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Synthesis and antirheumatic activity of novel tetrahydroquinoline-8-carboxylic acid derivatives

A study of the modification of N-alkylanthranilic acids to develop novel DMARDs is detailed. 1,2,3,4-Tetrahydroquinoline-8-carboxylic acid derivatives were found to exhibit a therapeutic effect on adjuvant arthritis and a suppressive effect on bone destruction.

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Reference£º
Pyridazine – Wikipedia,
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Discovery of 6-Chloropyridazine-3-carbonitrile

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Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds

[Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N866 – PubChem

 

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 35857-89-7 is helpful to your research. 35857-89-7

35857-89-7, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 35857-89-7, name is 6-Chloropyridazine-3-carbonitrile. In an article£¬Which mentioned a new discovery about 35857-89-7

Sodium Triethylborohydride-Catalyzed Controlled Reduction of Unactivated Amides to Secondary or Tertiary Amines

The first transition-metal-free catalytic protocol for controlled reduction of amide functions using cheap and bench-stable hydrosilanes as reducing agents has been established. By altering the hydrosilane and solvent, the new method enables the selective cleavage of unactivated C-O bonds in amides and allows the C-N bonds to selectively break via the deacylated cleavage. Overall, this novel process may offer a versatile alternative to current methodologies employing stoichiometric metal systems for the controlled reduction of carboxamides.

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Discovery of 35857-89-7

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 35857-89-7, molecular formula is C5H2ClN3, introducing its new discovery. 35857-89-7

TRICYCLIC COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE

A compound of the formula: wherein R1 is a 5- or 6-membered ring; Aemsp;Aemsp;Aemsp;Z1 is a 5- or 6-membered aromatic ring; Aemsp;Aemsp;Aemsp;Z2 is a group of -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; Aemsp;Aemsp;Aemsp;W is a group represented by wherein R3 and R3” are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n” are each an integer of 0 or 1 to 4; m and m” are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and Aemsp;Aemsp;Aemsp;R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atommay be converted to a quaternary ammonium or an oxide; or a salt thereof.psiThe compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.

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6′ SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY

The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I):wherein R1?R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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Alpha2C adrenoreceptor agonists

In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as alpha2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the alpha2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

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Phenylaminopropanol derivatives and methods of their use

The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.35857-89-7. In my other articles, you can also check out more blogs about 35857-89-7

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 35857-89-7, Name is 6-Chloropyridazine-3-carbonitrile, molecular formula is C5H2ClN3, 35857-89-7, In a Article, authors is Nirogi, Ramakrishna£¬once mentioned of 35857-89-7

Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: Novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists

Our initial findings around aryl sulfonamide series led to N-(3,5-dichloro-2-methoxyphenyl)-3-(1-methylpiperidin-4-ylamino)-4-methoxy benzenesulfonamide as potent and selective 5-HT6 receptor (5-HT 6R) antagonist with reasonable pharmacokinetic properties and activity in animal models of cognition. However, lack of brain penetration and P-glycoprotein liability makes this scaffold unsuitable for further development. Our goal was to identify small molecule 5-HT6R antagonist with adequate brain penetration, acceptable ADME properties, no P-glycoprotein, and no hERG liability. Several structural modifications including bringing conformational constraint around the sulfonamide -NH group and introduction of a heteroatom to modulate the physicochemical properties were attempted. This effort culminated in the discovery of series of novel, potent, selective, orally bioavailable, and adequately brain penetrant compounds with no hERG liability. These compounds showed activity in animal models of cognition like object recognition task and water maze and in brain microdialysis studies at lower doses.

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.35857-89-7,6-Chloropyridazine-3-carbonitrile,as a common compound, the synthetic route is as follows.

Step 2) 6-(4-((5-chloro-2-((2,3-dimethyl-2H-indazol-6-yl)amino)pyrimidin-4-yl)(methyl)amino)-3-ethylpiperidin-1-yl)pyridazine-3-carbonitrile To a solution of 5-chloro-N2-(2,3-dimethyl-2H-indazol-6-yl)-N4-(3-ethylpiperidin-4-yl)-N4-methylpyrimidine-2,4-diamine (134.5 mg, 0.33 mmol) in ethanol (5 mL) were added 6-chloropyridazine-3-carbonitrile (69.1 mg, 0.50 mmol) and triethanamine (0.15 mL, 1.1 mmol). The mixture was stirred at 30 C. overnight, and concentrated in vacuo. The residue was purified by preparative TLC (MeOH/DCM (v/v)=1/15) to afford the target compound as a yellow solid (87.4 mg, yield 52.0%). LC-MS (ESI, pos. ion) m/z: 517.3 [M+H]+. 1H NMR (600 MHz, CDCl3) delta (ppm): 8.05 (s, 1H), 7.99 (s, 1H), 7.48-7.42 (m, 2H), 7.05 (s, 1H), 6.91 (dd, J=8.9, 1.3 Hz, 1H), 6.88 (d, J=9.6 Hz, 1H), 4.83-4.81 (m, 1H), 4.61-4.54 (m, 2H), 4.03 (s, 3H), 3.33 (t, J=12.1 Hz, 1H), 3.04 (s, 3H), 2.84-2.76 (m, 1H), 2.57 (s, 3H), 2.17-2.14 (m, 1H), 1.85-1.77 (m, 2H), 1.63-1.59 (m, 1H), 1.16-1.09 (m, 1H), 0.95 (t, J=7.5 Hz, 3H)., 35857-89-7

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Reference£º
Patent; Sunshine Lake Pharma Co., Ltd.; Calitor Sciences, LLC; Xi, Ning; Li, Minxiong; Li, Xiaobo; Dai, Weilong; Hu, Haiyang; Zhang, Tao; Chen, Wuhong; (78 pag.)US2016/229837; (2016); A1;,
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35857-89-7, 6-Chloropyridazine-3-carbonitrile is a pyridazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 5-chloro-N2-(2,3-dimethylimidazo[1,2-a]pyridin-7-yl)-N4-(piperidin-4-yl)pyrimidine-2,4-diamine ( 87mg, 0.234mmol)And 6-chloronicotinonitrile (53 mg, 0.379 mmol)In EtOH (10mL) solutionTEA (85 mg, 0.840 mmol).The reaction system was stirred at room temperature overnight.After the reaction was completed, it was concentrated under reduced pressure.The residue was purified by silica gel column chromatography (EtOAc elut elut elut elutThe title compound was obtained as a yellow solid (60 mg, yield 54%).

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Reference£º
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jiatuo Sciences Corporation; Xi Ning; Li Minxiong; Peng Ju; Li Xiaobo; Zhang Tao; Hu Haiyang; Chen Wuhong; Bai Changlin; Ke Donghua; Chen Peng; (217 pag.)CN109776522; (2019); A;,
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