公开(公告)号：US07902193B2

公开(公告)日：2011-03-08

申请号：US12271308

申请日：2008-11-14

申请人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

发明人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

IPC分类号： C07D237/32 ,  A61K31/502 ,  A61P35/00

CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2. RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

摘要翻译： 式（I）的化合物：其中：A和B一起表示任选取代的稠合芳环; D选自：（i）其中Y1选自CH和N，Y2选自CH和N，Y3选自CH，CF和N; 和（ii）其中Q为O或S; RD是：其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2，CRC3RC4和C = O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H，R，C（= O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2。 RC1和RC2独立地选自H，R，C（= O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时，RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时，RC2和RC4可以一起形成附加键，使得在被RC1和RC3取代的原子之间存在双键。

公开(公告)号：US20060199803A1

公开(公告)日：2006-09-07

申请号：US11361213

申请日：2006-02-24

申请人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Peter Edwards ,  Ming-lai Loh ,  Graeme Smith

发明人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Peter Edwards ,  Ming-lai Loh ,  Graeme Smith

IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/519 ,  A61K31/5377 ,  C07D487/02

CPC分类号： C07D471/04

摘要： Compounds of formula l: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and RN4 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms and their use in treating diseases ameliorated by the inhibition of mTOR.

摘要翻译： 式1化合物及其异构体，盐，溶剂合物，化学保护形式及其前药之一，X 1，X 2和X 3， 是N，其他是CH; R N1和R N2与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环; R 3 N 3和R 4 N 4与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环，并且其用于治疗改善的疾病 通过抑制mTOR。

公开(公告)号：US20060135770A1

公开(公告)日：2006-06-22

申请号：US11315528

申请日：2005-12-22

申请人： Muhammad Javaid ,  Graeme Smith ,  Niall Martin ,  Sylvie Gomez ,  Vincent Loh ,  Xiao-Ling Cockcroft ,  Keith Menear

发明人： Muhammad Javaid ,  Graeme Smith ,  Niall Martin ,  Sylvie Gomez ,  Vincent Loh ,  Xiao-Ling Cockcroft ,  Keith Menear

IPC分类号： C07D403/14

CPC分类号： C07C235/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/08 ,  C07D215/36 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D241/44 ,  C07D261/10 ,  C07D261/18 ,  C07D263/32 ,  C07D271/12 ,  C07D277/18 ,  C07D295/14 ,  C07D295/18 ,  C07D295/26 ,  C07D307/14 ,  C07D307/52 ,  C07D317/68 ,  C07D333/34 ,  C07D333/62 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D495/04

摘要： A compound of the formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; n is 1 or 2; RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is selected from: where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and where Q is O or S.

摘要翻译： 式（I）的化合物及其异构体，盐，溶剂合物，化学保护形式及其前药，其中：R 2，R 3，R 3， 4和R 5独立地选自H，C 1-7烷氧基，氨基，卤素或羟基; n为1或2; R N1和R N2独立地选自H和R，其中R是任选取代的C 1-10烷基，C 3 -20个杂环基和C 5-20-20芳基; 或R N1和R N2，以及它们所连接的氮原子一起形成任选取代的5-7元含氮杂环; Het选自：其中Y 1和Y 3独立地选自CH和N，Y 2选自CX和N和X 是H，Cl或F; 而Q是O或S.

公开(公告)号：US20060106214A1

公开(公告)日：2006-05-18

申请号：US11329889

申请日：2006-01-11

申请人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

发明人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

IPC分类号： A61K31/522 ,  C07D473/04

CPC分类号： C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsufonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclyl group.

摘要翻译： 式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基， 烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基， 氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷基硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基 烷基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

公开(公告)号：US06063944A

公开(公告)日：2000-05-16

申请号：US195

申请日：1998-05-04

申请人： Francesco Di Renzo ,  Sylvie Gomez ,  Francois Fajula ,  Remy Teissier

发明人： Francesco Di Renzo ,  Sylvie Gomez ,  Francois Fajula ,  Remy Teissier

IPC分类号： B01J29/89 ,  C01B39/06 ,  C01B39/08 ,  C01B39/12 ,  C01B39/20 ,  C01B39/26 ,  C01B39/46 ,  C07D301/12

CPC分类号： C01B39/085 ,  B01J29/89 ,  C01B39/065 ,  C01B39/12

摘要： A method is provided for preparing fully lattice-inserted titanium zeolites by post-synthesis processing of the synthetic zeolite optionally containing titanium with an inorganic acid, wherein the post-synthesis processing comprises processing the zeolite in the presence of at least one titanium source with a solution containing at least one oxidizing inorganic acid having a higher redox potential than an acidic tetravalent titanium solution. The invention is also directed to the use of the zeolites.

摘要翻译： PCT No.PCT / FR96 / 01209 Sec。 371日期：1998年5月4日 102（e）日期1998年5月4日PCT提交1996年7月31日PCT公布。 出版物WO97 / 05060 日期1997年2月13日提供了一种用于通过后处理合成沸石制备完全晶格插入的钛沸石的方法，所述合成沸石任选地含有钛与无机酸，其中后合成工艺包括在至少存在下处理沸石 一种钛源与含有至少一种具有比酸性四价钛溶液更高的氧化还原电位的氧化性无机酸的溶液。 本发明还涉及沸石的用途。