专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06169183A Process for preparing pyridinecarboxylic esters 失效
标题翻译：制备吡啶羧酸酯的方法
公开(公告)号：US06169183A
公开(公告)日：2001-01-02
申请号：US09238506
申请日：1999-01-27
申请人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
发明人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
IPC分类号： C07D21330
CPC分类号： C07D213/79 , C07D213/61 , C07D213/80
摘要： A process for preparing pyridinecarboxylic esters of the general formula: wherein R1 is hydrogen, a C1-6-alkyl group, a C1-4-alkoxycarbonyl group, a C1-4-alkoxymethyl group or a fluorinated C1-6-alkyl group, R2 is a C1-4-alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacing the corresponding 2,3-dihalopyridines with carbon monoxide and a C1-4-alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
摘要翻译：一种制备通式如下的吡啶羧酸酯的方法：其中R1是氢，C1-6烷基，C1-4烷氧基羰基，C1-4烷氧基甲基或氟化C1-6烷基，R2 是C 1-4 - 烷基，X是氯或溴。吡啶羧酸酯通过在弱碱和钯与双（二苯基膦）的络合物存在下，用一氧化碳和C 1-4链烷醇取代相应的2,3-二卤代吡啶而得到。吡啶羧酸酯是制备除草剂和抗纤维化疾病药物的中间体。

2. 发明授权

US06780997B2 Cardioprotective phosphonates and malonates 失效
标题翻译：心脏保护膦酸盐和丙二酸盐
公开(公告)号：US06780997B2
公开(公告)日：2004-08-24
申请号：US10282328
申请日：2002-10-28
申请人： Wasimul Haque
发明人： Wasimul Haque
IPC分类号： C07D21330
CPC分类号： C07D213/66 , C07D213/65 , C07F9/58 , C07F9/6561
摘要： Pharmaceutical compositions including an effective amount of the compound of formula IV in which R1 is hydrogen or alkyl; R2 is —CHO, —CH2OH, —CH3 or —CO2R5 in which R5 is hydrogen, alkyl, or aryl; or R2 is —CH2O-alkyl- in which alkyl is covalently bonded to the oxygen at the 3-position instead of R1; R3 and R3′ are independently hydrogen or halo; or R3 and R3′ taken together constitute a second covalent bond between the carbons to which they are substituent; and R4 is hydrogen; or a pharmaceutically acceptable acid addition salt thereof, are taught. Also taught are methods of using the compositions, including for the treatment of myocardial infarctions, ischemia, congestive heart failure, arrhythmia, blood clots, hypertrophy, diabetes, insulin resistance, diabetes related damage, and obesity.
摘要翻译：药物组合物，包括有效量的式IV化合物，其中R 1是氢或烷基; R 2是-CHO，-CH 2 OH，-CH 3或-CO 2 R 5，其中R 5是氢，烷基或芳基; 或R 2是-CH 2 O-烷基 - 其中烷基在3-位上与氧共价结合而不是R 1; R 3和R 3'独立地是氢或卤素; 或R 3和R 3'组合在它们所取代的碳之间构成第二共价键; 和R 4是氢;或其药学上可接受的酸加成盐。还教导了使用组合物的方法，包括用于治疗心肌梗塞，缺血，充血性心力衰竭，心律失常，血凝块，肥大，糖尿病，胰岛素抵抗，糖尿病相关损伤和肥胖。

3. 发明授权

US06613784B1 Nitroxyderivatives having antinflammatory, analgesic and antithrombotic activity 失效
标题翻译：具有抗炎，镇痛和抗血栓形成活性的硝基衍生物
公开(公告)号：US06613784B1
公开(公告)日：2003-09-02
申请号：US09926095
申请日：2001-08-30
申请人： Francesca Benedini , Piero Del Soldato
发明人： Francesca Benedini , Piero Del Soldato
IPC分类号： C07D21330
CPC分类号： C07D213/30 , C07D401/12
摘要： Organic or inorganic salts of compounds of general formula: A—X1—N(O)z for use as medicaments having anti-inflammatory, analgesic and antithrombotic activity, wherein A is R(COXu)t wherein t is 0 or 1; u is 0 or 1 and X is O, NH, NR1c wherein R1c us a C1-C10 alkyl and R is, for example, (Ia) wherein R1 is acetoxy, preferably in ortho position with respect to —CO— and R2 is hydrogen or acetylsalicylsalicylic acid derivatives; and X1 is the formula (B), Y being a ring containing at least one salified nitrogen atom.
摘要翻译：用作具有抗炎，镇痛和抗血栓形成活性的药物的通式为A-X1-N（O）z的化合物的有机或无机盐，其中A为R（COXu）t，其中t为0或1; u为0或1，X为O，NH，NR1c，其中R1c为C1-C10烷基，R为例如（Ia），其中R1为乙酰氧基，优选为相对于-CO-的邻位，R2为氢或乙酰水杨基水杨酸衍生物; X1为式（B），Y为含有至少一个成盐氮原子的环。

4. 发明授权

US06506757B1 Carboxylic acid derivatives and drugs containing the same as the active ingredient 失效
标题翻译：羧酸衍生物和含有与活性成分相同的药物
公开(公告)号：US06506757B1
公开(公告)日：2003-01-14
申请号：US09623913
申请日：2000-09-11
申请人： Hisao Tajima , Yoshisuke Nakayama , Daikichi Fukushima
发明人： Hisao Tajima , Yoshisuke Nakayama , Daikichi Fukushima
IPC分类号： C07D21330
CPC分类号： C07D213/30 , A61K31/00 , C07C59/66 , C07C59/68 , C07C59/72 , C07C323/52 , C07D213/65 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/24 , C07D317/54 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
摘要： A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.
摘要翻译：含有式（I）的羧酸衍生物（其中所有符号如说明书中所定义），其无毒性酸或其水合物作为活性成分的过氧化物酶体增殖物激活受体调节剂。由于具有调节PPAR的作用，式（I）化合物可用作降血糖剂，降血脂药，用于代谢紊乱（糖尿病，肥胖症，综合征X，高胆固醇血症，高脂蛋白血症）的疾病的预防和/或补救措施等），高脂血症，动脉粥样硬化，高血压，循环系统疾病，暴饮暴食，冠心病等，HDL胆固醇升高剂，LDL胆固醇和/或VLDL胆固醇降低剂和用于缓解危险因素的药物疾病或综合征X.

5. 发明授权

US06376677B1 Process for the preparation of nicotinic acid 有权
标题翻译：制备烟酸的方法
公开(公告)号：US06376677B1
公开(公告)日：2002-04-23
申请号：US09597244
申请日：2000-06-20
申请人： Roderick J. Chuck , Uwe Zacher
发明人： Roderick J. Chuck , Uwe Zacher
IPC分类号： C07D21330
CPC分类号： C07D213/803
摘要： Nicotinic acid is produced from aqueous solutions of ammonium nicotinate by spray-drying. The nicotinic acid can be freed from residual ammonium nicotinate by a thermal post-treatment in a fluidized bed or under reduced pressure. The process is suitable in particular for the work-up of the reaction mixture produced in the oxidation of 3-methylpyridine with atmospheric oxygen, with the ammonia and, if appropriate, the water, being able to be recycled. Nicotinic acid (“vitamin PP”) is an important additive to foodstuffs and feedstuffs.
摘要翻译：烟酸通过喷雾干燥由烟酸铵的水溶液产生。通过在流化床中或减压下的热后处理，烟酸可以从残留的烟酸铵中除去。该方法特别适用于在3-甲基吡啶与大气氧气氧化反应生成的反应混合物中，与氨和适当的水一起被回收利用。烟酸（“维生素PP”）是食品和饲料的重要添加剂。

6. 发明授权

US06337305B1 Substituted 2-benz(o)ylpyridines, their preparation and their use as herbicides 失效
标题翻译：取代的2-苯并（o）吡啶，其制备及其作为除草剂的用途
公开(公告)号：US06337305B1
公开(公告)日：2002-01-08
申请号：US09381033
申请日：1999-09-15
申请人： Peter Schäfer , Gerhard Hamprecht , Markus Menges , Olaf Menke , Michael Rack , Cyrill Zagar , Karl-Otto Westphalen , Ulf Misslitz , Helmut Walter
发明人： Peter Schäfer , Gerhard Hamprecht , Markus Menges , Olaf Menke , Michael Rack , Cyrill Zagar , Karl-Otto Westphalen , Ulf Misslitz , Helmut Walter
IPC分类号： C07D21330
CPC分类号： C07D213/61 , A01N43/40
摘要： Substituted 2-benz(o)ylpyridines I and salts thereof where n=0, 1; X=CO, CH2, CH(C1-C4-alkyl), CH—OH, CH—CN, CH-halogen, C(halogen)2, CH—CONH2, CH—CO—O(C1-C4-alkyl), CH—O(C1-C4-alkyl), C(CN)(C1-C4-alkyl); R1=halogen, C1-C4-haloalkyl, C1-C4-alkylthio, C1-C4-alkylsulfinyl, C1-C4-alkylsulfonyl; R2=H, halogen; R3=H, NO2, OH, halogen, C1-C4-alkoxy; R4=H, NO2, OH, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy; R5=H, NO2, CN, halogen, C1-C8-alkyl, C3-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C1-C8-haloalkyl, C2-C8-haloalkenyl, C2-C8-haloalkinyl, C1-C4-alkoxy-C1-C4-alkyl, C2-C4-alkenyloxy-C1-C4-alkyl, C2-C4-alkynyloxy-C1-C4-alkyl, C1-C4-alkylthio-C1-C4-alkyl, C1-C4-alkylsulfinyl-C1-C4-alkyl, C1-C4-alkylsulfonyl-C1-C4-alkyl, cyano-C1-C8-alkyl, cyano-C2-C8-alkenyl, cyano-C3-C8-alkynyl, unsubstituted or substituted OH, SH, SO—H, —SO2—H, COOH or NH—COOH, —SO2Cl, —N(R9,R10), —NH—SO2—(C1-C8-alkyl), —N[—SO2—(C1-C8-alkyl)]2, —N(C1-C8-alkyl)[—SO2—(C1-C8-alkyl)], —SO2—N(R9,R10), —O—CO—NH—R9, unsubstituted or substituted CHO, —O—CHO or —NH—CHO, —NH—CO—NH—R9, —O—CS—NH2, —O—CS—N(C1-C8-alkyl)2, —CO—N(R9,R10), —CS—N(R9,R10), —CO—NH—SO2—(C1-C4-alkyl).
摘要翻译：取代的2-苯并（o）吡啶I和其中n = 0,1; X = CO，CH 2，CH（C 1 -C 4 - 烷基），CH-OH，CH-CN，CH-卤素，C（卤素） CH-CONH 2，CH-CO-O（C 1 -C 4 - 烷基），CH-O（C 1 -C 4 - 烷基），C（CN）（C 1 -C 4 - 烷基）; R 1 =卤素，C 1 -C 4卤代烷基， C 1 -C 4烷硫基，C 1 -C 4烷基亚磺酰基，C 1 -C 4烷基磺酰基; R 2 = H，卤素; R 3 = H，NO 2，OH，卤素，C 1 -C 4 - 烷氧基; R 4 = H，NO 2，OH，卤素， C 1 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 1 -C 4 - 烷氧基; R 5 = H，NO 2，CN，卤素，C 1 -C 8烷基，C 3 -C 8 - 烯基，C 3 -C 8炔基，C 3 -C 8 - 环烷基，C 1 -C 8 - 卤代烷基，C 2 -C 8 - 卤代烯基，C 2 -C 8 - 卤代炔基，C 1 -C 4 - 烷氧基-C 1 -C 4烷基，C 2 -C 4 - 烯氧基-C 1 -C 4烷基，C 2 -C 4 - C 1 -C 4烷基，C 1 -C 4烷硫基-C 1 -C 4烷基，C 1 -C 4烷基亚磺酰基-C 1 -C 4烷基，C 1 -C 4烷基磺酰基-C 1 -C 4 - 烷基，氰基-C 1 -C 8烷基，氰基-C 2 -C 8 - 烯基，氰基-C 3 -C 8 - 炔基，未取代或取代的OH，SH，SO-H，-SO 2 -H，COOH或NH-COOH，-SO 2 Cl，-N（R 9，R 10） NH-SO 2 - （C 1 -C 8 - 烷基），-N [-SO 2 - （C 1 -C 8 - 烷基）] 2，-N（C 1 -C 8 - 烷基） -SO 2 -N（R 9，R 10），-O-CO-NH-R 9，未取代的取代的CHO，-O-CHO或-NH-CHO，-NH-CO-NH-R9，-O-CS-NH2，-O-CS-N（C1-

7. 发明授权

US06455701B1 Substituted diaryl or diheteroaryl methanes, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity 失效
标题翻译：取代的二芳基或二杂芳基甲烷，具有类视黄醇激动剂，拮抗剂或反向激动剂型生物活性的醚和胺
公开(公告)号：US06455701B1
公开(公告)日：2002-09-24
申请号：US09708972
申请日：2000-11-08
申请人： Tae K. Song , Min Teng , Roshantha A. Chandraratna
发明人： Tae K. Song , Min Teng , Roshantha A. Chandraratna
IPC分类号： C07D21330
CPC分类号： C07D213/80 , C07C65/28 , C07C69/94 , C07C205/38 , C07C235/56 , C07C247/16
摘要： Compounds of the formula Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
摘要翻译：符号具有本说明书中定义的含义的化合物具有类视黄醇，维生素A拮抗剂或类视黄醇反向激动剂型生物活性。

8. 发明授权

US06388086B1 Process for production of 3-(3-pyridyl)-1-propanol derivatives 失效
标题翻译： 3-（3-吡啶基）-1-丙醇衍生物的制备方法
公开(公告)号：US06388086B1
公开(公告)日：2002-05-14
申请号：US09631678
申请日：2000-08-02
申请人： Akira Nishiyama , Kazumi Okuro , Kenji Inoue
发明人： Akira Nishiyama , Kazumi Okuro , Kenji Inoue
IPC分类号： C07D21330
CPC分类号： C07D213/30
摘要： A process for producing a 3-(3-pyridyl)-1-propanol derivative of use as a pharmaceutical intermediate expediently with an inexpensive material is provided. The process is concerned with a 3-(3-pyridyl)-1-propanol derivative (3): in the formula, R1 represents an alkyl group of 1 to 20 carbon atoms, aryl group of 6 to 20 carbon atoms or aralkyl group of 7 to 20 carbon atoms, which may be substituted, and comprises reacting a 3-methylpyridine with a strong base to prepare a 3-methylpyridine metal (1): in the formula, M represents lithium, sodium, potassium or a magnesium halide, where the halide is chloride or bromide, and then reacting said metal salt with an epoxy compound (2):
摘要翻译：提供了以便宜的材料制备用作药物中间体的3-（3-吡啶基）-1-丙醇衍生物的方法。该方法涉及3-（3-吡啶基）-1-丙醇衍生物（3）：式中，R1表示碳原子数为1〜20的烷基，碳原子数为6〜20的芳基或芳烷基可以被取代的7至20个碳原子，并且使3-甲基吡啶与强碱反应以制备3-甲基吡啶金属（1）：在该式中，M表示锂，钠，钾或卤化镁，其中卤化物是氯化物或溴化物，然后使所述金属盐与环氧化合物（2）反应：

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式