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NOVEL PHENYL AMIDE OR PYRIDYL AMIDE DERIVATIVES

This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N832 – PubChem

 

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The N-formylation of secondary amines and anilines using ammonium formate as a formylating agent is described. (C) 2000 Elsevier Science Ltd.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N924 – PubChem

 

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The syntheses of the thieno[2,3-b][1,4]thiazine derivatives 8 and 9 are described. Reaction of compound 4 with different acyl halides followed by substitution with various ethanamines gave the products 8 and 9. The new 3,4- dihydro-2H-1,4-benzoxazine derivatives 14, 16, 18 and 3,4-dihydro-2H-1,4- benzothiazine derivatives 15 and 17 with an urea moiety have been synthesized. Substitution of 10 respectively 11 with 4-nitrophenyl chloroformate gave the required reactivity for substitution with diamines. Structural modifications of the amino side chain were carried out.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N970 – PubChem

 

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This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N829 – PubChem

 

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FUEL ADDITIVES

An additive composition for use in a fuel for a spark-ignition internal combustion engine comprises an octane-boosting additive and one or more further fuel additives. The octane-boosting additive has a chemical structure comprising a 6-membered aromatic ring sharing two adjacent aromatic carbon atoms with a 6- or 7-membered saturated heterocyclic ring, the 6- or 7-membered saturated heterocyclic ring comprising a nitrogen atom directly bonded to one of the shared carbon atoms to form a secondary amine and an atom selected from oxygen or nitrogen directly bonded to the other shared carbon atom, the remaining atoms in the 6- or 7-membered heterocyclic ring being carbon. The additive composition increases the octane number of the fuel, thereby improving the auto-ignition characteristics of a fuel.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N824 – PubChem

 

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Dirhodium-catalyzed C-H arene amination using hydroxylamines

Primary and N-alkyl arylamine motifs are key functional groups in pharmaceuticals, agrochemicals, and functional materials, as well as in bioactive natural products. However, there is a dearth of generally applicablemethods for the direct replacement of aryl hydrogens with NH2/NH(alkyl) moieties. Here, we present a mild dirhodium-catalyzed C-H amination for conversion of structurally diverse monocyclic and fused aromatics to the corresponding primary and N-alkyl arylamines using NH2/NH(alkyl)-O-(sulfonyl)hydroxylamines as aminating agents; the relatively weak RSO2O-N bond functions as an internal oxidant. The methodology is operationally simple, scalable, and fast at or below ambient temperature, furnishing arylamines in moderate-to-good yields and with good regioselectivity. It can be readily extended to the synthesis of fused N-heterocycles.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N962 – PubChem

 

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CHROMANES AND THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS

Racemic Compounds of the formula I and their enantiomer and salts thereof are described. The compounds of formula I exhibit activity as inhibitors of 5-lipoxygenase and inhibit lipid peroxidation. They are, therefore, useful in the treatment of diseases caused or aggravated by excess oxidative metabolism of arachidonic acid via the 5-lipoxygenase pathway and in the treatment of inflammation, arthritis, allergies, asthma and psoriasis. The compounds of formula I can also be used to prevent peroxidation of lipids and thus protect lipid membranes from oxidative stress

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Pyridazine – Wikipedia,
Pyridazine | C4H4N894 – PubChem

 

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ETHER COMPOUNDS AND USES THEREOF

The present invention provides compounds that modulate protein function, to restore protein homeostasis and/or cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions of these compounds are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions are also provided.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N893 – PubChem

 

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Cobalt-Catalyzed Selective Functionalization of Aniline Derivatives with Hexafluoroisopropanol

A cobalt-catalyzed site-selective functionalization of aniline derivatives with hexafluoroisopropanol, which enables the synthesis of a wide array of fluoroalkylated anilines, a class of highly valuable building blocks for further preparation of fluorinated functional products, is reported. The developed transformation proceeds with operational simplicity, use of earth-abundant metal catalyst, broad substrate scope, good functional group tolerance, and mild reaction conditions.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1001 – PubChem

 

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One-pot synthesis of trifluoromethyl amines and perfluoroalkyl amines with CF3SO2Na and RfSO2Na

A newly developed CF3SO2Na-based trifluoromethylation of secondary amines has been disclosed, and the method has been successfully extended to the configuration of perfluoroalkyl amines using RfSO2Na, complementing the established synthesis strategy of trifluoromethyl amines. Advantages of the method include good functional group tolerance, mild conditions, and inexpensive or easy-to-handle materials. Mechanistic probes indicate that the thiocarbonyl fluoride formed in situ is the key intermediate in the reaction.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N943 – PubChem