20 results about "Diazepine" patented technology

In one aspect, the present application provides azabicyclo and diazepine derivatives useful as muscarinic receptor modulators. In another aspect, the present application provides pharmaceutical compositions for the treatment of ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulas (I) and (II):

The application discloses a kind of deuterated benzamide diazepine compounds and preparation method and purposes thereof, and structure is as shown in general formula I.The compound is used as selective OX2R antagonist, and shows good activity, selectivity, brain exposure, brain blood ratio (the ratio of drug concentration in brain and drug concentration in blood, is called B / P), little toxic side effect, moderate half-life effect etc..It can be used for preventing, treating and / or reducing the disease related to orexin receptor.General formula I

A biphenylthiourea carboxylic acid metal organic framework crystal material and a preparation method and application thereof.The material has the following chemical formula: {[Zn4O(L)3]·DMF·H2O} n , wherein L is a 6-thio-6,7-dihydro-5H-dibenzo[d,f][1,3]diazepine-3,9-dicarboxylate divalent anion, and n is a degree of polymerization.The metal organic framework crystal material of the present application is synthesized by a solvothermal method, is simple to operate, has low cost, high yield, and is easy to mass industrial production.The prepared metal organic framework crystal material has a high specific surface area (a BET specific surface area of 594 m 2 / g), and an adsorption amount of CO2 of 46.0 cm 3 / g at 1 atm and 273 K.The biphenylthiourea carboxylic acid metal organic framework crystal material of the present application can efficiently catalyze a Friedel-Crafts alkylation reaction of substituted indole and substituted trans-nitrostyrene to generate an indole 3-substituted derivative, and can also efficiently catalyze a Michael addition reaction of diethyl malonate and substituted trans-nitrostyrene, both of which have mild conditions, and the catalyst can be recycled with almost no activity loss, and are good heterogeneous catalysts.

The present invention relates to a method for efficiently producing a compound derived from the commercially available and readily available 3-((3S)-7-bromo-2-((2-hydroxypropyl)amino)-5-(pyridin-2-yl)-3H-benzo[e][1,4]diazepine-3-yl)propionate methyl ester, namely, the compound 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionate methyl ester benzenesulfonate (remimazolam besylate).

The present disclosure relates in some aspects to compositions, such as pharmaceutical compositions for topical administration, which are useful for treating or preventing hair loss, hair graying, and dermatological conditions in a subject, such as comprising a substituted diazepine, for example olanzapine. Also provided are kits comprising the compositions, and methods of using the compositions for treating or preventing hair loss, hair graying, and dermatological conditions.

The invention belongs to the technical field of organic chemical synthesis, and particularly relates to an inherent chiral tricyclic dinazone derivative as well as a preparation method and application thereof. The inherent chiral tricyclic diazonone derivative provided by the invention is a tricyclic molecule with inherent chirality and is good in enantioselectivity. Starting from a seven-membered ring lactam substrate, torsional tension is introduced through strategic N-functionalization to lock molecular conformation, and a series of tricyclic diazepine ketone derivatives with high enantioselectivity are directly synthesized from chiral precursors. Meanwhile, the method disclosed by the invention has the advantages of high efficiency, low cost, simple steps and strong enantioselectivity, and is suitable for large-scale production of the chiral tricyclic dinazone derivative. Furthermore, the compound provided by the invention can be prepared into a chiral drug molecule (+)-tilenezepine through later modification, which proves that the compound provided by the invention has a wide application prospect in the fields of medicinal chemistry and asymmetric catalysis.

A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N-oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.

The present invention relates to new crystalline forms of a pyrimido-diazepine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.

In one aspect, the invention relates to a process for preparing a compound of formula (XII), wherein PG is a protecting group, or a compound of formula (XI), comprising the steps of: (i) treating a compound of formula XIII, wherein PG is a protecting group, with N-methylpiperazine to form a compound of formula XII, wherein said compound of formula XII is in the form of a mixture of cis and trans isomers; (ii) combining the mixture formed in step (i) with an organic solvent and heating the solvent mixture so formed; (iii) isolating the trans-isomer of the compound of formula XII from the solvent mixture formed in step (ii); and (iv) optionally treating said trans-isomer of the compound of formula XII with an acid to form a compound of formula XI; and isolating said compound of formula XI. Further aspects of the invention relate to processes for preparing pyrimido-diazepinone derivatives using the above process and intermediates.

In one aspect, the invention relates to a process for preparing a compound of formula (XII), wherein PG is a protecting group, or a compound of formula (XI), comprising the steps of:(i) treating a compound of formula XIII, wherein PG is a protecting group, with N-methylpiperazine to form a compound of formula XII, wherein said compound of formula XII is in the form of a mixture of cis and trans isomers;(ii) combining the mixture formed in step (i) with an organic solvent and heating the solvent mixture so formed;(iii) isolating the trans-isomer of the compound of formula XII from the solvent mixture formed in step (ii); and(iv) optionally treating said trans-isomer of the compound of formula XII with an acid to form a compound of formula XI; and isolating said compound of formula XI.Further aspects of the invention relate to processes for preparing pyrimido-diazepinone derivatives using the above process and intermediates.

The invention discloses a synthesis method of a sulfonyl-containing indolo [1, 4] diazacycloheptanedione compound, and belongs to the technical field of organic chemistry. The method comprises the following steps: by taking N-alkyl-N-(2-(1H-indole-aryl) methacrylamide, aryl diazonium salt and a sulfur dioxide source as raw materials, carrying out heating reaction in a solvent under a catalyst-free condition, generating a sulfonyl free radical intermediate from the aryl diazonium salt and the sulfur dioxide source in situ, and carrying out free radical addition-cyclization reaction to obtain a target compound. According to the present invention, the method has characteristics of no catalyst, simple process, environmental protection, target product yield reaching up to 99%, strong substrate universality and strong functional group compatibility, and the synthesized compound has good in vitro proliferation inhibition activity on human colon cancer and breast cancer tumor cells, provides candidate molecules for anti-tumor drug research and development, and can easily achieve industrial production.

Quinazolin-4(3H)-one, 2,3-dihydroquinazolin-4(1H)-one, 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one, and 3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione compounds and derivatives inhibit WDR5 and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

The present invention relates to compounds of formula (I) that can modulate, e.g., inhibit or activate, one or more kinases, particularly LRRK2 and / or NUAK1 and / or TYK2, or mutants thereof. The compounds are useful for treating diseases such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases, and hormone-related diseases. The present description discloses the synthesis and characterization of exemplary compounds and their pharmacological data (e.g., pages 40-146; Examples 1-63; Compounds 1-248; Tables 1-3). Preferred compounds are, for example, 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. TIFF2022548246000158.tif64120

Pharmaceutical compositions of the invention comprise diazepines derivatives having a disease-modifying action in the treatment of diseases associated with biological effect that include disease state, and any disease type / class involving biological effect.

In one aspect, the present application provides azabicyclo and diazepine derivatives useful as muscarinic receptor modulators. In another aspect, the present application provides pharmaceutical compositions for the treatment of ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulas (I) and (II):

The present invention relates to new crystalline forms of a pyrimido-diazepine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.

The present invention relates to new crystalline forms of a pyrimido-diazepine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.

Substituted [benzo[f]imidazo[1,5-a][1,4]diazepine]-3-carboxylic acid compounds are GABA(A) receptor modulators and have utility to treat inflammation and / or inhibit smooth muscle contraction.