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31. 发明授权

US5077402A Novel alpha-aminoacetophenones as photoinitiators 失效
标题翻译：新型ALPHA-氨基丁二烯作为光敏剂
公开(公告)号：US5077402A
公开(公告)日：1991-12-31
申请号：US501409
申请日：1990-03-28
申请人： Vincent Desobry , Kurt Dietliker , Rinaldo Husler , Werner Rutsch , Manfred Rembold , Franciszek Sitek
发明人： Vincent Desobry , Kurt Dietliker , Rinaldo Husler , Werner Rutsch , Manfred Rembold , Franciszek Sitek
IPC分类号： C07D209/12 , C07C67/00 , C07C209/86 , C07C213/00 , C07C219/02 , C07C219/04 , C07C225/16 , C07C225/22 , C07C229/06 , C07C229/14 , C07C229/16 , C07C229/34 , C07C229/52 , C07C233/36 , C07C253/00 , C07C255/56 , C07C313/00 , C07C317/32 , C07C317/36 , C07C323/23 , C07C323/25 , C07C323/31 , C07C323/32 , C07C323/65 , C07D209/86 , C07D219/02 , C07D219/04 , C07D223/22 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D279/18 , C07D283/00 , C07D295/02 , C07D295/10 , C07D295/104 , C07D295/112 , C07D295/12 , C07D307/91 , C07F7/18 , C08F2/46 , C08F2/50 , C09D4/00 , C09D5/32 , C09D7/12 , C09D11/10 , G03F7/031
CPC分类号： C07D295/112 , C07D209/86 , C07D295/104 , C08F2/50 , G03F7/031
摘要： Compounds of the formula I, II, III and IIIa ##STR1## in which Ar.sup.1 is an unsubstituted or substituted aromatic radical and at least one of the radicals R.sup.1 and R.sup.2 is an alkenyl, cycloalkenyl or arylmethyl group, are effective photoinitiators for photopolymerization of unsaturated compounds. They are particularly suitable for photocuring of pigmented systems.
摘要翻译：式I，II，III和IIIa的化合物其中Ar1是未取代或取代的芳族基团，并且基团R 1和R 2中的至少一个是烯基，环烯基或芳基甲基是用于光聚合不饱和化合物的有效光引发剂。它们特别适用于着色系统的光固化。

32. 发明授权

US4794197A All-cis-1,3,5-triamino-2,4,6,-cyclohexanetriol derivatives, their use, processes for their preparation and pharmaceutical preparations containing them 失效
标题翻译：全顺式1,3,5-三氨基-2,4,6 - 环己烷三醇衍生物，其用途及其制备方法及含有它们的药物制剂
公开(公告)号：US4794197A
公开(公告)日：1988-12-27
申请号：US824950
申请日：1986-01-31
申请人： Walter Schneider , Isidor Erni , Hans K. Hegetschweiler
发明人： Walter Schneider , Isidor Erni , Hans K. Hegetschweiler
IPC分类号： C07C215/30 , A61K31/13 , A61K31/16 , A61K31/195 , A61K31/415 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/66 , A61K31/675 , A61P3/00 , A61P7/00 , C07C67/00 , C07C213/00 , C07C215/44 , C07C215/90 , C07C227/00 , C07C227/02 , C07C229/14 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/41 , C07D213/46 , C07D233/64 , C07F9/38 , C07F9/40 , C07C87/36 , C07C103/19
CPC分类号： C07F9/383
摘要： All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and represent hydrogen atoms, alkyl groups or --CO-alkyl groups wherein the alkyl in the alkyl or --CO-alkyl group has 1 to 18 carbon atoms and the alkyl and --CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R.sub.1 to R.sub.6 is one of the above mentioned unsubstituted or substituted alkyl groups or --CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.
摘要翻译：对应于通式I的全顺式-1,3,5-三氨基-2,4,6-三羟基环己烷衍生物，其中符号R1，R2，R3，R4，R5和R6相同或不同，代表氢原子，烷基或-CO-烷基，其中烷基或-CO-烷基中的烷基具有1至18个碳原子，并且烷基和-CO-烷基可以彼此独立地包含一个或多个相同的或不同的官能团，R 1至R 6中的至少一个是上述未取代或取代的烷基或-CO-烷基之一，以及它们与药理学常规使用的无机或有机酸及其季铵盐的盐，其制备方法及其用途，以及含有这些化合物的药物制剂。

33. 发明授权

US4602106A Process for producing hydroxyalkylaminoacetic acids 失效
标题翻译：制备羟烷基氨基乙酸的方法
公开(公告)号：US4602106A
公开(公告)日：1986-07-22
申请号：US713798
申请日：1985-03-20
申请人： Alain Blanc
发明人： Alain Blanc
IPC分类号： C07C227/02 , C07C67/00 , C07C227/00 , C07C227/08 , C07C227/12 , C07C229/12 , C07C229/14 , C07C99/00
CPC分类号： C07C227/08
摘要： Process for producing hydroxyalkylaminoacetic acids having the general formula (I):R--CHOH--CHR.sub.1 --NR.sub.2 --CH.sub.2 --COOH (I)in which:R represents a hydrogen atom, a C.sub.1 -C.sub.18 -alkyl group, with straight or ramified chain, or a phenyl group possibly substituted by one or more radicals (preferably one or two) selected from the group comprising: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alcoxy or halogeno radicals;R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group;R.sub.2 represents a C.sub.1 -C.sub.18 -alkyl group or R.sub.3 --CHOH--CHR.sub.4 --group in which R.sub.3 identical to R represents a hydrogen atom or a C.sub.1 -C.sub.18 -alkyl group with straight or ramified chain, and R.sub.4 is identical to R.sub.1, according to which glyoxal is reacted hot upon a secondary hydroxylated amine having the general formula (III): ##STR1## in which R, R.sub.1 and R.sub.2 have the meaning as given above.
摘要翻译：制备具有通式（I）的羟基烷基氨基乙酸的方法：R-CHOH-CHR1-NR2-CH2-COOH（Ⅰ）其中：R表示氢原子，直链或支链的C1-C18-烷基，或可以被一个或多个选自以下的基团（优选一个或两个）取代的苯基：C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基或卤代基; R1表示氢原子或C1-C4烷基; R2表示C1-C18-烷基或R3-CHOH-CHR4-基，其中与R相同的R3表示氢原子或具有直链或支链的C1-C18-烷基，R4与R1相同，根据（III）的仲羟基化胺：其中R 1，R 2和R 2具有如上所述的含义。

34. 发明公开

US20230406813A1 P62-ZZ CHEMICAL INHIBITOR 审中-公开
公开(公告)号：US20230406813A1
公开(公告)日：2023-12-21
申请号：US18238830
申请日：2023-08-28
申请人： ID4PHARMA, LLC
发明人： Xiang-Qun XIE
IPC分类号： C07C229/36 , C07D309/40 , C07C211/50 , C07C317/34 , C07C217/58 , C07C217/76 , C07C219/06 , C07D241/44 , C07C229/14 , C07D487/04 , C07C235/48 , C07C251/76 , A61K31/137 , A61K31/351 , A61K31/495 , A61K31/519 , A61K31/15 , A61K31/498 , A61K45/06 , C07C249/16 , C07D309/32 , C07D475/08 , C12N5/09 , A61K31/216
CPC分类号： C07C229/36 , C07D309/40 , C07C211/50 , C07C317/34 , C07C217/58 , C07C217/76 , C07C219/06 , C07D241/44 , C07C229/14 , C07D487/04 , C07C235/48 , C07C251/76 , A61K31/137 , A61K31/351 , A61K31/495 , A61K31/519 , A61K31/15 , A61K31/498 , A61K45/06 , C07C249/16 , C07D309/32 , C07D475/08 , C12N5/0693 , A61K31/216
摘要： A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

35. 发明申请

US20220340604A1 MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF 有权
公开(公告)号：US20220340604A1
公开(公告)日：2022-10-27
申请号：US17704892
申请日：2022-03-25
申请人： Navitor Pharmaceuticals, Inc.
发明人： Kristina Michelle FETALVERO , Sridhar Narayan , David John O'Neill , Eddine Saiah , Shomit Sengupta
IPC分类号： C07F7/08 , A61K38/00 , A61K31/198 , A61K31/223 , C07C261/04 , C07C311/13 , C07C311/19 , C07C311/51 , C07C229/28 , C07C233/40 , C07C233/83 , C07C237/06 , C07C237/12 , C07C237/30 , A61K31/197 , A61K31/221 , A61K31/275 , A61K31/341 , A61K31/41 , A61K31/695 , A61K45/06 , C07C229/12 , C07C229/14 , C07C229/18 , C07C229/20 , C07C233/07 , C07C233/47 , C07C233/49 , C07C233/51 , C07C233/63 , C07C255/61 , C07C311/06 , C07C311/10 , C07C311/14 , C07D257/04 , C07D307/33
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

36. 发明申请

US20210009508A1 Automated Synthesis of Small Molecules Using Chiral, Non-Racemic Boronates 有权
公开(公告)号：US20210009508A1
公开(公告)日：2021-01-14
申请号：US16936621
申请日：2020-07-23
申请人： The Board of Trustees of the University of Illinois
发明人： Martin D. Burke , Junqi Li , Eric P. Gillis
IPC分类号： C07C229/14 , C07C227/32 , C07F5/02 , C07C229/24 , C07D207/44 , C07D207/16 , C07D211/60
摘要： Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

37. 发明申请

US20200270221A1 ANALGESIC COMPOUNDS 审中-公开
公开(公告)号：US20200270221A1
公开(公告)日：2020-08-27
申请号：US16613397
申请日：2018-05-11
申请人： RECURIUM IP HOLDINGS, LLC
发明人： Chad Daniel Hopkins , Joseph Robert Pinchman , Kevin Duane Bunker , Deborah Helen Slee , Brant Clayton Boren , Mehmet Kahraman
IPC分类号： C07D277/28 , C07C237/04 , C07C271/24 , C07C217/52 , C07C211/38 , C07C215/08 , C07C235/14 , C07C229/14 , C07C211/40 , C07D235/14 , C07D263/56 , C07D239/26 , C07D213/38 , C07D277/64
摘要： Disclosed herein are compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), methods of synthesizing compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), and methods of using compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It) as an analgesic.

38. 发明授权

US10752577B2 Automated synthesis of small molecules using chiral, non-racemic boronates 有权
公开(公告)号：US10752577B2
公开(公告)日：2020-08-25
申请号：US16255453
申请日：2019-01-23
申请人： The Board of Trustees of the University of Illinois
发明人： Martin D. Burke , Junqi Li , Eric P. Gillis
IPC分类号： C07F5/02 , C07C229/14 , C07C227/32 , C07C229/24 , C07D207/44 , C07D207/16 , C07D211/60
摘要： Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

39. 发明授权

US10696628B2 Carbondisulfide derived zwitterions 有权
公开(公告)号：US10696628B2
公开(公告)日：2020-06-30
申请号：US16383075
申请日：2019-04-12
申请人： Thomas Daly
发明人： Thomas Daly
IPC分类号： C07C333/04 , C07C229/14 , C07C219/04 , C07C229/08 , C07C229/12 , C07C333/14 , C07D401/04 , E21C50/00 , A01N47/26 , C07C329/14 , C08L95/00
摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

40. 发明申请

US20200079800A1 MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF 审中-公开
公开(公告)号：US20200079800A1
公开(公告)日：2020-03-12
申请号：US16515788
申请日：2019-07-18
申请人： Navitor Pharmaceuticals, Inc.
发明人： Kristina Michelle Fetalvero , Sridhar Narayan , David John O'Neill , Eddine Saiah , Shomit Sengupta
IPC分类号： C07F7/08 , A61K38/00 , A61K31/198 , A61K31/223 , C07C261/04 , C07C311/13 , C07C311/19 , C07C311/51 , C07C229/28 , C07C233/40 , C07C233/83 , C07C237/06 , C07C237/12 , C07C237/30 , A61K31/197 , A61K31/221 , A61K31/275 , A61K31/341 , A61K31/41 , A61K31/695 , A61K45/06 , C07C229/12 , C07C229/14 , C07C229/18 , C07C229/20 , C07C233/07 , C07C233/47 , C07C233/49 , C07C233/51 , C07C233/63 , C07C255/61 , C07C311/06 , C07C311/10 , C07C311/14 , C07D257/04 , C07D307/33
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

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