5 results about "Azacyclobutane" patented technology

Provided herein are solid forms, e.g., polymorphs, of 2-(3-((7R,8aS)-7-fluorohexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)-1-(5-methyl-2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)azetidin-3-yl)acetonitrile, which are useful for treating kinase-related diseases or disorders. The solid forms, and compositions thereof, are useful for treating diseases in a subject, including, but not limited to, ocular diseases such as glaucoma, ocular hypertension, ocular wound repair, neurodegenerative ocular diseases, retinal detachment, and non-ocular diseases such as nerve injury, or skin wound repair, or inflammatory diseases, among others. (Compound 1) TIFF2026501674000028.tif4839

The invention relates to a stable imidazo [1, 2-a] pyridine derivative pharmaceutical composition and application thereof.The pharmaceutical composition comprises an active pharmaceutical ingredient and auxiliary materials, the active pharmaceutical ingredient is (azetidine-1-yl) (8-(2, 6-dimethyl benzylamino)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl) ketone or salt thereof, and the auxiliary materials are selected from the group consisting of 2-(2, 6-dimethyl benzylamino)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl)-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl) ketone or salt thereof. The auxiliary material comprises one or more selected from cyclodextrin or salts thereof, and the pharmaceutical composition also comprises a nitrite scavenger.

The invention belongs to the field of medical chemistry, and discloses Ilunocitinib as well as a preparation method and application thereof. 4-pyrazole boronic acid pinacol ester (I) is used as an initial raw material, the initial raw material and 3-(cyanomethylene) azetidine-1-tert-butyl formate (II) are subjected to a Michael addition reaction to prepare a compound III, and the compound III and the compound IV are subjected to a catalytic coupling reaction to prepare a compound V; removing a Boc protecting group from the compound V under an acidic condition to prepare a compound VI; carrying out sulfonamide reaction on the compound VI and cyclopropyl sulfonyl chloride in an organic solvent to obtain a compound VII; and removing a protecting group from the compound VII under an alkaline condition to obtain a final product Ilunocitinib. The preparation method of the Ilunociitinib has the advantages that the raw materials are easy to obtain, the process is simple, the operation is convenient, the reaction yield is higher than that recorded in the existing literature, and the industrial production is easy.

The invention provides a benzo ring type carbon dioxide-philic microsphere as well as a preparation method and application thereof. The preparation method of the benzo ring type carbon dioxide-philic microspheres comprises the following steps: mixing acrylamide, a benzo ring monomer, a propanesulfonic acid monomer and a cross-linking agent, and carrying out polymerization reaction under the action of an initiator; wherein the benzoring monomer comprises one or a combination of more than two of 4-vinyl benzocyclobutene, benzoazetidine, benzoxetane, benzothietane, 2, 3-indoline, 2, 3-dihydrobenzofuran and 2, 3-dihydrobenzothiophene, and the benzoring monomer comprises one or a combination of more than two of 4-vinyl benzocyclobutene, benzoazetidine, benzoxetane, benzothietane, 2, 3-indoline, 2, 3-dihydrobenzofuran and 2, 3-dihydrobenzothiophene. The mass ratio of the acrylamide to the benzo ring monomer to the propanesulfonic acid monomer is (5-20): (0.08-0.8): (0.4-1.6); the temperature of the polymerization reaction is 30-55 DEG C, and the time is 6-10 hours. The microsphere material can form a high-strength three-dimensional network, and in-situ physical plugging of a gas channeling channel is achieved.

The present invention relates to novel antagonists of the A2B adenosine receptor and pharmaceutical compositions comprising said antagonists as well as their uses for the treatment and prevention of disorders known to be susceptible to improvement by antagonism of the A2B receptor such as asthma, chronic obstructive pulmonary disorder (COPD), pulmonary fibrosis, vascular diseases, allergic diseases, hypertension, retinopathy, diabetes mellitus, inflammatory gastrointestinal tract disorders, inflammatory diseases, autoimmune diseases, renal diseases, neurological disorders and, in particular, cancers.In particular, the present invention relates to compounds of formula IwhereinR1 represents 1 to 3 identical or different R1 substituents, wherein said R1 is independently at each occurrence selected from hydrogen, halogen, C1-C8alkyl, C1-C8haloalkyl, C1-C8alkoxy, C1-C8hydroxyalkyl and C1-C8alkoxyalkyl; Ra is selected from phenyl, pyridinyl, pyrimidinyl, thiazolyl, thiodiazolyl, oxazolyl, pyrazolyl and triazolyl wherein said phenyl, pyridinyl, thiazolyl, thiodiazolyl, oxazolyl, pyrazolyl and triazolyl is independently optionally substituted by one or more substituents independently selected from halogen, hydroxyl, cycloalkyl, C1-C4alkyl-substituted cycloalkyl, C1-C8alkyl, C1-C8haloalkyl, C1-C8alkoxy, C1-C8alkylaminocarbonyl, C1-C8hydroxyalkyl, C1-C8dialkylaminoC1-C8alkyl, C1-C8aminoalkyl and a heterocycle selected from oxiran, oxetane, aziridine and azetidine wherein said oxiran, oxetane, aziridine and azetidine are independently optionally substituted by halogen, hydroxyl, C1-C4alkyl, C1-C2haloalkyl, C1-C2alkoxy; or Ra is —CONHR′ wherein R′ is selected from C1-C8alkyl, cycloalkyl, aryl, heteroaryl and C1-C8alkyl-N-morpholino, wherein said aryl, heteroaryl and C1-C8alkyl-N-morpholino is independently optionally substituted by [one or more] substituents selected from halogen, cycloalkyl, C1-C8alkyl, C1-C8alkoxy, C1-C8hydroxalkyl and C1-C8alkoxyalkyl;Ar / Het is selected from pyridinyl, phenyl and oxazolyl wherein said pyridinyl, phenyl and oxazolyl is independently optionally substituted by one or more substituents independently selected from halogen, cyano, C1-C8alkyl, C1-C8haloalkyl, C1-C8alkoxy, C1-C8hydroxyalkyl and C1-C8alkoxyalkyl;or pharmaceutically acceptable salt, or hydrate thereof.