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1. 发明申请

US20220267239A1 CANNABINOID DERIVATIVES 有权
公开(公告)号：US20220267239A1
公开(公告)日：2022-08-25
申请号：US17624585
申请日：2020-07-03
申请人： CANOPY GROWTH CORPORATION
发明人： JEFFREY ALAN OMEARA , QUANG HUY TO
IPC分类号： C07C43/267 , C07C43/275 , C07C43/315 , C07C271/16 , C07C271/28 , C07C65/28 , C07C69/28 , C07C69/96 , C07D205/04
摘要： The present invention provides cannabinoid derivatives, a pharmaceutical composition comprising said derivative and a method of using said derivatives in treating or preventing a disease associated with cannabinoid receptors. The claimed cannabinoid derivatives are described by formula (I) or an enantiomer, diastereomer, racemate, tautomer, or metabolite thereof, or a pharmaceutically acceptable salt, solvate or hydrate of the compound.

2. 发明授权

US11242317B2 EBNA1 inhibitors and their method of use 有权
公开(公告)号：US11242317B2
公开(公告)日：2022-02-08
申请号：US16519590
申请日：2019-07-23
申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY
发明人： Troy E. Messick , Garry R. Smith , Allen B. Reitz , Paul M. Lieberman , Mark E. McDonnell , Yan Zhang , Venkata Velvadapu
IPC分类号： A61K31/405 , A61K31/41 , A61K31/42 , A61K31/415 , A61K31/40 , C07D515/02 , C07D209/44 , C07D295/04 , C07D261/06 , C07D233/02 , C07D233/00 , C07D207/327 , A61K31/404 , A61K31/4439 , A61K31/496 , A61K31/192 , A61K31/44 , C07C229/56 , C07C255/54 , C07C255/55 , C07C211/27 , C07C217/84 , C07C233/11 , C07C233/64 , C07C233/65 , C07C235/58 , C07C311/08 , C07C311/16 , C07C311/17 , C07C317/14 , C07D235/06 , C07D403/10 , C07D239/26 , C07D409/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D209/08 , C07D295/155 , C07D213/55 , C07C53/18 , C07C63/66 , C07C65/19 , C07C65/28 , C07C229/64 , C07C317/44 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/70 , C07D213/64 , C07D213/74 , C07D215/14 , C07D231/12 , C07D249/06 , C07D277/30 , C07D307/79 , C07D333/54 , C07D401/04 , C07D401/10
摘要： Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

3. 发明授权

US10384997B2 Bio-stable cannabinoid compounds and methods for enhancing their physiological concentration 有权
公开(公告)号：US10384997B2
公开(公告)日：2019-08-20
申请号：US15813358
申请日：2017-11-15
申请人： Teewinot Technologies Limited
发明人： Malcolm J. Kavarana , Richard C. Peet , Jeffrey M. Korentur
IPC分类号： C07C43/23 , A61P25/00 , C12N9/02 , C07C65/28 , C12P7/22
摘要： The present disclosure provides biostable cannabinoid compounds according to Formula I: and methods for synthesizing and enhancing the biological concentrations of the compounds, where R1, R2, and R3 are defined as set forth in the disclosure.

4. 发明申请

US20180086699A1 EBNA1 INHIBITORS AND THEIR METHOD OF USE 审中-公开
公开(公告)号：US20180086699A1
公开(公告)日：2018-03-29
申请号：US15814600
申请日：2017-11-16
申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY
发明人： TROY E. MESSICK , GARRY R. SMITH , ALLEN B. REITZ , PAUL M. LIEBERMAN , MARK E. McDONNELL , YAN ZHANG , VENKATA VELVADAPU
IPC分类号： C07D207/327 , C07C311/08 , C07D207/16 , C07D211/70 , C07D213/64 , C07D213/74 , C07D215/14 , C07D231/12 , C07D249/06 , C07D277/30 , C07D307/79 , C07D333/54 , C07D401/04 , C07C53/18 , C07C63/66 , C07C65/19 , C07C65/28 , C07C229/64 , C07C317/44 , C07D207/08 , C07D401/10 , C07D207/14 , C07D213/55 , C07D295/155 , C07D209/08 , C07D487/04 , C07D471/04 , C07D417/10 , C07D409/10 , C07D239/26 , C07D403/10 , C07D235/06 , C07C229/56 , C07C235/58 , C07C233/65 , C07C233/64 , C07C233/11 , C07C217/84 , C07C211/27 , C07C255/55 , C07C255/54 , C07C317/14 , C07C311/17 , C07C311/16 , C07D207/12
摘要： Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

5. 发明申请

US20140171388A1 COMPOUND FOR TREATING CARTILAGE DISORDERS 有权
标题翻译：化合物用于治疗消化系统疾病
公开(公告)号：US20140171388A1
公开(公告)日：2014-06-19
申请号：US14237037
申请日：2012-08-03
申请人： Tetsuo Obitsi , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
发明人： Tetsuo Obitsi , Kousuke Tani , Hikaru Sugihara , Akio Nishiura , Shinsei Fujimura
IPC分类号： C07C405/00 , C07C235/16 , C07C59/56 , C07C65/28
CPC分类号： C07C59/56 , A61K9/0019 , A61K47/26 , A61K47/6951 , C07C235/06 , C07C235/16 , C07C405/00 , C07C2601/04 , C07C2601/08 , Y10T428/2982
摘要： The present invention provides a compound of which active |form| is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I): (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders. Since a suspension produced using this compound can be injected without requiring the incision of the affected part, it can reduce the burden on patients, and is extremely useful as a medicinal agent.
摘要翻译：本发明提供了一种活性成分的化合物由式（A）表示。并且其可以注射到作为疾病的一部分的关节腔中，并且可以以持续的方式累积在关节腔中以发挥其药理作用，以改善软骨疾病而不产生副作用。由式（I）表示的本发明化合物（其中所有符号如说明书中所定义）是可以实现上述目的的化合物。即使当化合物以有效量施用以显示软骨再生活性时，该化合物也不会对心血管系统显示任何副作用，因此作为软骨疾病的安全有效的预防和/或治疗剂非常有用。由于使用该化合物制备的悬浮液可以不需要切开患者部位而被注射，所以能够减轻患者的负担，作为药剂非常有用。

6. 发明申请

US20100267778A1 Diphenyl ether compound, process for producing the same, and use 审中-公开
标题翻译：二苯醚化合物，其制备方法和用途
公开(公告)号：US20100267778A1
公开(公告)日：2010-10-21
申请号：US10567363
申请日：2004-08-03
申请人： Shinya Kusuda , Yoshisuke Nakayama , Masaki Ima , Hisao Tajima , Sachiko Kato
发明人： Shinya Kusuda , Yoshisuke Nakayama , Masaki Ima , Hisao Tajima , Sachiko Kato
IPC分类号： A61K31/455 , C07C65/28 , A61K31/192 , A61P3/06 , A61K31/235 , C07C69/94 , C07C59/68 , C07D263/32 , A61K31/421 , C07D277/30 , A61K31/426 , C07D213/55 , A61K31/435 , C07C217/90 , A61K31/196
CPC分类号： C07D263/32 , C07C65/24 , C07C217/90 , C07D213/30
摘要： The present invention relates to a compound represented by formula (I): wherein ring A, ring B and ring D each independently represents a cyclic group which may have a substituent(s); W is a spacer having 1 to 8 atom(s) in its main chain; X is a spacer having 1 to 2 atom(s) in its main chain; Y is a binding bond or a spacer having 1 to 8 atom(s) in its main chain; and Z is an acidic group, or a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I) has a PPAR δ agonistic action and is useful as a preventive and/or treating agent for diseases where sugar and lipid metabolisms are abnormal (diabetes, hyperlipemia, arteriosclerosis, cardiovascular diseases, obesity and metabolic syndrome or the like), hypertension, circulatory diseases and skin inflammation diseases.
摘要翻译：本发明涉及由式（I）表示的化合物：其中环A，环B和环D各自独立地表示可以具有取代基的环状基团。 W是其主链中具有1至8个原子的间隔基; X是其主链中具有1至2个原子的间隔基; Y是其主链中具有1至8个原子的结合键或间隔基; 并且Z是酸性基团，或其盐，其溶剂合物或其前药。由式（I）表示的化合物具有PPARδ激动作用，并且可用作糖和脂质代谢异常（糖尿病，高脂血症，动脉硬化，心血管疾病，肥胖症和代谢综合征或疾病）的疾病的预防和/或治疗剂喜欢），高血压，循环系统疾病和皮肤炎症疾病。

7. 发明申请

US20090286882A1 Cyclopropylacetic Acid Derivatives and Use Thereof 失效
标题翻译：环丙基乙酸衍生物及其用途
公开(公告)号：US20090286882A1
公开(公告)日：2009-11-19
申请号：US12083761
申请日：2006-10-09
申请人： Eva-Maria Becker , Michael Hahn , Andreas Knorr , Christian Pilger , Johannes-Peter Stasch , Kari-Heinz Schlemmer , Frank Wunder
发明人： Eva-Maria Becker , Michael Hahn , Andreas Knorr , Christian Pilger , Johannes-Peter Stasch , Kari-Heinz Schlemmer , Frank Wunder
IPC分类号： A61K31/194 , A61P9/10 , A61P9/12 , C07C65/28
CPC分类号： C07C65/28
摘要： The present application relates to novel cyclopropylacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
摘要翻译：本申请涉及新的环丙基乙酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/或预防疾病，特别是治疗的药物的用途和/或预防心血管疾病。

8. 发明申请

US20050234131A1 Novel ligand antagonists of RAR receptors and pharmaceutical/cosmetic applications thereof 有权
标题翻译： RAR受体的新型配体拮抗剂及其药物/化妆品应用
公开(公告)号：US20050234131A1
公开(公告)日：2005-10-20
申请号：US11116344
申请日：2005-04-28
申请人： Philippe Diaz , Catherine Raffin , Thibaud Biadatti
发明人： Philippe Diaz , Catherine Raffin , Thibaud Biadatti
IPC分类号： A61K31/19 , A61K31/195 , A61P17/00 , C07C63/36 , C07C63/64 , C07C63/66 , C07C65/11 , C07C65/19 , C07C65/28 , C07C65/34 , C07C65/38 , C07C69/76 , C07C229/18 , C07C229/38 , C07C229/52 , C07C233/54 , C07C235/38 , C07C235/42 , C07C235/78 , C07C259/10 , C07C271/28 , C07C323/62 , C07C391/02 , C07D213/30 , C07D213/79 , C07D213/80 , C07D333/16
CPC分类号： C07D213/79 , C07B2200/07 , C07C63/36 , C07C63/64 , C07C63/66 , C07C65/11 , C07C65/19 , C07C65/28 , C07C65/34 , C07C65/38 , C07C69/76 , C07C229/18 , C07C229/38 , C07C229/52 , C07C233/54 , C07C235/38 , C07C235/42 , C07C235/78 , C07C259/10 , C07C271/28 , C07C323/62 , C07C391/02 , C07C2602/10 , C07D213/30 , C07D213/80 , C07D333/16
摘要： Novel ligand antagonists of the RAR receptors have the following structural formula (1): in which A is a CH2, CHOH, C═O or C═N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):
摘要翻译： RAR受体的新配体拮抗剂具有以下结构式（1）：其中A是CH 2，CHOH，C-O或C-N-OH基或硫或硒原子; B为选自式（a）〜（f）的基团：Ar为选自式（g）〜（i）的基团：

9. 发明授权

US6114175A Compound for the antemortem diagnosis of Alzheimer's Disease and in vivo imaging and prevention of amyloid deposition 失效
标题翻译：用于阿尔茨海默氏病的止血诊断和体内成像和预防淀粉样蛋白沉积的化合物
公开(公告)号：US6114175A
公开(公告)日：2000-09-05
申请号：US188244
申请日：1998-11-09
申请人： William E. Klunk , Jay W. Pettegrew , Chester A. Mathis, Jr.
发明人： William E. Klunk , Jay W. Pettegrew , Chester A. Mathis, Jr.
IPC分类号： A61K31/32 , A61K31/60 , A61K31/655 , A61K49/06 , A61M36/14 , C07B59/00 , C07C63/66 , C07C65/03 , C07C65/19 , C07C65/28 , C07C69/88 , C07C69/94 , C07D209/48 , C07D217/24 , C07D221/10 , C07D221/14 , C07D237/28 , C07D237/32 , C07D257/04 , C07D261/20 , C07D265/02 , C07D265/14 , C07D265/26 , C07D271/10 , C07F7/22 , C07F7/24 , C09B23/14 , G01N33/48 , G01N33/68
CPC分类号： C07D209/48 , A61K49/06 , C07B59/001 , C07B59/002 , C07C63/66 , C07C69/94 , C07D217/24 , C07D221/14 , C07D237/28 , C07D237/32 , C07D257/04 , C07D261/20 , C07D265/02 , C07D265/14 , C07D265/26 , C07D271/10 , C07F7/2212 , C09B23/141 , G01N33/6896 , G01N2800/2821
摘要： Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.
摘要翻译：描述了作为Chrysamine G的非偶氮衍生物的淀粉样蛋白结合化合物，含有药物组合物的方法，以及使用这些化合物在体内鉴定阿尔茨海默氏症并诊断特征为淀粉样变性的其它病理状态如唐氏综合征的方法。还描述了含有Chrysamine G的非偶氮衍生物的药物组合物和使用这种组合物在淀粉样变性相关病症中预防细胞变性和淀粉样蛋白诱导的毒性的方法。还描述了使用非偶氮Chrysamine G衍生物在活组织检查或尸检组织中染色或检测淀粉样蛋白沉积物的方法。还描述了使用非偶氮Chrysamine G衍生物来量化活组织检查和死后组织匀浆中的淀粉样沉积物的方法。

10. 发明授权

US5945561A Retinoid-like compounds 失效
标题翻译：类视黄醇样化合物
公开(公告)号：US5945561A
公开(公告)日：1999-08-31
申请号：US66206
申请日：1998-04-24
申请人： John E. Starrett, Jr. , Kenneth M. Tramposch , Xina Nair , Peter R. Reczek , Anna Ericsson , Anne Marinier , Alain Martel , Fred C. Zusi
发明人： John E. Starrett, Jr. , Kenneth M. Tramposch , Xina Nair , Peter R. Reczek , Anna Ericsson , Anne Marinier , Alain Martel , Fred C. Zusi
IPC分类号： C07C63/66 , C07C65/19 , C07C65/28 , C07C69/00 , C07C69/76 , C07C323/61 , C07D213/55 , C07D307/54 , C07C63/36
CPC分类号： C07C69/00 , C07C323/61 , C07C63/66 , C07C65/19 , C07C65/28 , C07C69/76 , C07D213/55 , C07D307/54 , C07C2103/00 , C07C2103/24
摘要： Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.
摘要翻译：某些具有通式的新的取代的（5,6） - 二氢蒽基化合物其中A，n，p，R1，R2，R3，R4，R5，R6，R7和R8如本说明书中所定义，表示类视黄醇样物质，特别适用于预防手术后粘连。

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