Tag: 200-300

On August 2, 2018, Capacci, Andrew George; Dechantsreiter, Michael; Enyedy, Istvan; Jones, John H.; Lin, Edward Yin-Shiang; Lucas, Brian Stuart; Ma, Bin published a patent.Synthetic Route of 869640-41-5 The title of the patent was Preparation of tetrahydroisoquinolines as Nrf2 activators useful in treatment of diseases caused by oxidative stress. And the patent contained the following:

Provided are tetrahydroisoquinoline derivatives as Nrf2 activators. The invention relates to preparation of tetrahydroisoquinolines of formula I as Nrf2 activators useful in treatment of diseases caused by oxidative stress. Compounds I wherein all the variables are as defined in the disclosure, are claimed. The example compound II was prepared by multistep synthesis (procedure given). Compounds I were tested for Nrf2 activating activity (data given). Compounds I, or pharmaceutically acceptable salts thereof, which are activators of nuclear factor erythroid 2 (NF-E2) -related factor 2 (Nrf2) and are useful to treat diseases caused by oxidative stress, such as neurodegenerative diseases or inflammation. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Synthetic Route of 869640-41-5

The Article related to tetrahydroisoquinoline prepare nrf2 activator oxidative stress disease treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Synthetic Route of 869640-41-5

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On May 11, 2018, Cheng, Zhanling; Wang, Jianhua; Wang, Min; Yang, Song published a patent.Synthetic Route of 869640-41-5 The title of the patent was Preparation of tetrahydroisoquinoline derivatives for use as anti-hepatitis b virus agents. And the patent contained the following:

Title compounds I [R1 and R2 independently = H, amino, alkoxy, cycloalkoxy, etc.; R3 = H, alkyl, or cycloalkyl; U = N, C(alkoxy), C(alkyl), etc.; V = H, N, C(alkyl), or C(cycloalkyl); W, X, and Y independently = N or CH], and their pharmaceutically acceptable salts, are prepared and disclosed as anti-hepatitis b virus agents. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in HBsAg inhibition assays, e.g., II demonstrated an IC50 value of 3.172 μM. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Synthetic Route of 869640-41-5

The Article related to tetrahydroisoquinoline preparation antihepatitis b virus agent, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Synthetic Route of 869640-41-5

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On November 22, 2007, Shishido, Yuji; Nakao, Kazunari; Nagayama, Satoshi; Tanaka, Hirotaka; Duncton, Matthew Alexander James; Cox, Matthew; Kincaid, John; Sahasrabudhe, Kiran; Estiarte-Martinez, Maria de Los Angeles published a patent.Recommanded Product: 958334-24-2 The title of the patent was Preparation of bicyclic amide derivatives as ion-channel ligands. And the patent contained the following:

The title compounds I [W, W1, X1, X1, Y, Y1, Z = CR8 or N; R1, R2 = H, halo, OH, etc.; R3 = H, halo, OH, etc.; R4, R5 = H, alkyl, halo, haloalkyl, hydroxyalkyl; R7 = alkyl; R8 = H, halo, OH, etc.] that may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of nonlimiting example, pain, inflammation, traumatic injury, and others, were prepared and formulated. A multistep synthesis of (1R)-II, starting from 1-(4-hydroxy-3-methylphenyl)ethanone, is described. Exemplified compounds I were evaluated in an acid stimulation assay (IC50 values of VR1 antagonists were given). The experimental process involved the reaction of Methyl 7-bromo-1,5-naphthyridine-3-carboxylate(cas: 958334-24-2).Recommanded Product: 958334-24-2

The Article related to bicyclic amide preparation ion channel ligand vr1 antagonist, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 958334-24-2

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On September 10, 2021, Li, Xiaolin; Xie, Yonghua; Shi, Feng; Li, Zizhong; Wu, Yiqin; Ma, Xiaoyun; Zhang, Shimeng; Wu, Qian published a patent.SDS of cas: 445490-78-8 The title of the patent was Preparation of pyrrolidine integrin modulator as antitumor agents. And the patent contained the following:

Disclosed are a compound, and a racemate, a stereoisomer, a tautomer, an isotopic marker, a nitrogen oxide, a solvate, a polymorph, a metabolite, an ester, and a prodrug thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, a preparation method therefor, and the medical use thereof. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).SDS of cas: 445490-78-8

The Article related to pyrrolidine preparation integrin modulator antitumor, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.SDS of cas: 445490-78-8

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On May 17, 2018, Zhao, Guohua; Devasthale, Pratik; Ye, Xiang-Yang; Selvakumar, Kumaravel; Dhanusu, Suresh; Balasubramanian, Palanikumar; Guernon, Leatte R.; Civiello, Rita; Han, Xiaojun; Parker, Michael F.; Jacutin-Porte, Swanee E. published a patent.Synthetic Route of 445490-78-8 The title of the patent was 3-Substituted propanoic acids as alpha V integrin inhibitors and their preparation. And the patent contained the following:

The invention provides compounds of formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αV-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αV-containing integrins, such as pathol. fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions Compounds of formula I wherein A, E and G are independently N, O, S, NH and derivatives, CHR6b and CR6b; M and L are N and C, with the proviso that M and L are not both N; Z is (un)substituted C1-6 alkylene; Z is a bond, O, S, NH, (un)substituted O-C1-3 alkylene, etc.; R1 is guanidino, (un)substituted imidazolylamino, (un)substituted pyridinylamino, (un)substituted benzimidazolyl, etc.; R2 is H and C1-6 alkyl; R3 is H, C1-6 alkyl, C3-10 carbocyclyl, C6-10 aryl, etc.; R2R3 an be taken together to form and (un)substituted carbocyclyl and heterocyclyl; R4 is H, C1-10 alkyl, C3-10 carbocyclyl, 3- to 10-membered heterocyclyl, R5 is H, (un)substituted C1-6 alkyl, (un)substituted Ph, (un)substituted benzyl, etc.; R6b is H, halo, CN, NO2, OH, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their αV integrin inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 50 nM, 2.4 nM, 1.5 nM and 262 nM towards αVβ6, αVβ3, αVβ5 and αVβ8, resp. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Synthetic Route of 445490-78-8

The Article related to substituted propanoic acid preparation alpha v integrin inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 445490-78-8

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On May 17, 2018, Ye, Xiang-Yang; Morales, Christian L.; Higgins, Mendi A.; Mull, Eric published a patent.Name: tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate The title of the patent was Indazole derivatives as αV integrin antagonists and their preparation. And the patent contained the following:

The invention provides compounds of formula I or II, or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αV- containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αV-containing integrins, such as pathol. fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions Compounds of formula I and II wherein A, E, G and J are independently N,C and NH, with the proviso that at least one of A, E, G and J is C and attached to Y; X is (un)substituted C1-4 alkylene; Y is a bond, O, S, NH, C1-3 alkoxy, etc.; R1 is guanidino, (un)substituted imidazolylamino, (un)substituted pyridinylamino, (un)substituted benzimidazolylamino, etc.; R2 is H, halo and c1-6 alkyl; R3 is H, C1-6 alkyl, C3-10 carbocyclyl, etc.; R3a is H; R3R2a can be taken together to form (un)substituted C3-6 carbocyclyl and (un)substituted 3- to 6-membered heterocyclyl; R4 is H, C1-6 alkyl, C3-10 carbocyclyl, etc.; R5 is H, (un)substituted C1-6 alkyl, (un)substituted Ph, (un)substituted benzyl, etc.; dashed bonds are single and double bonds; and pharmaceutically acceptable salts thereof, are claimed. Example compound III was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their αVβ6 integrin antagonistic activity. From the assay, it was determined that compound III exhibited IC50 value of 1600 nM. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Name: tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate

The Article related to indazole preparation integrin alpha v antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Name: tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On October 20, 2016, Fukunaga, Hirofumi; Dozono, Hiroyuki; Hino, Akihiro; Oshikiri, Shinobu; Nagano, Akio published a patent.Computed Properties of 445490-78-8 The title of the patent was Therapeutic or diagnostic agents for integrin-related disease comprising nitrogen-containing compounds metal complexes. And the patent contained the following:

Disclosed is a therapeutic or diagnostic agents for integrin-related disease comprising metal complexes with nitrogen-containing compounds The nitrogen-containing compounds are, represented by formula I [A1 = chelate group; R1, R2 = H, (un)substituted C1-6 alkyl, amino protective group; Z1-Z5 = N, CR3; R3 = H, halo, (un)substituted C1-6 alkyl, (un)substituted pyridinyl-containing sulfonyl group; L1 = [NR13(CR14CR15O)qCR16CO]r; L2, L3 = (un)substituted C1-6 alkylene; R13 = H, (un)substituted C1-6 alkyl, amino protective group; R14, R15 = H, (un)substituted C1-6 alkyl; R16 = H, (un)substituted C1-6 alkyl, aromatic or heterocycle amide-containing group]. Thus, reacting tetrahydronaphthyridine terminal-containing cysteic acid (preparation given) with tri-tert-Bu 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate, and deprotecting tert-Bu groups with aqueous LiOH, gave tetraazacyclododecane ring-containing tricarboxylic acid. The tetraazacyclododecane ring-containing tricarboxylic acid can give complexes with radioactive metals showing high concentration and retention in the cancer cells. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Computed Properties of 445490-78-8

The Article related to heterocycle metal complex preparation integrin disorder cancer radiopharmaceutical diagnostic, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Computed Properties of 445490-78-8

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On October 6, 2008, Harris, Craig S.; Germain, Herve; Pasquet, Georges published an article.Quality Control of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate The title of the article was Facile preparation of thiophene C2-ethers using the Mitsunobu reaction. And the article contained the following:

The preparation of thiophene ethers generally requires forcing conditions thus limiting the choice of alkyl substituent. Herein, we report the first successful generally applicable conditions for the selective O-alkylation of 2(5H)-thiophenone. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Quality Control of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate

The Article related to thiophenone alc mitsunobu alkylation, thiophene ether preparation, Heterocyclic Compounds (One Hetero Atom): Thiophenes and other aspects.Quality Control of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On May 20, 2010, Shipps, Gerald W., Jr.; Cheng, Cliff C.; Achab, Abdelghani Abe; Yao, Zhiping; Whitehurst, Charles E.; Zhang, Mingxuan; Yang, Xianshu; Herr, Robert Jason; Zych, Andrew John; Roy, Sudipta; Yang, Jinhai published a patent.Electric Literature of 445490-78-8 The title of the patent was Preparation of benzyltetrahydronaphthyridinylethylurea derivatives and analogs for use as HIV blockers. And the patent contained the following:

Title compounds I [L = (un)substituted urea, isothiourea, sulfamide, etc.; R1 = (un)substituted tetrahydronaphthalene, tetrahydronaphthyridine, dihydrobenzothio pyran; each R2 independently = H, (un)substituted alkyl, or cycloalkyl; each R3 independently = H, (un)substituted alkyl, cycloalkyl, or aryl; R4 = (un)substituted aryl, cycloalkyl, or heteroaryl ring containing 1 to 3 heteroatoms selected from O, S, or N; m = 1 to 3; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as HIV blockers. Thus, e.g., II was prepared by coupling of 3,4-dichlorobenzyl isocyanate with 2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethanamine hydrochloride. Select I were evaluated in HIV CXCR4 affinity assays, e.g., II demonstrated an IC50 value of 2.4 μM. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Electric Literature of 445490-78-8

The Article related to naphthyridinylethylurea benzyltetrahydro derivative preparation hiv blocker, benzyltetrahydronaphthyridinylethylurea analog preparation hiv blocker, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 445490-78-8

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

On December 13, 2007, Arnould, Jean-Claude; Delouvrie, Benedicte; Ducray, Richard; Lambert-Van Der Brempt, Christine Marie Paul published a patent.COA of Formula: C15H22N2O3 The title of the patent was Preparation of tyrosine derivatives, especially N-(benzoyl)-O-[2-[(pyridin-2-yl)amino]ethyl]-L-tyrosines and related compounds, as α5β1 integrin antagonists for treating solid tumors. And the patent contained the following:

The invention is related to tyrosine derivatives I [Xa = O, S; R1 = Br, Cl, cyclopentylmethyl, C1-3 alkyl, etc.; R2, each R3 = independently H, halo, CN, OH, NH2, (un)substituted alk(en/yn)yl, alkanoylamino, N-alkylsulfamoyl, etc.; or R2R3 = C1-3 alkylenedioxy; m = 0-3; R4 = H, (un)substituted heterocyclyl, heteroaryl, etc.; A = Ph, pyridinyl, thiophenyl; n = 0-4; each R5 = independently halo, OH, SH, carbamoyl, sulfamoyl, alkylsulfonyl, alkynoylamino, etc.; or 2 R5’s optionally form a C1-3 alkylenedioxy; X = a bond, O, S, SO, SO2, CO, (un)substituted CH:CH, etc.; Y = (un)substituted alkylene, cycloalk(en)ylene, heterocyclyl; Z = a bond, O, S, (un)substituted alkylene, CC, etc.;] and their pharmaceutically acceptable salts and prodrugs, to processes for preparing them, and to pharmaceutical compositions containing them for use as α5β1 integrin antagonists in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumors. The invention is also related to α5β1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins. Thus, etherification of tert-Bu 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate with Me N-(2,6-dichlorobenzoyl)-L-tyrosinate (preparation given), cleavage of the tert-butoxycarbonyl group and saponification of the Me ester gave tyrosine derivative II. The effects of compounds I as α5β1 integrin inhibitors were tested (e.g., the invention compound II had IC50 values of 0.0004 μM in a binding assay and 0.002 μM in an adhesion assay). The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).COA of Formula: C15H22N2O3

The Article related to tyrosine preparation alpha5beta1 integrin antagonist solid tumor, antitumor benzoyl pyridinylaminoethyl tyrosine derivative preparation alpha5beta1 integrin antagonist, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.COA of Formula: C15H22N2O3

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem