Month: October 2022

On May 16, 2005, Leonard, Kristi; Pan, Wenxi; Anaclerio, Beth; Gushue, Joan M.; Guo, Zihong; DesJarlais, Renee L.; Chaikin, Marge A.; Lattanze, Jennifer; Crysler, Carl; Manthey, Carl L.; Tomczuk, Bruce E.; Marugan, Juan Jose published an article.SDS of cas: 445490-78-8 The title of the article was Non-peptidic αvβ3 antagonists containing indol-1-ylpropionic acids. And the article contained the following:

The synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ3 are described. Indol-1-ylpropionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified. 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 indolylpropionic acid preparation vitronectin receptor antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.SDS of cas: 445490-78-8

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

On October 12, 2006, Roboisson, Pierre; Marugan Sanchez, Juan Jose published a patent.COA of Formula: C15H22N2O3 The title of the patent was Preparation of 4-substituted indoles for use as integrin antagonists. And the patent contained the following:

4-Substituted indoles I, wherein R is Ph or 3-pyridyl; X-Y is -CH2-O-, -CH2-NH-, or -CH2-CH2-; W can be II or III wherein R1 is hydrogen, alkyl, haloalkyl or halogen; R2 and R3 are independently hydrogen, halogen or alkyl; R4 and R5 are independently hydrogen, halogen, alkyl, alkoxy or aryl; R6 is hydrogen are prepared . Thus, IV was prepared and tested integrin antagonists, however, no biol. data was provided. Further, I may be used in the treatment of pathol. conditions mediated by avss3 and avss5 integrins, including but not limited to tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. 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 integrin antagonist human indole, indole preparation integrin antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C15H22N2O3

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

On August 8, 2002, Lu, Tianbao; Lafrance, Louis Vincent; Markotan, Thomas P.; Marugan, Juan Jose; Marder, Victor J.; U’Prichard, David C.; Anaclerio, Beth M.; Guo, Zihong; Pan, Wenxi; Leonard, Kristi A. published a patent.Computed Properties of 445490-78-8 The title of the patent was Preparation of indoles and their use as αvβ3 and αvβ5 integrin antagonists. And the patent contained the following:

Title compounds I [R1-R5 = H, halo, alkyl, etc.; R6-R9 = H, alkyl, hydroxyalkyl, etc.; R10-R13 = H, OH, alkyl, etc.; R14 = H, or a functionality that acts as a prodrug; X = O, S, CH2, etc.; a, k, v = 0, 1; i, j, m, n = 0-4], their pharmaceutically acceptable salts, prodrugs and formulations were prepared For example, hydrogenation of acrylic ester II, prepared from 7-[2-[1-(2-Methoxycarbonyl-1-(pyridin-3-yl)vinyl)-1H-indol-5-yloxy]ethyl]-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylic acid tert-Bu ester and pyridin-3-ylpropynoic acid Me ester, followed by BOC deprotection, and ester hydrolysis provided claimed indole III. Indole III inhibited human αvβ3-vitronectin interaction at an IC50 of 0.24 nM, studies for an addnl. 6 examples are provided, ranging in values from 670 to 0.24 nM. Compounds I may be used in treatment of pathol. conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, inflammation, rheumatoid arthritis, etc.. 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 preparation indole integrin antagonist antitumor antiinflammatory antirheumatic, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 445490-78-8

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

On November 7, 2002, Sanchez, Juan Jose Marugan; Marder, Victor J.; U’prichard, David C. published a patent.Quality Control of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate The title of the patent was Substituted benzofurans and benzothiophenes of use as integrin antagonists. And the patent contained the following:

Title compounds I [Y = O, S; X = O, S, CH2, NH; W = N heterocyclic, amino; Z = CR5R6(CH2)i(CR7R8)k(CH2)jCO2R9; R1-R4 = H, alkyl, haloalkyl, aryl, aralkyl; R5-R8 = H, OH, (un)substituted alkyl, alkoxy, cycloalkyl, aryl, heterocyclic; R5R7 = alkylene; R9 = H, alkyl, haloalkyl, aryl, aralkyl, aminoalkyl, alkoxyalkoxyalkyl, alkoxycarbonyloxyethyl; R10-R13 = H, (un)substituted alkyl, aryl; R10R11 = alkylene; i, j, m, n = 0-4; k = 0, 1] were prepared The compounds may be used in the treatment of pathol. conditions mediated by αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. Thus, the benzothiophene II was prepared from tert.-Bu 7-ethoxycarbonylmethyl-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylate and Et 3-(6-hydroxybenzo[b]thiophen-3-yl)propionate and had IC50 for inhibition of αvβ5-vitronectin in vitro of 8 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).Quality Control of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate

The Article related to benzothiophenepropionate preparation vitronectin inhibitor, benzofuranpropionate preparation vitronectin inhibitor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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 November 16, 2005, Strang, Ross Sinclair; Lunn, Graham; Mathias, John Paul published a patent.Formula: C15H16N2O The title of the patent was Preparation of tetrahydronaphthyridines as histamine H3 receptor ligands. And the patent contained the following:

The title compounds I or II [R1 = (un)substituted Het1; A = (CH2)mNR7R8 (wherein m = 2-6; R7, R8 = H, alkyl, cycloalkyl, hydroxyalkyl or (un)substituted NR7R8 = 4-7 membered saturated heterocyclyl optionally containing more heteroatoms), III (p = 0-2; Q = (un)substituted 4-6 membered saturated heterocyclyl); Het1 = monocyclic or bicyclic heteroaryl having 5-10 ring members which contain 1-4 heteroatoms selected from N, O ans S] which are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions, were prepared Thus, reacting 2-(3-pyrrolidin-1-ylpropoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine (preparation given) with 2-bromopyrimidine afforded 24% IV. The exemplified compounds I and II have been tested in the H3 assays and were found to have a Ki value of less than 1000 nM in the H3 cell based functional assay. The most preferred examples have a Ki value of less than 30 nM in the H3 cell based functional assay and a Ki value of greater than 4500 nM in the dofetilide binding assay. The pharmaceutical compositions comprising the compounds I or II alone or in combination with other pharmacol. active agent are disclosed. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Formula: C15H16N2O

The Article related to naphthyridine preparation histamine h3 receptor ligand, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Formula: C15H16N2O

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

On August 31, 1981, Ferrarini, Pier Luigi; Biagi, Giuliana; Livi, Oreste; Primofiore, Giampaolo; Carpene, Marino published an article.Quality Control of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one The title of the article was Synthesis of some 3-substituted [1,8]Naphthyrido[3,2-c][1,8]naphthyridines. A new heterocyclic ring system. And the article contained the following:

The title compounds (I; R = Me, Br, Cl, EtO, HS) were prepared by condensation of naphthyridinones (II) with 2-aminonicotinaldehyde. I were transformed into the fully aromatic compounds by refluxing with nitrobenzene. The experimental process involved the reaction of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one(cas: 76629-10-2).Quality Control of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one

The Article related to naphthyridonaphthyridine, condensation naphthyridinone aminonicotinaldehyde, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Quality Control of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one

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

On October 16, 2018, Jin, Haowen; Xu, Weiliang; Xu, Weizheng published a patent.Application of 958334-24-2 The title of the patent was Preparation method of 7-bromo-1,5-naphthyridine-3-carboxylic acid. And the patent contained the following:

The method comprises the steps of: providing 1,5-naphthyridine as a raw material, reacting to obtain 7-bromo-1,5-naphthyridin-3-carboxylate, and hydrolyzing in the presence of alkali to obtain 7-bromo-1,5-naphthyridin-3-carboxylate. The method has the advantages of simple process, low cost, accessible raw material, easy post-treatment, and high yield. The method is suitable for mass production The experimental process involved the reaction of Methyl 7-bromo-1,5-naphthyridine-3-carboxylate(cas: 958334-24-2).Application of 958334-24-2

The Article related to bromonaphthyridine carboxylic acid preparation naphthyridine bromination carbonylation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application of 958334-24-2

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

Da Settimo, Antonio; Biagi, Giuliana; Primofiore, Giampaolo; Ferrarini, Pier Luigi; Livi, Oreste; Marini, Anna Maria published an article in 1980, the title of the article was Synthesis of some 3,7-disubstituted quino[3,2-c][1,8]naphthyridines.Application In Synthesis of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one And the article contains the following content:

Quinonaphthyridines I (R = Me, Br, Cl, EtO, NH2; R1 = Me, Et; R2 = R3 = H) were prepared in 13-95% yields by cyclizing II with o-H2NC6H4COR1. Heating I (R2 = R3 = H) in PhNO2 gave I (R2R3 = bond). The experimental process involved the reaction of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one(cas: 76629-10-2).Application In Synthesis of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one

The Article related to quinonaphthyridine, naphthyridinone phenone cyclization, acetophenone naphthyridinone cyclization, benzophenone naphthyridinone cyclization, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of 7-Chloro-2,3-dihydro-1,8-naphthyridin-4(1H)-one

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

On May 14, 2015, Inukai, Takayuki; Takeuchi, Jun; Yasuhiro, Tomoko; Wolf, Mark Allan; Pawal, Vijay Dattaram; Chakrabarti, Anjan; Chittimalla, Santhosh Kumar published a patent.HPLC of Formula: 869640-41-5 The title of the patent was Pyrrolopyrimidine derivative and its use for pharmaceutical composition for prevention and/or treatment of Axl-related disease. And the patent contained the following:

The compound represented by general formula I [R1 = (un)substituted C1-8 alkyl, (un)substituted C3-7 carbocycle, 4- to 7-membered heterocycle; R2 = (un)substituted C1-8 alkyl, (un)substituted C2-8 alkenyl, (un)substituted C2-8 alkynyl, OH, (un)substituted C3-7 carbocycle, (un)substituted 4- to 7-membered heterocycle, halo, etc.; R3 = C1-4 (halo)alkyl, halo, OH, C1-4 (halo)alkoxy; R4 = H, (un)substituted C1-8 alkyl, (un)substituted C3-10 carbocycle, (un)substituted 4- to 10-membered heterocycle; R5 = H, C1-4 (halo)alkyl, halo; ring1 = 5- to 7-membered cyclic group; m, n = 0-3] has strong Axl inhibition activity by means of a pyridone ring structure being introduced into a pyrrolopyrimidine skeleton, and so the result can serve as a treatment agent for Axl-related diseases, for example cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors, renal disease, immune system disorders, and cardiovascular disease. Thus, N-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-pyridinyl]-2′,5′-dioxo-1′-phenyl-2′,5′,6′,8′-tetrahydro-1’H-spiro(cyclopropane-1,7′-quinoline)-3′-carboxamide (preparation given) inhibited Axl with IC50 of 0.0097 μmol. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).HPLC of Formula: 869640-41-5

The Article related to pyrrolopyrimidine preparation pharmaceutical axl inhibitor disease therapy anticancer, immune system cardiovascular disease treatment axl inhibitor pyrrolopyrimidine preparation and other aspects.HPLC of Formula: 869640-41-5

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

On April 20, 2011, Kroth, Heiko; Froestl, Wolfgang; Pfeifer, Andrea; Muhs, Andreas published a patent.Product Details of 445490-78-8 The title of the patent was Preparation of 2,6-diaminopyridine compounds for treating diseases associated with amyloid proteins, especially ocular diseases. And the patent contained the following:

The invention is related to the preparation of diaminopyridines I [the pyridine rings A, B, and C are independently (un)substituted by ≥1 substituents selected from alkyl, NH2 and derivatives, CN, NO2, CO2H, etc.; R1, R2 = independently H, (un)substituted 5-10 membered heteroaryl, alkynyl, cycloalkyl, etc.; L1, L2 = independently NR3CR4R5(CR6R7)p, (CR8R9)qCR10R11NR12; R3, R12 = independently H, CH(:NOH) and derivatives, CONH2 and derivatives, (un)substituted 5-10 membered heterocycloalkylalkyl, etc.; R4-11 = independently SO2NH2 and derivatives, aminocarbonylalkyl, halo, OCONH2 and derivatives, etc.; p = 1-2; q = 0-2] and their pharmaceutical acceptable salts that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The invention is also related to the use of I in the treatment of ocular diseases associated with pathol. abnormalities/changes in the tissues of the visual system. Thus, II was prepared by a multi-step synthesis from 2-bromo-6-methylpyridine and inhibited the aggregation of amyloid beta 1-42 peptide in a thioflavin T spectrofluorescence assay (IC50 = 12.9 mM). 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).Product Details of 445490-78-8

The Article related to pyridinediamine preparation amyloid beta protein abnormality ocular disease, glaucoma intraocular pressure amyloidosis naphthyridinylalkyl pyridinylalkyl pyridinediamine preparation and other aspects.Product Details of 445490-78-8

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