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    • 1. 发明申请
    • DIOXO-ALKANES AND DIOXO-ALKENES
    • 二氧化钛和二氧化钛
    • WO2008003978A3
    • 2008-12-31
    • PCT/GB2007002527
    • 2007-07-05
    • PHYTOPHARM PLCREES DARYL DAVIDGUNNING PHILIP JAMESORSI ANTONIAHOWSON PATRICK ABARRACLOUGH PAULCALLIZOT NOELLE
    • REES DARYL DAVIDGUNNING PHILIP JAMESORSI ANTONIAHOWSON PATRICK ABARRACLOUGH PAULCALLIZOT NOELLE
    • A61K31/12A61P11/06A61P17/06A61P29/00A61P37/08A61P43/00
    • A61K31/12C07C45/455C07C45/62C07C45/673C07C45/68C07C45/74C07C49/255C07C49/577C07C49/84C07C69/738C07C217/22C07C255/56C07C2601/02C07C2601/10C07C2601/14C07F7/1852Y02P20/582
    • 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。
    • 3. 发明专利
    • CHEMICAL COMPOUNDS
    • CA2660182A1
    • 2008-01-10
    • CA2660182
    • 2007-07-05
    • PHYTOPHARM PLC
    • HOWSON PATRICK ABARRACLOUGH PAULCALLIZOT NOELLEORSI ANTONIAGUNNING PHILIP JAMESREES DARYL DAVID
    • A61K31/12A23L33/00A61P11/06A61P17/06A61P29/00A61P37/08A61P43/00
    • 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.
    • 7. 发明专利
    • DERIVADOS DE SAPOGENINA Y SU USO EN EL TRATAMIENTO DE LA DISFUNCION COGNITIVA.
    • ES2228608T3
    • 2005-04-16
    • ES00964447
    • 2000-09-29
    • PHYTOPHARM PLC
    • BARRACLOUGH PAULHANSON JIMGUNNING PHILREES DARYLXIA ZONGQINHU YAER
    • A23L1/30A61K31/575A61K31/58A61K36/18A61K36/896A61P21/04A61P25/14A61P25/16A61P25/28C07J9/00C07J71/00
    • El uso, en la fabricación de un medicamento que aumente el número de receptores muscarínicos o que intensifique la función de los receptores muscarínicos en un ser humano o un animal no humano, de derivados de sapogenina de fórmula general I o II: y sus estereoisómeros y mezclas racémicas, sus profármacos y sales farmacéuticamente aceptables, en las que: en la fórmula general (I): - R1, R2, R3, R4, R5, R6, R7, R8, R10 son, independientemente uno de otro, H, OH, =O y OR, donde R= alquilo opcionalmente sustituido, acilo opcionalmente sustituido, carbamoílo opcionalmente sustituido, alcoxicarbonilo; - R9, R12, R11, R13 pueden ser H, OH, OR, donde R= alquilo opcionalmente sustituido, acilo opcionalmente sustituido, carbamoílo opcionalmente sustituido, alcoxicarbonilo; - R14= grupo alquilo opcionalmente sustituido; - R15= H, alquilo opcionalmente sustituido o acilo opcionalmente sustituido; - el hidrógeno en C5 puede ser o ; y ---------- representa un doble enlace opcional. y en las que la fórmula general (II): - R1, R2, R3, R4, R5, R6, R7, R8, R10, R17 son, independientemente uno de otro, H, -OH, =O u OR, donde R= alquilo opcionalmente sustituido, acilo opcionalmente sustituido, carbamoílo opcionalmente sustituido, alcoxicarbonilo; - R9, R12, R11, R13 pueden ser H, OH, OR, donde R= alquilo opcionalmente sustituido, acilo opcionalmente sustituido, carbamoílo opcionalmente sustituido, alcoxicarbonilo; - R14= grupo alquilo opcionalmente sustituido; - R15= H, alquilo opcionalmente sustituido o acilo opcionalmente sustituido; - R16= H, alquilo opcionalmente sustituido acilo opcionalmente sustituido; - El hidrógeno en C5 puede se o . y.............representa un doble enlace opcional.