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INHIBITORS OF HIF PROLYL HYDROXYLASE

The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N835 – PubChem

 

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Intramolecular vinylation of carbanions using N-acyl benzomorpholines as masked vinylureas and vinylcarbamates

Treatment of urea or carbamate derived benzomorpholines with lithium diisopropylamide generates N-vinyl ureas or N-vinyl carbamates by elimination of a phenoxide anion, cleaving the benzomorpholine ring. Simultaneous formation of a carbanion alpha to a stabilising aryl or nitrile group allows migration of the newly formed N-vinyl substituent to the carbanionic centre, in some cases with high enantiospecificity. Mild hydrolysis of the resulting urea or carbamate returns a C-vinylated amine, alcohol or hydantoin, in some cases with high enantiomeric purity. This ?masked? vinylation strategy avoids the need to use the reactive and volatile vinyl isocyanate as a starting material.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N912 – PubChem

 

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Catalytic selective oxyamidation of cyclic enamides using nitrenes

Yes, nitrenes did “N,O”! Intermolecular addition of nitrene to enecarbamates and enesulfonamides gives oxyamidated products in excellent yields of up to 98% and with good levels of stereoselectivity. Complete regioselectivity is also observed, leading to the formation of N,O-acetals which can further react with various nucleophiles under acidic conditions (see scheme; TcesNH2=trichloroethylsulfamate). Copyright

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Pyridazine – Wikipedia,
Pyridazine | C4H4N926 – PubChem

 

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A brief review of drug discovery research for Human African Trypanosomiasis

Human African Trypanosomiasis (HAT), a neglected disease endemic in Sub-Saharan Africa, is usually fatal if left untreated. It is caused by the parasite Trypanosoma brucei, and is spread by the tsetse fly. The drugs currently available to treat HAT are few, and limited in efficacy. Furthermore, resistance towards these drugs is beginning to grow. In the last 25 years, only one advance has been made into HAT treatment and consequently, there is an increasing need for new drugs to be sought that are able to effectively treat this disease. This review provides a brief overview of drug discovery research for HAT, focusing on research published in the last four years, identifying new molecules with the potential to be developed into anti-HAT agents. The methods of drug discovery have been grouped into three key areas; new molecules inspired by known antitrypanosomal agents, target-based screening, and phenotypic screening.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N913 – PubChem

 

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FUSED TETRACYCLIC PYRIDO[4,3-B]INDOLE AND PYRIDO[3,4-B]ONDOLE DERIVATIVES AND METHODS OF USE

This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4- b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N838 – PubChem

 

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REACTIVE CYANINE COMPOUNDS

The invention provides compounds and compositions of Formulas I-VII, and methods of using the compounds. The compounds can be used to prepare dye conjugates that are uniformly and substantially more fluorescent on proteins, nucleic acids or other biopolymers, than conjugates labeled with structurally similar known carbocyanine dyes. In addition to having more intense fluorescence emission than structurally similar dyes at virtually identical wavelengths, and decreased artifacts in their absorption spectra upon conjugation to biopolymers, the compounds can have greater photostability and/or higher absorbance (extinction coefficients) at the wavelength(s) of peak absorbance than such structurally similar dyes.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N849 – PubChem

 

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Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors

Herein we report the design and synthesis of a series of novel bicyclic DGAT1 inhibitors with a carboxylic acid moiety. The optimization of the initial lead compound 7 based on in vitro and in vivo activity led to the discovery of potent indoline and quinoline classes of DGAT1 inhibitors. The structure-activity relationship studies of these novel series of bicyclic carboxylic acid derivatives as DGAT1 inhibitors are described.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1002 – PubChem

 

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An efficient method for the N-formylation of amines under catalyst- and additive-free conditions

A simple catalyst- and additive-free method for the N-formylation of amines has been developed. The advantages of this protocol include a wide range of functional group tolerance, high efficiency and a lack of required extra promoters under mild conditions. This convenient strategy will provide a facile synthesis towards N-formamide natural products and pharmaceutical derivatives. A mechanism that involves difluorocarbene is proposed for this reaction.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N986 – PubChem

 

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Benzimidazole derivatives and their pharmaceutical use (by machine translation)

The invention discloses a benzimidazole derivative and its pharmaceutical use, and particularly discloses a formula I shown in the benzimidazole derivatives and their use in the preparation of the treatment and/or prevention of thrombotic or thromboembolic disease in use. (by machine translation)

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Pyridazine – Wikipedia,
Pyridazine | C4H4N861 – PubChem

 

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Synthesis, Pharmacological Activities and Physico-chemical Properties of 4-(Substituted amino/N4-arylpiperazinyl/aminocarbonyl)-2, 3-polymethylenequinolines

A series of N-substituted-aminoacridines (27-29) and 4-(substituted amino, N4-arylpiperazinyl and aminocarbonyl)-2,3-polymethylenequinolines (30-103) have been synthesized and tested for their CNS effects.Compounds with significant activity have been identified, which include 4-(n-butylamino)-2,3-tetramethylene quinoline (35, centbucridine) and 4-(n-heptylamino)-2,3-tetramethylenequinoline (40) as local anesthetics, 4-(n-butylamino)-2,3-pentamethylenequinoline (61) as antihistaminic and 4-(N4-phenylpiperazinyl)-2,3-pentamethylenequinoline (76) as analeptic.Witha view to determining relationship between the physico-chemical properties and biological activities of these molecules, pKa, lipophilicity and DNA binding of a few selected compounds of each type have been studied.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N902 – PubChem