Tag: 200-300

On August 6, 2014, Xiao, Dengming; Xu, Xinhe; Liu, Xijie; Hu, Yuandong; Yu, Honghao; Liu, Zhihua; Peng, Yong; Sun, Yinghui; Luo, Hong; Kong, Fansheng; Han, Yongxin; Sun, Jian published a patent.Safety of 3,5-Dibromo-4-methoxypyridine The title of the patent was Preparation of substituted 2-aminopyridine derivatives as protein kinase inhibitors. And the patent contained the following:

The present invention discloses substituted 2-aminopyridine derivatives I [wherein A1 = H, substituted aryl, aryloxymethyl, etc.; A2 = substituted Ph, pyridyl, pyrimidinyl, or pyrazolyl; A3 = H, arylamino, substituted heteroaryl, etc.; A5 = substituted heterocyclyl; with the proviso that at least one of A1 or A3 is H] or pharmaceutically acceptable salts thereof as inhibitors of protein kinase, specifically anaplastic lymphoma kinase (ALK), for treating non-small-cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroma, nasopharyngeal carcinoma, breast cancer, colorectal cancer, diffuse large B cell lymphoma, systemic histiocytosis, and neuroblastoma. For example, II was prepared in a multi-step synthesis, which showed inhibitory activity with IC50 of 9.8 nM against ALK. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Safety of 3,5-Dibromo-4-methoxypyridine

The Article related to preparation aminopyridine alk inhibitor treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 15, 2018, Chen, Xuxing; Geng, Meiyu; Jiang, Lei; Chen, Yi; Cao, Jianhua; Jiang, Qingyun; Shen, Qianqian; Ding, Jian; Yao, Yucai; Zhao, Zhao; Xiong, Yuanfang published a patent.Safety of 4-Bromo-2-isopropylpyridine The title of the patent was Pyrido five-element aromatic ring compound, preparation method therefor and use thereof. And the patent contained the following:

The present invention provides a pyrido five-element aromatic ring compound (e.g., I), and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Safety of 4-Bromo-2-isopropylpyridine

The Article related to pyridoarom ezh inhibitor antitumor autoimmune preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 4-Bromo-2-isopropylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 30, 2021, Zhou, Enxing; Liu, Yuan; Wang, Hanping; Wang, Jing; Shao, Ning; Wu, Guanglong published a patent.Product Details of 908267-63-0 The title of the patent was Preparation of heteroaromatics and their methods for inhibiting casein kinases. And the patent contained the following:

The disclosure provides methods for inhibiting CK1 delta or CK1 epsilon activity, comprising administering an effective amount of the compound of formula I, or a pharmaceutically acceptable salt thereof. Compounds of formula I wherein Ar1 is (un)substituted aryl; X1, X2 and X3 are independently C and N; R7 is absent and CN; ring A is absent, X1:CR2 and R3X1:CR2, 4- to 7-membered cycloalkyl, heterocycloalkyl, etc.; R2 is NH2, CN, carboxy, azido, etc.; R3 is halo and CN; ring B is absent, X2CR5, R6X2CH and R6X2CR5, 4- to 7-membered cycloalkyl, etc.; R5 is CO2-C1-6 alkyl, COR10, azido, amido, etc.; R10 is 4- to 7-membered cycloalkyl, heterocycloalkyl and 5- to 6-membered heteroaryl; R6 is C1-6 alkyl, azido, amido, aryl, etc.; dashed bonds are single and double bonds; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their casein kinase inhibitory activity. From the assay, it was determined that compound II exhibited 7.9 nM towards CK1δ. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Product Details of 908267-63-0

The Article related to heteroaromatic preparation casein kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 23, 1997, Onodera, Akira; Ninomiya, Hidetaka; Ohya, Hidenobu; Ishibashi, Daisuke; Komamura, Tawara; Katoh, Katsunori; Tanaka, Tatsuo; Morimoto, Hitoshi published a patent.Computed Properties of 28489-43-2 The title of the patent was Azomethine dyes and their use in ink-jet recording inks. And the patent contained the following:

A recording method comprises the step of ejecting an ink-jet recording ink on a receptor using an ink-jet printer, the ink comprising a dye represented by the formula I [R1, R2 = H, halogen, NH2, organic group; X = OH, NR3R4; R3, R4 = H, hydrocarbyl, heterocyclyl, or R1R3 or R3R4 form a ring; Y1, Y2 = N, CR; R = H, alkyl, acylamino; Y1 or Y2 = N; Z completes an (un)substituted 5- or 6-membered ring, which may bear another condensed ring; R2 or a substituent on Z has Hammett σp -0.3 to +1.0]. Thus, II was prepared in a 9-step synthesis from 6-methyl-2-pyridinamine and 5-tert-butyl-2-hydrazino-6H-1,3,4-thiadiazine. An ink with good color tone and storage stability was prepared from a I 3, H(OCH2CH2)2OH 10, Bu(OCH2CH2)3OH 7, PrOH 3, and H2O 77%. The experimental process involved the reaction of N,N-DIethyl-6-methyl-5-nitro-2-pyridinamine(cas: 28489-43-2).Computed Properties of 28489-43-2

The Article related to azomethine dye jet printing ink, pyrazolotriazole azomethine dye, aminopyridine azomethine dye, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Azo Dyes and Pigments and other aspects.Computed Properties of 28489-43-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 27, 2007, Arnold, James; Berg, Stefan; Chessari, Gianni; Congreve, Miles; Edwards, Phil; Holenz, Joerg; Kers, Annika; Kolmodin, Karin; Murray, Christopher; Patel, Sahil; Rakos, Laszlo; Rotticci, Didier; Sylvester, Mark; Oehberg, Liselotte published a patent.Computed Properties of 908267-63-0 The title of the patent was Substituted isoindoles as BACE inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cognitive impairment, Alzheimers disease, neurodegeneration and dementia. And the patent contained the following:

This invention relates to compounds having the structural formula I and to their pharmaceutically acceptable salt, compositions and methods of use. These compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer disease, neurodegeneration and dementia. Compounds of formula I wherein R1 is H, NO2, CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl;, CONH-C1-6 alkyl, etc.; R2 is Me, (un)substituted C0-3 alkyl-C3-6 cycloalkyl, NO2, CN, substituted C2-4 alkenyl, etc.; R3 is H, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, etc.; m is 0, 1, 2, and 3; and their pharmaceutically acceptable salts, solvates, salts of solvates thereof are claimed. Example compound II•TFA was prepared by Suzuki cross-coupling of [3-(3-bromo-4-hydroxyphenyl)-3-(4-methoxyphenyl)-3H-isoindol-1-yl]carbamic acid tert-Bu ester with 3-methoxyphenylboronic acid; the resulting [3-(6-hydroxy-3′-methoxybiphenyl-3-yl)-3-(4-methoxyphenyl)-3H-isoindol-1-yl]carbamic acid tert-Bu ester underwent hydrolysis to give compound II•TFA. All the invention compounds were evaluated for their BACE inhibitory activity. From the assay, it was determined that compound II exhibited an IC50 value of 67 nM. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Computed Properties of 908267-63-0

The Article related to substituted isoindole preparation bace inhibitor, treatment alzheimer disease neurodegeneration dementia cognitive impairment isoindole preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 7, 2014, Cammarano, Carolyn Michele; Christopher, Matthew P.; Dinsmore, Christopher; Doll, Ronald J.; Fradera Llinas, Francesc Xavier; Li, Chaomin; Machacek, Michelle; Martinez, Michelle; Nair, Latha G.; Pan, Weidong; Reutershan, Michael Hale; Shizuka, Manami; Steinhuebel, Dietrich P.; Sun, Binyuan; Thompson, Christopher Francis; Trotter, B. Wesley; Voss, Matthew Ernst; Wang, Yaolin; Yang, Liping; Panda, Jagannath; Kurissery, Anthappan Tony; Bogen, Stephane L. published a patent.COA of Formula: C8H10BrN The title of the patent was 2,6,7,8-Substituted purines as HDM2 inhibitors and their preparation and use in the treatment of cancer. And the patent contained the following:

The invention provides 2,6,7,8-substituted purines of formula I or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. Compounds of formula I wherein R1 is (un)substituted C1-6 alkyl, 5- to 6-membered nitrogen containing heteroaryl, heterocyclic ring, heterocyclenyl, etc.; R2 is (un)substituted aryl, heteroaryl, C3-8 cycloalkyl, etc.; R3 is C2-6 alkenyl, T-aryl, T-heteroaryl, etc.; R4 is C1-6 alkyl, (CRa2)0-2aryl, (CRa2)0-2heteoaryl, etc.; Ra is H, NH2, halo, etc.; T is C2-4 alkenyl, C=CH2, C=NH, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their HDM2 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 11.44 nM. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).COA of Formula: C8H10BrN

The Article related to purine preparation hdm2 inhibitor, Biomolecules and Their Synthetic Analogs: Others, Including Purines, Pyrimidine Nucleic Acid Bases, Flavins, Lignans and other aspects.COA of Formula: C8H10BrN

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 2, 2012, Austin, Joel Francis; Sharma, Lisa S.; Balog, James Aaron; Huang, Audris; Velaparthi, Upender; Darne, Chetan Padmakar; Saulnier, Mark George published a patent.Category: pyridine-derivatives The title of the patent was Preparation of sulfonamide compounds useful as CYP17 inhibitors. And the patent contained the following:

The title compounds I [ring A = II-IV (wherein X, Y and Q = N and/or CR6; U = N, NR8, and/or CH; W and Z = N and/or C; with the provisos); R1 = H, halo, OH, etc.; R2 = H, halo, alkyl; R3 = H, halo, alkyl, alkoxy; R4 = H, halo, alkyl, alkoxy, haloalkoxy; R5 = (un)substituted alkyl, alkenyl, cycloalkyl, etc.; R6 = H, halo, CN, etc.; R7 = halo, CN, haloalkyl, etc.; R8 = H, alkyl, SO2Ph], useful in the treatment of conditions related to CYP17 enzyme, such as cancer, were prepared E.g., a multi-step synthesis of V, starting from 3-bromo-4-methylpyridine, was described. Exemplified compounds I showed human CYP17 SPA IC50 values of less than 1 μM (specific data given for representative compounds I). Pharmaceutical compositions comprising compound I were disclosed. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Category: pyridine-derivatives

The Article related to sulfonamide preparation cytochrome p450 monooxygenase cyp17 inhibitor antitumor, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Sulfenic, Sulfinic, and Sulfonic Acids and Derivatives and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 15, 2004, Boys, Mark L.; Schretzman, Lori A.; Tollefson, Michael B.; Chandrakumar, Nizal S.; Khanna, Ish K.; Nguyen, Maria; Downs, Victoria; Mohler, Scott B.; Gesicki, Glen J.; Penning, Thomas D.; Chen, Barbara B.; Wang, Yaping; Khilevich, Albert; Desai, Bipinchandra N.; Yu, Yi; Wendt, John A.; Stenmark, Heather; Wu, Lisa; Huff, Renee M.; Nagarajan, Srinivasan R.; Devadas, Balekudru; Lu, Hwang-fun; Russell, Mark; Spangler, Dale P.; Parikh, Mihir D.; Clare, Michael published a patent.COA of Formula: C8H9BrN2O2 The title of the patent was Heteroarylalkanoic acids as integrin receptor antagonists. And the patent contained the following:

The present invention relates to pharmaceutical compositions comprising compounds I [A = (un)saturated and/or (un)substituted 4-8 membered monocyclic or 7-12 membered bicyclic ring, containing 1 to 5 heteroatoms selected from the group consisting of O, N or S; ring A may further contain a carboxamide, sulfone, sulfonamide, or an acyl group; A1 = (un)saturated and/or (un)substituted 5-9 membered monocyclic or 8-14 membered polycyclic heterocycle containing at least one N; or A1 = substituted urea, iminourea or thiourea alicyclic or cyclic analog; Z1 = CH2, CH2O, O, NH, CO, S, SO, CHOH, SO2; Z2 = (un)substituted 1-5 carbon linker optionally containing one or more heteroatoms; alternatively Z1-Z2 may contain a carboxamide, sulfone, sulfonamide, alkenyl, acyl group, or aryl or heteroaryl ring; X = CO, SO2, S, O, substituted amine, substituted CH; Y = CO, SO2, substituted amine, etc.; Y5 = C or N; Y3 and Y4 independently = H, halo, (un)substituted-alkyl, -aryl, -alkene, etc.; or Y3 and Y4 together form a (un)saturated and/or (un)substituted 3-8 membered monocyclic or a 7-11 membered bicyclic ring optionally containing heteroatoms; or X and Y3 form a 3-7 membered monocyclic ring optionally containing heteroatoms; Rb = OH, alkoxy, arylamine, etc.], or a pharmaceutically acceptable salt thereof, methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin, and methods to prepare I. Thus, e.g., II was prepared in four steps with oxadiazole ring forming via cyclization reaction of amide oxime III with cyclic anhydride IV (preparation given). I antagonize αvβ3 integrin with an IC50 values ranging from 0.1 nM to 100 μM in the 293-cell assay. Similarly, I also antagonized αvβ5 integrin with an IC50 values of < 50 μM in the cell adhesion assay. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).COA of Formula: C8H9BrN2O2

The Article related to butanoic acid heteroaryl derivative preparation integrin receptor antagonist, alkanoic acid heteroaryl derivative preparation integrin receptor antagonist, Aliphatic Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.COA of Formula: C8H9BrN2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 31, 1978, Da Settimo, A.; Biagi, G.; Primofiore, G.; Ferrarini, P. L.; Livi, O. published an article.Related Products of 68638-67-5 The title of the article was Synthesis of some 11H-indolo[3,2-c][1,8]naphthyridines. And the article contained the following:

Twelve 11H-indolo[3,2-c][1,8]naphthyridines I (R = OEt, OH, SH, H; R1 = H, F, Br, Me, MeO, OH; R2 = H, MeO, OH) were prepared in 11.9-93.6% yield by 2 methods, e.g., by the Fischer indole synthesis. The UV of I were discussed. Several I were prepared from II, which was prepared in 70.9% yield from 7-bromo-2,3-dihydro-1,8-naphthyridin-4(1H)-one. II displayed a passive cutaneous anaphylaxis inhibition when administered i.p. in the rat at a dose of 25 mg/kg, but it exhibited no oral activity. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Related Products of 68638-67-5

The Article related to anaphylaxis ethoxydihydronaphthyridinone, indolonaphthyridine uv nmr preparation, fischer indole synthesis indolonaphthyridine, 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.Related Products of 68638-67-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 1, 2019, Sun, Jiyun; Tang, Ruikun; Wang, Lu; Xu, Hao; Zhang, Xiaofei; Fan, Wei published a patent.Product Details of 1820711-82-7 The title of the patent was GluN2B subunit-targeted positron tracer for central nervous system and preparation thereof. And the patent contained the following:

The invention relates to GluN2B subunit-targeted positron tracer for central nervous system and preparation thereof, which has the advantages of stable structure, low metabolic rate, good electron tracing effect, mild reaction condition and high purity. In particular, the present invention relates to GluN2B subunit-targeted positron tracer for central nervous system with general formula I, wherein, R1 = Ph, benzene derivative, thienyl, thiophene derivatives GluN2B subunit-targeted positron tracer for central nervous system with general formulaIwas prepared by the following steps: methylation of the intermediate II with 11CH3I to obtain final product. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Product Details of 1820711-82-7

The Article related to glun2b subunit targeted positron tracer preparation central nervous system, 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.Product Details of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem