Category: 1133122-96-9

On November 21, 2019, Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.Category: amides-buliding-blocks The title of the patent was Substituted condensed thiophenes as modulators of STING protein and their preparation. And the patent contained the following:

The invention relates to substituted benzothiophenes, thienopyridines and thienopyrimidines of formula I and their use as pharmaceuticals for treating diseases ameliorated by modulation of STING protein. Compound of formula I wherein R1 is H, C3-6 cycloalkyl, (un)substituted C3-7 heterocyclyl and (un)substituted (un)branched C1-4 alkyl; A1 is CRA or N; A2 is CRB or N; A3 is CRC or N; A4 is CRD or N; where no more than two of A1, A2, A3, and A4 may be N; one or two of RA, RB, RC, and RD are selected from H, F, Cl, Br, Me, CF3, cyclopropyl, cyano, OMe, OEt, CH2OH, CH2OMe and CH2NMe2; the remainder of RA, RB, RC, and RD are H; Y is O, NH or CH2; R’ is (un)substituted arylcarboxamide, (un)substituted heteroarylcarboxamide and (un)substituted 3-aminobenzisoxazol-6-yl; are claimed. Example compound II was prepared by hydrolysis of Et 3-((4-carbamoylphenoxy)methyl)-4-fluorobenzo[b]thiophene-2-carboxylate. The invention compounds were evaluated for their STING modulatory activity (data given). The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Category: amides-buliding-blocks

The Article related to condensed thiophene preparation sting modulator, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On October 7, 2021, Giroux, Simon; Nuhant, Philippe Marcel; Bandarage, Upul Keerthi; Garcia Barrantes, Pedro Manuel; Liao, Yusheng; Gale-Day, Zachary; Gu, Wenxin; Karns, Alexander S.; Zhang, Hu; Allen, Emily Elizabeth; Xu, Jinwang; Deninno, Michael Paul; Tang, Qing; Boucher, Diane Marie; Fanning, Lev T.D.; Hall, Amy B.; Hurley, Dennis James; Johnson, Mac Arthur, Jr.; Maxwell, John Patrick; Swett, Rebecca Jane; Tapley, Timothy Lewis; Thomson, Stephen A.; Damagnez, Veronique; Cottrell, Kevin Michael published a patent.Quality Control of 2-Fluoro-4-hydroxybenzamide The title of the patent was Preparation of 1H-pyrazolo[4,3-g]isoquinoline and 1H-pyrazolo[4,3-g]quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency. And the patent contained the following:

1H-pyrazolo[4,3-g]isoquinoline and 1H-pyrazolo[4,3-g]quinoline derivatives(I) as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD). Compounds I wherein Z1-Z3 each independently -N, -NH, or -CH; V1 and V2 are each selected from C and N; W1 and W2 are each selected from -C=O, -CR2, N, etc.; etc., are claimed. The example compound II was prepared via 4-steps synthesis using (4-chlorophenyl)boronic acid as starting material reacting with intermediate (also prepared)(procedure given). Compounds I were evaluated for alpha-1-antitrypsin modulating activity (data given). Compounds I can be used for the treatment of α1-antitrypsin deficiency. The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Quality Control of 2-Fluoro-4-hydroxybenzamide

The Article related to pyrazoloquinoline preparation alpha1 antitrypsin deficiency treatment, pyrazoloisoquinoline preparation alpha1 antitrypsin modulator deficiency treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Quality Control of 2-Fluoro-4-hydroxybenzamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On January 27, 2022, Wu, Hao; Wu, Wenmao; Li, Ling; Zhang, Zhan; Wang, Feng; Yuan, Ding; Wu, Yunfei; Chen, Qiang; Han, Han; Guo, Jing; Lan, Hong; Ding, Lieming; Wang, Jiabing published a patent.Category: amides-buliding-blocks The title of the patent was Piperidine-spiro-fused heterocyclic compounds as SHP2 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to piperidine-spiro-fused heterocyclic compounds of formula I, which are serving as an Src homol. region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitors, as well as to their pharmaceutical compositions thereof, the preparation method therefor, and the use in treating an SHP2 mediation disease. The compounds of formula I exert effects by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis. Compounds of formula I wherein the dotted double bond is either a single bond, or a double bond; ring A is (un)saturated 5- to 10-membered (hetero)cyclic ring; ring C is (un)saturated 5- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl; each Rc is independently H, halo, CN, NO2, SF5, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, etc.; two of the Rc may be taken together with the atom attached to form C3-8 cycloalkyl, 3- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl, etc.; T is (CRc1Rc2)0-3; Rc1 and Rc2 are independently H, halo, C1-4 alkly, -OR5; Rc1Rc2 may be taken together with the atom attached to form C3-6 cycloalkyl, 3- to 6-membered heterocyclic ring; each R1 is independently H, halo, CN, NO2, C1-6 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, etc.; X is O, NH and derivatives, SO0-2, CO, -CO-O-, -CO-NH- and derivatives, etc.; M is O, NH and derivatives, (un)substituted CH; Y1 and Y2 are independently NH and derivatives, (un)substituted CH; each R4 is independently H, halo, CN, NO2, C1-8 alkyl, C2-8 alkenyl, etc.; R5 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkenyl, etc.; and their pharmaceutically acceptable salts, deuterium,stereoisomers, chelates, prodrugs as SHP2 inhibitors in the treatment of diseases thereof, are claimed. Example compound II was prepared by using spirocyclization, imination, reduction, cross-coupling as the key steps. All the invention compounds were evaluated for their SHP2 inhibitory activity. The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Category: amides-buliding-blocks

The Article related to piperidine spiro fused heterocyclic preparation shp2 inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics