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1. 发明授权

US09266853B2 Orally available viridiofungin derivative possessing anti-HCV activity 有权
标题翻译：具有抗HCV活性的口服有效的维生素E衍生物
公开(公告)号：US09266853B2
公开(公告)日：2016-02-23
申请号：US14421577
申请日：2013-08-16
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： Yasunori Kohchi , Kimitaka Nakama , Susumu Komiyama , Fumio Watanabe
IPC分类号： C07D293/00 , C07D317/00 , C07D317/36 , C07D293/06 , C07D317/34 , C07D317/40 , C07C235/28 , A61K31/192 , A61K31/357 , C07C235/74
CPC分类号： C07D317/36 , A61K31/192 , A61K31/357 , C07C235/28 , C07C235/74 , C07C2601/16 , C07D293/06 , C07D317/34 , C07D317/40
摘要： An object of the present invention is to provide a compound that is useful as an orally available anti-HCV agent. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. This compound has an anti-HCV activity and is useful as a medicine.
摘要翻译：本发明的目的是提供可用作口服抗HCV药剂的化合物。本发明涉及由式（1）表示的化合物或其药学上可接受的盐。该化合物具有抗HCV活性，可用作药物。

2. 发明授权

US09051259B2 Process for producing perfluorinated organic compounds 有权
标题翻译：生产全氟化有机化合物的方法
公开(公告)号：US09051259B2
公开(公告)日：2015-06-09
申请号：US13885867
申请日：2011-11-17
申请人： Vito Tortelli , Marco Galimberti
发明人： Vito Tortelli , Marco Galimberti
IPC分类号： C07D317/00 , C07C205/00 , C07C67/287 , C07D317/34 , C07D317/14 , C07C51/60 , C07C67/14 , C07D317/42 , C07C51/58
CPC分类号： C07C67/287 , C07C51/58 , C07C51/60 , C07C67/14 , C07C2601/14 , C07D317/14 , C07D317/34 , C07D317/42 , C07C69/63 , C07C53/50
摘要： A process for producing a perfluorinated functional compound comprises the steps of: A) converting an at least partially hydrogenated alcohol into an at least partially hydrogenated ester compound; and B) reacting said at least partially hydrogenated ester compound with fluorine in the presence of at least one (per)haloolefin comprising at least one carbon-carbon double bond and having at least one fluorine or chlorine atom on either one of the carbon atoms of said double bond, to obtain a perfluorinated ester compound.
摘要翻译：一种制备全氟化官能化合物的方法包括以下步骤：A）将至少部分氢化的醇转化成至少部分氢化的酯化合物; 和B）在至少一种包含至少一个碳 - 碳双键的卤代烯烃存在下使所述至少部分氢化的酯化合物与氟反应，并且在至少一个碳 - 碳双键的碳原子上具有至少一个氟或氯原子所述双键，以获得全氟化酯化合物。

3. 发明授权

US09018403B2 Method for producing tetrahydropyran compound and intermediate thereof 有权
标题翻译：四氢吡喃化合物及其中间体的制备方法
公开(公告)号：US09018403B2
公开(公告)日：2015-04-28
申请号：US14282584
申请日：2014-05-20
申请人： Nissan Chemical Industries, Ltd.
发明人： Hirotaka Kawanami , Kana Yamaguchi , Shota Murase
IPC分类号： C07D317/00 , C07H9/04 , C07D317/72
CPC分类号： C07H9/04 , C07D317/20 , C07D317/72 , C07D409/06 , C07D493/04
摘要： Disclosed is a method for producing a tetrahydropyran compound represented by general formula (5) shown in the scheme. Accordingly, a tetrahydropyran derivative is obtained in high yield and with high selectivity without using a highly toxic reagent, and an industrially useful method for producing a tetrahydropyran derivative and an intermediate thereof can be provided. In formulae (1) to (5), R1 and R2 each independently represent a hydrogen atom, a linear, branched, or cyclic alkyl group, or an aromatic group which may have a substituent, and R1 and R2 may be combined to form an alkylene group, thereby forming a ring; and R3 and R4 each independently represent a hydrogen atom or a linear, branched, or cyclic alkyl group, and R3 and R4 may be combined to form an alkylene group, thereby forming a ring.
摘要翻译：公开了一种制备方案中所示的由通式（5）表示的四氢吡喃化合物的方法。因此，可以高收率，高选择性地得到四氢吡喃衍生物，而不使用高毒性试剂，可以提供工业上有用的四氢吡喃衍生物及其中间体的制造方法。式（1）〜（5）中，R 1和R 2各自独立地表示氢原子，直链状，支链状或环状的烷基或可以具有取代基的芳香族基团，R1和R2可以组合形成亚烷基，从而形成环; R 3和R 4各自独立地表示氢原子或直链状，支链状或环状的烷基，可以将R 3和R 4结合形成亚烷基，形成环。

4. 发明授权

US08835659B2 Polysubstituted benzofurans and medicinal applications thereof 有权
标题翻译：多取代苯并呋喃及其药用
公开(公告)号：US08835659B2
公开(公告)日：2014-09-16
申请号：US13695971
申请日：2011-05-10
申请人： Fernando Pedro Cossio Mora , Leire Lidia Arias Echeverría , Yosu Ion Vara Zalazar , Eneko Aldaba Arévalo , Eider San Sebastián Larzabal , Aizpea Zubia Olascoaga
发明人： Fernando Pedro Cossio Mora , Leire Lidia Arias Echeverría , Yosu Ion Vara Zalazar , Eneko Aldaba Arévalo , Eider San Sebastián Larzabal , Aizpea Zubia Olascoaga
IPC分类号： C07D307/00 , C07D307/87 , C07D307/93 , C07D317/00 , C07D323/02 , A01N43/08 , A61K31/34 , C07D307/81 , C07D307/82 , C07D307/92 , C07D405/04 , C07D407/04 , C07D307/79 , C07D307/80
CPC分类号： C07D307/80 , C07D307/79 , C07D307/81 , C07D307/82 , C07D307/92 , C07D405/04 , C07D407/04
摘要： The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.
摘要翻译：本发明涉及式（I）化合物：以及其制备方法，包含其的药物组合物及其用于治疗和/或化学预防癌症，老化相关疾病或过程的用途，糖尿病和神经变性疾病

5. 发明授权

US08697881B2 Method for producing alcohol compound 有权
标题翻译：醇化合物的制备方法
公开(公告)号：US08697881B2
公开(公告)日：2014-04-15
申请号：US13126390
申请日：2008-12-11
申请人： Hideo Shimizu
发明人： Hideo Shimizu
IPC分类号： C07D211/70 , C07D211/82 , C07D213/46 , C07D307/00 , C07D317/00 , C07D323/02 , B01J31/00
CPC分类号： C07D307/42 , C07C29/141 , C07D307/44 , C07C33/14 , C07C33/30 , C07C33/22
摘要： Disclosed is a practical method for efficiently producing an alcohol compound by hydrogenating an aldehyde by using a homogeneous copper catalyst which is an easily-available low-cost metal species. Specifically disclosed is a method for producing an alcohol compound, which is characterized in that a hydrogenation reaction of an aldehyde compound is performed in the presence of a homogeneous copper catalyst, a monophosphine compound and an alcohol selected from the group consisting of primary alcohols, secondary alcohols and mixtures of those.
摘要翻译：公开了通过使用易于获得的低成本金属种类的均匀铜催化剂氢化醛来有效生产醇化合物的实用方法。具体公开了一种醇化合物的制造方法，其特征在于，在均匀的铜催化剂，单膦化合物和选自伯醇，二次碳酸酯的醇的存在下，进行醛化合物的氢化反应醇和它们的混合物。

6. 发明授权

US08680303B2 Epoxidation catalysts 有权
标题翻译：环氧催化剂
公开(公告)号：US08680303B2
公开(公告)日：2014-03-25
申请号：US13037060
申请日：2011-02-28
申请人： Timothy F. Jamison , Yutaka Ikeuchi
发明人： Timothy F. Jamison , Yutaka Ikeuchi
IPC分类号： C07D317/00
CPC分类号： C07F7/1804 , C07D317/20 , C07D317/26 , C07D493/20
摘要： The present invention generally relates to methods for the synthesis of catalysts, including epoxidation catalysts, and related compounds and catalyst compositions. Embodiments described herein may provide efficient processes for providing catalysts (e.g., epoxidation catalysts) in large quantities and using simplified methods.
摘要翻译：本发明一般涉及合成催化剂的方法，包括环氧化催化剂以及相关化合物和催化剂组合物。本文描述的实施方案可以提供大量提供催化剂（例如环氧化催化剂）和使用简化方法的有效方法。

7. 发明授权

US07671088B2 Water-soluble etoposide analogs and methods of use thereof 失效
标题翻译：水溶性依托泊苷类似物及其使用方法
公开(公告)号：US07671088B2
公开(公告)日：2010-03-02
申请号：US11619304
申请日：2007-01-03
申请人： Kuo-Hsiung Lee , Zhiyan Xiao , Kenneth F. Bastow
发明人： Kuo-Hsiung Lee , Zhiyan Xiao , Kenneth F. Bastow
IPC分类号： A01N43/26 , A01N43/00 , A01N43/04 , A61K31/335 , A61K31/33 , C07D307/77 , C07D307/00 , C07D317/00 , C07D323/02
CPC分类号： C07D493/04 , C07D497/04
摘要： Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
摘要翻译：具有改善的水溶性的依托泊苷类似物，例如4'-O-脱甲基-4' - （N'，N'-二甲基甘氨酰）-4＆bgr-（4“ - 硝基苯胺基）-4-脱氧鬼臼毒素（8）和描述了4'-O-脱甲基-4' - （N'，N'-二甲基甘氨酰基）-4＆bgr-（4“ - 氟苯胺基）-4-脱氧鬼臼毒素（9），以及含有它们的药物制剂，其使用方法和中间体及其制备方法。

8. 发明申请

US20070259948A1 Compounds with antifungal properties and process thereof 审中-公开
标题翻译：具有抗真菌性质的化合物及其制备方法
公开(公告)号：US20070259948A1
公开(公告)日：2007-11-08
申请号：US11498805
申请日：2006-08-04
申请人： Mukund Keshav Gurjar , Radhika Dilip Wakharkar , Hanumant Bapurao Borate , Ramesh Ganesh Kelkar , Andiappan Murugan , Mohan Anand Chandavarkar , Shreerang Vidyadhar Joshi , Sharangi Ravindra Vaiude
发明人： Mukund Keshav Gurjar , Radhika Dilip Wakharkar , Hanumant Bapurao Borate , Ramesh Ganesh Kelkar , Andiappan Murugan , Mohan Anand Chandavarkar , Shreerang Vidyadhar Joshi , Sharangi Ravindra Vaiude
IPC分类号： A61K31/381 , A61K31/341 , C07D307/26 , C07D317/00 , C07D409/02
CPC分类号： C07D307/58 , C07D317/30 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (1) wherein R is substituted alkyl, alkenyl, aryl, heteroaryl, 2-thienyl, 3-thienyl, halothienyl, haloalkyl, halophenyl, or pyrrolyl; and R1 and R2, each independent of the other, are hydrogen, halogen, or alkoxy. The invention also relates to a process for the preparation of said compounds by contacting the intermediate alcohol, prepared from 1,2-O-isopropylideneglyceraldehyde and substituted phenylacetates, with acid chlorides under appropriate conditions to obtain some of the preferred compounds of the invention.
摘要翻译：本发明涉及具有抗真菌活性的式（1）化合物，其溶剂合物和药学上可接受的盐，其药物组合物包含有效量的式（1）化合物，其中R是取代的烷基，烯基，芳基，杂芳基，噻吩基，3-噻吩基，卤代噻吩基，卤代烷基，卤代苯基或吡咯基; 和R 1和R 2各自独立地是氢，卤素或烷氧基。本发明还涉及一种制备所述化合物的方法，该方法是在适当的条件下使由1,2-碘异丙基甘油醛和取代的苯乙酸酯制备的中间体醇与酰氯接触，以获得本发明的一些优选化合物。

9. 发明授权

US06924276B2 Diacid-substituted heteroaryl derivatives as matrix metalloproteinase inhibitors 失效
标题翻译：二酸取代的杂芳基衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US06924276B2
公开(公告)日：2005-08-02
申请号：US10224234
申请日：2002-08-20
申请人： Roderick Joseph Sorenson
发明人： Roderick Joseph Sorenson
IPC分类号： C07D333/38 , A61K31/381 , A61K31/4025 , A61K31/426 , A61K31/427 , A61K31/433 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/06 , A61P13/12 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D277/20 , C07D277/34 , C07D277/56 , C07D285/135 , C07D333/40 , C07D333/70 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , A61K31/33 , C07D317/00 , C07D331/00 , C07D333/00
CPC分类号： C07D417/12 , C07D277/34 , C07D277/56 , C07D333/70
摘要： The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formula G1-(C(R1)R2)n-Q1-B-Q2-(C(R3)R4)m-G2 I or a pharmaceutically acceptable salt thereof, wherein G1, G2, R1, R2, R3, R4, n, m, Q1, Q2, and B are as defined in the specification. The invention compounds are inhibitors of matrix metalloproteinase enzymes, including MMP-13. This invention also provides pharmaceutical compositions and methods of treating diseases mediated by MMP-13, including arthritis, asthma, heart disease, atherosclerosis, and osteoporosis, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了二元羧酸取代的式？的杂芳基衍生物，其中：式（Ⅳ）式中的（C（R）SUB （1）R 2 - （C（R（R 1）2） R 3 -Q 2 -I-in-line-formula description =“In-line-formula”=“In- 或其药学上可接受的盐，其中G 1，G 2，R 1，R 2， R 2，R 3，R 4，N，m，Q 1，Q 2， >和B如说明书中所定义。本发明化合物是MMP-13基质金属蛋白酶抑制剂。本发明还提供了治疗由MMP-13介导的疾病，包括关节炎，哮喘，心脏病，动脉粥样硬化和骨质疏松症或其药学上可接受的盐的药物组合物和方法。

10. 发明授权

US6077850A Substituted benzopyran analogs for the treatment of inflammation 有权
公开(公告)号：US6077850A
公开(公告)日：2000-06-20
申请号：US175584
申请日：1998-10-20
申请人： Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J. Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
发明人： Jeffery S Carter , Mark G Obukowicz , Balekudru Devadas , John J Talley , David L Brown , Matthew J Graneto , Stephen R Bertenshaw , Donald J Rogier, Jr. , Srinivasan Raj Nagarajan , Cathleen E Hanau , Susan J. Hartmann , Cindy L Ludwig , Suzanne Metz , Donald E Korte
IPC分类号： C07D335/06 , A61K20060101 , A61K31/35 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/4184 , A61K31/443 , A61K31/4433 , A61K31/453 , A61K31/47 , A61K31/5377 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D215/54 , C07D221/00 , C07D307/00 , C07D311/00 , C07D311/12 , C07D311/22 , C07D311/38 , C07D311/58 , C07D311/92 , C07D317/00 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/052 , C07D493/04 , A61K31/44 , A61K31/495 , C07D215/16 , C07D221/06
CPC分类号： C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D335/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04
摘要： A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.

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