Patent classifications
C07D231/16
METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND, ULTRAPURE FORMS OF THE BIFUNCTIONAL COMPOUND, AND DOSAGE FORMS COMPRISING THE SAME
- Laura E.N. ALLAN ,
- Chungpin Herman CHEN ,
- Hanqing Dong ,
- Robert J. Duguid ,
- John A. GROSSO ,
- Royal J. HASKELL, III ,
- Casey Keith JAGER ,
- Venkata A. KATTUBOINA ,
- Aditya Mohan KAUSHAL ,
- Samuel Elliott KENNEDY ,
- Rhys LLOYD ,
- Miranda Annell NEESER ,
- Yuping QIU ,
- Hayley Reece ,
- Maxwell Marco REEVE ,
- Joseph P. REO ,
- Jerod ROBERTSON ,
- Mohammad Mehdi ZAHEDI
The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:
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The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
CARBAMATE COMPOUND AND USE THEREOF
A carbamate compound represented by formula (I), wherein, R.sup.1 represents a hydrogen atom or a C1-C3 alkyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group optionally having one or more halogen atoms, a C3-C4 cycloalkyl group optionally having one or more halogen atoms or a C1-C3 alkoxy group optionally having one or more halogen atoms; Z.sup.1 represents a halogen atom, a C1-C3 alkyl group or a C1-C3 alkoxy group; and m represents any one of integers from 0 to 3;
has an excellent effect of controlling plant diseases.
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CARBAMATE COMPOUND AND USE THEREOF
A carbamate compound represented by formula (I), wherein, R.sup.1 represents a hydrogen atom or a C1-C3 alkyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group optionally having one or more halogen atoms, a C3-C4 cycloalkyl group optionally having one or more halogen atoms or a C1-C3 alkoxy group optionally having one or more halogen atoms; Z.sup.1 represents a halogen atom, a C1-C3 alkyl group or a C1-C3 alkoxy group; and m represents any one of integers from 0 to 3;
has an excellent effect of controlling plant diseases.
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SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID
Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives.
METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID
Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives.
BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.
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HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
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PYRAZOLE DERIVATIVES FOR THE TREATMENT OF CYSTIC FIBROSIS
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof:
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It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.