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1. 发明授权

EP2308832B1 9-SUBSTITUTED MINOCYCLINE COMPOUNDS 有权
公开(公告)号：EP2308832B1
公开(公告)日：2018-09-12
申请号：EP10182900.0
申请日：2001-06-29
申请人： Trustees of Tufts College , Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Frechette, Roger , Viski, Peter , Ismail, Mohamed Y , Bowser, Todd , Dumornay, Jimmy , Rennie, Glen , Liu, Gui , Koza, Darrell , Sheahan, Paul , Stapleton, Karen , Hawkins, Paul , Bhatia, Beena , Verma, Atul , McIntyre, Laura , Warchol, Ted
IPC分类号： C07C237/26 , A61K31/65 , A61P31/04 , A61P17/00
CPC分类号： A61K31/65 , C07C237/26 , C07C255/59 , C07C271/22 , C07C271/28 , C07C271/30 , C07C271/58 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C275/50 , C07C275/54 , C07C311/06 , C07C311/21 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07F9/4006 , C07F9/4056 , Y02A50/473 , Y02A50/481
摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

2. 发明授权

EP2208721B1 HISTONE DEACETYLASE INHIBITOR, COMPOSITION AND USE THEREOF 有权
标题翻译：组蛋白去乙酰化酶抑制剂，组成及适当地使用该
公开(公告)号：EP2208721B1
公开(公告)日：2013-12-25
申请号：EP08854528.0
申请日：2008-10-27
申请人： Zhejiang Hisun Pharmaceutical Co. Ltd. , Central South University
发明人： YU, Niefang , LIU, Xiaoyu , HU, Xiaodong
IPC分类号： C07C259/06 , C07C233/51 , A61K31/16 , A61P35/00
CPC分类号： C07C323/63 , C07C259/06 , C07C275/42 , C07C311/07 , C07C335/22 , C07D213/53 , C07D333/20
摘要： The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.

3. 发明公开

EP2308832A1 9-Substituted minocycline compounds 有权
标题翻译： 9-取代的米诺环素化合物
公开(公告)号：EP2308832A1
公开(公告)日：2011-04-13
申请号：EP10182900.0
申请日：2001-06-29
申请人： Trustees Of Tufts College , Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Frechette, Roger , Viski, Peter , Ismail, Mohamed Y , Bowser, Todd , Dumornay, Jimmy , Rennie, Glen , Liu, Gui , Koza, Darrell , Sheahan, Paul , Stapleton, Karen , Hawkins, Paul , Bhatia, Beena , Verma, Atul , McIntyre, Laura , Warchol, Ted
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： A61K31/65 , C07C237/26 , C07C255/59 , C07C271/22 , C07C271/28 , C07C271/30 , C07C271/58 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C275/50 , C07C275/54 , C07C311/06 , C07C311/21 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07F9/4006 , C07F9/4056 , Y02A50/473 , Y02A50/481
摘要： The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
摘要翻译：本发明至少部分涉及新的9-取代的米诺环素化合物。这些米诺环素化合物可用于治疗许多四环素化合物应答状态，例如细菌感染和肿瘤，以及一般的米诺环素和四环素化合物的其它已知应用，例如一般阻断四环素化合物，如阻断四环素外排和基因表达的调节。

4. 发明授权

EP1303503B1 ANILINE DERIVATIVES 有权
标题翻译：苯胺衍
公开(公告)号：EP1303503B1
公开(公告)日：2010-01-27
申请号：EP01969367.0
申请日：2001-07-11
申请人： F. Hoffmann-La Roche AG
发明人： ACKERMANN, Jean , AEBI, Johannes , CHUCHOLOWSKI, Alexander , DEHMLOW, Henrietta , MORAND, Olivier , WALLBAUM, Sabine , WELLER, Thomas
IPC分类号： C07D295/08 , C07C311/21 , C07D211/70 , C07D211/46 , C07C311/29 , C07C275/34 , C07C271/28 , C07C335/18 , A61K31/16 , A61K31/33
CPC分类号： C07D213/75 , C07C233/29 , C07C233/75 , C07C235/56 , C07C235/84 , C07C255/57 , C07C271/28 , C07C271/58 , C07C275/34 , C07C275/38 , C07C307/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C323/44 , C07C335/18 , C07C335/22 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/18 , C07D207/14 , C07D207/20 , C07D209/42 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D213/81 , C07D213/82 , C07D215/36 , C07D239/42 , C07D261/10 , C07D295/088 , C07D307/14 , C07D307/52 , C07D317/58 , C07D319/18 , C07D333/24 , C07D333/34 , C07D333/38
摘要： The present invention relates to compounds of formula (I) and pharmaceutically acceptable salt and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemmia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译：本发明涉及式（I）化合物，其中U，Y，V，W，L，X，A 1，A 2，A 3，A 4，A 5和A <6>如描述和权利要求及其药学上可接受的盐和/或其药学上可接受的酯所定义。该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，寄生虫感染，胆结石，肿瘤和/或过度增殖性疾病相关的疾病，和/或治疗和/或预防糖耐量异常和糖尿病。

5. 发明授权

EP0977741B1 SUBSTITUTED PHENYL DERIVATIVES, THEIR PREPARATION AND USE 失效
标题翻译：取代的苯基衍生物，生产和使用
公开(公告)号：EP0977741B1
公开(公告)日：2003-09-03
申请号：EP98914851.5
申请日：1998-04-21
申请人： NEUROSEARCH A/S
发明人： CHRISTOPHERSEN, Palle , PEDERSEN, Ove
IPC分类号： C07D257/04 , C07D249/12 , C07D271/10 , C07D401/10 , C07D405/10 , C07D409/10 , A61K31/41
CPC分类号： C07C275/42 , C07C233/55 , C07C271/58 , C07C275/40 , C07C309/51 , C07C311/08 , C07C311/21 , C07C311/47 , C07C311/60 , C07C335/22

6. 发明公开

EP1224165A1 NOVEL COMPOUNDS 有权
标题翻译： NEER VERBINDUNGEN
公开(公告)号：EP1224165A1
公开(公告)日：2002-07-24
申请号：EP00973336.1
申请日：2000-10-27
申请人： New Pharma Research Sweden AB
发明人： MUZI, Sabrina , ABDUL-RAHMAN, Shoaá
IPC分类号： C07C275/28 , C07D277/82 , C07D295/16 , A61K31/17 , A61K31/425 , A61K31/495 , A61P33/02
CPC分类号： C07D213/75 , A23K20/105 , A23K20/111 , A23K20/116 , A23K50/75 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C279/24 , C07C279/28 , C07C281/16 , C07C281/18 , C07C335/16 , C07C335/18 , C07C335/22 , C07C335/28 , C07C335/42 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2603/24 , C07C2603/74 , C07D209/54 , C07D213/71 , C07D215/38 , C07D217/24 , C07D233/84 , C07D241/20 , C07D265/24 , C07D265/30 , C07D277/48 , C07D277/82 , C07D295/215 , C07D401/12 , C07D405/04 , C07D413/12 , C07D417/14
摘要： The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I), where Y is S or O and R is as defined in the specification.
摘要翻译：本发明涉及新化合物，含有该化合物的药物组合物以及治疗寄生虫病的方法，其中所述化合物被施用。本发明化合物特别适用于治疗球虫病，特别是在家禽中，并且它们具有通式（I）：其中Y是S或O，R如说明书中所定义。

7. 发明授权

EP0780372B1 3-Amino-2-mercaptobenzoic acid derivatives and processes for their preparation 失效
标题翻译： 3-氨基-2-巯基苯甲酸衍生物和它们的制备方法
公开(公告)号：EP0780372B1
公开(公告)日：2001-11-14
申请号：EP96810865.4
申请日：1996-12-12
申请人： Syngenta Participations AG
发明人： Kunz, Walter , Jau, Beat
IPC分类号： C07C323/63 , C07C327/26 , C07D277/82 , C07C335/22 , C07D285/14
CPC分类号： C07D285/14 , C07C319/02 , C07C319/12 , C07C323/63 , C07C327/26 , C07C335/22 , C07D277/82

8. 发明公开

EP0889877A1 META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS 失效
标题翻译：间位取代苯衍生物及其作为素αVβ3整合素拮抗剂或抑制剂的使用
公开(公告)号：EP0889877A1
公开(公告)日：1999-01-13
申请号：EP97916110.0
申请日：1997-03-26
申请人： G.D. SEARLE & CO.
发明人： CHANDRAKUMAR, Nizal , CHEN, Barbara, B. , CHEN, Helen , CLARE, Michael , GASIECKI, Alan, F. , HAACK, Richard, A. , MALECHA, James, W. , RUMINSKI, Peter, G. , RUSSELL, Mark, A.
IPC分类号： A61K31 , A61P1 , A61P19 , A61P27 , A61P35 , A61P43 , C07C45 , C07C49 , C07C205 , C07C257 , C07C259 , C07C275 , C07C279 , C07C311 , C07C317 , C07C323 , C07C335 , C07D223 , C07D233 , C07D235 , C07D239 , C07D311 , C07D405
CPC分类号： C07C45/673 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by Formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the αvβ3 integrin.

9. 发明公开

EP0850221A1 META-GUANIDINE, UREA, THIOUREA OR AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS INTEGRIN ANTAGONISTS 失效
标题翻译：元素 - 胍基，尿素，硫脲，亚胺基氨基酸，苯甲酸，氨基酸，氨基酸，氨基酸，氨基酸
公开(公告)号：EP0850221A1
公开(公告)日：1998-07-01
申请号：EP96932142.0
申请日：1996-08-27
申请人： G.D. SEARLE & CO.
发明人： RUMINSKI, Peter, Gerrard , CLARE, Michael , COLLINS, Paul, Waddell , DESAI, Bipinchandra, Nanubhai , LINDMARK, Richard, John , RICO, Joseph, Gerace , ROGERS, Thomas, Edward , RUSSELL, Mark, Andrew
IPC分类号： A61K31 , A61K38 , A61P5 , A61P25 , A61P35 , A61P43 , C07C275 , C07C279 , C07C311 , C07C313 , C07C317 , C07C323 , C07C335 , C07D207 , C07D209 , C07D211 , C07D213 , C07D215 , C07D223 , C07D231 , C07D233 , C07D235 , C07D239 , C07D249 , C07D295 , C07D307 , C07D317 , C07D319 , C07D333 , C07D401 , C07D405 , C07D413 , C07D417 , C07H15 , C07K5
CPC分类号： C07D231/06 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/19 , C07C311/37 , C07C317/50 , C07C323/59 , C07C323/62 , C07C323/63 , C07C335/22 , C07C335/28 , C07D207/14 , C07D211/72 , C07D213/55 , C07D213/61 , C07D215/14 , C07D223/12 , C07D231/12 , C07D231/14 , C07D233/50 , C07D239/14 , C07D239/26 , C07D239/545 , C07D249/14 , C07D295/215 , C07D307/54 , C07D307/79 , C07D307/81 , C07D317/60 , C07D319/18 , C07D333/24 , C07D333/28 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07H15/203
摘要： The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein A is (a) or (b) or (c) or (d) pharmaceutical compositions thereof and methods of using such compounds and compositions as αvβ3 integrin antagonists.

10. 发明公开

EP0780372A3 3-Amino-2-mercaptobenzoic acid derivatives and processes for their preparation 失效
标题翻译： 3-氨基-2-巯基苯甲酸衍生物及其制备方法
公开(公告)号：EP0780372A3
公开(公告)日：1997-09-17
申请号：EP96810865.4
申请日：1996-12-12
申请人： Novartis AG
发明人： Kunz, Walter , Jau, Beat
IPC分类号： C07C323/63 , C07C327/26 , C07D277/82 , C07C335/22 , C07D285/14
CPC分类号： C07D285/14 , C07C319/02 , C07C319/12 , C07C323/63 , C07C327/26 , C07C335/22 , C07D277/82
摘要： Compounds of the formula I
and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III
In the compounds of the formulae I and III:
X is halogen, n is 0, 1, 2 or 3; Z is CN, CO-A or CS-A, A is hydrogen, halogen, OR 1 , SR 2 and N(R 3 )R 4 ; R 1 to R 4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R 3 and R 4 , together with the nitrogen atom to which they are bonded, are a 5- or 6-membered, substituted or unsubstituted heterocyclic radical having 1-3 heteroatoms O, S and/or N. Processes for the preparation of compounds of the formula I are described.
摘要翻译：式I化合物及其二硫化物及其盐是用于制备具有式III的杀微生物和植物免疫作用的化合物的重要中间产物：在式I和III化合物中：X为卤素，n为0 ，1,2或3; Z是CN，CO-A或CS-A，A是氢，卤素，OR1，SR2和N（R3）R4; R1至R4是氢，含有不多于8个碳原子的取代或未取代的开链，饱和或不饱和烃基，取代或未取代的环状，含不多于10个碳原子的饱和或不饱和烃基，取代或未取代的苄基或苯乙基，取代或未取代的含不多于8个碳原子的烷酰基，取代或未取代的苯甲酰基或取代或未取代的杂环基; 或者R 3和R 4与它们所键合的氮原子一起为具有1-3个O，S和/或N杂原子的5或6元取代或未取代的杂环基团。制备描述公式I.

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