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    • 24. 发明申请
      US20100022541A1 Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors 审中-公开
    • Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
    • 细菌性肝细胞合成的化学抑制剂，其制备方法和所述抑制剂的生物应用
    • US20100022541A1
    • 2010-01-28
    • US12311278
    • 2007-09-25
    • Sonia Escaich , Alexis Denis , Francois Moreau , Vincent Gerusz , Nicolas Desroy
    • Sonia Escaich , Alexis Denis , Francois Moreau , Vincent Gerusz , Nicolas Desroy
    • A61K31/5377 , C12Q1/66 , C07D413/12 , A61K31/437
    • C07D417/14 , C07D401/12 , C07D405/12 , C07D417/12
    • The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C═NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
    • 本发明涉及具有式（I）的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药，其中A是芳基或杂环，任选被一个或多个相同或不同的R如H，C1 C 1 -C 10烷基-OR 1，C 1 -C 10烷基-NR 1 R 1，烷氧基，羟基，硫代烷基，芳基，杂环，卤素，硝基，氰基，CO 2 R 1，NR 1 R 1，NR 1 C（O）R 1，C（O）NR 1 R 1， NR 1 C（S）R 1，C（S）NR 1 R 1，SO 2 NR 1 R 1，SO 2 R 1，NR 1 SO 2 R 1，NR 1 C（O）NR 1 R 1，NR 1 C（O）OR 1，NR 1 C R1，芳氧基，硫代芳基，烯基，炔基R1相同或不同，是H或C1-C10烷基B1，B2，B3相同或不表示C，N，O，S，形成五元芳环，其中一至三碳 原子被选自S，O，N的杂原子替代，任选地被一个或多个相同或不同的R取代，如上定义。B4是C或NY是H，C1-C10烷基，烷氧基，硫代烷基，任选被一个 或几个iden 如W所定义的不同的R是C，O或N，被一个或多个C 1 -C 10烷基取代或不被取代，D是任选被一个或多个相同或不同的R如上所定义的R取代的杂环。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 25. 发明申请
      US20050014816A1 Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them 审中-公开
    • Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them
    • 噻吩氨基酸衍生物，其制备方法和含有它们的药物组合物
    • US20050014816A1
    • 2005-01-20
    • US10884059
    • 2004-07-02
    • Delphine Compere , Anne-Claude Dublanchet , Karine Courte , Stephane Blais , Pierre Ducrot , Philippe Cluzeau , Alexis Denis
    • Delphine Compere , Anne-Claude Dublanchet , Karine Courte , Stephane Blais , Pierre Ducrot , Philippe Cluzeau , Alexis Denis
    • A61K31/381 , A61K31/4436 , A61P11/00 , C07D333/34 , C07D333/38 , C07D409/10 , C07
    • C07D333/38 , C07D409/10
    • The invention provides compounds of Formula (I), stereoisomers thereof, or pharmaceutically acceptable salts of said compounds or stereoisomers, wherein R1, R2, m, p, q, R7 and R8 are as defined below, as well as compositions comprising the same, processes for making the same, and methods of using the same to treat a variety of diseases, including, those requiring interaction with metalloproteases, and more specifically with macrophage metalloelastase (MMP-12), and for the prevention and treatment of respiratory pathologies such as chronic obstructive bronchopneumopathy (COPD), emphysema, chronic bronchitis, chronic pulmonary inflammation, asthma, cystic fibrosis, acute respiratory distress syndrome (ARDS), respiratory allergies including allergic rhinitis, and also diseases associated with the production of TNFα including severe fibrotic pulmonary disease, pulmonary sarcoidosis and silicosis. The compounds of the present invention also show inhibitory activity on metalloprotease-13 (MMP-13), making them useful for the treatment of pathologies involving this enzyme, such as cancer, osteoporosis, osteoarthritis, arthritis, rheumatoid arthritis, atherosclerosis, multiple sclerosis and cardiac insufficiency.
    • 本发明提供式（I）化合物，其立体异构体或所述化合物或立体异构体的药学上可接受的盐，其中R 1，R 2，m，p，q，R 7和R 8如下所定义，以及包含其的组合物， 制备相同的方法，以及使用它们治疗各种疾病的方法，包括需要与金属蛋白酶相互作用的那些疾病，更具体地涉及巨噬细胞金属弹性蛋白酶（MMP-12），以及用于预防和治疗呼吸道病症如 慢性阻塞性支气管肺病（COPD），肺气肿，慢性支气管炎，慢性肺部炎症，哮喘，囊性纤维化，急性呼吸窘迫综合征（ARDS），包括过敏性鼻炎在内的呼吸系统过敏，以及包括严重纤维性肺病在内的TNFα产生相关疾病， 肺结节病和矽肺。 本发明的化合物还显示对金属蛋白酶-13（MMP-13）的抑制活性，使其可用于治疗涉及该酶的病理学，例如癌症，骨质疏松症，骨关节炎，关节炎，类风湿性关节炎，动脉粥样硬化，多发性硬化和 心功能不全
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 26. 发明授权
      US06664398B2 Derivatives of erythromycin, their preparation process and their use as medicaments 有权
    • Derivatives of erythromycin, their preparation process and their use as medicaments
    • 红霉素的衍生物，其制备方法及其作为药物的用途
    • US06664398B2
    • 2003-12-16
    • US10188394
    • 2002-07-02
    • Alexis Denis
    • Alexis Denis
    • C07D29300
    • C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07H17/08
    • A subject of the invention is the compounds of formula in which Y represents a hydrogen atom or a fluorine atom, n represents an integer comprised between 1 and 8, Z represents a hydrogen atom or the remainder of a carboxylic acid, optionally substituted on the heterocycle by one or more alkyl, alkenyl, alkynyl, O-alkyl, O-alkenyl, O-alkynyl, S-alkyl, S-alkenyl, S-alkynyl radicals containing up to 8 carbon atoms, one or more OH, NH2, C═N, NO2, CF3 radicals or one or more aryl radicals containing up to 14 carbon atoms or heteroaryl radicals containing one or more nitrogen oxygen or sulphur atoms, the aryl or heteroaryl radicals themselves being able to be substituted as well as their addition salts with acids, The products of formula (I) have antibiotic properties.
    • 本发明的主题是代表氢原子或氟原子的甲醛化合物，n表示1至8之间的整数，Z表示氢原子或羧基的其余部分，任选在杂环上被一个 或更多烷基，烯基，炔基，O-烷基，O-烯基，O-炔基，S-烷基，S-烯基，含有至多8个碳原子的S-炔基，一个或多个OH，NH 2，C = N， NO 2，CF 3基团或一个或多个含有至多14个碳原子的芳基或含有一个或多个氮氧原子或硫原子的杂芳基，芳基或杂芳基本身能够被取代，以及它们与酸的加成盐。 式（I）的产品具有抗生素特性。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 29. 发明授权
      US08217075B2 2-amino-2-phenyl-alkanol derivatives, their preparation and pharmaceutical compositions containing them 有权
    • 2-amino-2-phenyl-alkanol derivatives, their preparation and pharmaceutical compositions containing them
    • 2-氨基-2-苯基 - 链烷醇衍生物，其制备方法和含有它们的药物组合物
    • US08217075B2
    • 2012-07-10
    • US12360306
    • 2009-01-27
    • Jean Pachot , Christophe Dini , Alexis Denis
    • Jean Pachot , Christophe Dini , Alexis Denis
    • A61K31/27 , A61K31/235 , A61K31/24 , C07C261/00 , C07C69/00
    • C07C271/16 , A61K9/2054 , C07C219/22 , C07C271/22 , C07C271/48 , C07C333/04 , C07D213/80 , C07D213/82 , C07D317/40
    • 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5- or 6-member heterocycle optionally having another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least 2C between >N—R2 and the substituent; and R3 is alkyl (1 to 4C) straight or branched unless specifically mentioned, alkyl or acyl are straight or branched (1 to 7C), in their R or S forms or their mixtures, as well as their pharmaceutically acceptable salts when these exist.
    • 通式（I）的2-氨基-2-苯基 - 链烷醇酯衍生物，其中：R 1为H，直链或支链1至4C烷基，被OH，烷氧基，烷硫基，酰氧基，NH 2取代的直链或支链2至4C烷基 ，烷基氨基，二烷基氨基，烷基氨基甲酰氧基，烷氧基羰基氨基，脲基或烷基脲基，R2是-CO-R基团，其中R是H，烷基，芳基，杂环基，苄基或杂环基甲基，或R2是-CO-Y-R4基团， Y是-O - ， - S - ， - NH - ， - 烷基，其中alk是直链或支链（1-4C）烷基，R4是烷基，芳基，芳烷基或杂环基烷基，能够被一个或多个 卤原子或OH基团，直链或支链（1-4C）烷基，烷氧基，烷硫基，酰氨基烷硫基，烷氧基羰基或酰基氨基（1至4C）直链或支链或氧代，或能够被R5COO-取代，其中R5是烷基 任选地被苄氧羰基氨基，酰氨基或氨基酸残基取代，或表示杂环基， 或R 2是被OH，烷氧基，烷硫基，酰氧基，NH 2，烷基氨基，任选地与它们所连接的氮原子形成的二烷基氨基取代的任选具有另一个杂原子的5或6元杂环的（2至4C） O或N），或被烷基氨基甲酰氧基，烷氧基羰基氨基，脲基或烷基脲基取代，应理解所述直链或支链取代的烷基在> N-R2和取代基之间至少包含2C; 并且R 3是直链或支链烷基（1-4C），除非特别提及，烷基或酰基以R或S形式或其混合物为直链或支链（1至7C），以及它们的药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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