cas 39229-33-9, 2-(2-Chloroethoxy)acetyl Chloride

Articles about 39229-33-9Total 9 be found

Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva
Mutant activin receptor-like kinase-2 (ALK2) is associated with the pathogenesis of fibrodysplasia ossificans progressiva, making it an attractive target for therapeutic intervention. We synthesized a new series of bicyclic pyrazoles and evaluated their mutant ALK2 enzyme inhibitory activities, leading to the identification of 8 as the most potent inhibitor. This compound showed moderate microsomal metabolic stability and human ether-a-go-go related gene (hERG) safety. In C2C12 cells carrying mutant ALK2 (R206H), 8 efficiently inhibited the bone morphogenetic protein (BMP)-induced alkaline phosphatase activity.
Yamamoto, Hirofumi,Sakai, Naoki,Ohte, Satoshi,Sato, Tomohiro,Sekimata, Katsuhiko,Matsumoto, Takehisa,Nakamura, Kana,Watanabe, Hisami,Mishima-Tsumagari, Chiemi,Tanaka, Akiko,Hashizume, Yoshinobu,Honma, Teruki,Katagiri, Takenobu,Miyazono, Kohei,Tomoda, Hiroshi,Shirouzu, Mikako,Koyama, Hiroo
(2021/03/01)

TYK-2 INHIBITOR
Disclosed herein is a compound of Formula (I) for inhibiting TYK2 and treating a disease associated with the undesirable tyk-2 activity (tyk-2 related diseases), a method of using the compounds disclosed herein for treating inflammatory or autoimmune disease, and a pharmaceutical composition comprising the same.
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Paragraph 0596-0598

(2022/01/05)

Pyrazolopyridine compound and use thereof
The present invention relates to a pyrazolopyridine compound and use thereof, and further relates to a pharmaceutical composition comprising the pyrazolopyridine compound. The pyrazolopyridine compound or the pharmaceutical composition can be used as a so
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Paragraph 0397; 0399; 0400

(2018/11/03)

COMPOUNDS FOR THE MODULATION OF RIP2 KINASE ACTIVITY
The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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Page/Page column 76; 77

(2017/04/11)

One-pot, regiospecific assembly of (E)-benzamidines from δ- and γ-amino acids via an intramolecular aminoquinazolinone rearrangement
The efficient generation of novel, N-linked benzamidines resulting from a regiospecific rearrangement of quinazolinones is described. This methodology study explored reaction parameters including the effect of changing solvent and temperature, as well as varying electronic substituents on the structural core. The transformation was extensively optimized in terms of reaction conditions and scope, resulting in a protocol that consistently affords diversely functionalized amidines in high yield. The process permits regional structural derivatization that was previously inaccessible, and the multistep process was also reduced to a telescoped, five-step sequence that efficiently affords pharmacologically unique (E)-benzamidoamidines from N-BOC protected γ- and δ-amino acids.
Schroeder, Chad E.,Neuenswander, Sarah A.,Yao, Tuanli,Aubé, Jeffrey,Golden, Jennifer E.
supporting information
p. 3950 - 3955
(2016/06/06)

SUBSTITUTED BIARYLS, PROCESS FOR THEIR MANUFACTURE AND USE THEREOF AS MEDICAMENTS
The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
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Page/Page column 35-37

(2010/11/30)

1- [4- (SULFONYL) -PHENYL] -5- (BENZYL) -IH-I, 2, 4-TRIAZOL DERIVATIVES AS INHIBITORS OF CARBONIC ANHYDRASE FOR TREATING GLAUCOMA OR OCULAR HYPERTENSION
The invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4 and RA through RE are as defined herein. The invention also relates to methods of treating glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy, retinal vasculopathies and intraocular pressure in mammals by administering the compounds of formula I, and to pharmaceutical compositions which contain the compounds of formula I for such treatments. The invention also relates to methods of preparing the compounds of formula (I).
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Page/Page column 40; 41

(2008/12/06)

Practical and efficient processes for the preparation of 4-(4-aminophenyl)morpholin-3-ones on a larger scale: Precursor of factor Xa inhibitors
Factor Xa inhibitors are interesting targets for the development of antithrombotic agents. Our personal efforts in the discovery of small molecule inhibitors led to the compounds EMD 495235 and EMD 503982, which entered preclinical and clinical studies, respectively. Therefore, kilograms of both drugs in particular 4-(4-aminophenyl)morpholin-3-one moieties have to be provided. The scale-up results of these special P-4 ligands will be described herein.
Mederski, Werner W.K.R.,Wendel, Peter Ludwig,Woissyk, Markus
p. 437 - 445
(2008/09/17)

PROCESS FOR PRODUCING 3-ACYLAMINOBENZOFURAN-2-CARBOXYLIC ACID DERIVATIVE
The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: -N="or" -CH=; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof , which is useful as an inhibitor of activated blood coagulation factor X.
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Page/Page column 21

(2008/06/13)