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1. 发明申请

US20030166927A1 1,5-Benzothiazepines and their use as hypolipidaemics 失效
标题翻译： 1,5-苯并硫氮杂及其作为降血脂药的用途
公开(公告)号：US20030166927A1
公开(公告)日：2003-09-04
申请号：US10220877
申请日：2002-09-06
发明人： Ingemar Starke , Mickael Dahlstrom , David Blomberg
IPC分类号： A61K031/675 , A61K031/554 , C07D281/10
CPC分类号： C07D417/12 , C07D281/10 , C07F9/6536
摘要： The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2独立地选自C 1-6烷基; R4和R5中的一个是式（IA）的基团：R3，R6，R7，R8，R9，R10和R11，R4和R5中的另一个如本文所定义的药学上可接受的盐，溶剂合物，这些盐的溶剂化物，并且其用作回肠胆汁酸转运（IBAT）抑制剂用于治疗高脂血症。还描述了其制备方法和含有它们的药物组合物。

2. 发明授权

US5183743A Chromogenic dibenzoxazepinone and dibenzothiazepinone enzyme substrates 失效
标题翻译：显色二苯并氮杂酮和二苯并噻吖啶酮酶底物
公开(公告)号：US5183743A
公开(公告)日：1993-02-02
申请号：US800112
申请日：1991-11-29
申请人： Paul F. Corey
发明人： Paul F. Corey
IPC分类号： C07D267/18 , C07D281/14 , C07F9/6527 , C07F9/6536 , C07H17/00 , C12Q1/34
CPC分类号： C12Q1/34 , C07D267/18 , C07D281/14 , C07F9/6527 , C07F9/6536 , C07H17/00 , C12Q2334/00 , G01N2333/924
摘要： Chromogenic enzyme substrate compounds comprising a dibenz[b,e] [1,4]oxazepinone or dibenzo[b,e] [1,4]thiazepinone nucleus having an enzyme-cleavable group such as a radical of a sugar, carboxylic acid, amino acid, peptide, phosphoric acid, or sulfuric acid. The substrate compounds are, in general, highly soluble in aqueous media and only slightly colored, and produce, upon enzyme cleavage, a chromogen exhibiting a large change in absorbance and a pKa below 7. Such substrates find use as indicators for the determination of enzyme analytes and enzymes used as markers in a variety of assays, including immunoassays.
摘要翻译：包含具有酶切割基团的二苯并[b，e] [1,4]氧氮杂酮或二苯并[b，e] [1,4]噻吩酮核的显色酶底物化合物，例如糖，羧酸，氨基酸，肽，磷酸或硫酸。底物化合物通常在水性介质中高度可溶，仅稍微着色，并且在酶切割时产生显示出吸光度变化大的显色剂和低于7的pKa。这样的底物可用作测定酶的指示剂分析物和酶用于各种测定中的标记，包括免疫测定。

3. 发明授权

US06521769B1 Chiral phosphines, transition metal complexes thereof and uses thereof in asymmetric reactions 有权
标题翻译：手性膦，其过渡金属络合物及其在不对称反应中的用途
公开(公告)号：US06521769B1
公开(公告)日：2003-02-18
申请号：US09665456
申请日：2000-09-19
申请人： Xumu Zhang
发明人： Xumu Zhang
IPC分类号： C07F708
CPC分类号： B01J31/2414 , B01J31/1625 , B01J31/1683 , B01J31/2409 , B01J2531/46 , B01J2531/56 , B01J2531/64 , B01J2531/70 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/847 , B01J2531/96 , C07F1/005 , C07F7/003 , C07F9/005 , C07F9/5027 , C07F9/572 , C07F9/645 , C07F9/6527 , C07F9/653 , C07F9/6536 , C07F9/65527 , C07F9/655372 , C07F9/65539 , C07F9/65744 , C07F9/6596 , C07F13/005 , C07F15/004 , C07F15/0053 , C07F15/0066 , C07F15/008 , C07F15/0093 , C07F15/045 , C08F8/40
摘要： Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corresponding alcohols with 95-99.6% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.
摘要翻译：公开了基于用于不对称催化的这种手性配体的手性配体和过渡金属配合物。手性配体包括手性C1-C6 TunaPhos配体。钌金枪鱼配合物将酮降至具有95-99.6％对映体选择性的相应的醇。手性配体的过渡金属络合物可用于不对称氢化，氢化物转移，氢化硅烷化，氢化，氢化，加氢甲酰化，加氢羧化，异构化，烯丙基烷基化，环丙烷化，狄尔斯 - 阿尔德反应，Heck反应，异构化，醛醇反应，迈克尔加成和环氧化反应。

4. 发明授权

US5910494A Hypolipidemic 1,4-benzothiazepine-1,1-dioxides 失效
标题翻译：低脂血症的1,4-苯并硫氮杂-1,1-二氧化物
公开(公告)号：US5910494A
公开(公告)日：1999-06-08
申请号：US793040
申请日：1997-02-07
申请人： Lawrence Edward Brieaddy
发明人： Lawrence Edward Brieaddy
IPC分类号： A61K31/00 , A61K31/55 , A61K31/554 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , C07D281/10 , C07D417/04 , C07D513/04 , C07F9/6536
CPC分类号： C07D513/04 , A61K31/554 , C07D281/10 , C07F9/6536
摘要： The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermedites for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis. ##STR1##
摘要翻译： PCT No.PCT / GB95 / 01884第 371日期1997年2月7日 102（e）1997年2月7日PCT PCT 1995年8月9日PCT公布。出版物WO96 / 05188 日期1996年2月22日本发明涉及式（I）的新型降血脂化合物，其制备方法和新颖的中间体，含有它们的药物组合物及其在医药中的用途，特别是在预防和治疗高脂血症中，作为动脉粥样硬化。

5. 发明授权

US07192945B2 Benzothiazepine derivatives 有权
标题翻译：苯并硫氮杂衍生物
公开(公告)号：US07192945B2
公开(公告)日：2007-03-20
申请号：US10451262
申请日：2001-12-17
申请人： Ingemar Starke , Mikael Dahlstrom , David Blomberg
发明人： Ingemar Starke , Mikael Dahlstrom , David Blomberg
IPC分类号： A61P3/06 , A61K31/55 , C07D281/10
CPC分类号： C07D417/12 , A61K45/06 , C07D281/10 , C07F9/6536
摘要： The present invention relates to compounds of the formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described
摘要翻译：本发明涉及式（I）的化合物：（其中可变基团如本文所定义）其药学上可接受的盐，溶剂合物，这些盐及其前药的溶剂合物及其作为回肠胆汁转运（IBAT）抑制剂用于治疗的用途的高脂血症。还描述了其制备方法和含有它们的药物组合物

6. 发明申请

US20050282839A1 Pyrimidyl phosphonate antiviral compounds and methods of use 审中-公开
标题翻译：嘧啶膦酸酯抗病毒化合物及其使用方法
公开(公告)号：US20050282839A1
公开(公告)日：2005-12-22
申请号：US11033422
申请日：2005-01-11
申请人： Haolun Jin , Choung Kim
发明人： Haolun Jin , Choung Kim
IPC分类号： A61K31/513 , A61K47/48 , C07D239/54 , C07D239/557 , C07F9/38 , C07F9/40 , C07F9/58 , C07F9/6512 , C07F9/6536 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/4006 , A61K47/548 , C07D239/54 , C07D239/557 , C07F9/3808 , C07F9/58 , C07F9/6512 , C07F9/6536 , C07F9/65583 , C07F9/6561
摘要： Pyrimidine I and pyrimidinone II phosphonate compounds and methods for viral inhibition are disclosed. The compounds include at least one phosphonate group covalently attached at any site.
摘要翻译：公开了嘧啶I和嘧啶酮II膦酸盐化合物和病毒抑制方法。所述化合物包括至少一个共价连接在任何位点的膦酸酯基团。

7. 发明授权

US06906058B2 1,5-Benzothiazepines and their use as hypolipidaemics 失效
标题翻译： 1,5-苯并硫氮杂及其作为降血脂药的用途
公开(公告)号：US06906058B2
公开(公告)日：2005-06-14
申请号：US10220877
申请日：2001-03-05
申请人： Ingemar Starke , Mickael Dahlström , David Blomberg
发明人： Ingemar Starke , Mickael Dahlström , David Blomberg
IPC分类号： A61K31/554 , A61K45/00 , A61P1/16 , A61P3/06 , A61P43/00 , C07D281/10 , C07D417/12 , C07F9/6536 , A61K31/662 , C07D401/12
CPC分类号： C07D417/12 , C07D281/10 , C07F9/6536
摘要： The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及其中R 1和R 2独立地选自C 1-6烷基的式（I）化合物; R 4和R 5之一是式（IA）的基团：R 3，R 6， R 7，R 8，R 9，R 10和R 11和R 11和 R 4和R 5中的另一个如本文所定义的药学上可接受的盐，溶剂化物，这些盐和前药的溶剂化物，并且用作回肠胆汁转运（IBAT ）抑制剂用于治疗高脂血症。还描述了其制备方法和含有它们的药物组合物。

8. 发明申请

US20020183307A1 Novel 1,4-benzothiazephine and 1,5-benzothiazepine compounds as inhibitors of apical sodium co-dependent bile acid transport and taurocholate uptake 审中-公开
标题翻译：新型1,4-苯并噻嗪和1,5-苯并硫氮杂化合物作为顶端钠共同依赖性胆汁酸转运和牛磺胆酸摄取抑制剂
公开(公告)号：US20020183307A1
公开(公告)日：2002-12-05
申请号：US09912233
申请日：2001-07-25
发明人： Samuel J. Tremont , Kevin J. Koeller , William L. Neumann
IPC分类号： A61K031/554 , C07D285/36
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D281/10 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/04 , C07F9/6536 , C07F9/65583
摘要： Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject. The compounds of the present invention are apical sodium co-dependent bile acid transport inhibitors and are 1,4-benzothiazepine and 1,5-benzothiazepine compounds corresponding to Formula I: 1 wherein j, m, Y, Z, R1A, R1B, R2A, R2B and R6 are as defined in the specification.
摘要翻译：用于治疗受试者中高脂血症的化合物，药物组合物和方法。本发明化合物是顶端钠依赖性胆汁酸转运抑制剂，是对应于式Ⅰ的1,4-苯并硫氮杂和1,5-苯并硫氮杂化合物：其中j，m，Y，Z，R 1A，R 1B，R 2A， R2B和R6如说明书中所定义。

9. 发明授权

US5817848A Bidentate phosphine ligand 失效
标题翻译：二齿膦配体
公开(公告)号：US5817848A
公开(公告)日：1998-10-06
申请号：US746189
申请日：1996-11-06
申请人： Paulus C. J. Kamer , Mirko Kranenburg , Petrus W. N. M. van Leeuwen , Johannes G. de Vries
发明人： Paulus C. J. Kamer , Mirko Kranenburg , Petrus W. N. M. van Leeuwen , Johannes G. de Vries
IPC分类号： B01J31/24 , C07B61/00 , C07C45/50 , C07C47/02 , C07C67/36 , C07C69/533 , C07C253/10 , C07F9/6527 , C07F9/6533 , C07F9/6536 , C07F9/655 , C07F9/6553 , C07F9/6571 , C07F9/6596 , C07F9/02 , C07F15/00
CPC分类号： B01J31/2452 , B01J31/2457 , C07C253/10 , C07C45/50 , C07C67/36 , C07F9/6527 , C07F9/65335 , C07F9/6536 , C07F9/65522 , C07F9/65527 , C07F9/655372 , C07F9/65539 , C07F9/657163 , C07F9/6596 , B01J2231/32 , B01J2231/321 , B01J2231/4233 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/84
摘要： The invention relates to a bidentate phosphine ligand, the phosphorus atoms of the phosphine being connected via a bridge group, the bridge group of the bidentate phosphine ligand consisting of an ortho-anellated annular system, comprising two aryl groups, which aryl groups are connected by two bridges, the first bridge consisting of an --O-- or an --S-- atom and the second bridge being a group that contains an oxygen, sulphur, nitrogen, silicon or carbon atom or a combination of these atoms, the two phosphorus atoms being connected to the two aryl groups of the bridge group at the ortho-position relative to the --O-- or --S-- atom of the first bridge. The invention also relates to the use of this bidentate phosphium ligand in a catalyst system comprising also a transition metal compound which is used in the following type of reactions: hydroformylation hydrogenation, hydrocyanation, polymerization, isomerisation, carboxylation, cross coupling and metathesis.
摘要翻译：本发明涉及二齿膦配体，磷化氢的磷原子通过桥基连接，二齿膦配体的桥基由正角的环状体组成，包含两个芳基，该芳基通过两个桥，由-O-或-S-原子组成的第一桥，第二桥是含有氧，硫，氮，硅或碳原子或这些原子的组合的基团，两个磷原子是在相对于第一桥的-O-或-S-原子的邻位与桥基的两个芳基连接。本发明还涉及这种双齿磷配体在催化剂体系中的用途，该催化剂体系还包括用于以下类型反应的过渡金属化合物：加氢甲酰化氢化，氢化氰化，聚合，异构化，羧化，交联和复分解。

10. 发明授权

US4870063A Bisphosphonic acid derivatives, their production and use 失效
标题翻译：二膦酸衍生物，其生产和使用
公开(公告)号：US4870063A
公开(公告)日：1989-09-26
申请号：US90980
申请日：1987-08-10
申请人： Ernst T. Binderup , Sven Liisberg
发明人： Ernst T. Binderup , Sven Liisberg
IPC分类号： A61K31/675 , C07F9/6536 , C07F9/6544
CPC分类号： C07F9/6544 , C07F9/6536
摘要： Novel compounds of the formula I ##STR1## in which R.sub.1 -R.sub.11 can be the same or different and stand for hydrogen, a straight or branced aliphatic or alicyclic C.sub.1 -C.sub.10 hydrocarbon radical, an aryl or an aryl-C.sub.1 -C.sub.4 -alkyl radical; n is zero or one, and m is zero, one or two; or R.sub.2 and R.sub.4 when taken together form a saturated aliphatic 5-, 6- or 7-membered ring which may be substituted with one or more C.sub.1 -C.sub.4 alkyl radicals; and pharmaceutically acceptable salts and easily hydroyzable esters thereof, methods for producing said new compounds, pharmaceutical compositions containing the new compounds, dosage units of the compositions, and methods of treating patients using said compositions and dosage units.The present compounds are valuable in the human and veterinary practice by reducing bone resorption and surprisingly also stimulating bone alkaline phosphatase. A substantial increase in bone mass is actually observed during treatment with the present compounds.
摘要翻译： PCT No.PCT / DK86 / 00132 Sec。 371日期1987年8月10日 102（e）日期1987年8月10日PCT提交1986年12月10日PCT公布。第WO87 / 03598号公报日本1987年6月18日。式I的新型化合物（Ⅰ）其中R1-R11可以相同或不同，代表氢，直链或分支的脂族或脂环族C1-C10烃基，芳基或芳基-C 1 -C 4 - 烷基; n为零或一，m为零，一或二; 或者R 2和R 4一起形成可被一个或多个C 1 -C 4烷基取代的饱和脂肪族5-，6-或7-元环; 和其药学上可接受的盐和易于水解的酯，制备所述新化合物的方法，含有新化合物的药物组合物，组合物的剂量单位和使用所述组合物和剂量单位治疗患者的方法。本发明化合物在人和兽医学实践中通过减少骨吸收是有价值的，并且令人惊奇地也刺激骨碱性磷酸酶。实际上在用本发明化合物治疗期间观察到骨质量的显着增加。

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