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91. 发明申请

US20090305891A1 CYCLOALKYLPHENYL SUBSTITUTED CYCLIC KETOENOLS 有权
标题翻译：环丙基苯酚取代的环状酮
公开(公告)号：US20090305891A1
公开(公告)日：2009-12-10
申请号：US12280277
申请日：2007-02-08
申请人： Reiner Fischer , Thomas Bretschneider , Stefan Lehr , Dieter Feucht , Eva-Maria Franken , Olga Malsam , Alfred Angermann , Guido Bojack , Christian Arnold , Martin Jeffrey Hills , Heinz Kehne , Christopher Hugh Rosinger
发明人： Reiner Fischer , Thomas Bretschneider , Stefan Lehr , Dieter Feucht , Eva-Maria Franken , Olga Malsam , Alfred Angermann , Guido Bojack , Christian Arnold , Martin Jeffrey Hills , Heinz Kehne , Christopher Hugh Rosinger
IPC分类号： A01N43/42 , A01N43/36 , A01P7/00 , A01P13/00 , A01N43/26 , A01N43/56 , C07D487/04 , C07D209/54 , C07D207/38 , C07D307/94 , C07C255/32 , C07C321/20 , C07C243/18 , C07C229/34 , C07C69/738 , C07C69/73 , C07C69/616 , C07C69/612 , C07C57/03 , C07C57/34 , C07C49/88
CPC分类号： C07C233/51 , A01N37/10 , A01N37/46 , A01N43/16 , A01N43/36 , A01N43/38 , A01N43/90 , A01N47/06 , C07C69/616 , C07C2601/02 , C07D207/36 , C07D209/54 , C07D231/54 , C07D307/60
摘要： The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
摘要翻译：本公开涉及其中J，X，Y，m和CKE如上所定义的式（I）的新型环烷基苯基取代的环戊酮类，其制备方法和中间体及其作为农药和/或除草剂的用途。此外，本公开涉及选择性除草组合物，其包含首先是环烷基苯基取代的环酮酮醇，其次是作物植物相容性改善化合物。本公开还涉及增加包含式（I）化合物的作物保护组合物的活性，通过加入铵或鏻盐，如果合适的话，增加渗透剂。

92. 发明授权

US07605178B2 Therapeutic compounds 有权
标题翻译：治疗化合物
公开(公告)号：US07605178B2
公开(公告)日：2009-10-20
申请号：US11774411
申请日：2007-07-06
申请人： David W. Old , Vinh X. Ngo
发明人： David W. Old , Vinh X. Ngo
IPC分类号： A61K47/14 , A61K31/5575 , C07C69/612
CPC分类号： C07C323/55 , C07C229/32 , C07C233/50 , C07C2601/08 , C07D213/70 , C07D213/74 , C07D215/26 , C07D215/40 , C07D217/04 , C07D257/04 , C07D277/56 , C07D307/64 , C07D307/68 , C07D307/79 , C07D333/34 , C07D333/38 , C07D333/62
摘要： Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：本文公开了下式的化合物，还公开了与之相关的治疗方法，组合物和药物。

93. 发明申请

US20090076142A1 USE OF THE IRRITATING PRINCIPAL OLEOCANTHAL IN OLIVE OIL, AS WELL AS STRUCTURALLY AND FUNCTIONALLY SIMILAR COMPOUNDS 审中-公开
标题翻译：在橄榄油中使用主要的主要成分，如结构和功能类似化合物
公开(公告)号：US20090076142A1
公开(公告)日：2009-03-19
申请号：US11913729
申请日：2006-05-09
申请人： Qiang Han , Amos B. Smith, III , Gary K. Beauchamp , Paul A.S. Breslin , Russell S.J. Keast , Jianming Lin
发明人： Qiang Han , Amos B. Smith, III , Gary K. Beauchamp , Paul A.S. Breslin , Russell S.J. Keast , Jianming Lin
IPC分类号： A61K31/216 , C07C69/612 , A23L1/226 , C40B30/04 , A61P25/28 , A01P17/00 , A61P31/04 , C12Q1/68 , A23L1/48 , C12N9/99
CPC分类号： C07C67/56 , A61K31/222 , C07C67/313 , C07C67/58 , C07C69/738
摘要： The invention provides methods of synthesizing the purified enantiomers of oleocanthal. The invention further provides methods of using oleocanthals in various formulations including, food additives; pharmaceuticals; cosmetics; animal repellants; and discovery tools for mammalian irritation receptor genes, gene products, alleles, splice variants, alternate transcripts and the like.
摘要翻译：本发明提供合成油甘油的纯化对映异构体的方法。本发明还提供在各种制剂中使用油酸的方法，包括食品添加剂; 药品; 化妆品动物驱避剂; 和用于哺乳动物刺激受体基因，基因产物，等位基因，剪接变体，替代转录物等的发现工具。

94. 发明授权

US07074826B2 R-NSAID esters and their use 失效
标题翻译： R-NSAID酯及其用途
公开(公告)号：US07074826B2
公开(公告)日：2006-07-11
申请号：US10678430
申请日：2003-10-03
申请人： William J. Wechter , Elaine Benaksas Schwartz
发明人： William J. Wechter , Elaine Benaksas Schwartz
IPC分类号： A61K31/341 , A61K31/216 , C07D307/62 , C07C69/612
CPC分类号： C07D405/04 , C07D307/62 , C07D405/12 , C07D409/12 , C07D413/12 , C07D487/04 , C07D491/04
摘要： The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.
摘要翻译：本发明涉及基本上不含S-对映异构体的非甾族抗炎药的R-对映体的酯。本发明的化合物可用于治疗哺乳动物的疾病或疾病。为此，将含有上述化合物或其药学上可接受的盐形成的组合物以足以引发化学预防作用或化学保护作用或治疗效果或预防效果的量施用给哺乳动物。

95. 发明申请

US20050267167A1 Pentanoic acid derivatives 失效
公开(公告)号：US20050267167A1
公开(公告)日：2005-12-01
申请号：US11192002
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/20 , A61K31/00 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/23 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/00 , A61P25/04 , A61P25/28 , A61P43/00 , C07B61/00 , C07C51/06 , C07C51/36 , C07C53/126 , C07C53/128 , C07C53/134 , C07C53/19 , C07C53/21 , C07C53/23 , C07C57/03 , C07C57/30 , C07C59/125 , C07C59/135 , C07C59/68 , C07C67/303 , C07C69/02 , C07C69/22 , C07C69/24 , C07C69/34 , C07C69/533 , C07C69/612 , C07C69/63 , C07C69/708 , C07C231/12 , C07C233/05 , C07C233/07 , C07C233/11 , C07C233/12 , C07C233/22 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/54 , C07C323/52 , C07D213/40 , C07D213/72 , C07D213/75 , C07D295/18 , C07D295/185
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m— or F3C—CH2—, (ii) alkyl subsstituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).

96. 发明申请

US20050215794A1 Copper-catalyzed formation of carbon heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳杂原子和碳 - 碳键
公开(公告)号：US20050215794A1
公开(公告)日：2005-09-29
申请号：US11028500
申请日：2005-01-04
申请人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
发明人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
IPC分类号： B01J31/26 , C07B37/04 , C07B41/04 , C07B43/04 , C07B61/00 , C07C41/16 , C07C41/24 , C07C43/15 , C07C43/20 , C07C43/23 , C07C45/68 , C07C45/71 , C07C49/84 , C07C51/353 , C07C59/64 , C07C67/343 , C07C69/612 , C07C209/10 , C07C211/48 , C07C211/53 , C07C211/54 , C07C213/02 , C07C213/08 , C07C215/16 , C07C215/70 , C07C217/48 , C07C217/82 , C07C221/00 , C07C227/08 , C07C227/18 , C07C229/56 , C07C231/08 , C07C231/12 , C07C233/07 , C07C233/25 , C07C233/40 , C07C233/51 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C233/81 , C07C237/40 , C07C241/04 , C07C243/38 , C07C249/02 , C07C249/16 , C07C251/18 , C07C251/86 , C07C253/14 , C07C253/30 , C07C255/23 , C07C269/06 , C07C271/28 , C07C273/18 , C07C275/32 , C07C277/08 , C07C279/18 , C07C281/02 , C07C303/38 , C07C311/21 , C07C319/20 , C07C323/41 , C07D205/08 , C07D207/16 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/32 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/65 , C07D213/74 , C07D215/38 , C07D221/12 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/34 , C07D233/58 , C07D235/06 , C07D235/08 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D273/08 , C07D295/02 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07D521/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/4056 , C07B37/04 , C07B41/04 , C07B43/04 , C07C41/16 , C07C45/68 , C07C45/71 , C07C51/353 , C07C67/343 , C07C209/10 , C07C213/08 , C07C221/00 , C07C227/18 , C07C231/08 , C07C231/12 , C07C241/04 , C07C249/02 , C07C249/16 , C07C253/14 , C07C253/30 , C07C269/06 , C07C273/1854 , C07C277/08 , C07C281/02 , C07C303/38 , C07C319/20 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/08 , C07D207/16 , C07D207/267 , C07D207/27 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/74 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D235/06 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07C49/84 , C07C59/68 , C07C69/76 , C07C69/65 , C07C69/612 , C07C69/734 , C07C69/616 , C07C69/732 , C07C311/21 , C07C323/41 , C07C211/48 , C07C211/52 , C07C211/55 , C07C211/54 , C07C215/68 , C07C217/84 , C07C215/16 , C07C225/22 , C07C217/08 , C07C229/56 , C07C229/60 , C07C211/58 , C07C243/38 , C07C251/86 , C07C43/205 , C07C43/2055 , C07C43/235 , C07C43/23 , C07C43/16 , C07C43/215 , C07C43/225 , C07C237/30 , C07C255/58 , C07C233/07
摘要： The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.
摘要翻译：本发明涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在酰胺或胺部分的氮原子与芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在另外的实施方案中，本发明涉及在酰基肼的氮原子和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在其它实施方案中，本发明涉及在含氮杂芳族化合物（例如吲哚，吡唑和吲唑）的氮原子与芳基，杂芳基的活性炭之间形成碳 - 氮键的铜催化方法，或乙烯基卤化物或磺酸盐。在某些实施方案中，本发明涉及在醇的氧原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氧键的铜催化方法。本发明还涉及在包含亲核性碳原子的反应物（例如烯醇化物或丙二酸酯阴离子）和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。重要的是，由于催化剂所含的铜的低成本，本发明的所有方法都相对便宜。

97. 发明授权

US06921835B2 Cyclic amino acids and derivatives thereof useful as pharmaceutical agents 失效
公开(公告)号：US06921835B2
公开(公告)日：2005-07-26
申请号：US10448834
申请日：2003-05-30
申请人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
发明人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： A61P1/04 , A61K20060101 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/215 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07C20060101 , C07C61/04 , C07C61/06 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/00 , C07C229/28 , C07C229/32 , C07C229/34 , C07D209/96 , C07D221/20 , C07D307/94 , C07D311/96
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.

98. 发明授权

US06888032B2 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US06888032B2
公开(公告)日：2005-05-03
申请号：US10631480
申请日：2003-07-31
申请人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
发明人： Stephen L. Buchwald , Artis Klapars , Fuk Y. Kwong , Eric R. Streiter , Jacopo Zanon
IPC分类号： C07D333/38 , C07B39/00 , C07B61/00 , C07C17/20 , C07C21/17 , C07C25/02 , C07C25/18 , C07C45/63 , C07C49/807 , C07C51/363 , C07C57/60 , C07C67/307 , C07C69/612 , C07C201/12 , C07C205/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/53 , C07C255/54 , C07C255/55 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/60 , C07C303/40 , C07C311/16 , C07C319/14 , C07C321/28 , C07C321/30 , C07C323/09 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/32 , C07C323/37 , C07C323/56 , C07C323/62 , C07D207/267 , C07D209/08 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/85 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/10 , C07D271/107 , C07D307/68 , C07D333/62 , C07D333/68 , C07C319/04
CPC分类号： C07D213/70 , C07B39/00 , C07C17/208 , C07C45/63 , C07C51/363 , C07C67/307 , C07C201/12 , C07C231/12 , C07C233/15 , C07C253/14 , C07C253/30 , C07C255/53 , C07C303/40 , C07C319/14 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/18 , C07D215/54 , C07D231/14 , C07D271/107 , C07D333/62 , C07D333/68 , C07C25/18 , C07C21/17 , C07C25/02 , C07C49/807 , C07C57/60 , C07C69/65 , C07C323/62 , C07C323/37 , C07C323/32 , C07C323/22 , C07C323/20 , C07C323/12 , C07C323/09 , C07C321/28 , C07C311/16 , C07C255/35 , C07C255/50 , C07C255/52 , C07C255/54 , C07C255/57 , C07C255/58 , C07C205/12
摘要： One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodient of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
摘要翻译：本发明的一个方面涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在硫醇部分的硫原子和芳基，杂芳基或乙烯基卤化物或磺酸酯的活性炭之间形成碳 - 硫键的铜催化方法。在其它实施方案中，本发明涉及在酰胺的氮原子和芳基，杂芳基或卤化乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜（II）催化方法。在某些实施方案中，本发明涉及在氰化物离子的碳原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。在另一个实施方案中，本发明涉及将芳基，杂芳基或氯乙烯或溴化物转化为相应的芳基，杂芳基或碘乙烯的铜催化方法。本发明的另一个实施方案涉及串联方法，其可以在单个反应容器中实施，其中该方法的第一步骤涉及从相应的芳基铜催化形成芳基，杂芳基或乙烯基碘，杂芳基或氯乙烯或溴化物; 并且该方法的第二步涉及在第一步中形成的芳基，杂芳基或乙烯基腈，酰胺或硫化物从芳基，杂芳基或乙烯基碘形成铜催化的形成。

99. 发明授权

US6111133A Process for preparing substituted styrenes 失效
标题翻译：制备取代苯乙烯的方法
公开(公告)号：US6111133A
公开(公告)日：2000-08-29
申请号：US950388
申请日：1992-09-23
申请人： Francis Michael Houlihan
发明人： Francis Michael Houlihan
IPC分类号： C07C37/01 , C07C39/20 , C07C41/16 , C07C43/215 , C07C67/10 , C07C67/14 , C07C68/06 , C07C69/017 , C07C69/618 , C07C69/63 , C07C69/773 , C07C69/96 , C07C303/26 , C07C303/28 , C07C309/66 , C07C69/612
CPC分类号： C07C303/28 , C07C69/017 , C07C69/96
摘要： Substituted styrenes are synthesized by a simple, low temperature technique. A protected phenol styrene is reacted with an acid anhydride, dicarbonate, a halogen substituted alkyl, or an acid chloride in the presence of base to form a carbonyl substituted styrene. Unexpected yield decrease due to distillation is avoided because the product is sufficiently pure to be used without such distillation.
摘要翻译：取代的苯乙烯通过简单的低温技术合成。在碱的存在下，将保护的苯酚苯乙烯与酸酐，二碳酸酯，卤素取代的烷基或酰氯反应，形成羰基取代的苯乙烯。由于产物足够纯以便在没有蒸馏的情况下使用，所以避免了因蒸馏而产生的意外的产量下降。

100. 发明授权

US6100271A Therapeutic compounds containing xanthinyl 失效
标题翻译：含有黄原素的治疗化合物
公开(公告)号：US6100271A
公开(公告)日：2000-08-08
申请号：US483871
申请日：1995-06-07
申请人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
IPC分类号： C07D239/54 , A61K31/42 , A61K31/421 , A61K31/496 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/10 , A61P9/14 , A61P11/16 , A61P13/02 , A61P15/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07C47/198 , C07C47/277 , C07C49/175 , C07C49/255 , C07C57/46 , C07C59/64 , C07C65/21 , C07C69/06 , C07C69/14 , C07C69/24 , C07C69/608 , C07C69/612 , C07C225/06 , C07C233/01 , C07D239/56 , C07D241/18 , C07D263/30 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D513/04 , C07D521/00
CPC分类号： C07D487/04 , C07D473/04 , C07D473/06 , C07D473/10 , C07D513/04
摘要： Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyallyl; --A(R.sub.5).sub.m, A being N or O, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.
摘要翻译：具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中：或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟基烯基; -A（R5）m，A是N或O，m是一个或两个，R5是氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

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