- Selective Amination of Polyhalopyridines Catalyzed by a Palladium-Xantphos Complex
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(Matrix presented) Amination of 5-bromo-2-chloropyridine (1a) catalyzed by a palladium-Xantphos complex predominately gives 5-amino-2-chloropyridine product 3a in 96% isolated yield and excellent chemoselectivity (3a/4a = 97:3). Amination of 2,5-dibromopyridine (11) under the same conditions exclusively affords 2-amino-5-bromopyridine 4a.
- Ji, Jianguo,Li, Tao,Bunnelle, William H.
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- PYRAZOLOPYRIDINE COMPOUND AS RET INHIBITOR AND APPLICATION THEREOF
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Disclosed is a series of pyrazolopyridine compounds, and application thereof in the preparation of RET kinase inhibitors for treatment. Specifically disclosed is the compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
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Paragraph 0249; 0258-0260
(2022/02/19)
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- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson's disease, dementia due to Parkinson's (or neurocognitive disorder due to Parkinson's disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher's disease.
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Page/Page column 43; 48
(2021/06/26)
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- 3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof
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The invention discloses a 3-substituent-5-(substituted aryl)-7-azaindole derivative and application thereof. The structural formula of the 3-substituent-5-(substituted aryl)-7-azaindole derivative is shown in the specification, and the 3-substituent-5-(substituted aryl)-7-azaindole derivative has obvious anti-coronavirus activity. In-vitro binding experiments show that the 3-substituent-5-(substituted aryl)-7-azaindole derivative disclosed by the invention generally has relatively strong affinity with a drug target 3CLPro protease of coronavirus, can effectively inhibit the activity of the 3CLPro protease, and is a small molecular ligand for targeted inhibition of 3CLPro.
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Paragraph 0033; 0038-0040
(2021/09/01)
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- CDK9 inhibiting compound and application thereof
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The invention discloses a CDK9 inhibiting compound and application thereof, the structural formula of the CDK9 inhibiting compound is shown in the specification, A is alkyl diamine, X is halogen or H, and R is substituted benzyl. The compound can be used as a CDK9 inhibitor for down-regulating cancer cells PD-L1, and is used for tumor immunotherapy and AIDS treatment.
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Paragraph 0058; 0060; 0061
(2021/09/04)
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- Pyrazolo[1, 5-a]pyridine compound, and preparation method and application thereof
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The invention relates to a pyrazolo[1, 5-a]pyridine compound, a preparation method and application thereof, a pharmaceutical composition containing the compound as an active component, or a pharmaceutically acceptable salt of the compound. The invention further relates to application of the compound of formula (I) in the treatment and prophylaxis of diseases treatable with RET kinase inhibitors, including diseases or conditions mediated by RET kinases.
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Paragraph 0229-0232
(2021/06/12)
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- RET selective inhibitor as well as preparation method and application thereof
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The invention provides an RET selective inhibitor as well as a preparation method and application thereof. The present invention provides compounds of formula(I) and pharmaceutically acceptable salts,solvates, polymorphs or isomers thereof, pharmaceutical compositions comprising these compounds, and the use of such compounds in the treatment of RET-related diseases.
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Paragraph 0429-032
(2021/01/24)
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- COMPOUND SIMULTANEOUSLY INHIBITING LSD1 AND HDAC TARGETS AND APPLICATION THEREOF
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A compound having a general structural formula as shown in Formula I: X-AB-Y (Formula I); in the above Formula I, X is selected from any one of -CO2H, -CONHZ, -CH=CH-CO2H, -CH=CH-CONHZ, wherein Z is selected from any one of substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted aryl, and hydroxyl; Y = -NR1R2, wherein NR1R2 is a substituted or unsubstituted 3- to 9-membered nitrogen-containing heterocycloalkyl; A and B are each independently selected from substituted or unsubstituted phenylene, substituted or unsubstituted azaphenylene. The compound or corresponding pharmaceutical salt thereof can inhibit LSD1 and HDAC target proteins at the same time, thus inhibit the proliferation of many kinds of tumor cells and have good antitumor effect.
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Paragraph 0041; 0047-0048; 0052; 0056
(2020/11/26)
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- POLY-ADP RIBOSE POLYMERASE (PARP) INHIBITORS
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The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.
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Page/Page column 123
(2018/07/29)
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- Substituted pyridine compound and its method and use thereof
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The invention relates to a novel substitutive pyridine compound, and a pharmaceutically acceptable salt and a pharmaceutical preparation of the substitutive pyridine compound for regulating the activity of protein kinases and regulating signal responses between cells or in the cells. Meanwhile, the invention further relates to a pharmaceutical composition containing the compound provided by the invention, and a method for treating high proliferative diseases of mammals, especially human with the pharmaceutical composition.
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Paragraph 0359; 0360
(2018/06/21)
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- QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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Paragraph 0711; 0712
(2017/02/28)
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- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 111
(2017/09/15)
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- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 96
(2017/09/15)
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- SUBSTITUTED PIPERAZINE COMPOUNDS AND METHODS OF USE AND USE THEREOF
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The invention relates to substituted piperazine compounds and methods of use and uses thereof, and further to the pharmaceutical compositions comprising the compounds and uses thereof, wherein the compound has Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. The substituted piperazine compounds and pharmaceutical compositions comprising the compounds disclosed herein can be used for inhibiting 5-hydroxytryptamine reuptake and/or stimulating 5-HT1A receptors. The invention also relates to processes for preparing these compounds and pharmaceutical compositions, and their uses in the treatment of a central nervous system dysfunction.
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Page/Page column 65
(2016/12/22)
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- PDE 10a Inhibitors for the Treatment of Type II Diabetes
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Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
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Paragraph 0945; 0948-0949
(2015/01/06)
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- GLYCINE COMPOUND
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[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
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Page/Page column 17
(2012/07/28)
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- BRAIN/NEURONAL CELL-PROTECTING AGENT, AND THERAPEUTIC AGENT FOR SLEEP DISORDER
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A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an
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Page/Page column 45-46
(2008/06/13)
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- Derivatives of 1-piperazine-and 1-homopiperazine-carboxylates, preparation method thereof and use of same as inhibitors of the FAAH enzyme
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The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are
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Page/Page column 5
(2008/06/13)
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- 2-Pyrimidineamine derivatives and processes for their preparation
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Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group -X1-R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
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