- MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
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Paragraph 1250
(2020/10/09)
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- Compounds for inflammation and immune-related uses
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The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
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- Anti-tumor activity with acetylene derivatives
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The present invention relates to an aromatic ring disubstituted acetylene derivative of formula I, a pharmaceutical composition comprising the compound, and a use of the compound and of the pharmaceutical composition in the treatment and/or prevention of tumors, where A, B, T, M, Ra, Rb, Rt, m, n, and p are as defined in the present document.
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Paragraph 0293-0296
(2016/10/08)
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- Enzyme-Inspired Axially Chiral Pyridoxamines Armed with a Cooperative Lateral Amine Chain for Enantioselective Biomimetic Transamination
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Enzymatic transamination is catalyzed by pyridoxal/pyridoxamine, and it involves remarkable cooperative catalysis of a Lys residue in the transaminase. Inspired by transaminases, we developed a class of axially chiral pyridoxamines 11 bearing a lateral amine arm. The pyridoxamines exhibited high catalytic activity and excellent enantioselectivity in asymmetric transamination of α-keto acids, to give various α-amino acids in 67-99% yields with 83-94% ee's. The lateral amine arm likely participates in cooperative catalysis as the Lys residue does in biological transamination and has an important impact on the transamination in terms of activity and enantioselectivity.
- Liu, Yong Ethan,Lu, Zhaole,Li, Bo,Tian, Jiaxin,Liu, Feng,Zhao, Junyu,Hou, Chengkang,Li, Yingkun,Niu, Lili,Zhao, Baoguo
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supporting information
p. 10730 - 10733
(2016/09/09)
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- A 2-amino-thiazole compounds (by machine translation)
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The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
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Paragraph 0725-0727
(2016/10/08)
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- 3-Pyridyl enantiomers and their use as analgesics
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The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: STR1 or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.
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