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21. 发明申请

US20180334426A1 BIS-OCTAHYDROPHENANTHRENE CARBOXAMIDES AND PROTEIN CONJUGATES THEREOF 审中-公开
公开(公告)号：US20180334426A1
公开(公告)日：2018-11-22
申请号：US15975654
申请日：2018-05-09
申请人： Regeneron Pharmaceutical, Inc.
发明人： Amy HAN , Andrew J. MURPHY , William OLSON
IPC分类号： C07C237/52 , A61K47/64 , A61K47/68 , A61P3/06 , A61P25/28 , A61P29/00
CPC分类号： C07C237/52 , A61K47/64 , A61K47/6803 , A61P3/06 , A61P25/28 , A61P29/00 , C07C233/90
摘要： Provided herein are compounds, compositions and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.

22. 发明申请

US20120165495A1 RESORBABLE PHENOLIC POLYMERS 有权
标题翻译：可分离的酚醛聚合物
公开(公告)号：US20120165495A1
公开(公告)日：2012-06-28
申请号：US13414090
申请日：2012-03-07
申请人： Arikha Moses , Satish Pulapura , Arthur Schwartz , Qing Ge , Irene Shatova
发明人： Arikha Moses , Satish Pulapura , Arthur Schwartz , Qing Ge , Irene Shatova
IPC分类号： C08G63/193 , C07H15/18 , C07C69/716 , C07C235/52 , C07C237/52
CPC分类号： C08G69/48 , C07C235/34 , C07C235/52 , C08G63/6856 , C08G64/12 , C08G73/028
摘要： The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
摘要翻译：本发明提供具有式（I），式（II），式（III）或式（IV））的单体单元的生物相容性可再吸收聚合物。当植入体内时，聚合物随时间降解，并且可用作可植入医疗装置的组件。

23. 发明申请

US20120071664A1 BETA-AMINO ACIDS AND METHODS AND INTERMEDIATES FOR MAKING SAME 审中-公开
标题翻译： β-氨基酸和其制备方法和中间体
公开(公告)号：US20120071664A1
公开(公告)日：2012-03-22
申请号：US13237559
申请日：2011-09-20
申请人： Mukund P. SIBI , Craig P. Jasperse , Prabagaran Narayanasamy , Sandeep R. Ghorpade
发明人： Mukund P. SIBI , Craig P. Jasperse , Prabagaran Narayanasamy , Sandeep R. Ghorpade
IPC分类号： C07D261/20 , C07C229/22 , C07C229/20 , C07C229/08 , C07C227/02 , C07C229/34 , C07D207/16 , C07D261/04 , C07C237/52 , C07D317/60 , C07C229/48 , C07C229/30
CPC分类号： C07C227/02 , C07D261/04 , C07D261/20
摘要： Disclosed are β-amino acids that are unsubstituted in the β position; that are substituted in the β position with an aryl group; that are substituted in the α position with an aryl group; that bear two substituents in the α position; and/or that are substituted in the α and β positions with groups which, together with the carbon atoms at the α and β positions, form a ring. Also disclosed are methods for making the above-mentioned β-amino acids and other β-amino acids which involve providing an α,β-unsaturated imide; converting the α,β-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a β-amino acid.
摘要翻译：公开了在＆bgr中未被取代的 - 氨基酸; 位置; 在＆bgr中被替代位置与芳基; 其在α位被芳基取代; 在α位具有两个取代基; 和/或在α和bgr中被取代; 与α和α的碳原子一起的基团的位置; 职位，形成一个戒指。还公开了制备上述＆bgr-氨基酸和其它涉及提供α，bgr-不饱和酰亚胺的其它α-氨基酸的方法; 将α，bgr-不饱和酰亚胺转化成2-取代异恶唑烷-5-酮; 并将2-取代的 - 异恶唑烷-5-酮转化为“氨基酸”。

24. 发明申请

US20120046272A1 Novel Therapeutic Compounds 审中-公开
标题翻译：新型治疗化合物
公开(公告)号：US20120046272A1
公开(公告)日：2012-02-23
申请号：US13213672
申请日：2011-08-19
申请人： Ramesh SESHA
发明人： Ramesh SESHA
IPC分类号： A61K31/55 , C07C237/14 , C07D333/20 , C07C237/08 , C07D265/30 , A61K31/5375 , A61K31/16 , A61K31/381 , C07C237/52 , C07C271/64 , A61K31/27 , C07D491/06 , C07D211/22 , A61K31/451 , C07C229/28 , A61K31/215 , C07C229/08 , A61K31/221 , C07C69/96 , A61K31/265 , C07D489/02 , A61K31/485 , C07C217/62 , A61K31/138 , A61P25/16 , A61P25/28 , A61P29/00 , A61P25/24 , A61P1/00 , A61P35/00 , A61P25/04 , A61P25/00 , C07C237/04
CPC分类号： C07C237/04 , C07C217/62 , C07C229/08 , C07C229/28 , C07C237/08 , C07C237/12 , C07C237/14 , C07C271/54 , C07C271/64 , C07D211/32 , C07D211/42 , C07D265/30 , C07D333/16 , C07D489/02 , C07D491/06
摘要： The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z (I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—. The compounds are useful to treat neurodegenerative disorders, depression, Alzheimer's disease, cognitive disorders, motor disorders, Parkinson's disease, drug addiction, behavioral disorders, inflammatory disorders, stomach disorders, cancers, acute pain, chronic pain and recurrent pain.
摘要翻译：本发明描述了可用于治疗哺乳动物疾病的一系列治疗活性的式I化合物，X-Y-Z（I）。在式I中，X和Z可以相同或不同，独立地选自取代或未取代的烷基，取代或未取代的烯基，取代或未取代的环烷基，取代或未取代的环烷基烷基，取代或未取代的芳基，取代或未取代的芳基烷基，取代或未取代的杂芳基，取代或未取代的杂芳基烷基，取代或未取代的杂环基或取代或未取代的杂环基烷基; 并且Y是选自-O - ， - S - ， - NH - ， - （CH 2）n - ， - CO - ， - CONR a - ， - NR a CO - ， - NR a COO - ， - COO-，-CONRCOCO - -CONRCOCOO-和-COOCOO-。这些化合物可用于治疗神经变性疾病，抑郁症，阿尔茨海默病，认知障碍，运动障碍，帕金森病，药物成瘾，行为障碍，炎症性疾病，胃病，癌症，急性疼痛，慢性疼痛和复发性疼痛。

25. 发明申请

US20110269679A1 INHIBITORS OF AMYLOID FIBRIL FORMATION AND USES THEREOF 审中-公开
标题翻译： AMYLOID FIBRIL形成的抑制剂及其用途
公开(公告)号：US20110269679A1
公开(公告)日：2011-11-03
申请号：US12905773
申请日：2010-10-15
申请人： PAUL FRASER
发明人： PAUL FRASER
IPC分类号： A61K38/28 , C07C237/52 , A61K38/06 , A61K38/05 , G01N21/19 , C12N5/071 , C12Q1/18 , G01N33/68 , G01N23/04 , C07K5/08 , A61P3/10
CPC分类号： A61K38/08 , C07K14/4711 , C07K16/18 , G01N2333/4709 , G01N2500/04
摘要： The present invention provides new antifibrillogenic agents and peptides, compositions and cells containing same, compositions that bind to same, effective therapeutics for preventing or delaying the progression of, e.g., Alzheimer's disease and diabetes, methods for optimizing antifibrillogenic agents, and methods of using the antifibrillogenic agents, peptides, compositions, and cells of the invention for detecting and/or inhibiting amyloid fibril formation.
摘要翻译：本发明提供了新的抗纤维发生剂和含有其的肽，组合物和细胞，与其结合的组合物，用于预防或延缓进行例如阿尔茨海默病和糖尿病的有效治疗剂，优化抗纤维化发生剂的方法，以及使用用于检测和/或抑制淀粉样蛋白原纤维形成的本发明的抗原纤维发生剂，肽，组合物和细胞。

26. 发明申请

US20110046128A1 NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS 有权
标题翻译：新型化合物治疗中枢神经系统疾病和疾病的优势
公开(公告)号：US20110046128A1
公开(公告)日：2011-02-24
申请号：US12881068
申请日：2010-09-13
申请人： Amir Pesyan , Manuel F. Balandrin
发明人： Amir Pesyan , Manuel F. Balandrin
IPC分类号： A61K31/5375 , C07C233/08 , A61K31/165 , C07D319/18 , A61K31/353 , C07D317/46 , A61K31/36 , C07C255/57 , A61K31/277 , C07C237/52 , C07D241/04 , A61K31/495 , C07D265/30 , C07D211/08 , A61K31/445 , C07D207/16 , A61K31/40 , C07D213/56 , A61K31/44 , A61P25/28 , A61P25/00
CPC分类号： C07D295/155 , A61K31/165 , A61K31/353 , A61K31/36 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/5375 , A61K45/06
摘要： A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
摘要翻译：描述了一系列显示抗惊厥，化学对策和止痛活性的新型化合物。此类药物活性化合物还可用于治疗其它中枢神经系统（“CNS”）疾病和病症，例如焦虑，抑郁，失眠，偏头痛，精神分裂症，帕金森病，痉挛状态，阿尔茨海默病和双相情感障碍。此外，这些化合物还可用作止痛剂（例如，用于治疗慢性或神经性疼痛）和用作治疗中风，慢性神经变性疾病（如阿尔茨海默病和亨廷顿疾病）的神经保护剂，以及 /或创伤性脑部和/或脊髓损伤。此外，这些/这样的化合物也可用于治疗癫痫持续状态和/或作为化学应对措施。

27. 发明申请

US20100324086A1 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：US20100324086A1
公开(公告)日：2010-12-23
申请号：US12735822
申请日：2009-02-19
申请人： Johan Wannberg , Mathias Alterman , Patric Stenberg , Jacob Westman
发明人： Johan Wannberg , Mathias Alterman , Patric Stenberg , Jacob Westman
IPC分类号： A61K31/472 , C07C237/52 , A61K31/167 , A61P35/00 , A61P29/00 , C07D215/42 , A61K31/4706 , C07D217/02 , A61K31/44 , C07D213/40 , C07D235/30 , A61K31/4184 , C07D277/82 , A61K31/428
CPC分类号： C07D215/38 , C07C233/66 , C07C237/30 , C07C237/42 , C07C2601/14 , C07C2601/18 , C07C2602/06 , C07C2602/10 , C07D213/75 , C07D265/14 , C07D277/64
摘要： A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer.
摘要翻译：式（1）的化合物及其药学上可接受的盐，以及包含该化合物的药物组合物。该化合物可用于治疗由疼痛，发烧，炎症和癌症引起的疾病。

28. 发明授权

US06054483A Plant volatile elicitor from insects 失效
标题翻译：从昆虫植物挥发性诱发剂
公开(公告)号：US06054483A
公开(公告)日：2000-04-25
申请号：US757701
申请日：1996-12-03
申请人： James H. Tumlinson, III , Hans T. Alborn , John H. Loughrin , Theodoor C. J. Turlings , Tappey H. Jones
发明人： James H. Tumlinson, III , Hans T. Alborn , John H. Loughrin , Theodoor C. J. Turlings , Tappey H. Jones
IPC分类号： A01N37/46 , A01N63/00 , C07C237/52 , C07D233/64 , A01N37/44 , A01N37/06 , C07C233/46
CPC分类号： A01N63/00 , A01N37/46 , C07C237/52
摘要： The invention relates to fatty acids conjugated to amino acids and their derivatives that elicit the production and/or release of plant volatiles compounds which attract and/or retain beneficial insects and deter herbivorous insect feeding. These conjugates also induce plants to increase production of pharmacologically important compounds such as taxol, increase fragrance of flowers, and increase production of plant essential oil. The invention also relates to methods for isolating the compounds from herbivorous insect oral secretions and to chemically synthesizing the compounds and their active derivatives.
摘要翻译：本发明涉及与氨基酸及其衍生物缀合的脂肪酸，其引起植物挥发物化合物的产生和/或释放，其吸引和/或保留有益昆虫并阻止食草动物进食。这些缀合物还诱导植物增加药理学上重要的化合物如紫杉醇的生产，增加花香，并增加植物精油的产生。本发明还涉及从食草昆虫口腔分泌物中分离化合物和化学合成化合物及其活性衍生物的方法。

29. 发明授权

US5965772A Process for the preparation of 5-(acetyl(2,3-dihydroxypropyl)amino-N,N-bis(2,3-dihydroxypropyl)-2,4,6-t riiodo 失效
标题翻译：制备5-（乙酰基（2,3-二羟基丙基）氨基-N，N-双（2,3-二羟基丙基）-2,4,6-三碘代
公开(公告)号：US5965772A
公开(公告)日：1999-10-12
申请号：US84922
申请日：1998-05-28
申请人： Nicola Desantis
发明人： Nicola Desantis
IPC分类号： C07C233/00 , C07C229/62 , C07C231/02 , C07C231/08 , C07C233/33 , C07C237/46 , C07C237/52 , C07C233/05
CPC分类号： C07C227/18 , C07C231/02 , C07C231/08 , C07C237/52
摘要： A process for the preparation of 5-[acetyl(2,3-dihydroxypropyl)amino]-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide of formula (I), starting from 5-amino-1,3-benzenedicarboxylic acid of formula (II), comprising the following steps:step a) is the reaction in heterogeneous phase between 5-amino-2,4,6-triiodo-1,3-benzenedicarboxylic acid and thionyl chloride in a solvent selected from the group consisting of: straight or branched (C.sub.7 -C.sub.16) hydrocarbons, (C.sub.7 -C.sub.8) aromatic hydrocarbons, 1,1,1-trichloroethane, n-butyl acetate, diglyme (diethylene glycol dimethyl ether), in the presence of catalytic amounts of a tertiary amine, to give compound (III);step b) is the acetylation reaction of compound (III) with glacial acetic acid both as the solvent and the reagent and thionyl chloride;step c) is the formation of compound (V) by reaction of the compound (IV) with 1-amino-2,3-propanediol, by reaction of compound (IV) in a dipolar aprotic solvent, selected from the group of dimethylformamide (DMF), dimethylacetamide (DMA), dimethylsulfoxide (DMSO) or N-methyl-pyrrolidinone;step d) is the alkylation of the compound (V) in aqueous solution at basic pH, by addition of a sodium hydroxide-calcium hydroxide mixture, with 3-chloro-1,2-propanediol or epichlorohydrin, at a temperature of 40-90.degree. C.
摘要翻译：制备式（5）的5- [乙酰基（2,3-二羟丙基）氨基] -N，N'-双（2,3-二羟基丙基）-2,4,6-三碘-1,3-苯二甲酰胺的方法， I），由式（II）的5-氨基-1,3-苯二甲酸开始，包括以下步骤：步骤a）是非均相中5-氨基-2,4,6-三碘-1 （C7-C16）烃，（C7-C8）芳香族烃，1,1,1-三氯乙烷，乙酸正丁酯，二甘醇二甲醚（二乙烯基醚）的溶剂中选择3-苯二甲酸和亚硫酰氯，二乙二醇二甲醚），在催化量的叔胺的存在下，得到化合物（III）; 步骤b）是化合物（III）与冰乙酸作为溶剂和试剂和亚硫酰氯的乙酰化反应; 步骤c）是通过化合物（IV）与1-氨基-2,3-丙二醇的反应，通过化合物（IV）在偶极非质子溶剂中的反应，形成化合物（V），所述偶极非质子溶剂选自二甲基甲酰胺 DMF），二甲基乙酰胺（DMA），二甲基亚砜（DMSO）或N-甲基 - 吡咯烷酮; 步骤d）是在碱性pH下，通过在40-90℃的温度下加入氢氧化钠 - 氢氧化钙混合物与3-氯-1,2-丙二醇或表氯醇，将化合物（Ⅴ）在水溶液中烷基化 DEG C.

30. 发明授权

US11591291B2 Preparation of cationic surfactants 有权
公开(公告)号：US11591291B2
公开(公告)日：2023-02-28
申请号：US17551915
申请日：2021-12-15
申请人： Saudi Arabian Oil Company
发明人： Xuan Zhang , Ming Han , Jinxun Wang
IPC分类号： C07C237/52 , C07C231/02 , C07C233/36 , C07C233/38 , C09K8/584
摘要： Compositions that include cationic surfactants and methods of synthesizing compositions that include cationic surfactants. The surfactants include a quaternary amine and a saturated or unsaturated alkyl chain with 4 to 28 carbons. The surfactants can be generated by reacting a fatty acid modified with an amino alkyl group and an epihalohydrin in the presence of a base. The cationic surfactants can be generated by reacting a fatty acid modified with an amino alkyl group, an epihalohydrin, and a carboxylic acid. The cationic surfactants can be generated by reacting a carboxylic acid, an epihalohydrin, and a catalyst to afford a halo-substituted alkyl ester, followed by reacting the halo-substituted alky ester with a fatty acid modified with an amino alkyl group.

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