Category: 199522-66-2

On January 31, 2004, Crider, A. M.; Liu, S.; Li, T.; Mahajan, S.; Ankersen, M.; Stidsen, C. E. published an article.Category: pyridine-derivatives The title of the article was Somatostatin receptor subtype 4 (sst4) ligands: Synthesis and evaluation of indol-3-yl- and 2-pyridyl-thioureas. And the article contained the following:

Thiourea analogs of NNC 26-9100 (2) were prepared as somatostatin receptor subtype 4 (sst4) ligands. The indole 9 exhibited high affinity (Ki = 23 nM) and about a 100-fold selectivity at sst4 compared to sst2 receptors. The (imidazol-4-yl) Pr group appears to play a major role in the affinity and selectivity of these thioureas at sst4. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Category: pyridine-derivatives

The Article related to somatostatin receptor sst4 thiourea ligand, Pharmacology: Structure-Activity and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Marugan, Juan Jose; Huang, Wenwei; Motabar, Omid; Zheng, Wei; Xiao, Jingbo; Patnaik, Samarjit; Southall, Noel; Westbroek, Wendy; Lea, Wendy A.; Simeonov, Anton; Goldin, Ehud; DeBernardi, Maria A.; Sidransky, Ellen published an article in 2012, the title of the article was Non-iminosugar glucocerebrosidase small molecule chaperones.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine And the article contains the following content:

Small mol. chaperones are a promising therapeutic approach for the Lysosomal Storage Disorders (LSDs). Here, we report the discovery of a new series of non-iminosugar glucocerebrosidase inhibitors with chaperone capacity, and describe their structure-activity relationship (SAR), selectivity, cell activity and pharmacokinetics. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to glucocerebrosidase inhibitor chaperone pharmacokinetics brain ml156 msbar, Pharmacology: Structure-Activity and other aspects.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 19, 1998, Liu, Shenquan; Tang, Cheng; Ho, Bin; Ankersen, Michael; Stidsen, Carsten E.; Crider, A. Michael published an article.Synthetic Route of 199522-66-2 The title of the article was Nonpeptide Somatostatin Agonists with sst4 Selectivity: Synthesis and Structure-Activity Relationships of Thioureas. And the article contained the following:

Utilizing NNC 26-9100 as a structural lead, a variety of nonpeptide derivatives of somatostatin were synthesized and evaluated for sst2 and sst4 receptor binding affinity. A novel thiourea scaffold was utilized to attach (1) a heteroaromatic nucleus to mimic the Trp8 residue, (2) a nonheteroarom. nucleus to mimic Phe7, and (3) a primary amine or other basic group to mimic the Lys9 residue of somatostatin. Displacement studies were carried out using membranes from cell lines expressing ssts [BHK cells (sst4) and HEK 293 cells (sst2)] utilizing [125I]Tyr11-SRIF as the radioligand. Several thioureas and an urea derivative exhibited Ki values of less than 100 nM. Two thioureas and the urea derivative are believed to be the most potent nonpeptide sst4 agonists known with Ki of 6, 16, and 14 nM, resp. Since the thiourea and the urea derivatives exhibit high sst4 selectivity, these novel nonpeptide derivatives may be useful tools for studying the sst4 receptor. Studies are currently in progress to evaluate the therapeutic potential of NNC 26-9100 in the treatment of glaucoma. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Synthetic Route of 199522-66-2

The Article related to thiourea preparation structure somatostatin agonist, nnc26910 derivative somatostatin sst4 receptor agonist, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 10, 2015, Scobie, Martin; Wallner, Olov; Koolmeister, Tobias; Vallin, Karl Sven Axel; Henriksson, Carl Martin; Homan, Evert; Helleday, Thomas; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline; Fiskesund, Roland Julius Yu published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Diaminopyrimidines as MTH1 inhibitors for treatment of inflammatory and autoimmune conditions and their preparation. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions. Compounds of formula I wherein R2 is (un)substituted Ph, substituted 6-membered heteroaryl, 5- to 10-membered (mono/bi)cyclic heteroaryl, etc.; R2 is H, halo, CN, (un)substituted C1-3 alkyl, etc.; R3 is X-L-J, (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; X is (un)substituted C1-6 alkylene, and (un)substituted C0-2 alkyl-heterocycloalkylene-C0-2 alkyl; L is single bond, O, S, O-C1-6 alkylene, etc.; J is (un)substituted 6- to 10-membered aryl and (un)substituted 5- to 11-membered (mono/bi)cyclic heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of less than 200 nM. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to diaminopyrimidine preparation mth1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Scobie, Martin; Helleday, Thomas; Koolmeister, Tobias; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline published a patent.SDS of cas: 199522-66-2 The title of the patent was Preparation of pyrimidine-2,4-diamine derivatives for treatment of cancer. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1. Compounds of formula I wherein R1 is (un)substituted heteroaryl and (un)substituted aryl; R2 is H, halo, CN, (un)substituted C1-12 alkyl, etc.; R3 is (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; R2R3 can be taken together to form 5- to 8-membered nonaromatic ring; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity (data given). The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).SDS of cas: 199522-66-2

The Article related to pyrimidinediamine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 10, 2015, Scobie, Martin; Wallner, Olov; Koolmeister, Tobias; Vallin, Karl Sven Axel; Henriksson, Carl Martin; Homan, Evert; Helleday, Thomas; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline; Fiskesund, Roland Julius Yu published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Diaminopyrimidines as MTH1 inhibitors for treatment of inflammatory and autoimmune conditions and their preparation. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions. Compounds of formula I wherein R2 is (un)substituted Ph, substituted 6-membered heteroaryl, 5- to 10-membered (mono/bi)cyclic heteroaryl, etc.; R2 is H, halo, CN, (un)substituted C1-3 alkyl, etc.; R3 is X-L-J, (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; X is (un)substituted C1-6 alkylene, and (un)substituted C0-2 alkyl-heterocycloalkylene-C0-2 alkyl; L is single bond, O, S, O-C1-6 alkylene, etc.; J is (un)substituted 6- to 10-membered aryl and (un)substituted 5- to 11-membered (mono/bi)cyclic heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of less than 200 nM. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to diaminopyrimidine preparation mth1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Scobie, Martin; Helleday, Thomas; Koolmeister, Tobias; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline published a patent.SDS of cas: 199522-66-2 The title of the patent was Preparation of pyrimidine-2,4-diamine derivatives for treatment of cancer. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1. Compounds of formula I wherein R1 is (un)substituted heteroaryl and (un)substituted aryl; R2 is H, halo, CN, (un)substituted C1-12 alkyl, etc.; R3 is (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; R2R3 can be taken together to form 5- to 8-membered nonaromatic ring; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity (data given). The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).SDS of cas: 199522-66-2

The Article related to pyrimidinediamine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 29, 2005, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradei, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Category: pyridine-derivatives The title of the patent was Preparation of triazinyl and other carboxamides as inhibitors of histone deacetylase. And the patent contained the following:

The invention provides compounds and methods for inhibiting histone deacetylase enzymic activity. Such compounds include carboxamides I [Cy2 = (un)substituted cycloalkyl, aryl, heteroaryl, heterocyclyl (each of which is optionally fused to one or two aryl or heteroaryl rings, or to one or two (un)saturated cycloalkyl or heterocyclic rings); X1 = a bond, M1L2M1, L2M2L2 (wherein L2 = a bond, alkylene, alkenylene, alkynylene; M1 = O, S, SO, NHCO, etc.; M2 = M1, heteroarylene, heterocyclylene); Ar2 = (un)substituted (hetero)arylene; R5, R6 = H, alkyl, aryl, aralkyl; q = 0-1; Ay2 = (un)substituted 5-6 membered cycloalkkyl, heterocyclyl or heteroaryl substituted with an amino or hydroxy moiety; with provisos] which were prepared and claimed. E.g., a multi-step synthesis of II, starting from Me 4-(aminomethyl)benzoate.HCl, was given. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I are illustrated for colorectal, pulmonary and pancreatic neoplasms; also the combined antineoplastic effect of histone deacetylase inhibitors and histone deacetylase antisense oligonucleotides on tumor cells in vivo was demonstrated. Although the methods of preparation are not claimed, hundreds of example preparations are included. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Category: pyridine-derivatives

The Article related to carboxamide preparation inhibitor histone deacetylase hdac proliferative disease antitumor, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease antitumor and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 27, 2003, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradel, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Preparation of triazinyl and other carboxamides as inhibitors of histone deacetylase. And the patent contained the following:

The invention relates to triazines (shown as I; variables defined below; e.g. 4-[[4-amino-6-(2-indanylamino)-[1,3,5]triazin-2-ylamino]methyl]-N-(2-aminophenyl)benzamide) and Cy3-X1-Ar2-(C(R5):C(R6))qC(O)NH-Ay2 (II; variables defined below; e.g. ), many of which are N-(o-aminophenyl)carboxamides, as inhibitors of histone deacetylase (data included for many I and II). The invention provides compounds and methods for inhibiting histone deacetylase enzymic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I and II are illustrated for colorectal, pulmonary and pancreatic neoplasms; also the combined antineoplastic effect of histone deacetylase inhibitors and histone deacetylase antisense oligonucleotides on tumor cells in vivo was demonstrated. For I: R3 and R4 = H, L1, Cy1 and -L1-Cy1 (L1 = C1-C6 alkyl, C2-C6 heteroalkyl, or C3-C6 alkenyl; Cy1 = cycloalkyl, aryl, heteroaryl, or heterocyclyl) or R3 and R4 are taken together with the adjacent N atom to form a 5-, 6-, or 7-membered ring, wherein the ring atoms = C, O, S, and N, and wherein the ring is optionally substituted, and optionally forms part of a bicyclic ring system, or is optionally fused to one or two aryl or heteroaryl rings, or to one or two saturated or partially unsaturated cycloalkyl or heterocyclic rings, each of which rings and ring systems is optionally substituted. Y1 = -N(R1)(R2), -CH2-C(O)-N(R1)(R2), halogen, and H (R1 and R2 = H, L1, Cy1, and -L1-Cy1). Y2 = chem. bond or N(R0) (R0 = H, alkyl, aryl, aralkyl, and acyl); Ak1 = C1-C6 alkylene, C1-C6-heteroalkylene (preferably, in which one -CH2- is replaced with -NH-, and more preferably -NH-CH2), C2-C6 alkenylene or C2-C6 alkynylene; Ar1 = arylene or heteroarylene, either of which is optionally substituted; and Z1 = C(O)NH-Ay1 and CH:CHC(O)NH-Ay1 (Ay1 = aryl or heteroaryl, each of which is optionally substituted). For II: Cy2 = cycloalkyl, aryl, heteroaryl, or heterocyclyl; X1 = covalent bond, M1-L2-M1, and L2-M2-L2 (L2 = chem. bond, C1-C4 alkylene, C2-C4 alkenylene, and C2-C4 alkynylene, provided that L2 is not a chem. bond when X1 is M1-L2-M1; M1 = -O-, -N(R7)-, -S-, -S(O)-, S(O)2-, -S(O)2N(R7)-, -N(R7)S(O)2-, -C(O)-, -C(O)NH-, -NHC(O)-, -NHC(O)-O- and -OC(O)NH- (R7 = H, alkyl, aryl, aralkyl, acyl, heterocyclyl, and heteroaryl); and M2 = M1, heteroarylene, and heterocyclylene, either of which rings is optionally substituted). Ar2 = arylene or heteroarylene, each of which is optionally substituted; R5 and R6 = H, alkyl, aryl, and aralkyl; q is 0 or 1; and Ay2 is a 5-6 membered cycloalkyl, heterocyclyl, or heteroaryl substituted with an amino or hydroxy moiety (preferably these groups are ortho to the amide N to which Ay2 is attached) and further optionally substituted; provided that when Cy2 is naphthyl, X1 is -CH2-, Ar2 is Ph, R5 and R6 are H, and q is 0 or 1, Ay2 is not Ph or o-hydroxyphenyl. Although the methods of preparation are not claimed, hundreds of example preparations are included. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to carboxamide preparation inhibitor histone deacetylase proliferative disease treatment, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease treatment and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 20, 1997, Ankersen, Michael; Stidsen, Carsten Enggaard; Andersen, Henrik Sune published a patent.HPLC of Formula: 199522-66-2 The title of the patent was Preparation of thioureas and guanidines as somatostatin agonists and antagonists. And the patent contained the following:

The title compounds [I and II; m = 2-6; n = 1-3; p = 1-6; R1, R2 = H, (un)substituted C1-6 alkyl; X = S, O, NH, NC(O)Ph, N(CN); A, B, D = (un)substituted aryl, heteroaryl] and their salts, useful for treating medical disorders related to binding to human somatostatin receptor subtypes, were prepared and formulated. Thus, reaction of N-(4-bromobenzyl)-N-(3-isothiocyanatopropyl)-N-(pyridin-2-yl)amine and 3-(1-triphenylmethylimidazol-4-yl)propylamine in CHCl3 followed by treatment of the triphenylmethyl intermediate with HCl afforded 80% III.2HCl. Compounds I are effective at 0.001-50 mg/kg/day. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).HPLC of Formula: 199522-66-2

The Article related to somatostatin agonist antagonist thiourea guanidine preparation, thiourea preparation formulation somatostatin agonist antagonist, guanidine preparation formulation somatostatin agonist antagonist and other aspects.HPLC of Formula: 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem