- Five-membered heteroaromatic derivative, preparation method and application thereof
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The invention belongs to the technical field of medicines, and particularly relates to a five-membered heteroaromatic compound, a composition, a preparation method and application thereof. The compound or the composition can be used as an inhibitor of a retinoid-related orphan receptor [gamma]t (ROR [gamma]t). The invention also relates to a method for preparing the compound and the composition, and application of the compound and the composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
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Paragraph 1146-1150
(2021/07/08)
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- ROR [gamma]t inhibitor, preparation method and application thereof
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The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
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Paragraph 0993; 0996-0998
(2021/07/08)
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- RORγ ANTAGONIST AND APPLICATION THEREOF IN MEDICINE
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Provided herein are compounds as RORγ antagonist having Formula (I). The compounds or pharmaceutical composition thereof can be used for regulating Retinoid-related orphan receptor gamma t (RORγt). Also provided herein are methods of preparation of the compounds and composition thereof, and uses thereof in treating or preventing RORγt mediated inflammation or autoimmune diseases in mammals, particularly humans.
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Paragraph 00733; 00745; 00757; 00770
(2020/02/06)
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- CRYSTAL OF DIAZABICYCLEOCTANE DERIVATE AND METHOD FOR PRODUCING THE SAME
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The present invention provides a crystal of diazabicycleoctane derivate represented by the following formula (VII), especially formula (VII-1), and a method for producing the same.
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Paragraph 0118
(2017/02/02)
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- Production method for diazabicyclooctane derivative and intermediary body thereof
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The present invention provides a production method for a diazabicyclooctane derivative expressed by formula (IV), and an intermediary body thereof (in the formula: P is an acid-removable NH protective group; R1 represents a 2, 5-dioxopyrrolidine-1-yl, a 1, 3-dioxo-3a, a 4, 7, 7a-tetrahydro-1H-isoindole-2(3H)-yl, a 1, 3-dioxohexahydro-1H-isoindole-2(3H)-yl, or a 3, 5-dioxo-4-azatricyclo[5.2.1.02, 6]deca-8-en-4-yl; R2 represents hydrogen, C1CO-, or C13COCO-, R3 represents a C1-6 alkyl or a heterocyclyl, or joins with a bonded -O-NH- to form a 3-7 member heterocyclyl ring; and OBn represents a benzyloxy).
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Paragraph 0281; 0282; 0283
(2016/10/08)
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- CRYSTALLINE FORMS OF DIAZABICYCLOOCTANE DERIVATIVE AND PRODUCTION PROCESS THEREOF
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A crystalline form of a diazabicyclooctane derivative represented by the following Formula (VII), and processes for producing the same:
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Paragraph 0192
(2016/10/11)
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- (2S,5R/2R,5S)-Aminoethylpipecolyl aepip-aegPNA chimera: Synthesis and duplex/triplex stability
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This article reports the design and facile synthesis of novel chiral six-membered PNA analogues (2S,5R/2R,5S)-1-(N-Boc-aminoethyl)-5-(thymin-1-yl) pipecolic acid, aepipPNA IV that upon incorporation into standard aegPNA sequences effected stabilization of
- Shirude, Pravin S.,Kumar, Vaijayanti A.,Ganesh, Krishna N.
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p. 9485 - 9491
(2007/10/03)
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- Chimeric peptide nucleic acids incorporating (2S,5R)-aminoethyl pipecolyl units: Synthesis and DNA binding studies
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The design and facile synthesis of a novel chiral six-membered PNA analogue (2S,5R )-1-(N-Boc-aminoethyl)-5-(thymin-1-yl)pipecolic acid, aepipPNA, that upon incorporation into PNA sequences effected stabilization of complexes with target complementary DNA
- Shirude, Pravin S.,Kumar, Vaijayanti A.,Ganesh, Krishna N.
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p. 3085 - 3088
(2007/10/03)
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