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1. 发明公开

US20240083850A1 NOVEL LAPPACONITINE DERIVATIVE AND USE THEREOF 审中-公开
公开(公告)号：US20240083850A1
公开(公告)日：2024-03-14
申请号：US17905797
申请日：2021-03-05
申请人： QGENETICS CO., LTD.
发明人： Mun Seog CHANG , Tae Hee LEE , Ha Young KIM , Jung Bin MIN
IPC分类号： C07D223/32 , A61K9/20 , A61K9/48 , A61K47/26
CPC分类号： C07D223/32 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2059 , A61K9/4825 , A61K9/4858 , A61K9/4866 , A61K47/26
摘要： The present invention pertains to a novel lappaconitine derivative, a method for producing same, and a pharmaceutical use thereof using osteogenesis-promoting activity. The lappaconitine derivative induces the differentiation of stem cells into osteoblasts, increases bone mineral density when administered to animal models of osteoporosis, and induces bone formation in animal models of bone fracture, and thus can be advantageously used for preventing, ameliorating, or treating bone-related diseases such as osteoporosis, as well as treating non-disease fractures caused by physical trauma.

2. 发明授权

US10421763B2 Compositions of protein receptor tyrosine kinase inhibitors 有权
公开(公告)号：US10421763B2
公开(公告)日：2019-09-24
申请号：US15676039
申请日：2017-08-14
申请人： Purdue Pharma L.P.
发明人： Jay Jie-Qiang Wu , Ling Wang
IPC分类号： A61K31/496 , A61K31/497 , A61K45/06 , C07D403/14 , C07D407/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D215/20 , C07D221/06 , C07D223/32 , C07D241/44 , C07D261/20 , C07D265/36 , C07D279/16 , C07D295/13 , C07D307/77 , C07D498/06 , C07D493/06 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

3. 发明授权

US10272094B2 5-HT2C receptor agonists and compositions and methods of use 有权
公开(公告)号：US10272094B2
公开(公告)日：2019-04-30
申请号：US15748205
申请日：2016-07-28
申请人： Arena Pharmaceuticals, Inc.
发明人： Juerg Lehmann , Konrad Feichtinger , Albert S. Ren , Graeme Semple
IPC分类号： C07D223/16 , C07D223/32 , C07D491/052 , A61K31/55 , A61P25/32 , A61P25/08 , A61P3/04 , A61P3/10
摘要： Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.

4. 发明授权

US09755161B2 Organic light emitting display device 有权
公开(公告)号：US09755161B2
公开(公告)日：2017-09-05
申请号：US14919944
申请日：2015-10-22
申请人： LG Display Co., Ltd.
发明人： DoHan Kim , JungKeun Kim , Hyoseok Kim , Min Yun , SeungHee Yoon
IPC分类号： H01L51/54 , H01L51/00 , C07D223/14 , C07D403/04 , C07D409/10 , C09K11/06 , C07D223/32 , C09K11/02 , H01L51/50
CPC分类号： H01L51/0072 , C07D223/14 , C07D223/32 , C07D403/04 , C07D409/10 , C09K11/025 , C09K11/06 , C09K2211/1007 , C09K2211/1011 , C09K2211/1029 , C09K2211/1059 , C09K2211/1092 , C09K2211/185 , H01L51/0052 , H01L51/0056 , H01L51/0058 , H01L51/0067 , H01L51/0074 , H01L51/0085 , H01L51/5016 , H01L51/5072
摘要： An organic light emitting display device is disclosed. The organic light emitting display device comprises an anode, an organic layer over the anode, and a cathode over the organic layer. The organic layer may include a heterocyclic compound. Alternatively, the organic layer may include a spirobisfluorene compound with hole transfer properties and a material with electron transfer properties.

5. 发明授权

US09643947B2 7-membered fused heterocycles and methods of their synthesis 有权
公开(公告)号：US09643947B2
公开(公告)日：2017-05-09
申请号：US14466677
申请日：2014-08-22
申请人： Northwestern University
发明人： Karl A. Scheidt , Javier Izquierdo Ferrer
IPC分类号： C07D313/06 , C07D313/08 , C07D223/16 , C07D223/32
CPC分类号： C07D313/08 , C07D223/16 , C07D223/32
摘要： Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

6. 发明申请

US20150225355A1 AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS 有权
公开(公告)号：US20150225355A1
公开(公告)日：2015-08-13
申请号：US14694147
申请日：2015-04-23
申请人： Novira Therapeutics, Inc.
发明人： George D. Hartman
IPC分类号： C07D267/10 , A61K31/55 , A61K45/06 , C07D223/06 , C07D223/32 , A61K31/439 , A61K31/553 , C07D243/08 , A61K31/551 , C07D223/08 , C07D221/22
CPC分类号： C07D223/08 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K38/21 , A61K45/06 , A61K47/60 , C07D221/22 , C07D223/06 , C07D223/32 , C07D243/08 , C07D267/10 , C07D283/00 , C07D295/26 , C07D403/12 , A61K2300/00
摘要： Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

7. 发明申请

US20100267695A1 FUSED INDANE COMPOUND 有权
标题翻译：熔融印花化合物
公开(公告)号：US20100267695A1
公开(公告)日：2010-10-21
申请号：US12741307
申请日：2008-11-26
申请人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
发明人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
IPC分类号： A61K31/55 , A61K31/538 , A61K31/435 , A61K31/4365 , C07D223/32 , C07D265/34 , C07D495/04 , C07D491/048 , C07D221/16 , A61P25/22 , A61P25/16 , A61P25/28 , A61P25/24 , A61P25/06 , A61P25/30 , A61P25/18
CPC分类号： C07D209/94 , C07D221/16 , C07D223/32 , C07D265/34 , C07D333/78 , C07D401/06 , C07D401/12 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D513/06
摘要： [Problems] To provide a compound which is useful as an NMDA receptor antagonist.[Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.
摘要翻译： [问题]提供可用作NMDA受体拮抗剂的化合物。 [解决方案]本发明人研究了具有NMDA受体拮抗作用的化合物，并证实本发明的稠合茚满酮化合物具有优异的NMDA受体拮抗作用，从而完成了本发明。本发明的稠合吲哚化合物具有优异的NMDA受体拮抗作用，可用作阿尔茨海默氏病，脑血管性痴呆，帕金森病，难治性抑郁症，注意力缺陷多动障碍，偏头痛等的预防和/或治疗剂。

8. 发明授权

US5994537A Process for preparing azepinone compounds useful in the inhibition of ACE and NEP 失效
标题翻译：制备用于抑制ACE和NEP的氮杂酮化合物的方法
公开(公告)号：US5994537A
公开(公告)日：1999-11-30
申请号：US023995
申请日：1998-02-14
申请人： Jeffrey A. Robl
发明人： Jeffrey A. Robl
IPC分类号： C07D223/12 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D223/32 , C07D403/04 , C07F9/553 , C07F9/6558 , C07K5/078 , C07D223/10 , A61K31/675
CPC分类号： C07K5/06139 , A61K38/00
摘要： Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.
摘要翻译：具有下式I和II的化合物及其药学上可接受的盐，包括ACE和NEP的双重抑制剂和选择性ACE抑制剂：其中R，R1，R2，R3，R4，R5，R5a，R5b，R6，R7，R11 ，q和r在本文中定义。

9. 发明授权

US5990307A Process for the preparation of [2-((8.9)-Dioxo-2,6-Diazabicyclo [5.2.0]-Non-1(7)-en-2yl) Ethyl]Phosphonic acid 失效
标题翻译：制备[2 - （（8.9） - 二氧代-2,6-二氮杂双环[5.2.0] - 壬-1（7） - 壬-2-基）乙基]膦酸的方法
公开(公告)号：US5990307A
公开(公告)日：1999-11-23
申请号：US127202
申请日：1998-07-31
申请人： Andre A. Asselin , William A. Kinney , Jean Schmid
发明人： Andre A. Asselin , William A. Kinney , Jean Schmid
IPC分类号： C07F9/645 , C07D223/32 , C07C69/00
CPC分类号： C07F9/645
摘要： This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethylethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield. Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl)amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid dialkyl ester (c) in 58% yield. The phosphonic acid diethyl ester (c) was treated with bromotrimethylsilane to give compound I.
摘要翻译：本发明涉及制备式I化合物[2 - （（8,9） - 二氧代-2,6-二氮杂双环[5.2.0] - 壬-1（7） - 烯-2-基）乙基]膦酸，NMDA拮抗剂，用作抗惊厥药和神经保护剂，在涉及过度释放兴奋性氨基酸的情况下。在本发明的方法中，3-氨基丙基氨基甲酸1,1-二甲基乙酯与乙烯基膦酸二烷基酯反应得到N- [3-（叔丁氧基羰基 - 氨基）丙基] -2-氨基乙基膦酸二烷基酯（d ），产率为80％。（d）与3,4-二烷氧基环丙-3-烯-1,2-二酮的反应得到[3 - [[2-（二烷氧基磷酰基）乙基] - （2-烷氧基-3,4-二氧代-1,2 - 环丁-1-基）氨基]丙基]氨基甲酸1,1-二甲基乙酯（e），收率96％。（e）在三氟乙酸中的脱保护和环化得到[2 - （（8,9） - 二氧代-2,6-二氮杂双环[5.2.0] - 壬-1（7） - 烯-2-基）乙基]膦酸酸二烷基酯（c），收率58％。用溴代三甲基硅烷处理膦酸二乙酯（c），得到化合物I.

10. 发明授权

US5852199A Method for making carbamazephine derivative 失效
标题翻译：制备卡马西芬衍生物的方法
公开(公告)号：US5852199A
公开(公告)日：1998-12-22
申请号：US900769
申请日：1997-07-25
申请人： Chengrong Wang
发明人： Chengrong Wang
IPC分类号： G01N33/53 , A61K39/00 , C07D223/22 , C07D223/26 , C07D223/32 , G01N33/532 , G01N33/94 , C07C205/00 , C07C207/00 , C07C229/00 , C07C261/00
CPC分类号： G01N33/532 , C07D223/22 , C07D223/32 , G01N33/9473 , G01N33/9486 , Y10S435/969 , Y10S435/97 , Y10S435/975 , Y10S436/823 , Y10S530/806 , Y10T436/171538
摘要： The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.
摘要翻译：本发明提供了一种新颖的卡马西平肼化合物，其适用于共价连接到具有通式的聚合物颗粒试剂。本发明提供了一种新颖的卡马西平酸化合物，其适用于与用于生产卡马西平免疫原的蛋白质相连。本发明的卡马西平抗原具有以下通用结构：其中X为C = O，CH 2或SO 2; Y为C = O，CH 2，SO 2; R是烷基，P是蛋白质或半抗原。

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