- Tetrahydroisoquinoline amide compounds containing quaternary ammonium ion and pharmaceutical use thereof
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The invention relates to tetrahydroisoquinoline amide compounds containing quaternary ammonium ion, a preparation method of the compounds, and a use of the compounds in the treatment or prevention ofthromboembolic diseases.
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Paragraph 0322-0326
(2019/07/11)
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- Tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use
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The invention relates to a tetrahydroisoquinoline compound and its preparation method, pharmaceutical composition and use. The tetrahydroisoquinoline compound is shown by the general formula (1). In the general formula (1), the symbols have the same definitions as in the specification.
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Paragraph 0108
(2018/03/24)
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- COMPOUNDS AS TNIK, IKKEPSILON AND TBK1 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
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Paragraph 1539-1541
(2016/11/14)
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- SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
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The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
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Paragraph 00344
(2013/04/25)
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- Synthesis of chiral 1-substituted tetrahydroisoquinolines by the intramolecular 1,3-chirality transfer reaction catalyzed by Bi(OTf)3
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The intramolecular 1,3-chirality transfer reaction of chiral amino alcohols 1 with 99% ee was developed to construct chiral 1-substituted tetrahydroisoquinoline 2. Bi(OTf)3 (10 mol %)-catalyzed cyclization of 1 (R = H) afforded (S)-1-(E)-propenyl tetrahydroisoquinoline 2 (R = H) in 83% yield with a ratio of 98:2. The stereochemistry at the newly formed chiral center was produced by a syn SN2′-type process. In this reaction, the substituent on the benzene ring of 1 significantly affected the reactivities and selectivities. A plausible reaction mechanism was proposed.
- Kawai, Nobuyuki,Abe, Ryuzou,Matsuda, Mika,Uenishi, Jun'Ichi
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experimental part
p. 2102 - 2114
(2011/06/19)
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- 1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof.
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Page/Page column 21
(2010/08/08)
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