- Multigram Synthesis of Heterabicyclo[n.1.0]alkan-1-yl Trifluoroborates
-
An approach to the synthesis of oxa- and azabicyclo[n.1.0]alkan-1-yl trifluoroborates on a multigram scale was developed. Two synthetic strategies were evaluated: the first based on the lithiation–borylation of the corresponding 2-bromoallyl derivatives, and the other relying on regioselective hydroboration of the appropriate hetera-substituted enynes. The second method appeared to be more efficient in terms of scalability and substrate scope. Further steps included ring closing-metathesis, mild palladium-catalyzed cyclopropanation with diazomethane, and reaction with KHF2 and furnished the title compounds in up to 50 g scale in a single run (10–41 % overall yield, 4–5 steps).
- Kleban, Ihor,Krokhmaliuk, Yevhen,Reut, Sofiia,Shuvakin, Serhii,Pendyukh, Vyacheslav V.,Khyzhan, Oleksandr I.,Yarmoliuk, Dmytro S.,Tymtsunik, Andriy V.,Rassukana, Yuliya V.,Grygorenko, Oleksandr O.
-
p. 6551 - 6560
(2020/09/17)
-
- PURINES AND METHODS OF THEIR USE
-
Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.
- -
-
Page/Page column 77-78
(2021/12/28)
-
- BICYCLIC HETEROARENES AND METHODS OF THEIR USE
-
Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.
- -
-
Page/Page column 92-93
(2021/12/30)
-
- Substituted aza five-membered ring derivative and application thereof in medicine
-
The invention discloses a substituted aza-five-membered ring derivative and application thereof to medicines. , The invention provides a substituted aza five-membered ring compound or a stereoisomer, a tautomer, an oxynitride, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a pharmaceutical composition containing the compound of the present invention. The invention also discloses application of the compound or the pharmaceutical composition of the compound in preparation of a medicament for treating PDE4 related diseases such as atopic dermatitis (AD) or chronic obstructive pulmonary disease (COPD).
- -
-
Paragraph 0496; 0502-0505
(2021/10/30)
-
- INDOLO HEPTAMYL OXIME ANALOGUE AS PARP INHIBITOR
-
Disclosed is a type of indolo heptamyl oxime compounds as a PARP inhibitor. Specifically disclosed are a compound as represented by formula (II) and a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0151-0152
(2021/12/15)
-
- Tetrahydropyrrole compound, preparation method, pharmaceutical composition and application thereof
-
The invention discloses a tetrahydropyrrole compound and a preparation method, a pharmaceutical composition and application thereof. The tetrahydropyrrole compound of the invention is as shown in thegeneral formula (I). The tetrahydropyrrole compound of the invention has an excellent inhibitory effect on the positive symptom of schizophrenia, and has equivalent or stronger efficacy in comparisonwith the positive medicine olanzapine. In addition, the compound of the invention has a dual inhibitory effect on a D2 receptor and a DAT receptor, can effectively treat schizophrenia and improve negative symptoms and cognitive functions, and helps reduce side-effect of centrum and secretion of lactogen.
- -
-
Paragraph 0456; 0460-0462
(2019/07/16)
-
- COMPOUNDS
-
Disclosed are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis(ALS).
- -
-
Page/Page column 148
(2017/02/09)
-
- POLYCYCLIC ANAPLASTIC LYMPHOMA KINASE INHIBITOR
-
Provided is a polycyclic inhibitor of anaplastic lymphoma kinase as represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R4, and ring A are as defined in the description. The invention also relates to a method for preparing the compound, a pharmaceutical preparation and a pharmaceutical composition comprising the compound, and use of the compound, the pharmaceutically acceptable salt or stereoisomer thereof in manufacture of a medicament for the treatment and/or prevention of an anaplastic lymphoma kinase-mediated cancer or non-cancer related diseases.
- -
-
Paragraph 0203; 0204
(2018/02/06)
-
- PYRIDINE DERIVATIVES AND APPLICATION OF ANTI-MACOBACTERIUM THEREOF
-
The present invention provides a series of pyridine derivatives and their preparation method and application thereof. The series of pyridine derivatives can be applied to treating mycobacterium-related diseases, especially to treatments of fatal mycobacterium-related diseases. The fatal diseases may be related to mycobacterium tuberculosis, mycobacterium bovis, mycobacterium avium, and mycobacterium marinum.
- -
-
Paragraph 0142; 0143
(2016/10/08)
-
- CARBAZOLE DERIVATIVES
-
Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
- -
-
Page/Page column 125
(2016/05/24)
-
- DGAT1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
-
The present invention discloses a novel DGAT1 inhibitor, especially the compound of formula (I) or a pharmaceutically acceptable salt thereof, preparation and pharmaceutical composition thereof, as well as their uses in the preparation of a medicament for the prevention and treatment of Familial hyperchylomicronemia (FCS), obesity, hyperlipoproteinemia or hypertriglyceridemia.
- -
-
Paragraph 0317; 0319
(2016/08/23)
-
- NOVEL IMIDAZOLIDINE-2,4-DIONE DERIVATIVES
-
A subject of the present application is novel imidazolidine-2,4-dione derivatives of formula (I). These products have an anti-proliferative activity. They are particularly useful for treating the pathological states and the diseases linked to an abnormal cell proliferation such as cancers. The invention also relates to the pharmaceutical compositions containing said products and their use for the preparation of a medicament.
- -
-
Page/Page column 50
(2015/07/16)
-
- SUBSTITUTED NICOTINIMIDE INHIBITORS OF BTK AND THEIR PREPARATION AND USE IN THE TREATMENT OF CANCER, INFLAMMATION AND AUTOIMMUNE DISEASE
-
Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).
- -
-
Page/Page column 58-59
(2015/04/15)
-
- PYRROLIDINYL AND PIPERIDINYL COMPOUNDS USEFUL AS NHE-1 INHIBITORS
-
Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.
- -
-
-
- Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
-
Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).
- -
-
Page/Page column 91; 92
(2010/08/18)
-