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1. 发明授权

US07498335B2 Method of producing an antiangiogenic or vascular permeability reducing effect 失效
标题翻译：产生抗血管生成或血管通透性降低作用的方法
公开(公告)号：US07498335B2
公开(公告)日：2009-03-03
申请号：US10220140
申请日：2001-03-01
申请人： Laurent Francois Andre Hennequin , Graham Charles Crawley , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine Marie Paul Lambert
发明人： Laurent Francois Andre Hennequin , Graham Charles Crawley , Darren McKerrecher , Patrick Ple , Jeffrey Philip Poyser , Christine Marie Paul Lambert
IPC分类号： A61K31/517
CPC分类号： A61K31/519 , A61K31/517 , A61K31/5377
摘要： The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.
摘要翻译：本发明涉及使用式（I）的喹唑啉衍生物，其中Q1包括任选被诸如卤代，三氟甲基和氰基的基团取代的喹唑啉环，或下式的基团：Q 3 -X 1，其中X 1包括直接键和O和Q3包括芳基，芳基 - （1-6C）烷基，杂环基和杂环基 - （1-6C）烷基; R2和R3各自为氢或（1-6C）烷基; Z包括O，S和NH; 和Q2包括芳基和芳基 - （1-3C）烷基或其药学上可接受的盐在制备用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中，例如一个人。

2. 发明授权

US06630489B1 Quinoline derivatives as tyrosine kinase inhibitors 失效
标题翻译：喹啉衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US06630489B1
公开(公告)日：2003-10-07
申请号：US09913864
申请日：2001-08-20
申请人： Graham Charles Crawley
发明人： Graham Charles Crawley
IPC分类号： A61K3147
CPC分类号： C07D401/12 , C07D215/48 , C07D409/12 , C07D417/12
摘要： The invention concerns quinoline derivatives of formula (I) wherein n is 0-3 and each R4, which may be the same or different, is a substituent such as halogeno, hydroxy, amino, nitro, trifluoromethyl, trifluoromethoxy, cyano or (1-6C)alkyl, or optionally substituted phenyl, phenoxy, anilino, N-(1-6C)alkylanilino, benzoyl or pyridyloxy; R1 and R2 is hydrogen or optionally substituted (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the prevention or treatment of T cell mediated diseases or medical conditions
摘要翻译：本发明涉及式（I）的喹啉衍生物，其中n为0-3，每个R 4可以相同或不同，为取代基，如卤代，羟基，氨基，硝基，三氟甲基，三氟甲氧基，氰基或（1-6C）烷基或任选取代的苯基，苯氧基，苯胺基，N-（1-6C）烷基苯胺基，苯甲酰基或吡啶氧基; R 1和R 2是氢或任选取代的（1-6C）烷基，（2-6C）烯基或（2-6C）炔基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其在预防或治疗T细胞介导的疾病或医学病症中的用途

3. 发明授权

US4103023A Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US4103023A
公开(公告)日：1978-07-25
申请号：US780991
申请日：1977-03-24
申请人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
发明人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： Pharmaceutical compositions containing 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives including canadensolide and 3-epi-dihydrocanadensolide. Novel 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives bearing a variety of substituents in the 3- and 6-positions selected from alkyl, phenyl, alkoxycarbonyl, methylene, benzylthiomethyl and optionally substituted phenylthiomethyl. The compositions and novel compounds show anti-ulcer activity and are useful in the treatment of gastric or duodenal ulcers.
摘要翻译：含有3,3a，6,6a-四氢呋喃并[3,4-b]呋喃衍生物的药物组合物，包括卡那赖肽和3-表二氢甘油单宁。在选自烷基，苯基，烷氧基羰基，亚甲基，苄硫基甲基和任选取代的苯硫基甲基的3-和6-位上具有各种取代基的新颖的3,3a，6,6a-四氢呋喃并[3,4-b]呋喃衍生物。组合物和新化合物显示抗溃疡活性，可用于治疗胃或十二指肠溃疡。

4. 发明授权

US4070480A Hydroxy acids 失效
标题翻译：羟基酸
公开(公告)号：US4070480A
公开(公告)日：1978-01-24
申请号：US716284
申请日：1976-08-20
申请人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
发明人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
IPC分类号： A61K31/19 , A61K31/365 , A61P1/04 , C07C51/00 , C07C51/09 , C07C59/01 , C07C59/285 , C07C59/42 , C07C67/00 , C07C69/675 , C07D307/33 , C07D307/32 , C01B15/12
CPC分类号： C07D307/33 , C07C59/285 , Y10S514/926
摘要： The invention concerns novel racemic and optically active mono- and di-hydroxy alkanoic acids bearing phenyl and/or alkyl substituents, processes for their preparation, and pharmaceutical compositions for therapeutic use in the treatment of duodenal or gastric ulcers. Representative compounds of the invention are 2-(5.beta.-n-butyl-4.beta.-hydroxy-2-oxo-tetrahydrofuran-3.beta.-yl)-2.alpha.-methyl-acetic acid and 3.alpha.-methyl-5.beta.-(1.beta.-hydroxy-n-pentyl)-2-oxo-tetrahydrofuran-4.beta.-ylcarboxylic acid.
摘要翻译：本发明涉及带有苯基和/或烷基取代基的新型外消旋和光学活性的单 - 和二 - 羟基链烷酸，其制备方法和治疗用于治疗十二指肠或胃溃疡的药物组合物。本发明的代表性化合物是2-（5β-正丁基-4β-羟基-2-氧代 - 四氢呋喃-3β-基）-2α-甲基 - 乙酸和3α-甲基-5β-（ 1β-羟基 - 正戊基）-2-氧代 - 四氢呋喃-4β-基羧酸。

5. 发明授权

US4032651A 3,3A,6,6A-Tetrahydrofuro[3,4-b]furan derivatives and anti-ulcer composition containing them 失效
标题翻译： 3,3A，6,6A-TETRAHYDROFURO（3,4-B）FURAN衍生物和含有它们的抗坏血酸组合物
公开(公告)号：US4032651A
公开(公告)日：1977-06-28
申请号：US612531
申请日：1975-09-11
申请人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
发明人： David Cecil Aldridge , Graham Charles Crawley , Colin John Strawson
IPC分类号： A61K31/34 , C07C45/63 , C07C49/16 , C07D493/02 , C07D493/04
CPC分类号： C07D493/04 , C07C381/12 , C07C45/63 , C07C49/16 , Y10S514/926
摘要： Pharmaceutical compositions containing 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives including canadensolide and 3-epi-dihydrocanadensolide. Novel 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives bearing a variety of substituents in the 3- and 6-positions selected from alkyl, phenyl, alkoxycarbonyl, methylene, benzylthiomethyl and optionally substituted phenylthiomethyl. The compositions and novel compounds show anti-ulcer activity and are useful in the treatment of gastric or duodenal ulcers.

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