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1. 发明授权

US06706721B1 N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate 有权
标题翻译： N-（3-乙炔基苯基氨基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺甲磺酸盐水合物和一水合物
公开(公告)号：US06706721B1
公开(公告)日：2004-03-16
申请号：US09355534
申请日：1999-07-29
申请人： Douglas John Meldrum Allen , Timothy Norris , Jeffrey William Raggon , Dinos Paul Santafianos , Ravi Mysore Shanker
发明人： Douglas John Meldrum Allen , Timothy Norris , Jeffrey William Raggon , Dinos Paul Santafianos , Ravi Mysore Shanker
IPC分类号： C07D23994
CPC分类号： C07D239/94
摘要： The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.
摘要翻译：本发明涉及N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺甲磺酸盐的无水和水合物形式。本发明还涉及含有N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺甲磺酸盐的药物组合物和通过给予N-（3- 乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺甲磺酸酯。

2. 发明授权

US06358962B2 6,7-Dimethoxyquinazolines and therapeutic use thereof 失效
标题翻译： 6,7-二甲氧基喹唑啉及其治疗用途
公开(公告)号：US06358962B2
公开(公告)日：2002-03-19
申请号：US09779809
申请日：2001-02-08
申请人： Fatih M. Uckun , Xing-Ping Liu , Rama Krishna Narla
发明人： Fatih M. Uckun , Xing-Ping Liu , Rama Krishna Narla
IPC分类号： C07D23994
CPC分类号： C07D239/94
摘要： Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.
摘要翻译：喹唑啉化合物和治疗癌症和治疗过敏反应的方法。

3. 发明授权

US06617329B2 Aminoquinazolines and their use as medicaments 有权
标题翻译：氨基喹唑啉及其作为药物的用途
公开(公告)号：US06617329B2
公开(公告)日：2003-09-09
申请号：US09938314
申请日：2001-08-23
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： C07D23994
CPC分类号： C07D405/12 , A61K31/505 , A61K31/517 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.
摘要翻译：该化合物对由酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤疾病以及肺和空气疾病以及其制备。

4. 发明授权

US06476031B1 Quinazoline derivatives as medicaments 有权
标题翻译：喹唑啉衍生物作为药物
公开(公告)号：US06476031B1
公开(公告)日：2002-11-05
申请号：US09383825
申请日：1999-08-27
申请人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号： C07D23994
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译：本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。

5. 发明授权

US06649620B2 Quinoline and quinazoline compounds useful in therapy 失效
标题翻译：喹啉和喹唑啉化合物可用于治疗
公开(公告)号：US06649620B2
公开(公告)日：2003-11-18
申请号：US10252852
申请日：2002-09-23
申请人： Alan John Collis , David Nathan Fox
发明人： Alan John Collis , David Nathan Fox
IPC分类号： C07D23994
CPC分类号： C07D401/04 , C07D239/95 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要： Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.
摘要翻译：式I化合物，其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2表示任选被C 1-4烷基或SO 2 NH 2取代的芳基或杂芳基; R 3，表示含有至少一个选自N，O和S的杂原子的4-，5-，6-或7-元杂环，所述环任选地与苯环稠合或含有5或6元杂环至少一个选自N，O和S的杂原子，整个环系统任选被取代; X代表CH或N; 或不代表式Ia的环状基团，或表示式Ib的链和其药学上可接受的盐可用于治疗各种障碍，包括良性前列腺增生。

6. 发明授权

US06638939B2 6,7-dimethoxyquinazolines and therapeutic use thereof 失效
标题翻译： 6,7-二甲氧基喹唑啉及其治疗用途
公开(公告)号：US06638939B2
公开(公告)日：2003-10-28
申请号：US09923903
申请日：2001-08-07
申请人： Fatih M. Uckun , Xing-Ping Liu , Rama Krishna Narla
发明人： Fatih M. Uckun , Xing-Ping Liu , Rama Krishna Narla
IPC分类号： C07D23994
CPC分类号： C07D239/94
摘要： Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.
摘要翻译：喹唑啉化合物和治疗癌症和治疗过敏反应的方法。

7. 发明授权

US06316454B1 6,7-Dimethoxy-4-anilinoquinazolines 失效
标题翻译： 6,7-二甲氧基-4-苯胺基喹唑啉
公开(公告)号：US06316454B1
公开(公告)日：2001-11-13
申请号：US09361088
申请日：1999-07-26
申请人： Fatih M. Uckun , Rama Krishna Narla , Xing-Ping Liu
发明人： Fatih M. Uckun , Rama Krishna Narla , Xing-Ping Liu
IPC分类号： C07D23994
CPC分类号： C07D239/94 , C07D239/88
摘要： 6,7-Dimethoxy-4-anilinoquinaozolines of the formula: or pharmaceutically acceptable acid addition salts thereof are disclosed. These novel compounds are useful for inducing apoptosis and preventing metastases of brain tumor cells.
摘要翻译：公开了下式的6,7-二甲氧基-4-苯胺基喹唑啉或其药学上可接受的酸加成盐。这些新型化合物可用于诱导凋亡和预防脑肿瘤细胞的转移。

8. 发明授权

US06794389B2 Quinazoline derivatives and drugs 失效
标题翻译：喹唑啉衍生物和药物
公开(公告)号：US06794389B2
公开(公告)日：2004-09-21
申请号：US10239750
申请日：2002-09-25
申请人： Masahiko Okana , Kazuya Mori
发明人： Masahiko Okana , Kazuya Mori
IPC分类号： C07D23994
CPC分类号： C07D215/42
摘要： There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor. The present invention relates to a compound represented by the following formula: or a salt thereof. In the formula, X and Y are same or different and each represents a nitrogen atom or CH; R1 represents a hydrogen atom or alkyl and the like; A1 and A2 are same or different and each represents a single bond or a divalent aliphatic hydrocarbon group; Q represents a single bond, cycloalkylene group, phenylene group or divalent heterocyclic group; R2A, R2B, R2C and R2D are same or different and each represents a hydrogen atom, alkyl or phenyl; E represents a ethenylene group or —NRCO— (in which R is hydrogen or alkyl) and the like; R3 represents a phenyl group or a heterocyclic group; R4 and R5 are same or different and each represents a hydrogen atom, alkyl, alkoxy, aralkyloxy, halogen, nitro, hydroxy, alkoxycarbonyl, —NR6R7 (in which R6 and R7 are same or different and each represents a hydrogen atom or alkyl) and the like.
摘要翻译：提供了一种具有镇痛效果的优异的新型止痛剂，其通过作用于伤害感受肽受体而广泛地对抗包括伴有带状疱疹的慢性疼痛或异常性疼痛的疼痛。本发明涉及由下式表示的化合物：或其中X和Y相同或不同，分别表示氮原子或CH; R 1表示氢原子或烷基等; A 1和A 2相同或不同，各自表示单键或二价脂族烃基; Q表示单键，亚环烷基，亚苯基或二价杂环基; R 2A，R 2B，R 2C和R 2D相同或不同，各自表示氢原子，烷基或苯基; E表示亚乙基或-NRCO-（其中R是氢或烷基）等; R 3表示苯基或杂环基; R 4和R 5相同或不同，各自表示氢原子，烷基，烷氧基，芳烷氧基，卤素，硝基，羟基，烷氧基羰基，-NR 6 R 7（其中R 6，和R 7相同或不同，各自表示氢原子或烷基）等。

9. 发明授权

US06613772B1 Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments 有权
标题翻译：取代的2-芳基-4-氨基 - 噻唑啉酮，其生产和使用方法作为药物
公开(公告)号：US06613772B1
公开(公告)日：2003-09-02
申请号：US09581763
申请日：2000-06-16
申请人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel , Peter Schindler
发明人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel , Peter Schindler
IPC分类号： C07D23994
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.
摘要翻译： R1，R2，R3和Ar具有权利要求中所示含义的式Iin化合物适用于制备药物，例如预防和治疗心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物具有调节环鸟苷酸（cGMP）的内源性产生的能力，并且通常适用于治疗和预防与受干扰的cGMP平衡相关的疾病状态。

10. 发明授权

US06384223B1 Substituted quinazoline derivatives 失效
标题翻译：取代喹唑啉衍生物
公开(公告)号：US06384223B1
公开(公告)日：2002-05-07
申请号：US09564491
申请日：2000-05-04
申请人： Constantine Gletsos
发明人： Constantine Gletsos
IPC分类号： C07D23994
CPC分类号： C07D239/94
摘要： This invention provides a process for preparing compounds of formula 1: wherein: X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, amino, and alkanoylamino of 1-6 carbon atoms; R and R1 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, or trifluoromethyl; R2 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl; R3 is independently hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, or carboalkyl of 2-7 carbon atoms; n=2-4; or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different.
摘要翻译：本发明提供了制备式1化合物的方法：其中：X为任选被一个或多个选自卤素，1-6个碳原子的烷基，1-6个碳原子的烷氧基，羟基，三氟甲基，氰基，硝基，羧基，2-7个碳原子的烷氧基，2-7个碳原子的烷基，氨基和1-6个碳原子的烷酰基氨基; R和R1各自独立地为氢，卤素， -6个碳原子的烷氧基，1-6个碳原子的烷氧基，羟基或三氟甲基; R2是氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，羟基，三氟甲基; R3独立地是氢， -6个碳原子，羧基，1-6个碳原子的烷氧基，苯基或2-7个碳原子的烷基; n = 2-4;或其药学上可接受的盐，条件是Y的每个R 3可以是相同或不同

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