10 results about "Azabicyclo Compounds" patented technology

Provided is a method of treating malignant tumor by an azabicyclic compound, particularly, with eye disorder reduced. The present invention provides a method for treating malignant tumor, comprising administering an effective amount of 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide (compound 1) or a salt thereof to a patient in need thereof according to a dosing regimen, wherein the dosing regimen comprises administering the compound 1 or the salt thereof at a dose from 40 mg / body / day to 240 mg / body / day in terms of the amount of the compound 1 for consecutive days, and then providing a withdrawal period of at least 2 days.

The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, solvates, adducts, polymorphs, isomers such as stereoisomers and diastereomers, or derivatives thereof, that are useful as orexin antagonists, their preparation, their use in pharmaceutical compositions, and methods of using orexin antagonists to treat or prevent a disease or disorder mediated by orexin receptor activity.

Provided is a novel compound serving as an analogue to be removed from API or a preparation. Further provided is a reference standard of an analogue for use in the quality control of a medicament. Analogue 1: 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3,3′-di(propan-2-yl)-1′H-[1,4′-bipyrazolo[3,4-b]pyridin]-1′-yl}benzamide. Analogue 2: 3-ethyl-4-fluorobenzamide. Analogue 3: N-[1-(4-carbamoyl-2-ethylphenyl)-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide. Analogue 4: 3-ethyl-4-{14-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-13,23,33-tri(propan-2-yl)-31H-[11,24:21,34-terpyrazolo[3,4-b]pyridin]-31-yl}benzamide. Analogue 5: 4,4′-(1H,1′H-[4,4′-biimidazole]-1,1′-diylbis{[3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridine-4,1-diyl]})bis(3-ethylbenzamide). Analogue 6: 4-{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl }-3-ethylbenzonitrile. Analogue 7: 4-{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl }-3-ethylbenzamide. Analogue 8: 4-[4-ethoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]-3-ethylbenzamide. Analogue 9: 3-ethyl-4-[4-methoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide.

The disclosure relates to certain uses and methods of use of 3.1.0 and 4.1.0 azabicycle compounds of Formula (I), wherein X, Y, R1, R2a, and R2b are defined herein, and pharmaceutical compositions containing them, in the treatment of autism spectrum disorder, including Asperger's syndrome.

Provided herein are improved methods to produce diazabicyclo compounds, which may be useful in the production of small molecule KRAS inhibitors. Also provided are new intermediates compounds that may be useful in said processes.

In some embodiments, a thermally conductive composition may include an isocyanate component, the isocyanate component including a blocked isocyanate; an isocyanate reactive component comprising: one or more polyether amines, and one or more catalysts selected from the group consisting of carboxylate salts, tertiary amines, amidines, guanidines, and diazabicyclo compounds; and one or more internal release agents present in one or more of the isocyanate component and the isocyanate-reactive component, the internal release agents prepared from the reaction of one or more equivalents of a fatty acid with a branched C3 to C10 polyol; and a thermally conductive filler, wherein the thermally conductive composition has a thermal conductivity greater than 1 W / m.K.

This application discloses oxime-substituted azabicyclic compounds as selective dual agonists of muscarinic 1 and 4 receptors, and pharmaceutical compositions, preparation methods, and therapeutic uses thereof, as medicaments for treatment of neuropsychiatric disorders associated with muscarinic 1 and / or muscarinic 4 receptors, such as schizophrenia, bipolar disorder, and related conditions.

The present disclosure relates to a novel crystalline form of a tosylate of diazadicyclic compound of formula (I), preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of a drug for treating alopecia areata, psoriasis and ulcerative colitis.

Provided is a novel method for treating CRPC, particularly, CRPC which has acquired resistance to an antiandrogen agent. The present invention relates to an antitumor agent wherein 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a salt thereof and an antiandrogen agent are administered in combination.

Crystallines form or amorphous forms of bisdiazabicyclic compounds or salts thereof for the treatment and / or prevention of diseases or disorders related to hepatitis virus, and a preparation method and application thereof are provided. The crystalline forms or amorphous forms involved provide important reference value for the development and utilization of drugs in the future.