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    • 1. 发明申请
      WO2008003978A3 DIOXO-ALKANES AND DIOXO-ALKENES 审中-公开
    • DIOXO-ALKANES AND DIOXO-ALKENES
    • 二氧化钛和二氧化钛
    • WO2008003978A3
    • 2008-12-31
    • PCT/GB2007002527
    • 2007-07-05
    • PHYTOPHARM PLC , REES DARYL DAVID , GUNNING PHILIP JAMES , ORSI ANTONIA , HOWSON PATRICK A , BARRACLOUGH PAUL , CALLIZOT NOELLE
    • REES DARYL DAVID , GUNNING PHILIP JAMES , ORSI ANTONIA , HOWSON PATRICK A , BARRACLOUGH PAUL , CALLIZOT NOELLE
    • A61K31/12 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/08 , A61P43/00
    • A61K31/12 , C07C45/455 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/74 , C07C49/255 , C07C49/577 , C07C49/84 , C07C69/738 , C07C217/22 , C07C255/56 , C07C2601/02 , C07C2601/10 , C07C2601/14 , C07F7/1852 , Y02P20/582
    • Compounds of general formula (I) wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted -CO-(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted -CO-(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted -CO-(C2-10alkenyl), optionally substituted aryl, and optionally substituted -CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycloalkyl, optionally substituted C2-10alkenyl, and optionally substituted aryl; R4, R5 and R6 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, OH, optionally substituted C1-10alkoxy, halo, optionally substituted aryloxy, optionally substituted (C1-10alkyl)-S(O)n- where n = 0, 1 or 2, optionally substituted aryl-S(O)n- where n = 0, 1 or 2, or R4 is hydrogen and R5 and R6 together represent an optionally substituted saturated or unsaturated organic chain containing 1, 2, 3, 4, 5, 6 or 7 chain carbon atoms and optionally 1, 2 or 3 chain heteroatoms selected from O, N and S, provided that the chain is at least 3 atoms long; with the proviso that, when R1 = R2 = hydrogen, then any optionally substituted C1-10alkyl or optionally substituted C2-10alkenyl for R3 must have a branch point at one or more of the a and ß positions counted from the carbonyl group (or tautomeric form thereof) to which R3 is attached; or a physiologically acceptable salt, complex or prodrug thereof; are disclosed per se and for use in the treatment or prophylaxis of hypersensitivity, smooth muscle disorders, spasmodic conditions, allergic conditions, inflammatory conditions and/or pain.
    • 通式（I）的化合物，其中：R 1和R 2彼此独立地选自氢，任选取代的C 1-10烷基，任选取代的-CO-（C 1-10烷基），任选取代的C 3-10环烷基，任选取代的-CO - （C 3-10环烷基），任选取代的C 2-10烯基，任选取代的-CO-（C 2-10烯基），任选取代的芳基和任选取代的-CO-芳基，或者R 1和R 2一起表示任选取代的饱和或不饱和C1- 10个亚烷基或任选取代的饱和或不饱和的C 3-10亚烷基，或者R 1和R 2与它们所连接的碳原子一起代表任选取代的饱和或不饱和的含有3,4,5,6,7或8位的有机环 环碳原子和任选的1,2或3个选自O，N和S的环杂原子; 任选取代的C 1-10烷基，任选取代的C 3-10环烷基，任选取代的C 2-10烯基和任选取代的芳基; R 3可以相同或不同于R 1和R 2， R4，R5和R6彼此独立地选自氢，任选取代的C 1-10烷基，OH，任选取代的C 1-10烷氧基，卤素，任选取代的芳氧基，任选取代的（C 1-10烷基）-S（O） 其中n = 0,1或2，任选取代的芳基-S（O）n-，其中n = 0,1或2，或R 4是氢，R 5和R 6一起代表任选取代的饱和或不饱和有机链，其含有1,2 ，3,4,5,6或7个链碳原子和任选地1,2或3个选自O，N和S的链杂原子，条件是链长至少3个原子; 条件是当R 1 = R 2 =氢时，R 3的任何取代的C 1-10烷基或任选取代的C 2-10烯基必须在从羰基（或互变异构体）计数的a和ß位置中的一个或多个位置具有一个分支点 形式）; 或其生理学上可接受的盐，复合物或前药; 本身公开并用于治疗或预防超敏反应，平滑肌障碍，痉挛症状，过敏性疾病，炎性病症和/或疼痛。
    • 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
    • 2. 发明申请
      WO2004096231A2 USE OF PIPERAZINE PHENOTHIAZINE DERIVATIVES, OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ESTER THEREOF, IN THE MANUFACTURE OF A MEDICAMENT WITH NEUROPROTECTOR AND/OR NEUROTROPHIC EFFECTS ON CNS AND/OR PNS 审中-公开
    • USE OF PIPERAZINE PHENOTHIAZINE DERIVATIVES, OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ESTER THEREOF, IN THE MANUFACTURE OF A MEDICAMENT WITH NEUROPROTECTOR AND/OR NEUROTROPHIC EFFECTS ON CNS AND/OR PNS
    • 在具有神经元和/或神经营养因子对CNS和/或PNS的药物的制造中使用哌嗪类苯并恶嗪衍生物或其药学上可接受的盐或其衍生物
    • WO2004096231A2
    • 2004-11-11
    • PCT/EP2004005183
    • 2004-04-23
    • NEURO 3D , CALLIZOT NOELLE , APPERT COLLIN ALINE
    • CALLIZOT NOELLE , APPERT COLLIN ALINE
    • A61K31/5415 , A61P25/02 , A61P25/16 , A61P25/28 , A61P27/16
    • A61K31/5415
    • This invention relates to a new use of piperazinephenothiazine derivatives and their pharmaceutically acceptable salts or esters in the manufacture of a medicament with neuroprotector and/or neurotrophic effects on CNS and/or PNS. The piperazine phenothiazine derivatives are selected from compounds of formula (I) wherein A represents a straight or branched alkylene chain of from 2 to 6 carbon atoms separating the nitrogen atoms linked thereto by at least two carbon atoms ; R1 represents hydrogen, halogen, lower alkyl, lower alkoxy, lower alkanoyl, lower alkyl-mercapto, trifluoromethylmercapto, lower alkyl-sulfonyl (preferably methylsulfonyl), perfluoroalkyl of 1 to 3 carbon atoms; R2, R3, R4 and R5 each represent methyl, ethyl or hydrogen, R6 represents hydrogen, lower alkyl, hydroxy-lower-alkyl or aliphatic acyloxy-lower-alkyl having 1 to 4 carbon atoms in the acyloxy portion and 1 to 6 carbon atoms in the alkyl portion, CH2-CH2-O-R7 where R7 represents hydrogen, COR8 where R8 is a branched or straight chain alkyl radical of from seven to fourteen carbon atoms.
    • 本发明涉及哌嗪并噻嗪衍生物及其药学上可接受的盐或酯在制备对CNS和/或PNS具有神经保护素和/或神经营养作用的药物中的新用途。 哌嗪吩噻嗪衍生物选自式（I）的化合物，其中A表示2至6个碳原子的直链或支链亚烷基链，其与其连接的氮原子分开至少两个碳原子; R 1表示氢，卤素，低级烷基，低级烷氧基，低级烷酰基，低级烷基 - 巯基，三氟甲基巯基，低级烷基 - 磺酰基（优选甲基磺酰基），1〜3个碳原子的全氟烷基; R2，R3，R4和R5各自表示甲基，乙基或氢，R6表示氢，低级烷基，羟基 - 低级烷基或酰氧基中具有1至4个碳原子的脂族酰氧基 - 低级烷基和1至6个碳原子 在烷基部分，其中R 7表示氢的CH 2 -CH 2 -O-R 7，COR 8，其中R 8是具有7至14个碳原子的支链或直链烷基。
    • 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
    • 4. 发明专利
      CA2660182A1 CHEMICAL COMPOUNDS 未知
    • CHEMICAL COMPOUNDS
    • CA2660182A1
    • 2008-01-10
    • CA2660182
    • 2007-07-05
    • PHYTOPHARM PLC
    • HOWSON PATRICK A , BARRACLOUGH PAUL , CALLIZOT NOELLE , ORSI ANTONIA , GUNNING PHILIP JAMES , REES DARYL DAVID
    • A61K31/12 , A23L33/00 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/08 , A61P43/00
    • Compounds of general formula (I) wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, opti onally substituted -CO-(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted -CO-(C3-10cycloalkyl), optionally substituted C2-10a lkenyl, optionally substituted -CO-(C2-10alkenyl), optionally substituted ar yl, and optionally substituted -CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached repre sent an optionally substituted saturated or unsaturated organic ring contain ing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heter oatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alky l, optionally substituted C3-10cycloalkyl, optionally substituted C2-10alken yl, and optionally substituted aryl; R4, R5 and R6 are, independently of eac h other, selected from hydrogen, optionally substituted C1-10alkyl, OH, opti onally substituted C1-10alkoxy, halo, optionally substituted aryloxy, option ally substituted (C1-10alkyl)-S(O)n- where n =0, 1 or 2, optionally substitu ted aryl-S(O)n- where n = 0, 1 or 2, or R4 is hydrogen and R5 and R6 togethe r represent an optionally substituted saturated or unsaturated organic chain containing 1, 2, 3, 4, 5, 6 or 7 chain carbon atoms and optionally 1, 2 or 3 chain heteroatoms selected from O, N and S, provided that the chain is at least 3 atoms long; with the proviso that, when R1 = R2 = hydrogen, then any optionally substituted C1-10alkyl or optionally substituted C2-10alkenyl fo r R3 must have a branch point at one or more of the .alpha. and .beta. posit ions counted from the carbonyl group (or tautomeric form thereof) to which R 3 is attached; or a physiologically acceptable salt, complex or prodrug ther eof; are disclosed per se and for use in the treatment or prophylaxis of hyp ersensitivity, smooth muscle disorders, spasmodic conditions, allergic condi tions, inflammatory conditions and/or pain.
    • 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
    • 8. 发明专利
      MX2009000283A COMPUESTOS QUIMICOS. 未知
    • COMPUESTOS QUIMICOS.
    • MX2009000283A
    • 2009-01-26
    • MX2009000283
    • 2007-07-05
    • PHYTOPHARM PLC
    • BARRACLOUGH PAUL , GUNNING PHILLIP JAMES , REES DARYL DAVID , ORSI ANTONIA , HOWSON PATRICK A , CALLIZOT NOELLE
    • A61K31/12 , A23L33/00 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/08 , A61P43/00
    • Compuestos de la Fórmula general I (ver fórmula (I)) en donde: R1 y R2 son seleccionados independientemente uno de otro de hidrógeno, alquilo de C1-10 opcionalmente substituido, -CO-(alquilo de C1-10) opcionalmente substituido, cicloalquilo de C3-10 opcionalmente substituido, -CO-(cicloalquilo de C3-10) opcionalmente substituido, alquenilo de C2-10 opcionalmente substituido, -CO-(alquenil de C2-10) opcionalmente substituido, arilo opcionalmente substituido -CO-arilo opcionalmente substituido o R1 y R2 representando juntos un grupo alquilideno de C1-10 opcionalmente substituido saturado o no saturado o un grupo cicloalquilideno de C3-10 opcionalmente substituido saturado o no saturado o R1 y R2 juntos con el átomo de carbono al cual ellos son ligados representan un anillo orgánico saturado o no saturado que contiene 3, 4, 5, 6, 7 ó 8 átomos de carbono y opcionalmente un anillo de 1, 2 ó 3 heteroátomos seleccionado desde O, N y S; R3, el cual puede ser el mismo como, o diferente de, ya sea de R1 y R2, seleccionado desde un alquilo C1-10 opcionalmente substituido, cicloalquilo C3-10 opcionalmente substituido alquenilo de C2-10 opcionalmente substituido y arilo opcionalmente substituido; R4, R5 y R6 son seleccionados independientemente uno de otro desde hidrógeno, alquilo de C1-10 opcionalmente substituido, OH, alcoxi de C1-10 opcionalmente substituido, halo, ariloxi opcionalmente substituido, (alquilo de C1-10) opcionalmente substituido-S(O)n- donde n = 0, 1 o 2, aril-S(O)n- opcionalmente substituido donde n = 0, 1 ó 2, o R4 y R5 representan juntos una cadena orgánica opcionalmente substituido que contiene 1, 2, 3, 4 5, 6 ó 7 átomos de carbono y opcionalmente cadena 1, 2 ó 3 heteroátomos seleccionados desde O, N y S, contemplando que la cadena es de a lo menos tres átomos de largo; con la provisión que cuando R1 = R2 = hidrógeno, luego cualquier alquilo de C1-10 opcionalmente substituido o alquenilo de C2-10 opcionalmente substituido para R3 deben tener un punto de ramificación en una o más de las posiciones a y ß contadas desde el grupo carbonilo (o forma tautómera de estas) a los cuales ligado R3; o una sal fisiológicamente aceptable, complejo o profármaco de estos; son descritos per se y para el uso en el tratamiento o profilaxis de la hipersensibilidad desordenes del músculo liso, condiciones espasmódicas, condiciones alérgicas, condiciones inflamatorias y/o dolor.
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