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11. 发明授权

US06495695B2 Process for the preparation of a collidine and 2,3,5,6-tetramethyl pyridine 失效
标题翻译：制备可力丁和2,3,5,6-四甲基吡啶的方法
公开(公告)号：US06495695B2
公开(公告)日：2002-12-17
申请号：US09818279
申请日：2001-03-27
申请人： Shivanand Janardan Kulkarni , Kondapuram Vijaya Raghavan , Srinivas Nagabandi , Radha Rani Vippagunta
发明人： Shivanand Janardan Kulkarni , Kondapuram Vijaya Raghavan , Srinivas Nagabandi , Radha Rani Vippagunta
IPC分类号： C07D21302
CPC分类号： C07D213/08
摘要： The present invention provides a process for synthesis of tri- and tetra-alkylated pyridines (i.e. collidines) in high yields by reacting methyl ethyl ketone with formaldehyde in presence of ammonia in gas phase in the presence of a zeolite catalyst which comprises of silica-alumina with at least one metal ion and/or metal selected from the group consisting of lanthanum, lead, manganese, iron, copper and cobalt. This process provides eco-friendly, more economical and shape-selective heterogeneous method.
摘要翻译：本发明提供了一种通过甲基乙基酮与甲醛在氨气存在下在气相存在下，在沸石催化剂存在下，以高收率合成三烷基化和四烷基化的吡啶（即联结）的方法，所述沸石催化剂包括二氧化硅 - 氧化铝与至少一种选自镧，铅，锰，铁，铜和钴的金属离子和/或金属。该过程提供环保，更经济和形状选择的异质方法。

12. 发明授权

US06432962B1 Benzophenones as inhibitors of IL-1&bgr; and TNF-&agr; 有权
公开(公告)号：US06432962B1
公开(公告)日：2002-08-13
申请号：US09860492
申请日：2001-05-21
申请人： Anne Marie Horneman
发明人： Anne Marie Horneman
IPC分类号： C07D21302
摘要： Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.

13. 发明授权

US06329405B1 Cyclobutene derivatives, their preparation and their therapeutic uses 失效
标题翻译：环丁烯衍生物，其制备及其治疗用途
公开(公告)号：US06329405B1
公开(公告)日：2001-12-11
申请号：US09620741
申请日：2000-07-20
申请人： Hitoshi Kurata , Takafumi Kohama , Keita Kono , Ken Kitayama
发明人： Hitoshi Kurata , Takafumi Kohama , Keita Kono , Ken Kitayama
IPC分类号： C07D21302
CPC分类号： C07C309/14 , C07B2200/07 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C323/32 , C07C2601/04 , C07C2601/14 , C07D209/14 , C07D213/38 , C07D333/20
摘要： Compounds of formula (I): {wherein: R1 and R2 each represents a variety of organic groups; R3 and R4 each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1): [wherein: R5 represents hydrogen, hydroxy or alkyl, R6 represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulfur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group], G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an ═N—O— group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulfur atom, an —NH— group or a —CO— group}; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolemia.
摘要翻译：式（I）化合物：其中：R 1和R 2各自表示各种有机基团; R3和R4各自表示氢或各种有机基团; A表示式（A-1）基团：其中：R5表示氢，羟基或烷基，R6表示羟基，烷氧基，烷硫基或胺残基，X和Y各自表示氧或硫，Z表示直接单所示的氮原子和式（I）所示的苯环之间的键或亚烷基]，G表示单键，亚烷基或取代的亚烷基; 虚线表示单键或双键; 当虚线代表双键时，D表示碳原子; E表示= N-O-基; 当虚线表示单键时，D表示CH基或氮原子，E表示氧原子，硫原子，-NH-基或-CO-基}。其药学上可接受的盐，酯或其它衍生物具有抑制回肠胆汁转运蛋白的能力，因此可用于治疗或预防高胆固醇血症。

14. 发明授权

US06297381B1 Aromatic heterocyclic compounds as anti-inflammatory agents 有权
标题翻译：芳香杂环化合物作为抗炎剂
公开(公告)号：US06297381B1
公开(公告)日：2001-10-02
申请号：US09503385
申请日：2000-02-14
申请人： Pier F. Cirillo , Eugene R. Hickey , John R. Regan
发明人： Pier F. Cirillo , Eugene R. Hickey , John R. Regan
IPC分类号： C07D21302
CPC分类号： C07D231/12 , C07D207/34 , C07D233/56 , C07D249/08 , C07D307/68 , C07D333/38 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.
摘要翻译：公开了式（I）的新型芳族杂环化合物，其中Ar1，Ar2，L，Q和X在本文中描述。该化合物可用于治疗疾病或病理状况的药物组合物中。还公开了制备这些化合物的方法。

15. 发明授权

US06207688B1 Phenethyl-thiourea compounds and use 失效
公开(公告)号：US06207688B1
公开(公告)日：2001-03-27
申请号：US09338090
申请日：1999-06-23
申请人： Fatih M. Uckum , Taracad K. Ventatachalam
发明人： Fatih M. Uckum , Taracad K. Ventatachalam
IPC分类号： C07D21302
CPC分类号： C07D213/75
摘要： Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

16. 发明授权

US06172235B2 Asymmetric conjugate addition reaction 失效
标题翻译：不对称共轭加成反应
公开(公告)号：US06172235B2
公开(公告)日：2001-01-09
申请号：US09242143
申请日：1999-04-27
申请人： Ulf H. Dolling , Lisa F. Frey , Richard D. Tillyer , David M. Tschaen
发明人： Ulf H. Dolling , Lisa F. Frey , Richard D. Tillyer , David M. Tschaen
IPC分类号： C07D21302
CPC分类号： C07D401/04 , C07D263/06 , C07D405/06 , C07D413/04 , C07F7/1804 , C07F7/1892
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
摘要翻译：本发明涉及合成内皮素拮抗剂的关键中间体以及使用不对称缀合物加成反应合成该关键中间体。

17. 发明授权

US06768007B2 Substituted 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs, compositions thereof, and methods for using thereof 失效
标题翻译：取代的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物，其组合物及其使用方法
公开(公告)号：US06768007B2
公开(公告)日：2004-07-27
申请号：US10096107
申请日：2002-03-13
申请人： Kuo-Hsiung Lee , Lan Xie , Graham P. Allaway , Carl T. Wild
发明人： Kuo-Hsiung Lee , Lan Xie , Graham P. Allaway , Carl T. Wild
IPC分类号： C07D21302
CPC分类号： C07D471/04 , C07D493/04 , C07D495/04 , C07F9/6561
摘要： 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.
摘要翻译：已经发现根据本发明的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物具有抗HIV活性。本发明的化合物具有下式：或其药学上可接受的盐，酯或前药，其中R 1，R 2，R 3，R 4，X和Z被置于规格。本发明还涉及包含一种或多种式I化合物的药物组合物，任选地还包含一种或多种抗病毒剂或免疫刺激剂。此外，本发明涉及式I化合物用于抑制动物细胞或组织中的逆转录病毒感染，用于治疗患有逆转录病毒相关病理学的患者，用于预防HIV传播感染艾滋病毒的孕妇到胎儿的感染，以及在性交期间预防艾滋病毒感染的传播。

18. 发明授权

US06649767B2 Process for preparing 1,4-dihydropyridine compounds 失效
标题翻译：制备1,4-二氢吡啶化合物的方法
公开(公告)号：US06649767B2
公开(公告)日：2003-11-18
申请号：US10224928
申请日：2002-08-20
申请人： Kunio Satake , Noriaki Murase
发明人： Kunio Satake , Noriaki Murase
IPC分类号： C07D21302
CPC分类号： C07D417/06
摘要： A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.
摘要翻译：一种制备1,4-二氢吡啶化合物的方法，包括使烯胺化合物和具有在碱存在下的结构的化合物接触; 并在温和的反应条件下，在酸或酸的组合存在下处理由此得到的反应混合物。得到的1,4-二氢吡啶化合物可用作抗炎剂等。

19. 发明授权

US06632945B2 Inhibitors of P38 失效
标题翻译： P38抑制剂
公开(公告)号：US06632945B2
公开(公告)日：2003-10-14
申请号：US09746722
申请日：2000-12-21
申请人： Francesco Salituro , Vincent Galullo , Steven Bellon , Guy Bemis , John Cochran
发明人： Francesco Salituro , Vincent Galullo , Steven Bellon , Guy Bemis , John Cochran
IPC分类号： C07D21302
CPC分类号： C07D213/74 , C04B35/01 , C07D213/56 , C07D213/75 , C07D217/22
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
摘要翻译：本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。本发明还涉及生产这些抑制剂的方法。本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

20. 发明授权

US06610704B1 Antithrombotic amides 失效
标题翻译：抗血栓酰胺
公开(公告)号：US06610704B1
公开(公告)日：2003-08-26
申请号：US09857747
申请日：2001-06-08
申请人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Pineiro-Nunez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Pineiro-Nunez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： C07D21302
CPC分类号： C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14
摘要： This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermidates thereof.
摘要翻译：本申请涉及如本文所定义的式（I）化合物（或其药学上可接受的盐），其药物组合物及其作为因子Xa抑制剂的用途，以及其制备方法及其中间体。

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