Abstract

The present invention provides a preparation method for a tivozanib key intermediate compound of formula I, 2-chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)-aniline. Compound of formula VI, 4-chloro-6,7-dimethoxyquinoline and compound of formula III, 3-chloro-4-nitrophenol are used as raw materials, a Williamson ether formation reaction is performed to obtain compound of formula II, 2-chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)-nitrobenzene, and then a reduction reaction is performed to obtain the compound of formula I, 2-chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)-aniline. According to the method, the reaction activity is high, the raw materials are easy to obtain, the cost is low, reaction conditions are mild, the product is easy to purify, the yield is high, and thus the method is suitable for industrial mass production.

IPC Classes  ?

• C07C 209/36 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of nitrogen-to-oxygen or nitrogen-to-nitrogen bonds by reduction of nitro groups by reduction of nitro groups bound to carbon atoms of six-membered aromatic rings
• C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
• C07C 217/88 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 43/247 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring and to a carbon atom of a ring, other than a six-membered aromatic ring containing halogen
• C07D 215/14 - Radicals substituted by oxygen atoms

Abstract

The present invention provides a huperzine B crystal and a preparation thereof. Specifically, the present invention provides a crystal form A of the huperzine B crystal. An X-ray diffraction pattern of the crystal form A has the following 2θ angular characteristic absorption peak: 9.56±0.2, 13.90±0.2, 14.88±0.2, 16.00±0.2, 25.39±0.2, and 28.78±0.2.

IPC Classes  ?

• C07D 471/08 - Bridged systems
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine

Abstract

An N-alkyl tryptanthrin derivative, a preparation method for same, and an application thereof are provided. The structure of the derivative is as represented by formula I. The N-alkyl tryptanthrin derivative can serve as a highly active IDO inhibitor, for use in preparing a medicament for prevention and/or treatment of a disease having a pathological characteristic of an IDO-mediated tryptophan metabolic pathway.

IPC Classes  ?

• A61K 31/50 - PyridazinesHydrogenated pyridazines
• C07D 487/04 - Ortho-condensed systems

Abstract

An N-alkyl tryptanthrin derivative, a preparation method for same, and an application thereof. The structure of the derivative is as represented by formula I. The N-alkyl tryptanthrin derivative can serve as a highly active IDO inhibitor, for use in preparing a medicament for prevention and/or treatment of a disease having a pathological characteristic of an IDO-mediated tryptophan metabolic pathway.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents
• A61P 27/12 - Ophthalmic agents for cataracts
• A61P 25/24 - Antidepressants
• A61P 25/22 - Anxiolytics
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia