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1. 发明授权

US09539287B2 Triterpenoids and compositions containing the same 有权
标题翻译：三萜类化合物和含有它们的组合物
公开(公告)号：US09539287B2
公开(公告)日：2017-01-10
申请号：US14496488
申请日：2014-09-25
申请人： Trustees of Dartmouth College
发明人： Gordon W. Gribble , Liangfeng Fu , Michael B. Sporn , Karen T. Liby
IPC分类号： A61K31/56 , C07J63/00 , A61K35/44 , C07C61/29 , C07C62/38 , C07C229/50 , C07C235/78 , C07C255/47 , C07C291/10 , C07C317/44 , C07C323/55 , A61K35/12 , C07C62/32 , C07J71/00
CPC分类号： A61K35/44 , A61K31/56 , A61K35/12 , C07C61/29 , C07C62/32 , C07C62/38 , C07C229/50 , C07C235/78 , C07C255/47 , C07C291/10 , C07C317/44 , C07C323/55 , C07C2603/52 , C07J63/008 , C07J71/0005
摘要： The present invention provides triterpenoids produced from natural compounds such as oleanolic acid, ursolic acid, betulinic acid, and hederagenin.
摘要翻译：本发明提供由天然化合物如齐墩果酸，熊果酸，桦木酸和雌雄agen素生产的三萜类化合物。

2. 发明授权

US08669367B2 Method for producing 2-azaadamantane 有权
标题翻译： 2-氮杂金刚烷的制备方法
公开(公告)号：US08669367B2
公开(公告)日：2014-03-11
申请号：US13585592
申请日：2012-08-14
申请人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
发明人： Toshimasa Hamada , Noriaki Nagahama , Masami Kozawa , Yoshiharu Iwabuchi , Masatoshi Shibuya , Masaki Tomizawa , Yusuke Sasano
IPC分类号： C07D451/14 , C07C61/29 , C07C211/41 , C07C247/00 , C07C271/24
CPC分类号： C07D451/14
摘要： To provide a method whereby a 2-azaadamantane can easily be obtained in good yield.A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.
摘要翻译：提供可以容易地以良好的产率获得2-氮杂金刚烷的方法。一种制备由式（1）表示的2-氮杂金刚烷的方法，其包括在酸存在下环化下式（2）表示的化合物。

3. 发明申请

US20130011421A1 TRITERPENE SAPONINS, METHODS OF SYNTHESIS, AND USES THEREOF 有权
标题翻译：三萜皂苷，合成方法及其用途
公开(公告)号：US20130011421A1
公开(公告)日：2013-01-10
申请号：US13613312
申请日：2012-09-13
申请人： David Gin , Michelle Adams , Kai Deng , Nicholas Perl , Annie Won , Philip Livingston , Govind Ragupathi
发明人： David Gin , Michelle Adams , Kai Deng , Nicholas Perl , Annie Won , Philip Livingston , Govind Ragupathi
IPC分类号： A61K39/39 , C07H23/00 , A61P37/04 , C07H15/18 , C07C61/29 , C07H15/256 , A61K39/00
CPC分类号： C07H15/256 , A61K31/7024 , A61K31/704 , A61K39/385 , C07H13/08 , C07H15/24
摘要： The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
摘要翻译：本发明涉及三萜糖苷皂苷衍生的佐剂，其合成，其中间体及其用途。 QS-7是一种有效的免疫佐剂，其毒性明显低于QS-21，相关的皂苷是目前抗癌和抗病毒疫苗中有利的佐剂。繁琐的分离和纯化方案阻碍了QS-7的临床发展。提供了一种新的半合成方法，其中使用水解的前配皂素混合物合成QS-7，QS-21及相关类似物，极大地方便了QS-7和QS-21类似物的临床前和临床评估。

4. 发明申请

US20110190388A1 URSOLIC ACID DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF 有权
标题翻译：尿酸衍生物和药物组合物
公开(公告)号：US20110190388A1
公开(公告)日：2011-08-04
申请号：US12782395
申请日：2010-05-18
申请人： Chun-Nan Lin , Huang-Yao Tu , A-Mei Huang , Bai-Luh Wei , Kim-Hong Gan , Tzyh-Chyuan Hour , Shyh-Chyun Yang , Yeong-Shiau Pu , Shen-Jeu Won
发明人： Chun-Nan Lin , Huang-Yao Tu , A-Mei Huang , Bai-Luh Wei , Kim-Hong Gan , Tzyh-Chyuan Hour , Shyh-Chyun Yang , Yeong-Shiau Pu , Shen-Jeu Won
IPC分类号： A61K31/365 , C07C61/29 , A61K31/19 , A61P35/00 , A61P29/00 , C07C69/757 , A61K31/215 , C07C69/145 , C07C69/533 , C07C69/34 , C07D313/08 , C12N5/02
CPC分类号： A61K31/56 , A61K31/19 , A61K31/215 , A61K31/365 , A61K31/58 , A61K31/585 , C07C61/29 , C07C69/145 , C07C69/34 , C07C69/533 , C07C69/757 , C07D313/08
摘要： Several ursolic acid derivatives and pharmaceutical compositions thereof are provided. The ursolic acid derivatives and the pharmaceutical compositions thereof have at least one of an anticancer and an anti-inflammatory effects. A method for increasing a reactive oxygen species in a cell is also provided. The method comprises a step of providing the cell with a pharmaceutical composition including an ursolic acid derivative.
摘要翻译：提供了几种熊果酸衍生物及其药物组合物。熊果酸衍生物及其药物组合物具有抗癌和抗炎作用中的至少一种。还提供了增加电池中活性氧的方法。该方法包括向细胞提供包含熊果酸衍生物的药物组合物的步骤。

5. 发明申请

US20110105611A1 USE OF MASLINIC ACID FOR THE TREATMENT OF PATHOLOGIES AND THEIR SYMPTOMS THROUGH THE INHIBITION OF COX-2 审中-公开
标题翻译：通过抑制COX-2的方法治疗病理学的主要用途及其症状
公开(公告)号：US20110105611A1
公开(公告)日：2011-05-05
申请号：US12920435
申请日：2009-04-03
申请人： José Prados Osuna , Andrés Garcia-Granados Lopez De Hierro , Andrés Parra Sánchez , Antonio Martínez Rodríguez
发明人： José Prados Osuna , Andrés Garcia-Granados Lopez De Hierro , Andrés Parra Sánchez , Antonio Martínez Rodríguez
IPC分类号： A61K31/19 , C07C61/29 , A61P29/00 , A61P17/00 , A61P19/02 , A61P19/04 , A61P19/00
CPC分类号： A61K31/191 , A61K9/7023
摘要： The invention relates to the use of maslinic acid or natural, synthetic or semi-synthetic maslinic-rich mixtures or of a composition containing said acid for the treatment of pathological processes associated with COX-2 activation, intended, inter alia, for the symptomatic and/or regenerative treatment of arthrosis, rheumatoid arthritis, fibromyalgia, sciatica and other articular disorders that are difficult to diagnose. The invention also relates to the topical administration thereof.
摘要翻译：本发明涉及使用马斯酸或天然的，合成的或半合成富马酸的混合物或含有所述酸的组合物用于治疗与COX-2活化相关的病理过程的用途，其特别用于症状和 /或再生治疗关节病，类风湿关节炎，纤维肌痛，坐骨神经痛等难以诊断的关节疾病。本发明还涉及其局部给药。

6. 发明申请

US20080097117A1 Aralkyltetrahydropyridines, Their Preparation and Pharmaceutical Compositions Containing Them 失效
标题翻译：芳烷基四氢吡啶，它们的制备和含有它们的药物组合物
公开(公告)号：US20080097117A1
公开(公告)日：2008-04-24
申请号：US11958476
申请日：2007-12-18
申请人： Marco BARONI , Bernard BOURRIE , Rosanna CARDAMONE , Pierre CASELLAS
发明人： Marco BARONI , Bernard BOURRIE , Rosanna CARDAMONE , Pierre CASELLAS
IPC分类号： C07C61/29
CPC分类号： C07D401/04 , C07D211/70
摘要： The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; n is an integer from 1 to 5; A represents a partially saturated carbonaceous bi- or tricycle; it also relates to their salts, solvates, N-oxides, the pharmaceutical compositions containing them, a method for their preparation and synthesis intermediates in this method.
摘要翻译：本发明涉及式（I）化合物：其中X表示N或CH; R 1表示氢或卤素原子或CF 3 N 3基团; n为1〜5的整数; A表示部分饱和的碳质二元或三轮车; 它还涉及它们的盐，溶剂合物，N-氧化物，含有它们的药物组合物，其制备方法和该方法中的合成中间体。

7. 发明申请

US20070093552A1 Early insulin secretion stimulator 审中-公开
标题翻译：早期胰岛素分泌刺激剂
公开(公告)号：US20070093552A1
公开(公告)日：2007-04-26
申请号：US10572460
申请日：2004-09-22
申请人： Futoshi Matsuyama , Yutaka Seino , Mitsuo Fukushima , Toshihiro Miura , Takeshi Fujita , Tetsuo Kaneko
发明人： Futoshi Matsuyama , Yutaka Seino , Mitsuo Fukushima , Toshihiro Miura , Takeshi Fujita , Tetsuo Kaneko
IPC分类号： A61K31/20 , C07C61/29
CPC分类号： A61K31/20 , C07J63/008
摘要： The invention provides an early insulin secretion stimulator consisting of corosolic acid, etc. The early insulin secretion stimulator of the invention is capable of rapidly inducing secretion of insulin immediately after meals without inducing secretion of excess insulin in the absence of blood glucose increase.
摘要翻译：本发明提供了由科罗索酸等组成的早期胰岛素分泌刺激剂。本发明的早期胰岛素分泌刺激剂能够在饭后立即迅速诱导胰岛素分泌，而不会在没有血糖升高的情况下诱导分泌过量的胰岛素。

8. 发明授权

US6083982A Natriuretic compounds 失效
标题翻译：利尿钠化合物
公开(公告)号：US6083982A
公开(公告)日：2000-07-04
申请号：US57731
申请日：1998-04-09
申请人： William J. Wechter , David E. Murray , Darko Kantoci , Barry H. Levine , Elaine J. Benaksas
发明人： William J. Wechter , David E. Murray , Darko Kantoci , Barry H. Levine , Elaine J. Benaksas
IPC分类号： C07D333/58 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/39 , A61P7/10 , B01J31/02 , C07B61/00 , C07C51/09 , C07C59/52 , C07C59/84 , C07C59/90 , C07C61/29 , C07C61/39 , C07C61/40 , C07C62/32 , C07C62/34 , C07C67/343 , C07C69/732 , C07C69/738 , C07C69/76 , C07C211/26 , C07C211/29 , C07C211/34 , C07C211/37 , C07C211/44 , C07C231/24 , C07C233/11 , C07C235/32 , C07C235/78 , C07C317/32 , C07C317/44 , C07D307/33 , C07D311/58 , C07D311/72 , C07D333/60 , C07D333/64 , C07D335/06 , C07D337/08 , C07D337/16 , C07D493/04 , G11C11/407 , G11C16/02 , G11C29/14 , A61K31/215 , A61K31/19 , A61K31/235
CPC分类号： C07D307/33 , A61K31/353 , A61K31/365 , C07C59/90 , C07C69/732 , C07C69/738 , C07D311/72 , C07D493/04
摘要： Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.
摘要翻译：化合物，方法和组合物用于在哺乳动物中诱导利尿。还提供了分离和合成利尿钠化合物的方法。还提供了使用利尿钠化合物的治疗方法。利钠化合物能够在哺乳动物中诱导钠排泄，而不引起相应的延长的钾排泄。

9. 发明授权

US4720504A Use of bis-platinum complexes as antitumor agents 失效
标题翻译：使用双铂配合物作为抗肿瘤剂
公开(公告)号：US4720504A
公开(公告)日：1988-01-19
申请号：US819967
申请日：1986-01-21
申请人： Peter J. Andrulis, Jr. , Paul Schwartz
发明人： Peter J. Andrulis, Jr. , Paul Schwartz
IPC分类号： C07C51/41 , C07C61/04 , C07C61/08 , C07C61/29 , C07C63/313 , C07C63/40 , C07C65/03 , C07C65/05 , C07F15/00 , A61K31/28
CPC分类号： C07F15/0093 , C07C51/418 , C07C61/04 , C07C61/08 , C07C61/29 , C07C63/313 , C07C63/40 , C07C65/03 , C07C65/05
摘要： Bis-platinum complexes having the formula ##STR1## wherein A is a ligand having two pairs of platinum-coordinating acidic groups which are each independently a carboxylate, phenolate, sulfonate or phosphonate group, each said pair being capable of coordinating with a platinum ion to form a 5-10 membered chelate ring; Z is a water-solubilizing group; n is 0 or a positive integer, with the proviso that n is 0 only when at least one of said platinum-coordinating acidic groups is sulfonate or phosphonate or when at least one platinum ion is a Pt(IV) ion; and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently H or a C.sub.1-20 alkyl, aryl, aralkyl, or alkaryl group, or together form one or more C.sub.1-30 alkylene, cycloalkylene, arylene, aralkylene or alkarylene groups; or a pharmaceutically acceptable salt thereof, are used as readily water-soluble antitumor agents in antitumor therapy against tumors susceptible to treatment with a platinum complex.
摘要翻译：具有式的双铂络合物，其中A是具有两对铂配位酸性基团的配体，其各自独立地为羧酸酯，酚盐，磺酸酯或膦酸酯基团，每个所述对能够与铂离子配位，形成5-10元螯合环; Z是水溶性基团; n为0或正整数，条件是仅当所述铂配位的酸性基团中的至少一个为磺酸盐或膦酸盐时或当至少一个铂离子为Pt（IV）离子时n为0; 并且R 1，R 2，R 3，R 4，R 5和R 6各自独立地为H或C 1-20烷基，芳基，芳烷基或烷芳基，或一起形成一个或多个C 1-30亚烷基，亚环烷基，亚芳基，亚芳基或亚烷基 ; 或其药学上可接受的盐作为容易水解的抗肿瘤剂用于针对易于用铂络合物治疗的肿瘤的抗肿瘤治疗。

10. 发明授权

US4289852A Process for producing novel bicyclodecadiene compounds 失效
标题翻译：生产新型双环癸二烯化合物的方法
公开(公告)号：US4289852A
公开(公告)日：1981-09-15
申请号：US98894
申请日：1979-11-29
申请人： Shingo Marumo , Masato Katayama
发明人： Shingo Marumo , Masato Katayama
IPC分类号： C07C47/445 , C07C51/00 , C07C61/29 , C07C67/00 , C07G11/00 , C12P1/02 , C12P7/24 , C12P7/40 , C12R1/645
CPC分类号： C12P7/40 , C07C47/445 , C07C61/29 , C12P7/24 , Y10S435/911
摘要： 5-Isopropyl-8-methyl bicyclo[5.3.0]deca-2,8-diene-2-carboxylic acid having a chemical structure represented by the following formula: ##STR1## and 5-isopropyl-8-methyl bicyclo[5.3.0]deca-2,8-diene-2-carboaldehyde having a chemical structure represented by the following formula: ##STR2## can be obtained by cultivating a microbial strain belonging to Genus Sclerotinia and having an ability to produce them, and collecting them from the cultivated mixture.
摘要翻译：具有由下式表示的化学结构的5-异丙基-8-甲基双环[5.3.0]癸-2,8-二烯-2-羧酸：5-异丙基-8-甲基双环[5.3。 0]癸-2,8-二烯-2-甲醛，其具有由下式表示的化学结构：可以通过培养属于核盘菌属的微生物菌株并具有产生它们的能力，并从栽培的混合物。

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