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1. 发明授权

US06740651B2 Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases 有权
标题翻译：抑制由酪氨酸激酶介导的信号转导的氨基喹唑啉
公开(公告)号：US06740651B2
公开(公告)日：2004-05-25
申请号：US09934631
申请日：2001-08-22
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： C07D41312
CPC分类号： C07D413/12
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, and the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract.
摘要翻译：对酪氨酸激酶介导的信号转导具有抑制作用的化学式及其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病的用途。

2. 发明授权

US06586424B2 Tyrosine kinase inhibitors 失效
公开(公告)号：US06586424B2
公开(公告)日：2003-07-01
申请号：US10062351
申请日：2002-02-01
申请人： Mark T. Bilodeau , George D. Hartman , Peter J. Manley
发明人： Mark T. Bilodeau , George D. Hartman , Peter J. Manley
IPC分类号： C07D41312
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

3. 发明授权

US06583282B1 Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents 有权
标题翻译：用作抗炎剂的杂芳基取代的脲化合物的合成方法
公开(公告)号：US06583282B1
公开(公告)日：2003-06-24
申请号：US09611109
申请日：2000-07-06
申请人： Lin-Hua Zhang , Lei Zhu
发明人： Lin-Hua Zhang , Lei Zhu
IPC分类号： C07D41312
CPC分类号： C07D401/12 , C07D231/40 , C07D401/14 , C07D405/12
摘要： Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
摘要翻译：公开了用于制备式（I）的芳基 - 和杂芳基取代的脲化合物的新方法和新型中间体化合物，其中Ar1，Ar2，L，Q和X在本文中描述。产品化合物可用于治疗涉及炎症的疾病或病理状况的药物组合物，例如慢性炎性疾病。

4. 发明授权

US06503901B1 Amino lactam sulfonamides as inhibitors of A&bgr; protein production 有权
标题翻译：氨基内酰胺磺酰胺作为Abeta蛋白质生产的抑制剂
公开(公告)号：US06503901B1
公开(公告)日：2003-01-07
申请号：US09684718
申请日：2000-10-07
申请人： Lorin Andrew Thompson , Amy Qi Han
发明人： Lorin Andrew Thompson , Amy Qi Han
IPC分类号： C07D41312
CPC分类号： C07D401/12 , C07D243/10 , C07D243/24 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译：本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

5. 发明授权

US06764996B1 9a-azalides with antibacterial activity 有权
标题翻译：具有抗菌活性的9a-azalides
公开(公告)号：US06764996B1
公开(公告)日：2004-07-20
申请号：US09624849
申请日：2000-07-25
申请人： Yat Sun Or , Robert F. Keyes , Zhenkun Ma
发明人： Yat Sun Or , Robert F. Keyes , Zhenkun Ma
IPC分类号： C07D41312
CPC分类号： C07D413/14 , C07D413/12
摘要： Compounds of formula (I) formula (II) formula (III) and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthetic intermediates employed in the processes, and methods for treatment and prevention of bacterial infections are disclosed.
摘要翻译：式（I）式（II）式（III）和式（IV）的化合物或其药学上可接受的盐或前药是抗菌剂。公开了含有化合物的组合物，制备该化合物的方法，该方法中使用的合成中间体以及用于治疗和预防细菌感染的方法。

6. 发明授权

US06562966B2 Kinetic resolutions of chiral 2- and 3-substituted carboxylic acids 有权
标题翻译：手性2-取代和3-取代羧酸的动力学分辨率
公开(公告)号：US06562966B2
公开(公告)日：2003-05-13
申请号：US09919371
申请日：2001-07-31
申请人： Li Deng , Jianfeng Hang , Liang Tang
发明人： Li Deng , Jianfeng Hang , Liang Tang
IPC分类号： C07D41312
CPC分类号： C07D263/20 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C51/00 , C07C51/487 , C07C67/12 , C07C227/34 , C07C269/06 , C07D317/36 , C07D401/14 , C07D453/02 , Y02P20/582 , C07C59/56 , C07C59/48 , C07C59/01 , C07C69/732 , C07C69/675 , C07C271/22
摘要： One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e., a kinetic resolution wherein the yield of the resolved enantiomer or diastereomer, respectively, exceeds the amount present in the original mixture due to the in situ equilibration of the enantiomers or diastereomers under the reaction conditions prior to the resolution step.
摘要翻译：本发明的一个方面涉及手性化合物的外消旋和非对映体混合物的动力学拆分方法。该方法的关键元素是：非外消旋手性叔胺催化剂; 手性底物，例如环状碳酸酯或环状氨基甲酸酯的外消旋或非对映体混合物; 和亲核试剂，例如醇，胺或硫醇。本发明的优选实施方案涉及一种实现α和β-氨基，羟基和硫代羧酸的衍生物的外消旋和非对映体混合物的动力学拆分的方法。在某些实施方案中，本发明的方法实现了底物的外消旋或非对映体混合物的动态动力学拆分，即动力学拆分，其中分辨的对映异构体或非对映体的产率分别超过原始混合物中存在的量涉及在分离步骤之前的反应条件下对映异构体或非对映异构体的原位平衡。

7. 发明授权

US06476016B2 Cyclic oxyguanidine pyrazinones as protease inhibitors 有权
标题翻译：环氧乙酰吡嗪酮作为蛋白酶抑制剂
公开(公告)号：US06476016B2
公开(公告)日：2002-11-05
申请号：US09905883
申请日：2001-07-17
申请人： Aihua Wang , Bruce Edward Tomczuk , Tianbao Lu , Richard M. Soll , John Curtis Spurlino , Roger Francis Bone
发明人： Aihua Wang , Bruce Edward Tomczuk , Tianbao Lu , Richard M. Soll , John Curtis Spurlino , Roger Francis Bone
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07D413/14
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了环状氧基胍吡嗪酮化合物，包括式I的化合物：其中R 3，R 4，R 5，W和A如说明书中所述，以及其水合物，溶剂合物或其药学上可接受的盐。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性。描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。另外，化合物可以被可检测地标记并用于血栓的体内成像。

8. 发明授权

US06372911B1 Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones 失效
标题翻译：制备β-羟基氨基甲酸酯及其转化为恶唑烷酮的方法
公开(公告)号：US06372911B1
公开(公告)日：2002-04-16
申请号：US09482799
申请日：2000-01-13
申请人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
发明人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07C271/16 , C07D211/18 , C07D263/38
摘要： A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.
摘要翻译：公开了一种制备β-羟基氨基甲酸酯产物的方法。该方法包括使含有至少一个碳 - 碳双键的烯烃化合物与氨基甲酸酯在水溶剂中反应，并在碱，锇催化剂，选自卤代乙内酰脲，卤代异氰脲酸和卤代异氰尿酸的碱金属盐和任选的不对称配体，以形成含有β-羟基氨基甲酸酯产物的反应混合物。该方法任选地还包括用另外的碱处理β-羟基氨基甲酸酯产物以形成恶唑烷酮。恶唑烷酮可用作手性助剂，也可用作形成药物活性物质如α1肾上腺素能受体拮抗剂的中间体。还公开了制备恶唑烷酮的氮官能化衍生物的方法。

9. 发明授权

US06239152B1 Oxazolidinone combinatorial libraries, compositions and methods of preparation 失效
标题翻译：恶唑烷酮组合文库，组合物和制备方法
公开(公告)号：US06239152B1
公开(公告)日：2001-05-29
申请号：US09235771
申请日：1999-01-22
申请人： Mikhail F. Gordeev , Gary W. Luehr , Dinesh V. Patel , Zhi-Jie Ni , Eric Gordon
发明人： Mikhail F. Gordeev , Gary W. Luehr , Dinesh V. Patel , Zhi-Jie Ni , Eric Gordon
IPC分类号： C07D41312
CPC分类号： C07D263/20 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/653 , C40B40/00
摘要： Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
摘要翻译：提供了恶唑烷酮及其合成方法。还提供了包含恶唑烷酮的组合文库，以及制备文库的方法。还提供制备生物活性恶唑烷酮的方法以及包含恶唑烷酮的药学上可接受的组合物。文库制备的方法包括将恶唑烷酮与固体支持物的连接。在一个实施方案中化合物制备的方法涉及亚氨基磷烷与含羰基的聚合物载体的反应。

10. 发明授权

US06605629B1 Neurotrophin production secretion promoting agent 有权
标题翻译：神经营养蛋白生成分泌促进剂
公开(公告)号：US06605629B1
公开(公告)日：2003-08-12
申请号：US09868304
申请日：2001-06-29
申请人： Yu Momose , Katsuhito Murase
发明人： Yu Momose , Katsuhito Murase
IPC分类号： C07D41312
CPC分类号： C07D263/34 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/38 , C07D263/46 , C07D263/48 , C07D277/32 , C07D277/40 , C07D277/54 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/14
摘要： A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.
摘要翻译：一种神经营养因子产生/分泌促进剂，其包含下式的唑衍生物：其中R1表示卤素原子，可任意取代的杂环基，可任选被取代的羟基，可任选被取代的硫醇基，或可任选被取代的氨基; A表示可任选被取代的酰基，可任选被取代的杂环基，可任意取代的羟基或可任意被酯化或酰胺化的羧基; B表示可任选被取代的芳族基团; X表示可任选被取代的氧原子，硫原子或氮原子; Y表示二价烃基或杂环基，或其盐; 其可用作预防或治疗神经病的药剂。

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