Category: 596114-50-0

On April 1, 2021, Liu, Xiangyong; Qiu, Changyong; Sheng, Haitong; Liu, Mengqiang; Shen, Qichao; Du, Guolong; Song, Xiaodong; Ding, Lieming; Wang, Jiabing published a patent.Related Products of 596114-50-0 The title of the patent was Egfr inhibitor, composition and preparation method therefor. And the patent contained the following:

A compound of formula I, a method for using these compounds as an EGFR inhibitor, and a pharmaceutical composition comprising these compounds The compound was used in the treatment, prevention or amelioration of diseases or conditions such as cancer or infection. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to heterocyclic phosphine oxide preparation egfr inhibitor, antitumor activity heterocyclic phosphine oxide, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 18, 2014, Amans, Dominique; Atkinson, Stephen John; Harrison, Lee Andrew; Hirst, David Jonathan; Law, Robert Peter; Lindon, Matthew; Preston, Alexander; Seal, Jonathan Thomas; Wellaway, Christopher Roland published a patent.Application of 596114-50-0 The title of the patent was Preparation of acylaminotetrahydroquinoline derivatives for use as bromodomain inhibitors. And the patent contained the following:

Title compounds I [A = NH, O, S, SO, etc.; V = (un)substituted Ph, heteroaromatic, or pyridone; W and Z independently = CH or N; X or Y independently = C or N; R1 = alkyl; R2 = alkyl, cycloalkyl, heterocyclyl, CH2CF3, or CH2OMe; R3 = alkyl, CH2F, CH2OH, or CH2OC(O)Me; R4 = absent, H, OH, halo, CN, CO2H, etc.; R5 = absent, H, halo, OH, or alkoxy], and their pharmaceutically acceptable salts, are prepared and disclosed as bromodomain inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in BRD4 BD2 TR-FRET assays, e.g., II demonstrated a pIC50 value of ≥7.0. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Application of 596114-50-0

The Article related to quinoline acylaminotetrahydro preparation bromodomain inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 10, 2022, Zhang, Xuejun; Chang, Shaohua; Lei, Sijun; Ding, Xiaohua; Chen, Haomin; Jing, Zhenzhong; Yang, Chengbing; Liu, Lifei; Yang, Jun; Li, Lie published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of nitrogen-substituted heterocyclic thiophenes and their uses in preparation of a medicament for the treatment of LPAR-related diseases. And the patent contained the following:

The present invention relates to the preparation of nitrogen-substituted heterocyclic thiophenes and their uses in preparation of a medicament for the treatment of LPAR-related diseases. In particular, the nitrogen-substituted heterocyclic thiophene compound I (wherein, R1 = -H, -CN, halogen, -Z-Ra, the following groups (un)substituted by Rb: C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkylamino, C1-6 alkoxy; Z = single bond, -O-, -S- or -CO-; Ra is = C1-6 alkyl, C1-6 alkyl substituted by halogen, amino, C1-3 alkylamino; Rb = -CN, halogen, C1-6 alkyl, C1-6 alkoxy groups; R2 = -H, -CN, halogen, -Y-Rd, the following groups (un)substituted by Re: C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkylamino, C1-6 alkoxy; Y = single bond or -O-, -S-; Rd = C1-6 alkyl, C1-6 alkyl group substituted by halogen; Re = -CN, halogen, C1-6 alkyl, C1-6 alkoxy groups). Further, ( X1, X2, X3 = C or N, and X1, X2, X3 = not N at the same time; Rg is selected from H, F, Cl, methyl; L1 = single bond, -N(R3)- or -O-; L2 = single bond, -O-, C1-6 alkylene (un)substituted by C1-3 alkyl, unsubstituted or cyclopropyl substituted by C1-3 alkyl; R3 = -H, C1-3 alkyl; R4 = -H, -CN, halogen, the following groups (un)substituted by Rh: C1-6 alkyl, C3-8 cycloalkyl; and Rh = -H, halogen, C1-6 alkyl, C1-6 alkyl substituted by halogen, C1-6 alkoxy substituted by halogen groups) was prepared The compound of the present invention has good antagonism to LPAR1, and has good antagonism to LPAR3. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to nitrogen substituted heterocyclic thiophene preparation lpar antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 1, 2011, Barba, Oscar; Bell, James Charles; Dupree, Tom Banksia; Fry, Peter Timothy; Bertram, Lisa Sarah; Fyfe, Matthew Colin Thor; Gattrell, William; Jeevaratnam, Revathy Perpetua; Keily, John; Krulle, Thomas Martin; Mcdonald, Russell Walker; Morgan, Trevor; Rasamison, Chrystelle Marie; Schofield, Karen Lesley; Stewart, Alan John William; Swain, Simon Andrew; Withall, David Matthew published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of heteroarylpiperidinylmethoxypyrimidinylpyrrolidinylamine derivatives and analogs for use as GPR119 antagonists. And the patent contained the following:

Title compounds I [A = para-substituted Ph or para-substituted heteroaryl containing 1 to 3 N atoms; each Q independently = (CHR9)p; X = O, CH2, NH, etc.; Y = O, CH2, N-alkyl, etc.; Z = CO2aryl, SO2heteroaryl, C(O)alkyl, etc.; R1 = H, halo, CN, alkyl, etc.; R2 = (un)substituted Ph, pyridyl, N-pyrazolyl, etc.; R9 = H, halo, OH, alkyl, etc.; R11 = H, halo, alkyl, haloalkyl, or alkoxy; n = 0 or 1; each p independently = 0 to 2; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as GPR119 antagonists. Thus, e.g., II·HCl was prepared by a multistep procedure (preparation given). Select I were evaluated in GPR119 yeast reporter assays (data given). The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to pyrimidinylpyrrolidinylamine piperidinylmethoxy derivative preparation gpr119 antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 12, 2012, Nakamura, Tsuyoshi; Namiki, Hidenori; Terasaka, Naoki; Shima, Akiko; Hagihara, Masahiko; Iwase, Noriaki; Takata, Katsunori; Kikuchi, Osamu; Tsuboike, Kazunari; Setoguchi, Hiroyuki; Yoneda, Kenji; Sunamoto, Hidetoshi; Ito, Koji published a patent.Formula: C7H9ClN2 The title of the patent was Preparation of tetrahydroquinoline compounds as CETP inhibitors. And the patent contained the following:

Title compounds I [R1 = H, alkyl, hydroxyalkyl, etc.; or pharmacol. acceptable salts thereof], useful for the treatment of dyslipidemia, hypercholesterolemia, arteriosclerosis, etc., were prepared For example, conversion of 4,4-difluorocyclohexanecarboxylic acid Et ester into II [PMB = p-methoxybenzyl] in a multi-step process followed by treatment with 4-CF3PhMgBr, diastereomeric separation, fluorination, de-alkoxycarbonylation, chiral separation, reaction with 2-bromopyrimidine, and debenzylation afforded compound III [R = pyrimidin-2-yl]. In CETP (cholesteryl ester transfer protein) inhibition assays, IC50 of III [R = 5-(4-methylpiperazin-1-yl)pyrimdin-2-yl] was 19 nM. Pharmaceutical formulations containing I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Formula: C7H9ClN2

The Article related to tetrahydroquinoline preparation cetp inhibitor, dyslipidemia hypercholesterolemia arteriosclerosis treatment tetrahydroquinoline cetp inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C7H9ClN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 20, 2012, Kawamura, Madoka; Kobashi, Yohei; Matsuda, Daisuke; Shiozawa, Fumiyasu; Suga, Yoichiro; Fusegi, Keiko; Kakinuma, Hiroyuki; Otake, Norikazu published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

Title compounds I [p = 0-2; q = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O- or -NR3-; R3 = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl or aryl), alkylsulfonyl, alkylcarbonyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction using LiAlH4, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound II. In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 4, 2014, Kawamura, Madoka; Shiozawa, Fumiyasu; Matsuda, Daisuke; Kakinuma, Hiroyuki; Otake, Kenichi published a patent.Related Products of 596114-50-0 The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

Title compounds I [spiro moiety represented by Q1 in I is optionally substituted with alkyl or fluoro, may combine with cycloalkane to form a spiro ring, and may form a bridged ring with alkanediyl or alkenediyl; p = 0-3; q = 1-3; n1 = 0-2; n2 = 0-2 such as n1 + n2 = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O-, -S- or -NRx-; Rx = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl), haloalkyl, cycloalkyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound II. In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 30, 2014, Kawamura, Madoka; Shiozawa, Fumiyasu; Kakinuma, Hiroyuki; Otake, Kenichi; Matsuda, Daisuke; Kobashi, Yohei; Suga, Yoichiro; Fusegi, Keiko published a patent.Quality Control of 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:

The title compounds [I; p = 0-2; q = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O- or -NR3-; R3 = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl or aryl), alkylsulfonyl, alkylcarbonyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction using LiAlH4, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound (II). In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Quality Control of 2-Chloro-5-isopropylpyrimidine

The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Quality Control of 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 4, 2010, Carpenter, Andrew J.; Fang, Jing; Peckham, Gregory published a patent.Reference of 2-Chloro-5-isopropylpyrimidine The title of the patent was Pyridazinyl derivatives as GPR119 agonists and their preparation and use in the treatment of metabolic disorders. And the patent contained the following:

The invention relates to compounds of formula I that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds Compounds of formula I wherein R1 is C1-3 alkyl and halo; A is (un)substituted phenylene, (un)substituted pyridinyl and (un)substituted pyrazinyl; R3 is H, C1-5 alkyl and C3-7 cycloalkyl; R4 is COCOR5, CO2R5, COR5, SO2C1-5 alkyl, SO2NH2 and derivatives, etc.; R5 is C1-5 alkyl and C3-7 cycloalkyl, Ph, phenyl-C1-4 alkylene, 3- to 7-membered heterocyclic ring and (un)substituted C1-5 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their GPR119 agonistic activity. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Reference of 2-Chloro-5-isopropylpyrimidine

The Article related to pyridazinyl derivative preparation gpr119 agonist treatment metabolic disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Reference of 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 26, 2011, Carpenter, Andrew J.; Fang, Jing; Peckham, Gregory published a patent.Related Products of 596114-50-0 The title of the patent was Chemical compounds and uses. And the patent contained the following:

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to pyridazinyl derivative preparation gpr119 agonist treatment metabolic disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia