Category: 64987-16-2

On July 21, 2011, Kallander, Lara S.; Lawhorn, Brian Griffin; Philip, Joanne; Zhao, Yongdong published a patent.Formula: C6H8N2O2S The title of the patent was 3-[(6-Aminopyrimidin-4-yl)amino]benzenesulfonamide compounds useful as TNNI3K inhibitors, their preparation, and methods of use in the treatment of congestive heart failure. And the patent contained the following:

Title compounds I are disclosed [wherein R1 = C1-4 alkyl; R2 = H, halo; R3 = H, halo, (un)substituted alkyl or alkoxy, aryl, OH, cycloalkyl, alkylthio, amino, (di)(alkyl)amino; R4 = H, halo, (un)substituted alkyl or alkoxy, OH, (halo)alkylthio, alkylsulfonyl, (un)substituted amino; R5 = H; or R4 and R5 form a 5 or 6 membered ring, optionally substituted or containing one or two addnl. N/O/S atoms; R6 = alky(en/yn)yl, cycloalkyl, (un)substituted (hetero)aryl; and salts]. I are inhibitors of cardiac troponin I-interacting kinase (TNNI3K), also known as CARK (for cardiac ankyrin repeat kinase), a protein kinase that exhibits highly selective expression for cardiac tissues and which has been shown to interact with components of the sarcomere, including troponin I. Approx. 380 compounds I are claimed as the free base, and were prepared as salts and/or free bases. Numerous intermediates were also prepared For instance, the intermediate 3-[(6-chloro-4-pyrimidinyl)amino]-N-methylbenznesulfonamide and 3-biphenylamine were microwaved together in isopropanol in the presence of concentrated HCl at 150° for 20 min to give invention compound II, isolated as the trifluoroacetate. In bioassays using human TNNI3K, I exhibited pXC50 ≥ approx. 6.0. For instance, two compounds I inhibited hTNNI3K with a mean pXC50 of approx. 7.0. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Formula: C6H8N2O2S

The Article related to pyrimidinylamino benzenesulfonamide preparation tnni3k inhibitor treatment congestive heart failure, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C6H8N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 13, 2008, Yamashita, Haruhisa; Odai, Osamu; Harada, Hiroshi; Iwata, Mitsutaka published a patent.Formula: C6H8N2O2S The title of the patent was Preparation of fused heterocyclic derivatives as glucokinase (GK) activators. And the patent contained the following:

Title compounds I [A = -N(R3)(CH2)m-, -N(R3)CO(CH2)m- or -N(R3)SO2(CH2)m-; m = 0-2; X1, X2 = -CO-, -CS- or -C(R4)(R5)-; X3 = -C(R4)(R5)-; R1 = H, (un)substituted alkyl, (un)substituted cycloalkyl, etc.; R2 = H, (un)substituted alkyl, (un)substituted alkenyl, etc.; R3 = H, (un)substituted alkyl or (un)substituted cycloalkyl; R4, R5 = H, halo or (un)substituted alkyl; n = 1 or 2] or their pharmaceutically acceptable salts were prepared For example, Pd2(dba)3 catalyzed reaction of compound II [R = Cl], e.g., prepared from Et 4-oxopiperidine-3-carboxylate hydrochloride in 3 steps, with 2-aminothiazole afforded compound II [R = thiazol-2-ylamino], which showed 328% GK activation. Compounds I are claimed useful for the treatment of diabetes. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Formula: C6H8N2O2S

The Article related to fused heterocycle preparation glucokinase gk activator, diabetes treatment fused heterocycle preparation gk activation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C6H8N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On October 18, 2012, Holcomb, Ryan C.; Sebahar, Paul R.; Suzuki, Kazuyuki; McLeod, Donald A.; Dastrup, David M.; Hoarau, Christophe; Halter, Robert J.; Bursavich, Matthew Gregory; Shenderovich, Mark D.; Richards, Burt; Bartel, Paul L. published a patent.Product Details of 64987-16-2 The title of the patent was Preparation of substituted pyrimidinylbenzonitriles as IKK-related kinase ε and TANK-binding kinase 1 inhibitors. And the patent contained the following:

The invention relates to compounds I [R1 = (un)substituted heteroaryl, heterocyclyl, heteroarylalkylene, etc.; R2 = alkyl, cycloalkyl, aryl, etc.; R3-R7 = alkyl, cycloalkyl, aryl, etc.; with the provisos], pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders. Two-hundred-fifty-three compounds I were prepared E.g., a multi-step synthesis of II, starting from 5-bromo-2-hydroxybenzonitrile and tetrahydro-2H-pyran-4-ol, was described. Exemplified compounds I were tested in in vitro IKKε and TBK1 kinase assays (data given). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Product Details of 64987-16-2

The Article related to pyrimidinylbenzonitrile preparation ikk epsilon tbk1 kinase inhibitor, pyrimidinyl benzonitrile preparation tank binding kinase 1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 7, 2019, Tarby, Christine M.; Norris, Derek J.; Lo, Julian C.; Ahuja, Vijay T.; Seitz, Steven P.; Gavai, Ashvinikumar V.; Tokarski, John S.; Rajasagi, Mohini; Wichroski, Michael; Broekema, Matthias published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of uracil derivatives as Mer-Axl inhibitors. And the patent contained the following:

The invention relates generally to compounds I [Ar1 = aryl or heteroaryl containing 1-4 heteroatoms selected from N, O or S; Ar2 = heteroaryl containing 1-4 heteroatoms selected from N, O or S; Q1 = NHCO, CONH, NHSO2, etc.; Q2 = O or NH; R1 and R2 = (independently) H, (un)substituted alkyl, (CH2)r(cycloalkyl), etc.; R3 and R4 = (independently) H, halo, CF3, etc.; X and Y = (independently) H, halo, alkyl, etc.; r = 0-2] or pharmaceutically acceptable salts, tautomers or stereoisomers thereof, that are Mer-Axl inhibitors, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. Over one-hundred-forty compounds I were prepared E.g., a multi-step synthesis of II, starting from di-Et 2-(aminomethylene)malonate and 1-fluoro-4-isocyanatobenzene, was described. The inhibitory activity of compounds I was tested in the MERTK, AXL, and TYRO3 activity assays (data given for representative compounds I). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to uracil derivative preparation mer axl tyro3 kinase inhibitor antitumor, proliferative disorder dysregulated apoptosis treatment uracil derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On September 15, 1977, Kamiya, Takashi; Tanaka, Kunihiko; Nakai, Yoshiharu; Sakane, Kazuo published a patent.Category: thiazole The title of the patent was 3,7-Disubstituted-3-cephem-4-carboxylic acid derivatives. And the patent contained the following:

Cephalosporin derivatives (∼100 compounds) including I (X = CO, CHOH; X1 = S, NMe, X2 = CH; X1 = S, O, X2 = CHMe; X1 = NMe, X2 = N) were prepared Thus, the aminothiazolylacetate II (R = H, R1 = Et, X = CH2) was formylated, I (R = CHO, R1 = Et, X = CH2) oxidized with SeO2, I (R = CHO, R1 = Et, X = CO) hydrolyzed, and I (R = CHO, R1 = H, X = CO) used to acylate 3-(1-methyl-5-tetrazolylthiomethyl)-7-amino-3-cephem-4-carboxylic acid, followed by cleavage of the formyl group with POCl3 to give I (X = CO, X1 = NMe, X2 = N). This compound had a min. inhibitory concentration against Escherichia coli 0.05 μg/mL. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Category: thiazole

The Article related to cephalosporin, aminothiazolylacetamidocephem, thiazolylacetamidocephem, Heterocyclic Compounds (More Than One Hetero Atom): Thiazines (Including Cephalosporins) and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On April 25, 2013, Ogamino, Takahisa; Yamazaki, Yukiyoshi; Tanikawa, Shin; Okuda, Ayumu; Fukuda, Tomoaki; Tokuda, Okihisa; Miyake, Yoshiharu; Itoh, Shinsuke; Ishiwata, Hiroyuki published a patent.Product Details of 64987-16-2 The title of the patent was Preparation of spiroindoline compounds for activating glucokinase. And the patent contained the following:

Title compounds I [ring A = nitrogen-containing heterocyclyl; R1, R2 = independently H, halo, haloalkyl, etc.; R3 = H, (un)substituted alkyl, -COR7, etc.; R7 = H, (un)substituted alkyl, haloalkyl, etc.; R4 = H, halo, cyano, etc.; or salts or solvates thereof], useful for the treatment of diabetes, glucose intolerance, metabolic syndrome, etc., were prepared For example, reaction of 2-amino-5-chlorothiazole·HCl with 4-nitrophenyl chloroformate, treatment with tert-Bu 5-bromospiro[indoline-3,3′-pyrrolidine]-1′-carboxylate, deprotection using CF3CO2H, and acetylation afforded compound II. The invention compounds activated glucokinase activity in vitro assay, e.g., III showed 1192% activation at 1 μmol/L. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Product Details of 64987-16-2

The Article related to spiroindoline preparation glucokinase activator, diabetes glucose intolerance metabolic syndrome treatment spiroindoline glucokinase activation, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Product Details of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On October 15, 2009, Hahn, Michael; Becker, Eva-Maria; Knorr, Andreas; Schneider, Dirk; Stasch, Johannes-Peter; Schlemmer, Karl-Heinz; Wunder, Frank; Stoll, Friederike; Heitmeier, Stefan; Muenter, Klaus; Griebenow, Nils published a patent.Category: thiazole The title of the patent was Preparation of phthalazinones as soluble guanylate cyclase inhibitors. And the patent contained the following:

Title compounds I [X = L1-M-L2CO2H; L1 = bond, methylene, etc.; M = phenylene, 5 or 6-membered heteroaryl with provisos; L2 = bond, methylene with provisos; A = 5-7 membered heterocycle ring with provisos; R1 = H, alkyl, cycloalkyl; R2 = H, halo, CN, etc.; R3 = alkyl, alkenyl, etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, NaOH/dioxane/H2O mediated saponification of ester II [Y = Me] afforded acid II [Y = H]. In soluble guanylate cyclase inhibition assays, 19 examples of compounds I exhibited MEC values ranging from 1-300 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Category: thiazole

The Article related to phthalazinone preparation soluble guanylate cyclase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On October 22, 2009, Hahn, Michael G.; Becker, Eva-Maria; Knorr, Andreas; Schneider, Dirk; Stasch, Johannes-Peter; Schlemmer, Karl-Heinz; Wunder, Frank; Stoll, Frederike; Heitmeier, Stefan; Muenter, Klaus; Griebenow, Nils; Lampe, Thomas; El Sheikh, Sherif; Li, Volkhart Min-Jian published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of phthalazinones as soluble guanylate cyclase inhibitors. And the patent contained the following:

Title compounds I [X = L1-M-L2CO2H; L1 = bond, methylene, etc.; M = phenylene, 5 or 6-membered heteroaryl with provisos; L2 = bond, methylene with provisos; A = 5-7 membered heterocycle ring with provisos; R1 = H, alkyl, cycloalkyl; R2 = H, halo, CN, etc.; R3 = alkyl, alkenyl, etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, NaOH/dioxane/H2O mediated saponification of ester II [Y = Me] afforded acid II [Y = H]. In soluble guanylate cyclase inhibition assays, 48-examples of compounds I exhibited MEC values ranging from 0.1-300 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to phthalazinone preparation soluble guanylate cyclase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.HPLC of Formula: 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 22, 2014, Lemieux, Rene M.; Popovici-Muller, Janeta; Salituro, Francesco G.; Saunders, Jeffrey O.; Travins, Jeremy; Chen, Yongsheng published a patent.Electric Literature of 64987-16-2 The title of the patent was Preparation of substituted bisthiadiazoles as glutaminase inhibitors. And the patent contained the following:

The invention relates to compounds of formula I as glutaminase inhibitors; their preparation and use in the treatment of cancer. Compounds of formula I wherein X is C3-7 cycloalkylene; each W, Y and Z is independently S, CH, O, N, etc.; A is (CH2)0-2; each R1 and R2 are independently NH2, NR3COR4, CONR3R4, etc.; R3 is H, C1-6 alkyl and aryl; R4 is C1-6 alkyl, aryl, heteroaryl, etc.; each R6 is H, F, OH, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their glutamase inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 100 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to substituted bisthiadiazole preparation glutaminase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 14, 2009, Bouillot, Anne Marie Jeanne; Laroze, Alain published a patent.Formula: C6H8N2O2S The title of the patent was Triazole derivatives as SCD inhibitors and their preparation, pharmaceutical compositions and use in the treatment of SCD-mediated diseases. And the patent contained the following:

The invention relates to substituted triazole compounds of the formula I: and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming AB42 peptide such as Alzheimer’s disease and the like. Compounds of formula I wherein X is CONH, NHCO and CH2NH; R1 is (un)substituted C6-10 aryl; R2 is H, C1-6 alkyl and C1-3 alkyl-O-C1-3 alkyl; R3 is (un)substituted C5-9 heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by 1-[(3,4-dichlorophenyl)methyl]-5-methyl-1H-1,2,3-triazole-4-carboxylic acid with 2-amino-6-methoxybenzothiazole. All the invention compounds were evaluated for their SCD inhibitory activity. Example compound II and several other example compounds exhibited pIC50 values of greater than 5.5. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Formula: C6H8N2O2S

The Article related to triazole preparation stearoyl coa desaturase inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Formula: C6H8N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica