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1. 发明授权

US11407772B2 Optically-active cyclopentenone derivatives 有权
公开(公告)号：US11407772B2
公开(公告)日：2022-08-09
申请号：US17269762
申请日：2019-09-13
申请人： Tohoku University , Genesis Research Institute, Inc. , Ouchi Shinko Chemical Industrial Co., Ltd.
发明人： Hitoshi Kasai , Yoshitaka Koseki , Takaaki Kamishima , Shigenobu Aoyagi
IPC分类号： C07F7/18 , C07B51/00 , C07B63/02 , C12P7/38
摘要： The present invention provides: industrially desirable and novel optically-active cyclopentenone derivatives; and a novel industrial manufacturing method. The novel optically-active cyclopentenone derivatives and method for manufacturing the same are, respectively: an intermediate for industrially desirable and novel prostaglandin derivatives and the like; and a method for manufacturing the same. It is expected that the present invention will be commercialized and industrialized.

2. 发明授权

US10822357B2 Benzyl compound 有权
公开(公告)号：US10822357B2
公开(公告)日：2020-11-03
申请号：US15755705
申请日：2016-08-25
申请人： SEKISUI MEDICAL CO., LTD.
发明人： Shinya Yano , Yuki Wakasugi , Yosuke Iwanaga
IPC分类号： C07F7/18 , C07B51/00 , C07K1/06
摘要： The purpose of the present invention is to provide a protecting group which improves the solubility of a compound having a functional group protected with the protecting group in an organic solvent and which is easily separated and purified after a reaction with avoiding solidification or insolubilization. Provided is a benzyl compound represented by Formula (1) where X1 represents —CH2OR14 (where R14 represents a hydrogen atom, a halogenocarbonyl group, or an active ester-type protecting group), —CH2NHR15 (where R15 represents a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group), a halogenomethyl group, a methyl azide group, a formyl group, or an oxime; and at least one of R1, R2, R3, R4, and R5 is a group represented by Formula (2), and the remainders each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or an alkoxy group having 1 to 4 carbon atoms, where R6 represents a linear or branched alkylene group having 1 to 16 carbon atoms; X2 represents O or CONR16 (where R16 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms); and A represents a group represented by Formula (3), (4), (5), (6), (7), (8), (9), (10), (11), (12), or (13).

3. 发明授权

US10717698B2 Resveratrol glycolate and tartrate derivatives and synthetic methods therefor 有权
公开(公告)号：US10717698B2
公开(公告)日：2020-07-21
申请号：US16081842
申请日：2017-03-06
申请人： ELC MANAGEMENT LLC
发明人： Fatemeh Mohammadi , Elham Tavasoli
IPC分类号： C07C67/317 , C07C69/675 , C07C67/14 , A61K8/37 , A61Q19/08 , A61Q19/00 , C09B23/14 , C07B51/00
摘要： The present invention relates to compounds of ester derivative of resveratrol, compositions comprising ester derivatives of resveratrol, processes for synthesizing an ester of resveratrol, and use thereof.

4. 发明授权

US10703725B2 Process for producing novel 4-benzoazonine derivatives 有权
公开(公告)号：US10703725B2
公开(公告)日：2020-07-07
申请号：US15755275
申请日：2016-08-26
申请人： NIPPON ZOKI PHARMACEUTICAL CO., LTD.
发明人： Taizo Ito , Xiaoming Liao , Zihua Li
IPC分类号： C07D223/04 , A61K31/55 , A61P29/00 , C07D223/14 , C07B51/00
摘要： An object of the present invention is to provide a novel tetrahydroazepine compound and a process for producing the same.The present invention relates to a tetrahydroazepine compound represented by the formula (10) or a salt thereof, anda process for producing the said compound or a salt thereof. (In the formula, R1 is an optionally substituted alkyl group, R2 is an optionally substituted alkyl group and one of the X—Y bond and the Y—Z bond is a carbon-carbon double bond and the other is a carbon-carbon single bond).

5. 发明授权

US10414720B2 Process for the preparation of lacosamide 有权
公开(公告)号：US10414720B2
公开(公告)日：2019-09-17
申请号：US16076486
申请日：2017-06-12
申请人： UNICHEM LABORATORIES LTD
发明人： Dhananjay G. Sathe , Arijit Das , Sanjay Raikar , Rahul Bhagwatkar , Ramdas Ahire
IPC分类号： C07C231/02 , C07C269/04 , C07C269/06 , C07C237/00 , C07B51/00 , C07C237/22
摘要： The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.

6. 发明申请

US20190276416A1 METHOD FOR PREPARING NOTA DERIVATIVE 审中-公开
公开(公告)号：US20190276416A1
公开(公告)日：2019-09-12
申请号：US15912734
申请日：2018-03-06
申请人： INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN, R.O.C.
发明人： YU CHANG , CHENG-FANG HSU
IPC分类号： C07D255/02 , C07C303/38 , C07C303/28 , C07C311/18 , C07C309/30 , C07B51/00
摘要： A method for preparing a NOTA derivative is revealed. The method includes a plurality of steps. First take 4-toluenesulfonyl chloride and diethylenetriamine to carry out tosylation reaction and obtain a first product. Then the first substitution reaction takes place upon addition of the first product with sodium methoxide to get the second product. Next take 4-toluenesulfonyl chloride to react with ethylene glycol for preparing a third product by tosylation reaction therebewteen. Then a coupling reaction between the third product and the second product is carried out to produce a fourth product. The second substitution reaction occurs involving the fourth product in the presence of sulfuric acid. Lastly take the reaction product and hydrochloric acid to have bonding reaction and obtain a final product. The method solves the water-absorption problem of the cyclic organic compound TACN, a NOTA derivative.

7. 发明申请

US20190276389A1 SYNTHESIS OF ARYL CYCLOHEXANE ESTER DERIVATIVES USEFUL AS SENSATES IN CONSUMER PRODUCTS 审中-公开
公开(公告)号：US20190276389A1
公开(公告)日：2019-09-12
申请号：US15378547
申请日：2016-12-14
申请人： The Procter & Gamble Company
发明人： John August WOS , Kenneth Edward YELM , Gregory Mark BUNKE , Heath Alan FREDERICK , Michael REILLY , John Christian HAUGHT , Koti Tatachar SREEKRISHNA , Yakang LIN
IPC分类号： C07C237/22 , C07C231/16 , C07B51/00 , C07C231/12 , C07C231/02
摘要： Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.

8. 发明申请

US20190225631A1 NOVEL DIPHENYLMETHANE PROTECTIVE AGENT 审中-公开
公开(公告)号：US20190225631A1
公开(公告)日：2019-07-25
申请号：US16307105
申请日：2017-06-19
申请人： SEKISUI MEDICAL CO., LTD.
发明人： Shinya YANO , Hideki KUBOTA
IPC分类号： C07F7/18 , C07B51/00
摘要： An object of the present invention is to develop a protecting group, which can prevent solidification or insolubilization of a compound by protecting a functional group to achieve easy separation and purification after a reaction.A diphenylmethane compound represented by general formula (1): wherein Y represents —OR19 (wherein R19 represents a hydrogen atom or an active ester-type protecting group), —NHR20 (wherein R20 represents, for example, a hydrogen atom, a C1-6 linear or branched alkyl group, or an aralkyl group, at least one of R1 to R10 represents a group represented by formula (2): —O—O—R11—X-A (2) and the others each independently represent a hydrogen atom, a halogen atom, a C1-4 alkyl group, or a C1-4 alkoxy group; R11 represents a C1-16 linear or branched alkylene group; X represents O or CONR21 (wherein R21 represents a hydrogen atom, or a C1-4 alkyl group; and A represents, for example, a group represented by formula (3)

9. 发明授权

US10160694B2 Agent for introducing protecting group for hydroxy group and/or mercapto group 有权
公开(公告)号：US10160694B2
公开(公告)日：2018-12-25
申请号：US15517899
申请日：2015-09-30
申请人： KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
发明人： Kohei Torikai
IPC分类号： C07C41/16 , C07B41/02 , C07C43/164 , C07C43/174 , C07B51/00 , C07C309/63 , C07C15/14 , C07C22/04 , C07D209/04 , C07D215/02 , C07D333/72
摘要： A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R1, R2, R3, and R4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO2R5 (R5=an aryl group or an alkyl group).

10. 发明申请

US20180002318A1 SYNTHESIS OF CYCLOPROPYL INDOLES AND CYCLOHEPTA[B]INDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD OF USING THEM 审中-公开
公开(公告)号：US20180002318A1
公开(公告)日：2018-01-04
申请号：US15545858
申请日：2015-12-03
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION
发明人： Weiping Tang , Xiaoxun Li
IPC分类号： C07D405/08 , B01J31/40 , B01J31/22 , C07B37/10 , C07D209/08 , C07B51/00
CPC分类号： C07D405/08 , B01J31/2265 , B01J31/4046 , B01J2231/325 , C07B37/10 , C07B51/00 , C07D209/08 , Y02P20/55
摘要： Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst.

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