29421-99-6Relevant academic research and scientific papers
2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
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Paragraph 00162; 00224, (2021/06/26)
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
PKB inhibitor
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Paragraph 0119; 0120; 0121; 0122, (2021/03/13)
The invention provides a PKB inhibitor, particularly relates to a compound shown as a formula I or a pharmaceutically acceptable salt thereof. The invention further provides a preparation method of the compound.
IMIDAZO [1,5-A]PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00768, (2017/11/04)
The invention provides substituted imidazo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-imidazo[1,5-a]pyrirnidine-8-carboxamide compounds and variants thereof.
Direct bromination of ethyl 5-alkylthiophene-2-carboxylates
Taydakov, Ilya V.,Krasnoselskiy, Sergey S.
scheme or table, p. 2965 - 2968 (2010/10/19)
Approaches to brominated thiophene-2-carboxylic acids by electrophilic bromination of the corresponding acids and esters were compared and investigated. A synthetic route was developed involving direct bromination of ethyl 5-alkylthiophene-2-carboxylates followed by saponification of the resulting ethyl 5-alkyl-4-bromothiophene-2-carboxylates. The key bromination step is selective in dichloromethane solution at 0-5 °C and furnishes the corresponding ethyl 5-alkyl-4-bromothiophene-2-carboxylates in excellent yields. No migration or isomerization of the alkyl substituents was observed. Georg Thieme Verlag Stuttgart New York.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 36-37, (2010/09/03)
Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
INTEGRASE INHIBITORS 3
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Page/Page column 57, (2008/06/13)
The present invention provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.
Design and Synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors
Rudolph,Illig, Carl R.,Subasinghe, Nalin L.,Wilson, Kenneth J.,Hoffman, James B.,Randle, Troy,Green, David,Molloy, Chris J.,Soll, Richard M.,Lewandowski, Frank,Zhang, Marie,Bone, Roger,Spurlino, John C.,Deckman, Ingrid C.,Manthey, Carl,Sharp, Celia,Maguire, Diane,Grasberger, Bruce L.,DesJarlais, Renee L.,Zhou, Zhao
, p. 491 - 495 (2007/10/03)
A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of a variety of substituents at the thiophene 5-position. The 5-alkyl substituted and unsubstituted thiophenes were prepared using organolithium chemistry. Heteroatom substituents were introduced at the 5-position using a novel displacement reaction of 5-methylsulfonylthiophenes and the corresponding oxygen or sulfur anions. Small alkyl group substitution at the 5-position provided inhibitors equipotent with 3 but possessing improved solubility.
Compounds and compositons for treating C1s-mediated diseases and conditions
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, (2008/06/13)
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
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, (2008/06/13)
The present invention is directed to compounds of Formula I: wherein X is O, S or NR7and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
