Category: 869640-41-5

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 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 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 April 1, 2021, Benz, Joerg; Gobbi, Luca; Grether, Uwe; Hanlon, Steven Paul; Hornsperger, Benoit; Kroll, Carsten; Kuhn, Bernd; Kuratli, Martin; Liu, Guofu; O’Hara, Fionn; Richter, Hans; Ritter, Martin published a patent.Quality Control of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one The title of the patent was Heterocyclic compounds as MAGL inhibitors and their preparation. And the patent contained the following:

The invention provides heterocyclic compounds of formula I, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds Compounds of formula I wherein U is CH2; V is O, NH, CH2, S, SO, SO2, CHOH, CHF and CF2; W is CR’ and CH; X is CH and COH; WX and UV can be taken together to form C:C; both E and G are absent and CH2; Z is CH and N; Q is CR” and N; L is a bond, CHR5, O, OCH2, CH2O, CH2OCH2, etc.; A is C6-14 aryl, 5- to 14-membered heteroaryl and 3- to 14-membered heterocyclyl; R1 and R2 are independently H, halo and C1-6 alkyl; R1R2 can be taken together to form C3-10 cycloalkyl; R3 and R4 are independently H, halo, SF5, CN, etc.; R5 is H and C6-14 aryl; R’ is halo and C1-6 alkyl; R” is H, halo, OH, C1-6 haloalkyl and C1-6 alkyl; with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of bis(trichloromethyl) carbonate with (4aR,8S,8aS)-8-methylhexahydro-2H-pyrido[4,3-b][1,4]oxazin-3(4H)-one with 3-((2-fluoro-4-(trifluoromethyl)benzyl)oxy)azetidine 4-methylbenzenesulfonate. The invention compounds were evaluated for their MAGL inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 4.4 nM. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Quality Control of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one

The Article related to heterocycle preparation magl inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.Quality Control of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one

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

On February 7, 2019, Huang, Peter Qinhua; Boren, Brant Clayton; Bunker, Kevin Duane; Liu, Hui; Paliwal, Sunil published a patent.Application of 869640-41-5 The title of the patent was Preparation of pyrazolopyrimidinones and salts thereof as WEE1 kinase inhibitors useful in treatment of cancer and other proliferative diseases. And the patent contained the following:

The invention relates to prepn of pyrazolopyrimidinones and salts thereof as WEE1 kinase inhibitors. The example compound I was prepared accordingby a procedure (procedure given). The compounds of the invention were evaluated for their biol. activity (data given). The compounds of the invention, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Application of 869640-41-5

The Article related to pyrazolopyrimidinone preparation wee1 kinase inhibitor antitumor antiproliferative, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 869640-41-5

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

On June 30, 2016, Inukai, Takayuki; Takeuchi, Jun; Yasuhiro, Tomoko published a patent.Electric Literature of 869640-41-5 The title of the patent was Preparation of quinoline derivatives for the treatment of Axl-related diseases. And the patent contained the following:

The present invention provides quinoline derivatives I [R1 = (un)substituted alkyl, carbocycle or heterocycle; R2 = (un)substituted alkyl, alkenyl, alkynyl, carbocycle, etc.; R3 = alkyl, halogen, haloalkyl or OR31; R4 = alkoxy, haloalkyl, alkyl, alkenyloxy, etc.; R31 = H, alkyl or haloalkyl; A = CH or N; L = O, NH, C(O), S, etc.; ring 1 = 5- to 7-membered cyclic group; m = 0-3; n = 0-3; q = 0-4] or their salts. For example, 2,5-dioxo-1-phenyl-1,2,5,6,7,8-hexahydro-3-quinolinecarboxylic acid was subjected to reaction with hydroxylamine hydrochloride followed by coupling with 5-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-pyridinamine to provide N-[(5E)-5-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-pyridinyl]-5-(hydroxyimino)-2-oxo-1-phenyl-1,2,5,6,7,8-hexahydro-3-quinolinecarboxamide, which underwent Beckmann rearrangement to provide compound II. Compound II exhibited inhibitory activity against Axl with an IC50 value of 0.0015 μM. The invention compounds have strong Axl inhibitory activities and can be useful as therapeutic agents for Axl-related diseases, for example, cancers such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer and glioma, kidney diseases, immune system diseases and cardiovascular diseases. The experimental process involved the reaction of 7-Benzyl-5,6,7,8-tetrahydro-1,7-naphthyridin-2(1H)-one(cas: 869640-41-5).Electric Literature of 869640-41-5

The Article related to quinoline derivative preparation axl inhibitor cancer treatment, kidney disease immune system disease cardiovascular disease treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Electric Literature of 869640-41-5

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