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1. 发明授权

US06306912B1 Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases 失效
标题翻译：在用于治疗神经障碍和疾病的受体操作的钙通道上的新位点处有活性的化合物
公开(公告)号：US06306912B1
公开(公告)日：2001-10-23
申请号：US08483294
申请日：1995-06-07
申请人： Alan L. Mueller , Bradford C. VanWagenen , Eric G. DelMar , Manuel F. Balandrin , Scott T. Moe , Linda D. Artman
发明人： Alan L. Mueller , Bradford C. VanWagenen , Eric G. DelMar , Manuel F. Balandrin , Scott T. Moe , Linda D. Artman
IPC分类号： A61K31135
CPC分类号： A61K31/135 , A61K31/136 , A61K31/137 , A61K31/138 , A61K31/165 , A61K31/295 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/4409 , A61K31/4462 , A61K31/4465 , C07C233/22 , C07C235/34 , C07C237/22 , C07C279/14 , C07D209/18 , G01N2800/28
摘要： Method for identifying a compound useful for the therapeutic treatment of a neurological disease or disorder such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease or Parkinson's Disease, or useful as a muscle relaxant, analgesic, or adjuvant to general anesthetics. The compound is active on a receptor-operated calcium channel, including, but not limited to, that present as part of an NMDA receptor-ionophore complex, a calcium-permeable AMPA receptor, or a nicotinic cholinergic receptor, as a noncompetitive antagonist. The method includes identifying a compound which binds to the receptor-operated calcium channel at the site bound by the arylalkylamines Compound 1, Compound 2 or Compound 3.
摘要翻译：用于鉴定可用于治疗性治疗诸如中风，头部创伤，脊髓损伤，癫痫，焦虑或神经变性疾病如阿尔茨海默氏病，亨廷顿舞蹈病或帕金森病的神经系统疾病或障碍的化合物或用作肌肉的化合物的方法松弛剂，止痛剂或佐剂用于全身麻醉剂。该化合物在受体操作的钙通道上是有活性的，包括但不限于作为非竞争性拮抗剂的NMDA受体 - 离子载体复合物，钙可渗透AMPA受体或烟碱型胆碱能受体的一部分。该方法包括鉴定在由芳烷基胺化合物1，化合物2或化合物3结合的位点处与受体操作的钙通道结合的化合物。

3. 发明授权

US6017965A Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases 失效
公开(公告)号：US6017965A
公开(公告)日：2000-01-25
申请号：US763480
申请日：1996-12-11
申请人： Alan L. Mueller , Manuel F. Balandrin , Bradford C. VanWagenen , Scott T. Moe , Eric G. DelMar , Linda D. Artman , Robert M. Barmore , Daryl L. Smith
发明人： Alan L. Mueller , Manuel F. Balandrin , Bradford C. VanWagenen , Scott T. Moe , Eric G. DelMar , Linda D. Artman , Robert M. Barmore , Daryl L. Smith
IPC分类号： A61K31/135 , A61K31/136 , A61K31/137 , A61K31/138 , A61K31/155 , A61K31/165 , A61K31/295 , A61K31/381 , A61K31/40 , A61K31/4409 , A61K31/4462 , A61K31/4465 , C07C201/14 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/40 , C07C211/42 , C07C211/54 , C07C211/55 , C07C215/28 , C07C215/54 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/60 , C07C217/62 , C07C233/11 , C07C233/13 , C07C233/22 , C07C235/34 , C07C237/06 , C07C237/22 , C07C257/14 , C07C279/14 , C07D207/08 , C07D207/12 , C07D207/20 , C07D209/42 , C07D211/18 , C07D213/30 , C07D213/32 , C07D213/38 , C07D231/20 , C07D333/20
CPC分类号： C07D207/08 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/138 , A61K31/155 , A61K31/165 , A61K31/295 , A61K31/381 , A61K31/40 , A61K31/4409 , A61K31/4462 , A61K31/4465 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/40 , C07C211/42 , C07C211/54 , C07C211/55 , C07C215/28 , C07C215/54 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/60 , C07C217/62 , C07C233/11 , C07C233/13 , C07C233/22 , C07C235/34 , C07C237/06 , C07C237/22 , C07C257/14 , C07C279/14 , C07D207/12 , C07D207/20 , C07D209/42 , C07D211/18 , C07D213/30 , C07D213/32 , C07D213/38 , C07D231/20 , C07D333/20 , C07B2200/07 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2103/32
摘要： Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

4. 发明授权

US06617358B1 Anticonvulsant and central nervous system-depressing bis(fluorophenyl)alkylamides and their uses 失效
标题翻译：抗惊厥和中枢神经系统抑制双（氟苯基）烷基酰胺及其用途
公开(公告)号：US06617358B1
公开(公告)日：2003-09-09
申请号：US09587179
申请日：2000-06-02
申请人： Manuel F. Balandrin , Bradford C. VanWagenen , Linda D. Artman , Alan L. Mueller , Daryl Smith , Scott T. Moe
发明人： Manuel F. Balandrin , Bradford C. VanWagenen , Linda D. Artman , Alan L. Mueller , Daryl Smith , Scott T. Moe
IPC分类号： A61K31165
CPC分类号： A61K31/16 , A61K31/165 , A61K31/192 , C07C233/11 , C07C233/22
摘要： Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacological half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.
摘要翻译：已经化学合成了双（氟苯基）烷基酰胺，其具有可用于治疗神经疾病或病症（例如癫痫，抽搐和癫痫发作）的有益的药理学性质（例如抗惊厥活性）。本发明优选的化合物在癫痫的动物模型中也引起很少的镇静作用并具有较高的治疗和保护指标。这些化合物还具有长的药理学半衰期，其在实际临床治疗应用中应该转化为每天一次给药，对患有这些疾病和/或病症的患者是非常有益的。这些化合物还可用于治疗中枢和周围神经系统的其他疾病和病症，或受其影响的疾病或病症，包括但不限于痉挛性，骨骼肌痉挛和疼痛，不宁腿综合征，焦虑和压力和双相情感障碍。

5. 发明授权

US5648541A Chiral reductions of imines leading to the syntheses of optically active amines 失效
标题翻译：亚胺的手性还原导致光学活性胺的合成
公开(公告)号：US5648541A
公开(公告)日：1997-07-15
申请号：US535469
申请日：1995-09-28
申请人： Bradford C. VanWagenen , Robert M. Barmore
发明人： Bradford C. VanWagenen , Robert M. Barmore
IPC分类号： C07C209/44 , C07C209/52 , C07C211/27 , C07C211/29 , C07C211/30 , C07C213/02 , C07C215/46 , C07C217/54 , C07C227/04 , C07C229/38 , C07C231/18 , C07C237/30 , C07C253/30 , C07C255/58
CPC分类号： C07C209/52
摘要： A process for preparing an R enantiomer of a compound of the formula (I): ##STR1## wherein Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF.sub.3, CF.sub.2 H, CFH.sub.2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH.sub.2 CF.sub.3, OH, CN, NO.sub.2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH--Me), C(O)N-lower alkyl.sub.2 (e.g., C(O)NMe.sub.2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH--C(O)-lower alkyl (e.g., NH--C(O)Me), where "lower alkyl" is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I). The process is especially useful to produce compounds (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorophenyl)propanamine and (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(phenyl)propanamine. Enantiomeric excess of the R enantiomer over S enantiomer of greater than 65% have been achieved.
摘要翻译：制备式（I）化合物的R对映异构体的方法：其中Ar是3-甲氧基苯基，3-氯苯基或1-萘基，X独立地选自H ，F，Cl，Br，I，苯基，CF 3，CF 2 H，CFH 2，低级烷基（例如Me），O-低级烷基（例如OMe），OCH 2 CF 3，OH，CN，NO 2，C（O）（例如C（O）Me），C（O）O-低级烷基（例如C（O）OMe），C（O）NH-低级烷基（例如C（O）NH-Me） O）N-低级烷基2（例如C（O）NMe 2），OC（O） - 低级烷基（例如OC（O）Me）和NH-C（O） - 低级烷基（例如，NH-C O）Me），其中“低级烷基”选自1至6个碳原子，m为1至5之间的整数，通过用还原剂/手性助剂络合物不对称和对映选择性还原亚胺，因此以便在式（I）化合物的S对映异构体上产生式（I）化合物的对映异构体的对映异构体。该方法特别适用于制备化合物（R） - （+） - N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯基）丙胺和（R） - （+） - N- [ - （3-甲氧基苯基）乙基] -3-（苯基）丙胺。 R对映异构体超过S对映异构体的对映体过量已达到大于65％。

6. 发明授权

US5504253A Amine preparation 失效
标题翻译：胺制剂
公开(公告)号：US5504253A
公开(公告)日：1996-04-02
申请号：US276214
申请日：1994-07-15
申请人： Bradford C. VanWagenen , Thomas E. D'Ambra
发明人： Bradford C. VanWagenen , Thomas E. D'Ambra
IPC分类号： C07C213/10 , C07C217/58 , C07C233/22 , C07C209/48 , C07C209/50
CPC分类号： C07C217/58 , C07C213/10 , C07C233/22
摘要： A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.
摘要翻译：制备（R）-N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯）丙胺的方法，其涉及用合适的还原剂还原合适的酰胺基或亚氨基前体。合适的酰氨基或亚氨基前体由涉及使用（R）-3-甲氧基-α-甲基苄胺的合成制备。将腈与伯胺或仲胺缩合形成亚胺的方法涉及腈与氢化二异丁基铝的反应; 然后使所得化合物与伯胺或仲胺反应形成亚胺。该方法特别适用于产生对映体纯的手性亚胺，最终产生胺。典型的这种亚胺具有下式：其中R，R 1，R 2和R 3独立地选自氢，取代或未取代的烷基，芳基和芳烷基。

7. 发明授权

US5648540A Amine preparation 失效
标题翻译：胺制剂
公开(公告)号：US5648540A
公开(公告)日：1997-07-15
申请号：US446491
申请日：1995-05-22
申请人： Bradford C. VanWagenen , Steven R. Duff , William A. Nelson , Thomas E. D'Ambra
发明人： Bradford C. VanWagenen , Steven R. Duff , William A. Nelson , Thomas E. D'Ambra
IPC分类号： C07C213/10 , C07C217/58 , C07C233/22 , C07C209/50 , C07C209/52
CPC分类号： C07C217/58 , C07C213/10 , C07C233/22
摘要： A method of making (R)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.
摘要翻译：制备（R）-N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯）丙胺的方法，其包括用合适的还原剂还原合适的酰胺基或亚氨基前体。合适的酰氨基或亚氨基前体由涉及使用（R）-3-甲氧基-α-甲基苄胺的合成制得。将腈与伯胺或仲胺缩合形成亚胺的方法涉及腈与氢化二异丁基铝的反应; 然后使所得化合物与伯胺或仲胺反应形成亚胺。该方法特别适用于产生对映体纯的手性亚胺，最终产生胺。典型的这种亚胺具有下式：其中R，R 1，R 2和R 3独立地选自氢，取代或未取代的烷基，芳基和芳烷基。

8. 发明授权

US5633404A N-((R)-.alpha.-methyl-3-methoxybenzyl)-3-(2-chlorobenzene)propanamide 失效
标题翻译： N - （（R）-α-甲基-3-甲氧基苄基）-3-（2-氯苯）丙酰胺
公开(公告)号：US5633404A
公开(公告)日：1997-05-27
申请号：US639935
申请日：1996-04-19
申请人： Bradford C. VanWagenen , Steven R. Duff , William A. Nelson
发明人： Bradford C. VanWagenen , Steven R. Duff , William A. Nelson
IPC分类号： C07C213/10 , C07C217/58 , C07C233/22
CPC分类号： C07C217/58 , C07C213/10 , C07C233/22
摘要： A method of making ( R)- N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of ( R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.
摘要翻译：制备（+ E，uns R + EE） - + E，非N + EE - [1-（3-甲氧基苯基）乙基] -3-（2-氯苯）丙胺的方法，其涉及还原合适的酰胺基或亚氨基前体用合适的还原剂。合适的酰胺基或亚氨基前体由涉及使用（+ E，不R + EE）-3-甲氧基-α-甲基苄胺的合成制备。将腈与伯胺或仲胺缩合形成亚胺的方法涉及腈与氢化二异丁基铝的反应; 然后使所得化合物与伯胺或仲胺反应形成亚胺。该方法特别适用于产生对映体纯的手性亚胺，最终产生胺。典型的这种亚胺具有下式：其中R，R 1，R 2和R 3独立地选自氢，取代或未取代的烷基，芳基和芳烷基。

9. 发明授权

US5461032A Insecticidally effective peptides 失效
标题翻译：杀虫有效肽
公开(公告)号：US5461032A
公开(公告)日：1995-10-24
申请号：US215084
申请日：1994-03-18
申请人： Karen J. Krapcho , J. R. Hunter Jackson , Bradford C. VanWagenen , Robert M. Kral, Jr.
发明人： Karen J. Krapcho , J. R. Hunter Jackson , Bradford C. VanWagenen , Robert M. Kral, Jr.
IPC分类号： A01N63/02 , C07K14/435 , C12N15/82 , C12N15/866 , A61K38/00 , C12N15/85
CPC分类号： C12N15/86 , A01N63/02 , C07K14/43518 , C12N15/8286 , C07K2319/08 , C12N2710/14143
摘要： The invention provides insecticidally effective peptides isolatable from Diguetia spider venom, methods for preparing and using insecticides, and DNA encoding such insecticidally effective peptides.
摘要翻译：本发明提供可从Diguetia蜘蛛毒液分离的杀虫有效肽，制备和使用杀虫剂的方法，以及编码这种杀虫有效肽的DNA。

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