Category: 1162054-86-5

On November 4, 2021, Bartlett, Mark J.; Chin, Gregory F.; Clarke, Michael O.; Cosman, Jennifer L.; Ensan, Deeba; Goyal, Bindu; Ho, Stephen; Hui, Hon C.; Mackman, Richard L.; Mish, Michael R.; Schroeder, Scott D.; Shapiro, Nathan; Siegel, Dustin S.; Tang, Doris T.; Yang, Hai published a patent.Electric Literature of 1162054-86-5 The title of the patent was Preparation of CD73 inhibiting 2,4-dioxopyrimidine compounds. And the patent contained the following:

The present disclosure provides pyrimidine dione compounds I [Y = a bond, alkyl, cycloalkyl, etc.; one or two of Z1-Z3 = CR2 and the remaining one or two of Z1-Z3 = N; one of W1 and W2 = N and the other = C; R1 = H, CN, alkyl, etc.; R2 = (independently) H, halo, CN, etc.] or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, for treating cancer, including solid tumors. E.g., a multi-step synthesis of II, starting from 8-bromo-6-chloro-2-methyl-imidazo[1,2-b]pyridazine and cyclopropylboronic acid, was described. Exemplified compounds I were tested in the CD73 biochem. IC50 assay and in the MDA-MB-231 cell based CD73 activity assay (data given). The compounds I can be used alone or in combination with other anti-cancer agents. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Electric Literature of 1162054-86-5

The Article related to dioxopyrimidine pyrimidinedione imidazopyridazinyl preparation cd73 inhibitor antitumor solid tumor, combination chemotherapy cd73 inhibitor antitumor pyrimidinedione imidazopyridazinyl preparation and other aspects.Electric Literature of 1162054-86-5

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On July 23, 2009, Hartz, Richard A.; Ahuja, Vijay T.; Arvanitis, Argyrios G.; Rafalski, Maria; Yue, Eddy W.; Denhart, Derek J.; Schmitz, William D.; Ditta, Jonathan L.; Deskus, Jeffrey A.; Brenner, Allison B.; Hobbs, Frank W.; Payne, Joseph; Lelas, Snjezana; Li, Yu-Wen; Molski, Thaddeus F.; Mattson, Gail K.; Peng, Yong; Wong, Harvey; Grace, James E.; Lentz, Kimberley A.; Qian-Cutrone, Jingfang; Zhuo, Xiaoliang; Shu, Yue-Zhong; Lodge, Nicholas J.; Zaczek, Robert; Combs, Andrew P.; Olson, Richard E.; Bronson, Joanne J.; Mattson, Ronald J.; Macor, John E. published an article.Quality Control of (S)-1-Methoxypropan-2-amine hydrochloride The title of the article was Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of N3-Phenylpyrazinones as Novel Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists. And the article contained the following:

Evidence suggested that corticotropin-releasing factor-1 (CRF1) receptor antagonists may offer therapeutic potential for the treatment of diseases associated with elevated levels of CRF such as anxiety and depression. A pyrazinone-based chemotype of CRF1 receptor antagonists was discovered. Structure-activity relationship studies led to the identification of numerous potent analogs including I, a highly potent and selective CRF1 receptor antagonist with an IC50 value of 0.26 nM. The pharmacokinetic properties of I were assessed in rats and Cynomolgus monkeys. Compound I was efficacious in the defensive withdrawal test (an animal model of anxiety) in rats. The synthesis, structure-activity relationships and in vivo properties of compounds, e.g., I, within the pyrazinone chemotype were described. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Quality Control of (S)-1-Methoxypropan-2-amine hydrochloride

The Article related to pyrazinone arylamino asym preparation corticotropin releasing factor receptor antagonist, arylamino pyrazinone corticotropin releasing factor receptor antagonist sar activity, anxiolytic agent pyrazinone arylamino crf receptor antagonist sar activity and other aspects.Quality Control of (S)-1-Methoxypropan-2-amine hydrochloride

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Taglang, Celine; Martinez-Prieto, Luis Miguel; del Rosal, Iker; Maron, Laurent; Poteau, Romuald; Philippot, Karine; Chaudret, Bruno; Perato, Serge; Sam Lone, Anais; Puente, Celine; Dugave, Christophe; Rousseau, Bernard; Pieters, Gregory published an article in 2015, the title of the article was Enantiospecific C-H activation using ruthenium nanocatalysts.Safety of (S)-1-Methoxypropan-2-amine hydrochloride And the article contains the following content:

The activation of C-H bonds has revolutionized modern synthetic chem. However, no general strategy for enantiospecific C-H activation has been developed to date. We herein report an enantiospecific C-H activation reaction followed by deuterium incorporation at stereogenic centers. Mechanistic studies suggest that the selectivity for the α-position of the directing heteroatom results from a four-membered dimetallacycle as the key intermediate. This work paves the way to novel mol. chem. on nanoparticles. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Safety of (S)-1-Methoxypropan-2-amine hydrochloride

The Article related to enantiospecific ch activation reaction deuterium incorporation ruthenium nanocatalyst nanoparticle, langmuir hinshelwood deuteration mechanism ab initio dimetallacycle, ch activation, ab initio calculations, deuterium, isotopic labeling, nanoparticles and other aspects.Safety of (S)-1-Methoxypropan-2-amine hydrochloride

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On November 11, 2010, Kanzawa, Keizo; Kawaguchi, Kenichi; Matsumoto, Shunichiro; Nomura, Takaho; Susumu, Takashi; Seo, Tatsushi published a patent.Category: ethers-buliding-blocks The title of the patent was Preparation of azolecarboxamide compounds or their salts as antagonists of neurotrophic factor receptors (TrkA). And the patent contained the following:

N-Ph, N-pyridyl, or N-pyrazolylthiazole-4-carboxamides and oxazole-4-carboxamides the title compounds [I; X = S, O; R1 = Q, Q1, 3-methoxymethylmorpholin-4-yl, NR1cR1d; R1a = H, HO, lower alkoxy, cycloalkyloxy; R1b = H, lower alkoxy; R1c = H, lower alkyl; R1d = lower alkyl optionally substituted by lower alkoxy; R2 = H, lower alkyl optionally substituted by F or lower alkoxy, 3-tetrahydrofuryl, 4-tetrahydropyranyl; A = R2, Q3, Q4; R3 = CO2Me, Q5, CH2R3B; R00 = lower alkyl; R3B = OH, lower alkoxy, Q6, Q7, Q8, Q10, hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl; R0 = H, lower alkyl; m = 1,2; Ra = H, F, Ph, lower alkoxy-lower alkyl; R4 = lower alkyl optionally substituted by lower alkoxy] or salts thereof are prepared These compounds possess potent inhibitory activity against neurotrophic factor receptors (TrkA) and provide therapeutic and/or preventive agents for various lower urinary tract diseases accompanied by lower urinary tract pains such as interstitial cystitis and chronic prostatitis, urinary frequency accompanied by various lower urinary tract diseases including overactive bladder, feeling of micturition urgency, urinary incontinence, and various diseases accompanied by pain based on the TrkA-inhibitory activity. Thus, 67 mg (8aR)-octahydropyrrolo[1,2-a]pyrazine and 216 mg Cs2CO3 were added to a mixture of 200 mg N-[4-(chloromethyl)-2-[(2-methoxyethyl)carbamoyl]phenyl]-2-((3S)-3-methoxypyrrolidin-1-yl)-1,3-thiazole-4-carboxamide and 2 mL DMF and the resulting mixture was stirred at room temperature for 18 h to give, after workup and silica gel chromatog. and salt formation with fumaric acid, N-[4-[((8aR)-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl)methyl]-2-[(2-methoxyethyl)carbamoyl]phenyl]-2-((3S)-3-methoxypyrrolidin-1-yl)-1,3-thiazole-4-carboxamide (II) difumarate. II difumarate and N-phenylthiazole-4-carboxamide derivative (III) in vitro inhibited the NGF-induced increase in cellular calcium ion in HEK293 cells stably expressing human trkA receptor with IC50 of 19 and 16 nM, resp. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Category: ethers-buliding-blocks

The Article related to azolecarboxamide preparation antagonist neurotrophic factor receptor trka, thiazolecarboxamide oxazolecarboxamide preparation antagonist neurotrophic factor receptor trka, pain urinary tract disease treatment prevention thiazolecarboxamide oxazolecarboxamide preparation and other aspects.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem