Category: 85386-20-5

On October 6, 2016, Jones, Alison; Kemp, Mark; Stockley, Martin; Gibson, Karl; Whitlock, Gavin published a patent.Category: pyrimidines The title of the patent was 1-Cyanopyrrolidine compounds as USP30 inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I and method for the manufacture of inhibitors of deubiquitylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of formula I wherein Z is absent and CR6R7; Y is a bond, C0-3 alkylene-NR11-C0-3 alkylene and (un)substituted C1-3 alkylene; R1, R6, R7 and R8 are independently H, F, CN, OH, (un)substituted C1-3 alkyl and (un)substituted C1-3 alkoxy; R2 is H, (un)substituted C1-6 alkyl, (un)substituted C1-6 alkoxy, (un)substituted 4- to 10-membered heteroaryl, etc.; R3, R4 and R5 are independently (un)substituted alkyl and (un)substituted C1-3 alkoxy; R9 is H, CN, OH, (un)substituted C1-6 alkyl, etc.; R10 is H, (un)substituted C1-6 alkyl; R11 is H, (un)substituted C1-6 alkyl, 4- to 10-membered heteroaryl, heterocyclyl, aryl, etc.; R9R10 can be taken together to form (un)substituted heterocyclic ring; R10R11 can be taken together to form (un)substituted (mono/bi)cyclic ring; R12 is (un)substituted (mono/bi/tri)cyclic 3- to 14-membered heteroaryl, heterocyclyl, cycloalkyl and aryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 5-phenylpyridine-2-carboxylic acid with (R)-3-amino-1-(tert-butoxycarbonyl)pyrrolidine; the resulting tert-Bu (R)-3-(5-phenylpicolinamido)pyrrolidine-1-carboxylate underwent hydrolysis to give (R)-5-phenyl-N-(pyrrolidin-3-yl)picolinamide TFA, which underwent cyanation to give compound II. The invention compounds were evaluated for their USP30 inhibitory activity (data given). The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Category: pyrimidines

The Article related to cyanopyrrolidine preparation usp30 inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 6, 2016, Jones, Alison; Kemp, Mark; Stockley, Martin; Gibson, Karl; Whitlock, Gavin published a patent.Category: pyrimidines The title of the patent was 1-Cyanopyrrolidine compounds as USP30 inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I and method for the manufacture of inhibitors of deubiquitylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of formula I wherein Z is absent and CR6R7; Y is a bond, C0-3 alkylene-NR11-C0-3 alkylene and (un)substituted C1-3 alkylene; R1, R6, R7 and R8 are independently H, F, CN, OH, (un)substituted C1-3 alkyl and (un)substituted C1-3 alkoxy; R2 is H, (un)substituted C1-6 alkyl, (un)substituted C1-6 alkoxy, (un)substituted 4- to 10-membered heteroaryl, etc.; R3, R4 and R5 are independently (un)substituted alkyl and (un)substituted C1-3 alkoxy; R9 is H, CN, OH, (un)substituted C1-6 alkyl, etc.; R10 is H, (un)substituted C1-6 alkyl; R11 is H, (un)substituted C1-6 alkyl, 4- to 10-membered heteroaryl, heterocyclyl, aryl, etc.; R9R10 can be taken together to form (un)substituted heterocyclic ring; R10R11 can be taken together to form (un)substituted (mono/bi)cyclic ring; R12 is (un)substituted (mono/bi/tri)cyclic 3- to 14-membered heteroaryl, heterocyclyl, cycloalkyl and aryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 5-phenylpyridine-2-carboxylic acid with (R)-3-amino-1-(tert-butoxycarbonyl)pyrrolidine; the resulting tert-Bu (R)-3-(5-phenylpicolinamido)pyrrolidine-1-carboxylate underwent hydrolysis to give (R)-5-phenyl-N-(pyrrolidin-3-yl)picolinamide TFA, which underwent cyanation to give compound II. The invention compounds were evaluated for their USP30 inhibitory activity (data given). The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Category: pyrimidines

The Article related to cyanopyrrolidine preparation usp30 inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 28, 2011, Eidam, Hilary Schneck; Fox, Ryan Michael published a patent.Safety of 5-Phenylpyrimidine-2-carboxylic acid The title of the patent was TRPV4 antagonists as pharmaceutical agents. And the patent contained the following:

The invention discloses indole or benzothiophene analogs I [R1= C1-3 alkyl, C1-3 alkoxy, CF3, halo, etc.; R2= C1-4 alkyl, CH2C3-6 cycloalkyl, CH2Ph; R3= (un)substituted pyrrole, (un)substituted pyridazine, (un)substituted imidazole, (un)substituted indole, etc.; X= bond, CH2; Y= NR4, S; R4= H, C1-3 alkyl; R5= H, C1-5 alkyl; G= (un)substituted heterocycle, (un)substituted cyclopentyl, (un)substituted cyclohexyl, etc.; i= 0,1,2,3], pharmaceutical compositions containing them and their use as TRPV4 antagonists. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Safety of 5-Phenylpyrimidine-2-carboxylic acid

The Article related to trpv4 antagonist indole benzothiophene derivative pharmaceutical agent, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Safety of 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 25, 2009, Goldfarb, David Scott published a patent.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid The title of the patent was Method using lifespan-altering compounds for altering the lifespan of eukaryotic organisms, and screening for such compounds. And the patent contained the following:

The invention discloses a method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan-altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

The Article related to lifespan alteration compound screening dead assay, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 30, 1993, Oleynik, I. V.; Zagulyaeva, O. A. published an article.Formula: C11H8N2O2 The title of the article was Chemical properties of ylidene derivatives of azines. 7. Transformations of 5-methyl(phenyl)-substituted 1,2-dihydro-2-pyrimidinylidenemalononitriles by action of nitric acid. And the article contained the following:

Reaction of title compounds I (R = Me, Ph) with HNO3, depending on the conditions, gave either the corresponding 2-pyrimidinecarboxylic acids or acetonitrile derivatives, e.g., II. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Formula: C11H8N2O2

The Article related to malononitrile pyrimidinylidene reaction nitric acid, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C11H8N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 31, 1986, Mikhaleva, M. A.; Kolesnichenko, G. A.; Rubina, K. I.; Gol’dberg, Yu. Sh.; Savel’ev, V. A.; Leitis, L. Ya.; Shimanskaya, M. V.; Mamaev, V. P. published an article.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid The title of the article was Synthesis of 5-arylpyrimidine-2-carboxylic acids and liquid crystalline properties of their aryl esters. And the article contained the following:

5-Arylpyrimidine-2-carboxylic acids I (R = H, MeO, BuO, R1 = H) were prepared by hydrolysis of 5-aryl-2-cyanopyrimidines and by phase-transfer catalyzed oxidation of 5-aryl-2-styrylpyrimidines. Aryl esters of these acids I (R1 = Ph, substituted Ph) were obtained and their liquid crystalline properties were studied. p-Substituted 5-phenyl-2-pyrimidinecarboxylates do not exhibit mesomorphism, but introduction of a butoxy group in the para position of the pyrimidine attached Ph ring leads to the appearance of nematic properties. In addition, aryl 5-phenylpyrimidincarbonyloxybenzoates are nematic liquid crystals with a thermally stable mesophase at 50-80° during their lifetimes. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

The Article related to aryl arylpyrimidinecarboxylate liquid crystal, pyrimidinecarboxylic acid liquid crystal, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 28, 1983, Baram, S. G.; Shkurko, O. P.; Mamaev, V. P. published an article.Recommanded Product: 85386-20-5 The title of the article was Determination of substituent constants of p-substituted 2- and 5-pyrimidine groups using carbon-13 NMR. And the article contained the following:

The 13C NMR chem. shifts of I and II (R = H, Cl, MeO, NH2, Me2N, CO2Et, cyano) were used to calculate the inductive and resonance substituent constants of these 5-substituted 2-pyrimidyl and 2-substituted 5-pyrimidyl groups. Equations were obtained for the calculation of substituent constants for any 5(or 2)-substituted 2(or 5)-pyrimidyl groups. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Recommanded Product: 85386-20-5

The Article related to nmr carbon phenylpyrimidine lfer, pyrimidine phenyl nmr carbon, substituent constant monosubstituted pyrimidyl group, Physical Organic Chemistry: Resonance Spectra (Electron Spin, Nuclear Magnetic and Fourier Transform Nuclear Magnetic, Quadrupole, etc.) and other aspects.Recommanded Product: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 28, 2010, Bury, Michael Jonathan; Cheung, Mui; Eidam, Hilary Schenck; Fox, Ryan Michael; Goodman, Krista; Manas, Eric Steven published a patent.SDS of cas: 85386-20-5 The title of the patent was Preparation of diazabicycloheptyl amino acid derivatives as transient receptor potential channel TRPV4 antagonists. And the patent contained the following:

Title compounds I [R1′ = (R1)i; i = 0-3; R1 = alkyl, alkoxy, CF3, halo, OCF3, CN, etc.; R2 = alkyl, cycloalkylmethyl, benzyl; R3 = (un)substituted pyrrolyl, pyrazolyl, tetrazolyl, isoquinolinyl,pyrimidinyl, etc.; ; G = (S,S)- or (R,R)-2,5-diazabicycloheptyl; X = a bond, CH2; Y = NH, N-alkyl, S; R5 = H, alkyl; and their pharmaceutically acceptable salts], were prepared Thus, a 5-step synthesis using 1,1-dimethylethyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, 3-methyl-N-[[(phenylmethyl)oxy]carbonyl]-L-valine, and 1H-indole-2-carboxylic acid gave II. Tested title compounds inhibited TRPV4 with IC50 in the range of 1 nM to 10 μM. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).SDS of cas: 85386-20-5

The Article related to diazabicycloheptylaminoacid preparation transient receptor potential channel trpv4 antagonist, overactive bladder pain cardiovascular disease arthritis treatment diazabicycloheptane preparation and other aspects.SDS of cas: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 28, 2010, Bury, Michael Jonathan; Cheung, Mui; Eidam, Hilary Schenck; Fox, Ryan Michael; Goodman, Krista; Manas, Eric Steven published a patent.SDS of cas: 85386-20-5 The title of the patent was Preparation of diazabicycloheptyl amino acid derivatives as transient receptor potential channel TRPV4 antagonists. And the patent contained the following:

Title compounds I [R1′ = (R1)i; i = 0-3; R1 = alkyl, alkoxy, CF3, halo, OCF3, CN, etc.; R2 = alkyl, cycloalkylmethyl, benzyl; R3 = (un)substituted pyrrolyl, pyrazolyl, tetrazolyl, isoquinolinyl,pyrimidinyl, etc.; ; G = (S,S)- or (R,R)-2,5-diazabicycloheptyl; X = a bond, CH2; Y = NH, N-alkyl, S; R5 = H, alkyl; and their pharmaceutically acceptable salts], were prepared Thus, a 5-step synthesis using 1,1-dimethylethyl (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, 3-methyl-N-[[(phenylmethyl)oxy]carbonyl]-L-valine, and 1H-indole-2-carboxylic acid gave II. Tested title compounds inhibited TRPV4 with IC50 in the range of 1 nM to 10 μM. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).SDS of cas: 85386-20-5

The Article related to diazabicycloheptylaminoacid preparation transient receptor potential channel trpv4 antagonist, overactive bladder pain cardiovascular disease arthritis treatment diazabicycloheptane preparation and other aspects.SDS of cas: 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 24, 2005, Kishino, Hiroyuki; Moriya, Minoru; Sakamoto, Toshihiro; Takahashi, Hidekazu; Sakuraba, Shunji; Suzuki, Takao; Kanatani, Akio published a patent.Computed Properties of 85386-20-5 The title of the patent was Preparation of imidazopyridine derivatives as melanin-concentrating hormone receptor antagonists. And the patent contained the following:

Title compounds I [R1, R2 = H, halo, etc., further detail on R1, R2 is given; R3 = H, halo, etc.; R4 = H, alkyl; W = single bond, etc.; Ar = optionally substituted aromatic ring, etc. with R7; R7 = halo, etc.] were prepared For example, Pd-catalyzed hydrogenation of 2-isopropyl-6-nitroimidazo[1,2-a]pyridine hydrobromide followed by HATU-mediated acylation with 4′-fluoro-1,1′-biphenyl-4-carboxylic acid afforded compound II. In MCH (Melanin Concentrating Hormone) binding inhibition assays, the IC50 value of compound II was 3.1 nM. Compounds I are claimed useful for the treatment of obesity, diabetes, etc. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Computed Properties of 85386-20-5

The Article related to imidazopyridine preparation melanin concentrating hormone mch receptor antagonist, antiobesity agent imidazopyridine preparation mch receptor antagonist, antidiabetic agent imidazopyridine preparation mch receptor antagonist and other aspects.Computed Properties of 85386-20-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia