO2006000555A2 NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES 审中-公开
标题翻译：新型不饱和四氢呋喃衍生物衍生物
公开(公告)号：WO2006000555A2
公开(公告)日：2006-01-05
申请号：PCT/EP2005/052891
申请日：2005-06-21
申请人： JANSSEN PHARMACEUTICA N.V. , CID-NÚÑEZ, José, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino
发明人： CID-NÚÑEZ, José, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino
IPC分类号： C07D307/93
CPC分类号： C07D307/935 , C07D303/10 , C07D317/26 , C07D333/80 , C07D335/04 , C07D405/06 , C07D405/12 , C07D491/04 , C07D491/10 , C07D493/04 , C07D495/04 , C07D495/14
摘要： This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT 2A and 5-HT 2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I), and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N -oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及对5-羟色胺受体具有结合亲和力的新型取代的不饱和四环四氢呋喃衍生物，特别是5-HT

7. 发明申请

WO2013142873A2 COMPLEX AND STRUCTURALLY DIVERSE COMPOUNDS 审中-公开
标题翻译：复杂和结构多样化合物
公开(公告)号：WO2013142873A2
公开(公告)日：2013-09-26
申请号：PCT/US2013033746
申请日：2013-03-25
申请人： HERGENROTHER PAUL J , HUGIENS III ROBERT W , MORRISON KAREN C , HICKLIN II ROBERT W , FLOOD JR TIMOTHY A , UNIV ILLINOIS
发明人： HERGENROTHER PAUL J , HUGIENS III ROBERT W , MORRISON KAREN C , HICKLIN II ROBERT W , FLOOD JR TIMOTHY A
CPC分类号： C07C69/757 , C07B37/06 , C07B37/08 , C07C59/205 , C07C62/32 , C07C62/38 , C07C2601/16 , C07C2602/44 , C07C2603/86 , C07D223/14 , C07D303/10 , C07D307/93 , C07D311/94 , C07D313/06 , C07D313/08 , C07D401/04 , C07D401/14 , C07D405/06 , C07D405/12 , C07D413/06 , C07D471/04 , C07D471/08 , C07D493/08 , C07D513/04 , C07D519/00 , C07J21/008 , C07J69/00 , C07J71/001 , C07J71/0031 , C07J73/005 , C07J73/008 , C07J75/005
摘要： The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
摘要翻译：本发明提供了创造具有高结构和立体化学复杂性的小分子的新颖，一般和简便的策略。方法的方面包括系统应用的环系变形反应，以将易于获得的天然产物快速转化成具有不同分子结构的结构复杂的化合物。通过评估化学性质，包括sp3碳的分数，ClogP和立体中心数，这些化合物显示出比标准筛选收集中显着更复杂和多样化。用三种不同结构类别的天然产物（赤霉酸，肾上腺素和奎宁）证明了这一方法，并且描述了将该策略应用于任何合适的天然产物的方法。

8. 发明申请

WO2012083408A8 ANTI-MALARIA PHARMACEUTICAL COMPOSITIONS CONTAINING KAURENIC DITERPENE DERIVATIVES 审中-公开
标题翻译：含鞣质二萜衍生物的抗疟药物组合物
公开(公告)号：WO2012083408A8
公开(公告)日：2012-12-06
申请号：PCT/BR2011000513
申请日：2011-12-23
申请人： UNIV MINAS GERAIS , OLIVEIRA ALAIDE BRAGA DE , VAROTTI FERNANDO DE PILLA , BATISTA RONAN
发明人： OLIVEIRA ALAIDE BRAGA DE , VAROTTI FERNANDO DE PILLA , BATISTA RONAN
IPC分类号： A61K31/215 , A61K31/336 , A61K31/395 , A61P33/06
CPC分类号： A61K31/215 , A61K31/336 , A61K31/505 , C07D303/10 , C07D493/10
摘要： The present invention describes pharmaceutical compositions containing kaurenic derivatives produced from kaurenoic acid and other diterpenes, as well as the anti-malaria activity of these kaurenic derivatives, which can be used in isolation or in combination for the treatment of malaria.
摘要翻译：本发明描述了含有由kaurenoic酸和其它二萜生产的钙硬脂酸衍生物以及这些kaurenic衍生物的抗疟疾活性的药物组合物，其可以分离或组合用于治疗疟疾。

9. 发明申请

WO2003091189A1 CANNABINOIDS 审中-公开
标题翻译：大麻
公开(公告)号：WO2003091189A1
公开(公告)日：2003-11-06
申请号：PCT/US2002/019569
申请日：2002-06-20
申请人： VIRGINIA COMMONWEALTH UNIVERSITY , MARTIN, Billy, R. , RAZDAN, Raj, K.
发明人： MARTIN, Billy, R. , RAZDAN, Raj, K.
IPC分类号： C07C39/17
CPC分类号： C07D317/72 , C07D303/10 , C07D309/06 , C07D309/22 , C07D333/16 , C07D335/02
摘要： Compounds of the formula: wherein R, R1 and R4 are defined in the specification, and pharmaceutically acceptable salts, esters and tautomers thereof, having activity at peripheral cannabinoid receptors, commonly designated the CB2 receptor class. The compounds are useful for therapy, especially in the treatment of pain, inflammation and autoimmune disease.
摘要翻译：其中R，R 1和R 4在本说明书中定义的化合物及其药学上可接受的盐，酯和互变异构体，其外周大麻素受体具有活性，通常称为CB2受体类。这些化合物可用于治疗，特别是治疗疼痛，炎症和自身免疫性疾病。

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