141120-33-4Relevant academic research and scientific papers
Synthesis of 1-substituted epibatidine analogues and their in vitro and in vivo evaluation as α4β2 nicotinic acetylcholine receptor ligands
Heugebaert, Thomas S.A.,Van Overtveldt, Melissa,De Blieck, Ann,Wuyts, Benjamin,Augustijns, Patrick,Ponce-Gamez, Eugenia,Rivera, Alicia,De Groote, Dominic,Lefebvre, Romain A.,Wouters, Patrick,Meert, Theo,Devulder, Jacques,Stevens, Christian V.
, p. 2226 - 2234 (2014)
The highly potent natural alkaloid epibatidine remains a source of inspiration in the search for new analgesic drugs. In this paper, we describe an expansion of our previously reported synthesis of epibatidine analogues, and five synthetic alkaloids chara
CYCLOALKYLIDENE CARBOXYLIC ACIDS AND DERIVATIVES AS BTK INHIBITORS
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, (2021/03/05)
The present invention relates to novel cycloalkylidene carboxylic acids and derivatives thereof useful as Bruton tyrosine kinase (BTK) inhibitors. The present disclosure also relates to processes for their preparation, pharmaceutical compositions containing one or more such compounds, and to the use of such compounds and pharmaceutical compositions for the treatment of disorders involving mediation of BTK in humans (Formula I).
3-(dimethylaminomethyl) cyclohex-4-alcohol derivative as well as preparation method and pharmaceutical application thereof
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, (2021/05/08)
The invention belongs to the field of pharmacy, and relates to a 3-(dimethylaminomethyl) cyclohex-4-alcohol derivative with a general formula (I) or a salt thereof and a preparation method, and relates to an application of the compound in treatment of opioid receptor mediated diseases. The present invention provides a pharmaceutically acceptable solvate or hydrate of a compound of formula (I), and also provides a pharmaceutical composition comprising: a compound of formula (I) or a pharmaceutically acceptable salt, solvate or hydrate thereof; and a pharmaceutically acceptable carrier. The medicine prepared from the compound can be used for treating or improving diseases related to an opioid receptor; wherein the diseases can be selected from but not limited to pain, gastrointestinal diseases and depression.
RET Inhibitor. Pharmaceutical composition and use thereof
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, (2021/10/27)
The invention belongs to the field of medicines, and relates to RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prophylaxis of diseases and disorders associated and RET.
BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Paragraph 00719, (2020/07/07)
Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
QUINAZOLINONES AS PARP14 INHIBITORS
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Paragraph 0298; 0390; 0391, (2019/07/10)
The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
PYRIDINYL PYRAZOLES AS MODULATORS OF RORyT
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, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
6-AMINOPYRIDIN-3-YL PYRAZOLES AS MODULATORS OF RORgT
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, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, Q, R3, R4, R5, R6, A1, and A2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
PHENYL AND PYRIDINYL SUBSTITUTED IMIDAZOLES AS MODULATORS OF RORyT
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, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
PHENYL SUBSTITUTED PYRAZOLES AS MODULATORS OF RORgT
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, (2020/01/09)
The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, R7, R8, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
