cas 1297538-32-9, ODM-201 | Articles data

Articles about 1297538-32-9Total 11 be found

Pyrazoleamide derivative and synthesis method and application
The present invention discloses a pyrazoleamide derivative and a synthetic method and application as an androgen receptor antagonist and the preparation of anti-prostate cancer drugs. The present invention provides a method of synthesizing a pentabasole r
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(2022/01/10)

Synthesis process of darolutamide
The invention relates to a synthesis process of darolutamide. Compared with an existing synthetic process route in which the reaction steps are 10 steps or more, the process of the invention has the advantages of less reaction steps in the route, high reaction yield of each step, simplicity and convenience in operation, and effective improvement of the total yield and industrial operability of thereaction.
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(2020/05/30)

Method for preparing antitumor drug darolutamide
The invention relates to a method for preparing an antitumor drug darolutamide. A one-step Suzuki reaction is carried out, and then deprotection, hydroxylamine condensation and amide condensation reactions are carried out to obtain the darolutamide. The method has the advantages of few reaction steps, high reaction yield of each step, and simplicity in operation, so the total yield of the whole route is high, and the method has good experiment operationality.
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Paragraph 0059-0065

(2020/05/30)

Synthesis method of polyamidoamine (by machine translation)
To the synthesis method, acetyl - 2 2-chlorobenzonitrile and 4 - are reacted to obtain the compound formula DMF · DMA, the synthesis route 2, is synthesized by two methods, the route, efficiency 6: is greatly improved, the, process cost Boc is reduced, and the reaction formula of the final, finished product purity, suitable for amplification: production, is shown below 10; is greatly shortened. (by machine translation)
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(2020/05/11)

Preparation method of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide
The invention relates to a preparation method of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide, and in particular relates to two novel methods for preparing an intermediate (S)-4-(1-(2-aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile and a method for preparing N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide from the intermediate.
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(2020/01/03)

Discovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants
Androgen receptor (AR) has been a target of prostate cancer (PC) for nearly six decades. Recently, downregulating or degrading AR and the mutants especially the splice variant 7 (AR-V7) lacking ligand binding domain (LBD) emerged as an advantageous therapeutic approach to overcome drug resistance. Here, the structural modification of darolutamide resulted in the discovery of dual-action AR inhibitors and down-regulators. Unlike other traditional AR antagonists targeting the AR-LBD, compounds 4k and 4b not only inhibit the activities of wt-AR and AR-F876L mutant but also downregulate the protein expression of full-length (AR-full) and AR variant 7 (AR-V7) at mRNA level. In cell proliferation assays, compounds 4k and 4b exhibited better antiproliferative activities than darolutamide and enzalutamide against AR-V7-positive 22Rv1 cells and VCaP cells. In addition, 4k demonstrated better antitumor activity than clinically used enzalutamide in castration-resistant VCaP xenograft model. Collectively, combining the activities of AR inhibition and downregulation, compound 4k is proposed as an advantageous lead compound to disrupt AR signaling and overcome resistance.
Yu, Jiang,Zhou, Peiting,Hu, Mingxing,Yang, Liuqing,Yan, Guoyi,Xu, Ruixue,Deng, Yufang,Li, Xinghai,Chen, Yuanwei
(2019/08/20)

PROCESS FOR PREPARATION OF NOVEL ANDROGEN RECEPTOR ANTAGONIST
A process for the preparation of a novel androgen receptor antagonist is provided, comprising essentially conducting cyclization reaction of a compound of formula V to obtain a compound of formula VI. This method has the advantages of easily obtainable starting material, high atomic utilization rate, mild reaction conditions, and simply post-treatment. In addition, ODM-201 and its single isomers can be synthesized directionally by controlling the stereochemistry of starting material, with the advantages of simple and controllable process and suitability for industrial production.
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Page/Page column 30; 31

(2018/07/05)

MANUFACTURE OF A CRYSTALLINE PHARMACEUTICAL PRODUCT
The present invention relates to crystalline particles of N-((S)-l-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1 H-pyrazole-3-carboxamide (I) having specific surface area (SSA) in the range from about 8 to about 16 m2/g, preferably from about to about 15 m2/g, and to the method for the preparation of such particles. Compound (I) is a potent androgen receptor (AR) modulator which is useful as a medicament for example in the treatment of prostate cancer.
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Page/Page column 12

(2018/09/28)

PROCESS FOR THE PREPARATION OF ANDROGEN RECEPTOR ANTAGONISTS AND INTERMEDIATES THEREOF
The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H- pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3- carboxamide (1A) and key intermediates thereof such as 2-chloro-4- (IH-pyrazol-3-yl)benzonitrile (V). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired.
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Page/Page column 17

(2016/10/31)

ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14′, R15, R15′, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
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Page/Page column

(2015/05/06)

ANDROGEN RECEPTOR MODULATING COMPOUNDS
Compounds of formula (I) wherein R1 to R16, A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
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Page/Page column 66-67

(2011/05/11)