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1. 发明授权

US09789096B2 Methods and compositions for selective and targeted cancer therapy 有权
公开(公告)号：US09789096B2
公开(公告)日：2017-10-17
申请号：US14916644
申请日：2014-09-04
申请人： Board of Regents of the University of Texas System
发明人： Joseph M. Ready , Deepak Nijhawan , Stephen S. Gonzales , Pano Theodoropoulos
IPC分类号： A61K31/428 , A61K31/426 , C07C235/88 , C07D333/70 , C07D409/12 , C07D417/12 , C07D513/04 , C12N9/99 , A61K31/381 , C07D405/14 , C07D213/75 , C07D215/48 , C07D217/02 , C07D405/12 , C07D409/14 , C07D239/90 , C07D417/14 , C07D209/08 , C07D277/82 , C07D209/44 , C07C271/44 , C07C271/46 , C07C271/48 , C07C275/24 , C07C275/30 , C07C275/54 , C07C233/56 , C07C233/73 , C07C235/38 , C07C235/56 , C07C235/66 , C07C235/70 , C07C237/08
CPC分类号： A61K31/426 , A61K31/381 , A61K31/428 , C07C233/56 , C07C233/73 , C07C235/38 , C07C235/56 , C07C235/66 , C07C235/70 , C07C235/88 , C07C237/08 , C07C271/44 , C07C271/46 , C07C271/48 , C07C275/24 , C07C275/30 , C07C275/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/26 , C07D209/08 , C07D209/44 , C07D213/75 , C07D215/48 , C07D217/02 , C07D239/90 , C07D277/82 , C07D333/70 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04 , C12N9/99
摘要： Provided herein are methods and compositions for selective and targeted cancer therapy, in particular certain benzothiophenes, benzothiazoles, oxalamides, N-acyl ureas and chromones, and their use in selectively treating certain adenocarcinomas. In some embodiments, the selective toxicity of the compounds may be mediated through SCD1 and/or CYP450 such as CYP4F11.

2. 发明授权

US09714238B2 Therapeutic agents for ocular hypertension 有权
公开(公告)号：US09714238B2
公开(公告)日：2017-07-25
申请号：US14136089
申请日：2013-12-20
申请人： Allergan, Inc.
发明人： David W. Old
IPC分类号： C07D409/12 , C07C235/78 , C07D333/24 , C07D215/14 , C07C233/75 , C07C235/66
CPC分类号： C07D409/12 , C07C233/75 , C07C235/66 , C07C235/78 , C07D215/14 , C07D333/24
摘要： This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.

3. 发明授权

US09309187B2 EP2 receptor agonists 有权
标题翻译： EP2受体激动剂
公开(公告)号：US09309187B2
公开(公告)日：2016-04-12
申请号：US14397319
申请日：2013-04-30
申请人： TAKEDA GMBH
发明人： Angelika Hoffmeyer , Rainer Boer , Manuela Hessmann , Andreas Pahl , Torsten Dunkern , Simone Hartung , Christof Zitt , Jurgen Volz , Christiane Praechter , Mahindra Makhija , Hiteshkumar Jain , Sandip Gavade , Arati Prabhu , Manojkumar Tiwari , Ashish Keche , Sarvesh Patel
IPC分类号： C07D265/30 , C07C233/81 , C07C233/75 , C07C235/66 , C07C237/40 , C07C237/42 , C07D295/155 , A61K31/196 , A61K31/27 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C237/52 , C07C271/42
CPC分类号： C07C233/81 , A61K31/196 , A61K31/27 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/75 , C07C235/66 , C07C237/40 , C07C237/42 , C07C237/52 , C07C271/42 , C07D295/155
摘要： The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
摘要翻译：其中R1，R4，A和X具有说明书中给出的含义的式（1）化合物是新型有效的EP2激动剂。

4. 发明申请

US20140221411A1 2-HYDROXYARYLAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER CONTAINING SAME AS ACTIVE INGREDIENT 有权
标题翻译： 2-羟基胺衍生物或药物可接受的盐，其制备方法和用于预防或治疗含有作为活性成分的癌症的药物组合物
公开(公告)号：US20140221411A1
公开(公告)日：2014-08-07
申请号：US14256808
申请日：2014-04-18
申请人： Korea Research Institute of Bioscience and Biotechnology
发明人： Semi KIM , Ill Young LEE , Hye-Jin MIN , Eun-Hee NAM , Pilho KIM , Chang Soo YUN , Dong Joon KO
IPC分类号： C07C235/64 , C07D215/38 , C07D285/135 , C07D213/75 , C07D417/04 , C07D277/46 , C07D213/82 , C07D215/56 , C07D277/82 , C07C235/66 , C07D239/42
CPC分类号： C07D417/04 , A61K31/167 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/4709 , A61K31/505 , A61K31/5377 , C07D213/75 , C07D213/82 , C07D215/38 , C07D215/56 , C07D239/42 , C07D277/46 , C07D277/82 , C07D285/135
摘要： The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.
摘要翻译：本发明涉及2-羟基芳基酰胺衍生物或其药学上可接受的盐，其制备方法和用于预防或治疗癌症的药物组合物，其包含其作为活性成分。通过本发明制备的2-羟基芳基酰胺衍生物对TMPRSS4丝氨酸蛋白酶的活性的抑制和TMPRSS4表达的癌细胞的浸润的抑制是优异的，因此可以用作通过抑制来预防或治疗癌症的组合物 TMPRSS4在癌细胞，特别是结肠直肠癌，肺癌，乳腺癌，前列腺癌，卵巢癌，胰腺癌或胃癌细胞中过度表达。

5. 发明申请

US20110301179A1 NAPHTHAMIDES AS ANTICANCER AGENTS 失效
标题翻译：萘烷作为反应剂
公开(公告)号：US20110301179A1
公开(公告)日：2011-12-08
申请号：US13125289
申请日：2009-10-21
申请人： Xiangshu Xiao , Bingbing Li
发明人： Xiangshu Xiao , Bingbing Li
IPC分类号： A61K31/4965 , C07C69/773 , C07C229/66 , C07C235/66 , C07D213/74 , A61P35/02 , A61K31/167 , A61K31/24 , A61K31/4402 , A61K31/4409 , A61P35/00 , C07C237/48 , C07D241/20
CPC分类号： C07D213/75 , C07C235/66 , C07C237/40 , C07D241/20
摘要： A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.
摘要翻译：根据式I的化合物（特别可用于抑制癌症）或其药学上可接受的盐，其中：x为0或1; R 1 -R 6各自独立地为H，-CN，-NO 2，-NO，-OH，卤素，羟基烷基，羧基，取代的羧基，氨基羰基，烷氧基，羰基或取代的羰基; R7是H，烷基，烷基氨基，氨基酰基，羟基酰基，杂芳基，杂环烷基，烷基杂芳基或烷基杂环烷基; R8是H或烷基; A是O或N; 并且Ar是芳基，取代的芳基，杂芳基或取代的杂芳基，条件是如果R 7为H，则Ar为被烷基氨基取代的芳基。

7. 发明授权

US06891072B2 Process for production of dimers or aromatic monohydroxyl compounds 失效
标题翻译：二聚体或芳族单羟基化合物的制备方法
公开(公告)号：US06891072B2
公开(公告)日：2005-05-10
申请号：US10433908
申请日：2002-04-18
申请人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori , Hikari Hirai
发明人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori , Hikari Hirai
IPC分类号： C07B61/00 , C07C37/11 , C07C39/14 , C07C45/39 , C07C46/08 , C07C49/653 , C07C67/343 , C07C69/94 , C07C231/12 , C07C235/66 , C07C273/18 , C07C275/54 , C07D307/52 , C07C39/12
CPC分类号： C07D307/52 , C07C37/11 , C07C46/08 , C07C67/343 , C07C231/12 , C07C273/1854 , C07C2603/50 , C07C50/10 , C07C50/08 , C07C69/94 , C07C235/66 , C07C275/54 , C07C39/14
摘要： The present invention provides a method for preparing dimer of a monohydroxy aromatic compound. In the method of the present invention, oxidative coupling reaction of a monohydroxy aromatic compound represented by formula [I]: Ar—OH [I] wherein Ar represents an optionally substituted aromatic group is carried out in a nitrogen containing polar solvent in the presence of a copper salt. By the method of the instant invention, dimer of the monohydroxy aromatic compound can be obtained in high yield.
摘要翻译：本发明提供一种制备单羟基芳族化合物的二聚体的方法。在本发明的方法中，由式[I]表示的单羟基芳族化合物的氧化偶联反应：<？in-line-formula description =“In-line Formulas”end =“lead”→Ar-OH [I ]其中Ar表示可以具有取代基的芳族基团，在含铜极性溶剂中，在铜盐存在下进行。通过本发明的方法，可以高产率获得单羟基芳族化合物的二聚体。

8. 发明授权

US06849742B2 Binaphthol derivative and process for producing the same 失效
标题翻译：联萘酚衍生物及其制备方法
公开(公告)号：US06849742B2
公开(公告)日：2005-02-01
申请号：US10250442
申请日：2002-04-18
申请人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori
发明人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori
IPC分类号： C07B57/00 , C07B61/00 , C07C51/09 , C07C51/353 , C07C51/367 , C07C51/60 , C07C65/11 , C07C65/24 , C07C67/31 , C07C67/343 , C07C69/94 , C07C231/12 , C07C235/66 , C07C273/18 , C07C275/54 , C07D263/56 , C07D263/57 , C07D263/62 , C07D263/64 , C07D277/66 , C07D307/52 , C07D277/62
CPC分类号： C07D263/57 , C07B2200/07 , C07C51/09 , C07C51/367 , C07C51/60 , C07C65/11 , C07C65/24 , C07C67/31 , C07C67/343 , C07C69/94 , C07C235/66 , C07C2603/50 , C07D263/64 , C07D277/66 , C07D307/52
摘要： The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.
摘要翻译：本发明提供由式[1]表示的联萘酚化合物及其盐。本发明的联萘酚化合物可用于制备防腐化合物或手性催化剂。根据本发明的方法，可以低成本高收率制备联萘酚化合物。

9. 发明申请

US20030187301A1 Process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine 有权
标题翻译：制备5,6-二乙基-2,3-二氢-1H-茚-2-胺的方法
公开(公告)号：US20030187301A1
公开(公告)日：2003-10-02
申请号：US10367402
申请日：2003-02-14
发明人： Mahavir Prashad , Bin Hu , Olivier Lohse
IPC分类号： C07C235/66
CPC分类号： C07C209/62 , C07C211/42 , C07C233/06 , C07C233/32 , C07C233/33 , C07C2602/08
摘要： A process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine and acid addition salts thereof from 2-aminoindan. The process comprises protecting the amino group of 2-aminoindan, acetylating the ring in the protected compound, reducing the acetyl group to ethyl to form a monoethyl derivative, acetylating the monoethyl derivative, reducing the acetyl group to form a diethyl derivative, deprotecting the latter by hydrolysis and recovering the product in free or salt form. The process does not use deleterious Grignard reagents or nitrites such as isoamyl nitrite, and provides high regioselectivity and high yield of 5,6-diethyl-2,3-dihydro-1H-inden-2-amine. In addition, the process uses acetyl halide as both a reactant and a solvent.
摘要翻译：从2-氨基茚满制备5,6-二乙基-2,3-二氢-1H-茚-2-胺及其酸加成盐的方法。该方法包括保护2-氨基茚满的氨基，乙酰化保护的化合物中的环，将乙酰基还原为乙基以形成单乙基衍生物，乙酰化单乙基衍生物，还原乙酰基以形成二乙基衍生物，使后者脱保护通过水解并以游离或盐形式回收产物。该方法不使用有害的格氏试剂或亚硝酸盐，例如亚硝酸异戊酯，并且提供高的区域选择性和高收率的5,6-二乙基-2,3-二氢-1H-茚-2-胺。此外，该方法使用乙酰卤作为反应物和溶剂。

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