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2. 发明申请

US20100035999A1 Additives and products includings oligoesters 有权
标题翻译：添加剂和产品包括低聚物
公开(公告)号：US20100035999A1
公开(公告)日：2010-02-11
申请号：US12586442
申请日：2009-09-22
申请人： Abel G. Pereira , Helena S. Barinova , Christopher Westergom
发明人： Abel G. Pereira , Helena S. Barinova , Christopher Westergom
IPC分类号： A61K47/00 , C07C233/12
CPC分类号： A61Q15/00 , A61K8/45 , A61K8/585 , A61Q5/02 , A61Q5/12 , A61Q17/04
摘要： The present invention relates to oligoesters and their use for the creation of additives. Oligoester containing additives and/or oligoesters themselves may be used for formulating pharmaceutical preparations, cosmetics or personal care products such as shampoos and conditioners. These oligoesters are particularly useful for the creation of multi-purpose additives that can impart conditioning, long substantivity and/or UV protection. Individual oligoesters and oligoester mixtures are described.
摘要翻译：本发明涉及低聚酯及其用于产生添加剂的用途。含有添加剂和/或低聚酯本身的低聚酯本身可用于配制药物制剂，化妆品或个人护理产品如洗发剂和调理剂。这些低聚酯特别可用于产生可赋予调理性，长时间亲和性和/或紫外线防护的多用途添加剂。描述了单独的低聚酯和低聚酯混合物。

3. 发明授权

US07256307B2 Substituted phenypropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor α(PPAR) 失效
标题翻译：取代的苯丙酸衍生物作为人类过氧化物酶体增殖物激活受体α（PPAR）的激动剂
公开(公告)号：US07256307B2
公开(公告)日：2007-08-14
申请号：US10499378
申请日：2002-12-18
申请人： Eva-lotte Alstermark Lindstedt , Anna Christina Olsson , Lanna Li
发明人： Eva-lotte Alstermark Lindstedt , Anna Christina Olsson , Lanna Li
IPC分类号： C07C229/00 , C07C233/12
CPC分类号： A61K31/16 , A61K31/195 , A61K45/06 , C07C235/20 , C07C2601/14 , Y02P20/55 , A61K2300/00
摘要： The present invention provides the S enantiomer of a compound of formula (I); wherein R1 represents 2,4-difluorophenyl or cyclohexyl as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明提供式（I）化合物的S对映异构体; 其中R 1表示2,4-二氟苯基或环己基以及其药学上可接受的盐，溶剂合物，结晶形式和前药，用于制备这些化合物的方法，用于治疗临床病症包括脂质无论是否与胰岛素抵抗相关的疾病（血脂异常），其治疗用途的方法和含有它们的药物组合物。

4. 发明授权

US06972295B2 Substituted amides 有权
标题翻译：取代酰胺
公开(公告)号：US06972295B2
公开(公告)日：2005-12-06
申请号：US10387265
申请日：2003-03-12
申请人： William K. Hagmann , Linus S. Lin , Shrenik K. Shah , Ravindra N. Guthikonda , Hongbo Qi , Linda L. Chang , Ping Liu , Helen M. Armstrong , James P. Jewell , Thomas J. Lanza, Jr.
发明人： William K. Hagmann , Linus S. Lin , Shrenik K. Shah , Ravindra N. Guthikonda , Hongbo Qi , Linda L. Chang , Ping Liu , Helen M. Armstrong , James P. Jewell , Thomas J. Lanza, Jr.
IPC分类号： A61K31/165 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/405 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4436 , A61K31/445 , A61K31/4453 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/5377 , A61K31/553 , A61P1/04 , A61P1/10 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/24 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/10 , A61P17/00 , A61P19/02 , A61P19/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , C07C233/12 , C07C233/13 , C07C235/06 , C07C235/18 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C237/06 , C07C255/55 , C07C255/60 , C07C271/14 , C07C271/22 , C07C275/30 , C07C311/03 , C07C323/41 , C07D207/27 , C07D209/08 , C07D209/34 , C07D209/52 , C07D209/94 , C07D211/34 , C07D213/36 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/89 , C07D215/06 , C07D231/12 , C07D233/36 , C07D233/70 , C07D233/80 , C07D237/14 , C07D237/28 , C07D237/32 , C07D239/34 , C07D249/04 , C07D249/08 , C07D249/12 , C07D249/18 , C07D261/08 , C07D261/20 , C07D263/58 , C07D267/14 , C07D277/20 , C07D277/30 , C07D277/36 , C07D277/64 , C07D277/74 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/15 , C07D401/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D513/04 , C07D521/00 , A61K31/4412 , C07D213/70
CPC分类号： C07D213/64 , C07C233/13 , C07C235/06 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C237/06 , C07C255/55 , C07C255/60 , C07C271/14 , C07C271/22 , C07C275/30 , C07C311/03 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D209/34 , C07D209/94 , C07D211/34 , C07D213/65 , C07D213/68 , C07D215/06 , C07D231/12 , C07D233/56 , C07D233/70 , C07D237/28 , C07D237/32 , C07D239/34 , C07D249/04 , C07D249/08 , C07D249/12 , C07D263/58 , C07D267/14 , C07D277/30 , C07D277/36 , C07D295/13 , C07D295/15 , C07D513/04
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗物质滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

5. 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).

6. 发明授权

US5399759A Process for conducting chemical reactions with formaldehyde 失效
标题翻译：与甲醛进行化学反应的方法
公开(公告)号：US5399759A
公开(公告)日：1995-03-21
申请号：US872775
申请日：1992-04-22
申请人： Gilbert Rodriguez
发明人： Gilbert Rodriguez
IPC分类号： C07C47/045 , C07C41/56 , C07C231/10 , C07C233/66 , C07C249/02 , C07C251/04 , C07C233/12
CPC分类号： C07C41/56 , C07C231/10 , C07C249/02
摘要： A formaldehyde reactant is provided to a chemical process or reaction, in the form of a formaldehyde-alcohol complex, by contacting paraformaldehyde with from about 0.25 to about 3 mole equivalents of an aliphatic alcohol in the presence of a catalytic amount of a base. In a preferred embodiment the chemical process is a process for the production of an aromatic azomethine by reaction of an aniline with formaldehyde. The azomethine may then be used to produce a haloacetanilide.
摘要翻译：通过在催化量的碱存在下，将多聚甲醛与约0.25至约3摩尔当量的脂族醇接触，将甲醛反应物以甲醛 - 醇络合物的形式提供给化学过程或反应。在优选的实施方案中，化学方法是通过苯胺与甲醛的反应来生产芳族偶氮甲碱的方法。然后可以使用偶氮甲碱来制备卤代乙酰苯胺。

8. 发明授权

US5331099A Process for preparing p-nitroaromatic amides and products thereof 失效
标题翻译：对硝基芳族酰胺及其制备方法
公开(公告)号：US5331099A
公开(公告)日：1994-07-19
申请号：US45309
申请日：1993-04-16
申请人： Michael K. Stern , James K. Bashkin
发明人： Michael K. Stern , James K. Bashkin
IPC分类号： C07C209/50 , C07C209/36 , C07C209/62 , C07C211/50 , C07C211/51 , C07C211/52 , C07C231/08 , C07C231/12 , C07C233/12 , C07C233/56 , C07C233/64 , C07C233/65 , C07C233/66 , C07C233/80 , C07C235/56 , C07C237/40
CPC分类号： C07C231/08 , C07C209/62 , Y02P20/582
摘要： A process for preparing p-nitroaromatic amides is provided which comprises contacting an amide and nitrobenzene in the presence of a suitable solvent system, and reacting the amide and nitrobenzene in the presence of a suitable base and a controlled amount of protic material at a suitable temperature in a confined reaction zone. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide starting material which can be recycled or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the amide starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine. The p-nitroaromatic amide can be reacted with ammonia under conditions which produce the corresponding p-nitroaromatic amine and the amide starting material which can be recycled or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-nitroaromatic amine and the acid or salt thereof corresponding to the amide starting material. In one embodiment, the p-nitroaromatic amine is reduced to produce p-aminoaromatic amine. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine. In another embodiment, the p-nitroaromatic amine is reductively alkylated to produce p-aminoaromatic amine.
摘要翻译：提供了制备对硝基芳族酰胺的方法，其包括在合适的溶剂体系存在下使酰胺和硝基苯接触，并在合适的碱和受控量的质子物质的存在下，在合适的温度下使酰胺和硝基苯反应在一个有限的反应区。本发明的对硝基芳族酰胺可以还原成对氨基芳族酰胺。在一个实施方案中，在产生相应的对氨基芳香胺和酰胺起始物质的条件下，对氨基芳香酰胺进一步与氨反应，所述对氨基芳族胺和酰胺起始物质可在合适的碱性或酸性催化剂存在下在可生产相应的对氨基芳香胺及其对应于酰胺起始原料的酸或其盐。在另一个实施方案中，将对氨基芳族胺还原烷基化以产生烷基化的对氨基芳族胺。在产生相应的对硝基芳族胺和酰胺起始物质的条件下，对硝基芳族酰胺可以与氨反应，所述对硝基芳族胺和酰胺原料可以在合适的碱性或酸性催化剂存在下再循环或与水反应，硝基芳族胺及其对应于酰胺起始原料的酸或其盐。在一个实施方案中，还原对硝基芳族胺以产生对氨基芳族胺。在另一个实施方案中，将对氨基芳族胺还原烷基化以产生烷基化的对氨基芳族胺。在另一个实施方案中，对硝基芳族胺被还原烷基化以产生对氨基芳族胺。

9. 发明授权

US5326755A Certain 2,4-pentadienamide pestacides 失效
标题翻译：某些2,4-戊二烯酰胺类杀虫剂
公开(公告)号：US5326755A
公开(公告)日：1994-07-05
申请号：US923970
申请日：1992-09-10
申请人： Robert J. Blade , George S. Cockerill
发明人： Robert J. Blade , George S. Cockerill
IPC分类号： A01N37/18 , A01N37/28 , A01N43/40 , A01N49/00 , A01N55/10 , A01P7/02 , A01P7/04 , C07C233/09 , C07C233/13 , C07C233/22 , C07C233/91 , C07C313/28 , C07D213/71 , C07F7/10 , A01N55/00 , C07C233/12 , C07C222/47
CPC分类号： A01N49/00 , C07C233/91 , C07C313/28 , C07D213/71 , C07C2101/02
摘要： The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-5 alkylcarbonyl or aryl or CO.sub.2 R.sup.9 where R.sup.9 is an C.sub.1-4 alkyl or aryl, and a is 1 or 2;(B) --CR.sup.15 R.sup.16 X.sup.3 R.sup.17 where R.sup.15 and R.sup.16 are hydrogen or C.sub.1-4 alkyl, X.sup.3 is oxygen or sulphur and R.sup.17 is C.sub.1-4 alkyl, C.sub.1-5 alkylcarbonyl or aralkylcarbonyl R.sup.17,R.sup.15 X.sup.3, their preparation, pesticidal compositions containing them and their use against pests.
摘要翻译： PCT No.PCT / GB91 / 00539 Sec。 371日期：1992年9月10日 102（e）日期1992年9月10日PCT 1991年4月8日PCT PCT。 WO91 / 16301 PCT出版物 1991年10月31日。本申请公开了式I的杀虫活性化合物：QQ1CR1 = CR2CR3 = CR4C（= X1）NR5R6或其盐，其中Q为单环芳环，或Q为二卤代乙烯基或基团 R7-C = C-，其中R7是C1-4烷基，三C1-4烷基甲硅烷基，卤素或氢; Q1是任选被一个或多个选自C 1-3烷基，卤素，C 1-3卤代烷基，炔基或氰基的基团取代的1,2-环丙基环; R 1，R 2，R 3和R 4相同或不同，至少一个为氢，其余独立地选自氢，卤素，C 1-4烷基或C 1-4卤代烷基; X1是氧或硫; R 5为任选取代的C 1-8烃基，卤素，氰基，三氟甲基，三氟甲硫基或C 1-6烷氧基; 并且R 6选自：（A）-Y = X 2 - （R 8）a，其中X 2为O或S，Y为碳，R 8为氢，C 1-4烷基，C 1-4烷氧基，C 1-5烷基羰基或芳基或 CO 2 R 9，其中R 9为C 1-4烷基或芳基，a为1或2; （B）-CR15R16X3R17其中R15和R16为氢或C1-4烷基，X3为氧或硫，R17为C1-4烷基，C1-5烷基羰基或芳烷基羰基R17，R15X3，其制备方法，含有它们的杀虫组合物及其用途反对有害生物

10. 发明授权

US5130474A Optically-active derivatives of (R) 5-pentylamino-5-oxopentanoic acid with antagonistic activity towards cholecystokin in and a method for their preparation 失效
标题翻译：具有拮抗活性的（R）5-戊基氨基-5-氧代戊酸的光学活性衍生物及其制备方法
公开(公告)号：US5130474A
公开(公告)日：1992-07-14
申请号：US637583
申请日：1991-01-04
申请人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
发明人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
IPC分类号： C07C231/00 , A61K31/195 , A61P1/00 , A61P25/00 , A61P25/08 , C07C231/02 , C07C231/18 , C07C233/12 , C07C233/83 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/22
CPC分类号： A61K31/195 , C07C231/02 , C07C233/12 , C07C233/83 , C07C237/00
摘要： There are described optically active derivatives (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorobenzoyl and 3,4-dimethylbenzoyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.
摘要翻译：描述了对缩胆囊素具有拮抗作用的旋光活性衍生物（R）5-戊基氨基-5-氧代戊酸及其药学上可接受的盐，并具有下式：其中R 1选自2- 萘基，3,4-二氯苯甲酰基和3,4-二甲基苯甲酰基，R2是具有4个碳原子的戊基或烷氧基烷基，其中中心手性基团上的取代基（在式（I）中用星号标记）），有R（直肠）构象。

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