- 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 1799; 1801-1803
(2021/07/08)
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- DIHYDROPYRIMIDINE COMPOUNDS AND USES THEREOF IN MEDICINE
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Provided herein are a dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B. Specifically, provided herein is a compound having Formula (I) or (Ia), or a stereisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B.
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Paragraph 00170-00172
(2019/05/10)
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- COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS
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Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
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Page/Page column 81; 82; 140; 141; 142; 143
(2017/03/08)
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- Production of cis-4-hydroxyproline
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PROBLEM TO BE SOLVED: To produce cis-4-hydroxyproline useful as a raw material of medicines and agrochemicals by an industrially suitable method.SOLUTION: The method for producing cis-4-hydroxyproline includes: hydrolyzing a hydroxyproline derivative represented by formula (1), wherein Rdenotes a 1-6C alkylcarbonyl group, an arylcarbonyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, or an aralkyloxycarbonyl group, in the presence of a hydrochloric acid catalyst; neutralizing the resultant with an organic base; and thereafter diluting the resultant with an alcohol.
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Paragraph 0053
(2018/11/24)
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- PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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Page/Page column 58
(2014/01/17)
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- PROLINE DERIVATIVES FOR USE IN THE TREATMENT OF DIABETES
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The present invention provides novel heterocyclic compounds and methods of preparing such compounds. The compounds of the invention are useful for palliative, curative or prophylactic treatment of diseases or conditions of diabetes and/or hypertension. This invention also relates to pharmaceutical compositions containing the compounds of the present invention, and methods for palliative, curative or prophylactic treatment of diseases or conditions of diabetes and/or hypertension. The present invention also provides pharmaceutical compositions consisting of the heterocyclic compounds along with one or more dyslipidemic agents, antiobesity agents, anti-hyperglycemic agents, antihypertensive agents and anti-inflammatory agents.
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Page/Page column 31-32
(2011/08/21)
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- METHOD FOR PREPARING (CIS)-4-HYDROXYPROLINE DERIVATIVE
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PROBLEM TO BE SOLVED: To provide a method for preparing a (cis)-4-hydroxyproline derivative by a simple operation. SOLUTION: The (cis)-4-hydroxyproline derivative useful as an intermediate for drugs can be prepared in a good yield by a simple operation by adding a basic compound on the hydrolysis of a (trans)-4-hydroxyproline ester derivative to perform the reaction at a high temperature (50-120°C), and thereafter lowering the temperature of the reaction solution to 0-40°C to add the basic compound again.
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Page/Page column 8
(2008/06/13)
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- Pyrrolidine carbamate nucleic acids: Synthesis and DNA binding studies
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An efficient solid phase synthesis of pyrrolidine carbamate nucleic acids is reported. The protected (2S, 4S)-4-aminopyrrolidine-2-methanol with nucleobases thymine and cytosine attached to the ring nitrogen through an acetyl linker can be activated as ni
- Meena,Kumar, Vaijayanti A.
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p. 3393 - 3399
(2007/10/03)
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- Two prolines with a difference: contrasting stereoelectronic effects of 4R/S-aminoproline on triplex stability in collagen peptides [pro(X)-pro(Y)-Gly]n.
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4R/S-Aminoprolines when present in the X-position of collagen peptide [pro(X)-pro(Y)-Gly]n exhibit pH- and stereochemistry-dependent effects on triplex stability.
- Umashankara,Babu, I Ramesh,Ganesh, Krishna N
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p. 2606 - 2607
(2007/10/03)
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- Synthesis and evaluation of prolyl carbamate nucleic acids (PrCNA)
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Carbamate linked prolyl nucleic acids are obtained in high yield and purity under mild conditions in solution and solid phase. p-Nitrophenylchloroformate is used as the activating reagent for alcohol. Homooligomers of PrCNA do not bind to DNA. The introduction of this modification in PNA sequences destabilizes the triplxes, inspite of enhancement in the base stacking.
- Meena,Kumar,Ganesh
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p. 1193 - 1196
(2007/10/03)
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- Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems - I. 2-alkoxymethyl derivatives
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The synthesis and in vitro antibacterial activity of a novel series of 2-alkoxymethyl-4-pyrrolidinylthio-1β-methyl carbapenems are described. As a result of these studies, we discovered that FR27743 (19j) containing a novel 2-fluoroethoxymethyl substituen
- Azami, Hidenori,Tsutsumi, Hideo,Matsuda, Keiji,Barrett, David,Hattori, Kouji,Nakajima, Takashi,Kuroda, Satoru,Kamimura, Toshiaki,Murata, Masayoshi
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p. 2069 - 2087
(2007/10/03)
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- Synthesis of new didemnin B analogs for investigations of structure/biological activity relationships
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Modifications were introduced in the side chain of didemnin B to afford several analogs (1f-1j) for biological testing in order to identify the features responsible for the bioactivity of the natural products (1a-1c). To achieve our goal, two changes were made in the proline ring of the b-turn side chain. Initially, a hydroxyl group was incorporated at the C-4 position of the ring to increase the polar nature of the molecule. Secondly, unsaturation was introduced at C-3 and C-4 to increase the rigidity of the ring and to provide a site for tritiation to follow the drug pathway in biological systems. Improvements were also introduced in the macrocycle construction to produce gram quantities of this unit (1d) for the preparation of the planned analogs. The linear precursor to the macrocycle was oxidized more effectively with 1,1,1-triacetoxy-1,1-dihydro-1,2-benziodoxol-3(1H)-one (Dess-Martin periodinane reagent), and cyclization yields were increased substantially by using a new coupling reagent, pentafluorophenyl diphenylphosphinate (FDPP). (1H-1,2,3-benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP) and pentafluorophenyl trifluoroacetate were also used to improve other coupling reactions.
- Mayer,Ramanjulu,Vera,Pfizenmayer,Joullie
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p. 5192 - 5205
(2007/10/02)
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- 3-pyrrolidinylthio-1-azabicyclo(3.2.0)-hept-2-ene-2-carboxylic acid compounds and antimicrobial activity thereof
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This invention consists of 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and their use as antimicrobial agents in the treatment of infectious diseases.
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