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1. 发明申请

US20180127435A1 NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE 审中-公开
公开(公告)号：US20180127435A1
公开(公告)日：2018-05-10
申请号：US15860058
申请日：2018-01-02
申请人： ANGUS Chemical Company
发明人： Daniel M. Trauth , George D. Green , Raymond J. Swedo , Richard L. James , Ian A. Tomlinson
IPC分类号： C07D498/10 , A01N43/76 , C07C215/28 , C07C205/04 , C07C205/05 , C07C205/15 , C07C205/16 , C07C215/20 , A01N43/90 , C07C201/08 , C07C201/12 , C07C205/02 , C07C205/06 , C07C205/18 , C07C215/08 , C07C215/42 , C07C239/10 , C07D263/04 , C07D263/52 , C08G18/32 , C07D498/04
CPC分类号： C07D498/10 , A01N43/76 , A01N43/90 , C07C201/08 , C07C201/12 , C07C205/02 , C07C205/04 , C07C205/05 , C07C205/06 , C07C205/15 , C07C205/16 , C07C205/18 , C07C215/08 , C07C215/20 , C07C215/28 , C07C215/42 , C07C239/10 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D263/04 , C07D263/52 , C07D498/04 , C08G18/3271 , Y02P20/582
摘要： Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.

2. 发明申请

US20170152253A1 Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV 审中-公开
公开(公告)号：US20170152253A1
公开(公告)日：2017-06-01
申请号：US15429250
申请日：2017-02-10
申请人： Janssen Pharmaceuticals, Inc.
发明人： Dominic John Ormerod , Dominique Paul Michel Depre , Andras Horvath
IPC分类号： C07D417/04 , C07C61/06 , C07C235/82 , C07C69/757 , C07C205/57 , C07D491/22 , C07C215/20
CPC分类号： C07D417/04 , C07B2200/07 , C07C51/02 , C07C51/412 , C07C51/43 , C07C61/06 , C07C67/03 , C07C67/31 , C07C69/757 , C07C201/12 , C07C205/57 , C07C215/20 , C07C215/30 , C07C231/12 , C07C235/40 , C07C235/82 , C07C255/57 , C07C317/44 , C07C2601/08 , C07D251/28 , C07D251/30 , C07D309/30 , C07D417/14 , C07D491/18 , C07D491/22 , C07C62/24
摘要： A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(−)-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(−)-ephedrine from the precipitated salt obtained in step (b).

3. 发明授权

US08829196B2 TRPA1 antagonists 有权
标题翻译： TRPA1拮抗剂
公开(公告)号：US08829196B2
公开(公告)日：2014-09-09
申请号：US13499844
申请日：2010-09-28
申请人： Mark T. Bilodeau , Melissa Egbertson , Ahren Green , John C. Hartnett , Yiwei Li
发明人： Mark T. Bilodeau , Melissa Egbertson , Ahren Green , John C. Hartnett , Yiwei Li
IPC分类号： C07D215/38 , C07C215/20 , C07C211/34 , C07C25/02 , A61K31/133
CPC分类号： C07C215/20 , A61K31/133 , C07C25/02 , C07C211/34 , C07C215/44 , C07C255/58 , C07C2602/10 , C07D215/38 , C07D215/44 , C07D311/74 , C07D311/76 , C07D405/04 , C07D405/06
摘要： The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.
摘要翻译：本发明涉及调节至少一种TRP家族成员的组合物和方法。具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关与TRPA1表达或功能调节或失调。本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。

4. 发明授权

US08716529B2 Amine derivative compounds for treating ophthalmic diseases and disorders 失效
标题翻译：用于治疗眼科疾病和病症的胺衍生物化合物
公开(公告)号：US08716529B2
公开(公告)日：2014-05-06
申请号：US13278925
申请日：2011-10-21
申请人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Feng Hong , Thomas L. Little , Ryo Kubota
发明人： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Feng Hong , Thomas L. Little , Ryo Kubota
IPC分类号： C07C213/00
CPC分类号： A61K31/382 , A61K31/138 , A61K31/165 , A61K31/351 , C07C211/27 , C07C213/00 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/42 , C07C217/16 , C07C217/48 , C07C217/54 , C07C217/72 , C07C217/74 , C07C219/22 , C07C225/16 , C07C225/18 , C07C233/18 , C07C235/34 , C07C235/54 , C07C237/20 , C07C237/38 , C07C237/40 , C07C257/14 , C07C279/08 , C07C317/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/38 , C07D309/06 , C07D333/16 , C07D333/20 , C07D335/02
摘要： Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
摘要翻译：提供的是胺衍生物化合物，其药物组合物，以及使用所述化合物和组合物治疗眼科疾病和失调症的方法，例如年龄相关性黄斑变性和Stargardt氏病。

5. 发明申请

US20140046095A1 Method of Preparing (S)-2-amino-5-Methoxytetralin Hydrochloride 有权
标题翻译：（S）-2-氨基-5-甲氧基四氢萘盐酸盐的制备方法
公开(公告)号：US20140046095A1
公开(公告)日：2014-02-13
申请号：US13570210
申请日：2012-08-08
申请人： Qingyun HUANG , Qingguo HUANG , Meixian LOU
发明人： Qingyun HUANG , Qingguo HUANG , Meixian LOU
IPC分类号： C07C213/02 , C07C217/74 , C07C249/02 , C07C251/20
CPC分类号： C07C213/02 , C07B2200/07 , C07C213/08 , C07C217/74 , C07C249/02 , C07C251/20 , C07C2602/10 , C07C215/20
摘要： A method of preparing (S)-2-amino-5-methoxytetralin hydrochloride[(S)-2-amino-5-methoxyl-1,2,3,4-tetrahydronaphthalene hydrochloride], comprising the steps of: (1) producing a compound (I) by addition-elimination reaction of 5-methoxy-2-tetralone and R-(+)-a-phenylethylamine; (2) producing a compound (II) by reduction reaction of the compound (I) with a reducing agent; and (3) producing a compound (II) hydrochloride by reacting the compound (II) with a salt-forming agent, then carrying out reduction reaction with a palladium-carbon catalyst to produce (S)-2-amino-5-methoxytetralin hydrochloride. The method can significantly increase the yield of (S)-2-amino-5-methoxytetralin hydrochloride with short synthetic path, low preparation cost and less pollution, which is environmentally friendly and is suitable for medical industrialized production. The structural formulae of the compound (I) and the compound (II) are: resepectively.
摘要翻译：制备（S）-2-氨基-5-甲氧基-1,2,3,4-四氢萘盐酸盐[（S）-2-氨基-5-甲氧基-1,2,3,4-四氢萘盐酸盐]的方法，包括以下步骤：（1）通过5-甲氧基-2-四氢萘酮和R - （+） - α-苯基乙胺的加成消除反应的化合物（I）（2）通过化合物（I）与还原剂的还原反应制备化合物（II）; 和（3）通过使化合物（II）与成盐剂反应制备盐酸化合物（II），然后与钯 - 碳催化剂进行还原反应，生成（S）-2-氨基-5-甲氧基环丁烷盐酸盐。该方法可以显着提高盐酸（S）-2-氨基-5-甲氧基四氢萘酯的合成路径短，制备成本低，污染少，环保，适用于医疗工业化生产。化合物（I）和化合物（II）的结构式是：重新进行。

6. 发明授权

US08541408B2 Aminodihydrothiazine derivatives substituted with a cyclic group 失效
标题翻译：用环状基团取代的氨基二氢噻嗪衍生物
公开(公告)号：US08541408B2
公开(公告)日：2013-09-24
申请号：US13417786
申请日：2012-03-12
申请人： Yuusuki Tamura , Shinji Suzuki , Yukio Tada , Chiaki Fujikoshi , Sae Matsumoto , Yuuji Kooriyama
发明人： Yuusuki Tamura , Shinji Suzuki , Yukio Tada , Chiaki Fujikoshi , Sae Matsumoto , Yuuji Kooriyama
IPC分类号： C07D417/12 , C07D417/14 , A61K31/497 , A61K31/54
CPC分类号： C07C215/20 , A61K9/0019 , A61K9/1623 , A61K9/2018 , C07D279/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.
摘要翻译：本发明提供式（I）的化合物：其中环A为任选取代的碳环基或任选取代的杂环基; R1是任选取代的低级烷基，任选取代的低级烯基，任选取代的低级炔基; R2a和R2b各自独立地为氢，任选取代的低级烷基或任选取代的酰基; R3a，R3b，R3c和R3d各自独立地为氢，卤素，羟基或任选取代的低级烷基等; 其药学上可接受的盐或溶剂合物，其可用于治疗由淀粉样β蛋白的产生，分泌和/或沉积诱导的疾病。

7. 发明申请

US20130150454A1 TARGETING OF T-LYMPHOCYTES TO TREAT AMYOTROPHIC LATERAL SCLEROSIS 有权
标题翻译： T淋巴细胞趋化因子治疗多发性前列腺切除术
公开(公告)号：US20130150454A1
公开(公告)日：2013-06-13
申请号：US13689375
申请日：2012-11-29
申请人： ALS THERAPY DEVELOPMENT INSTITUTE
发明人： Steven Perrin , John Lincecum , Alan Gil , Fernando Vieira
IPC分类号： C07C215/20
CPC分类号： C07C215/20 , A61K31/137 , A61K31/145
摘要： Methods and therapeutic compositions are disclosed for treating neurodegenerative disorders and, in particular Amyotrophic Lateral Sclerosis, using sphingosine1-phosphate receptor modulators, such as fingolimod or a pharmaceutically acceptable salt, hydrate, or solvate thereof.
摘要翻译：公开了用于治疗神经变性疾病，特别是肌营养不良性侧索硬化的方法和治疗组合物，其使用鞘氨醇1-磷酸受体调节剂，如芬戈莫德或其药学上可接受的盐，水合物或溶剂化物。

8. 发明授权

US07820858B2 Concise β2-amino acid synthesis via organocatalytic aminomethylation 有权
标题翻译：通过有机催化氨基甲基化合成简便的2-氨基酸合成
公开(公告)号：US07820858B2
公开(公告)日：2010-10-26
申请号：US11691249
申请日：2007-03-26
申请人： Yonggui Chi , Samuel H. Gellman , William C. Pomerantz , William S. Horne , Li Guo , Emily P. English
发明人： Yonggui Chi , Samuel H. Gellman , William C. Pomerantz , William S. Horne , Li Guo , Emily P. English
IPC分类号： C07C213/00 , C07C215/28 , C07C271/22 , C07C269/06 , C07C217/64 , C07D209/14 , C07D209/26
CPC分类号： C07C213/00 , C07B2200/07 , C07C227/02 , C07C269/06 , C07C2601/14 , C07D209/26 , C07C215/08 , C07C215/20 , C07C215/24 , C07C215/28 , C07C217/64 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/66 , C07C229/22
摘要： The present invention provides a method for the synthesis of β2-amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β2-amino acids.
摘要翻译：本发明提供了合成2-氨基酸的方法。该方法还提供了产生α-取代的 - 氨基醛和取代的γ-氨基醇的方法。根据本发明的本发明的方法允许增加的产率和更容易的纯化使用最小的色谱或结晶。本文描述的方法基于醛氨基甲基化，其涉及醛和来自甲醛的N，O-缩醛（亚胺前体）和催化剂（例如L-脯氨酸或吡咯烷）之间的曼尼希反应。本发明允许大规模商业化制备2-氨基酸。

9. 发明申请

US20100105680A1 SUBSTITUTED DIMETHYLCYCLOBUTYL COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS 审中-公开
标题翻译：取代的二甲基胆碱化合物，其制备和用于药物
公开(公告)号：US20100105680A1
公开(公告)日：2010-04-29
申请号：US12376283
申请日：2007-08-03
申请人： Maria Rosa Cuberes Altisent , Jordi Corbera Arjona , Jorg Holenz , Rosa Maria Ortuno Mingarro , Sandra Izquierdo Salado
发明人： Maria Rosa Cuberes Altisent , Jordi Corbera Arjona , Jorg Holenz , Rosa Maria Ortuno Mingarro , Sandra Izquierdo Salado
IPC分类号： A61K31/5377 , A61K31/4545 , A61K31/454 , C07D413/08 , C07D401/08 , A61P25/00
CPC分类号： C07C69/675 , C07C215/20 , C07C2601/04 , C07D211/14 , C07D295/096 , C07D295/112 , C07D295/135
摘要： The present invention relates to substituted dimethylcyclobutyl compounds of general formula I, a process for their preparation, medicaments comprising said substituted dimethylcyclobutyl compounds as well as the use of said substituted dimethylcyclobutyl compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via sigma receptors.
摘要翻译：本发明涉及通式I的取代的二甲基环丁基化合物，其制备方法，包含所述取代的二甲基环丁基化合物的药物以及所述取代的二甲基环丁基化合物用于制备药物的用途，其特别适用于预防和/ 或治疗通过西格玛受体至少部分介导的病症或疾病。

10. 发明授权

US07309717B2 Process and intermediates for the preparation of (1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylates or salts thereof 有权
标题翻译：制备（1R，2S，5S）-6,6-二甲基-3-氮杂双环[3,1,0]己烷-2-羧酸盐或其盐的方法和中间体
公开(公告)号：US07309717B2
公开(公告)日：2007-12-18
申请号：US10867602
申请日：2004-06-15
申请人： Jeonghan Park , Anantha Sudhakar , George S. Wong , Minzhang Chen , Juergen Weber , Xiaojing Yang , Daw-Jong Kwok , Ingyu Jeon , Ramani R. Raghavan , Maria Tamarez , Weidong Tong , Eugene J. Vater
发明人： Jeonghan Park , Anantha Sudhakar , George S. Wong , Minzhang Chen , Juergen Weber , Xiaojing Yang , Daw-Jong Kwok , Ingyu Jeon , Ramani R. Raghavan , Maria Tamarez , Weidong Tong , Eugene J. Vater
IPC分类号： A61K31/21 , C07D209/52
CPC分类号： C07C233/58 , C07B2200/07 , C07C69/74 , C07C215/20 , C07C271/18 , C07C2601/02 , C07D209/52
摘要： In one embodiment, the present application relates to a process of making a compound of formula I. and to certain intermediate compounds that are made within the process of making the compound of formula I.
摘要翻译：在一个实施方案中，本申请涉及制备式I化合物和在制备式I化合物的方法中制备的某些中间体化合物的方法。

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