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A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body’s production of cyclic guanosine monophosphate (” cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

More research is needed about 4-Iodoisoxazole

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Non-steroidal anti-inflammatory drugs are widely used therapeutic agents in the treatment of inflammation, pain and fever. Cyclooxygenase catalyzes the initial step of biotransformation of arachidonic acid to prostanoids, and exist as three distinct isozymes; COX-I, COX-II and COX-III. Selective COX-II inhibitors are a class of potential anti-inflammatory, analgesic, and antipyretic drugs with reduced gastrointestinal (GI) side effects compared to nonselective inhibitors. 3,4-Diarylisoxazole scaffold is recurrently found in a wide variety of NSAIDs, protein kinase inhibitors, hypertensive agents, and estrogen receptor (ER) modulators. In the present review, we document on the recent synthetic strategies of 3,4-diarylisoxazolyl scaffolds of valdecoxib and its relevant structural analogues.

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The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same

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Isoxazole – Wikipedia,
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A direct functionalization of unsubstituted isoxazole (1) was achieved by generation of 4-isoxazolyl anion species (3). An efficient 4-iodination of isoxazole and halogen?metal exchange reaction using a turbo Grignard reagent (iPrMgCl? LiCl) were essential for the generation of 3, which reacted with various electrophiles to give 4-functionalized isoxazoles in good to high yields. Isoxazolyl boronate, boronic acid, and stannane were also synthesized as useful building blocks from 1. The current methods enabled us to synthesize multi-functionalized isoxazoles by introducing each substituent into the desired positions. Furthermore, total synthesis of triumferol, which was isolated from Triumfetta rhomboidea, was achieved from 1 in only three steps.

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Transition metals in organic synthesis: Highlights for the year 2001

A review with 1663 references to transition-metal catalyzed or mediated reactions and functional group preparations.

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DABCO-Mediated [4+1] Cycloaddition of beta,beta-Dihalo Peroxides with Sodium Azide toward Isoxazoles

The isoxazole skeleton is one of key structural motifs, which displays widespread applications in drugs, agriculture, and synthetic intermediates. Herein, we disclose the DABCO-mediated [4+1] cycloaddition of beta,beta-dihalo peroxides and sodium azide for synthesis of multisubstituted isoxazoles. The cycloaddition proceeds through the formation of N?C and N?O bonds. This method shows excellent regioselectivity and good scalability.

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SELECTIVE ESTROGEN RECEPTOR DOWNREGULATORS AND USES THEREOF

The invention relates to novel tetrahydroisoquinoline compounds that are selective estrogen receptor downregulators (SERDs). The present invention also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and to the use of the compounds in the treatment of estrogen receptor (ER) mediated or dependent diseases or conditions, for example cancer such as breast cancer.

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Isoxazole – Wikipedia,
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Microwave-Assisted Metal-Free Decarboxylative Iodination/Bromination of Isoxazole-4-carboxylic Acids

A microwave-assisted metal-free route to substituted 4-haloisoxazoles via decarboxylative halogenation of substituted isoxazole-4-carboxylic acids using N-iodosuccinimide (NIS) and N-bromosuccinimide (NBS) in the presence of K3PO4 is described. It was discovered that the substitutions present at the 3-position of differently 3,5-disubstituted isoxazoles influenced the outcome of the protocol. The methodology is compatible for performing decarboxylative halogenation followed by decarboxylative Suzuki-Miyaura and Sonogashira couplings as one-pot process.

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Isoxazole – Wikipedia,
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[00460] Step 2: Synthesis of 3-(isoxazol-4-yl)benzaldehyde: To a mixture of 4- iodoisoxazole (1 g, 5.13 mmol), 3-formylphenylboric acid (923 mg, 6.15 mmol) and sodium carbonate in DME/H20/Toluene/EtOH (15 mL, 3/1/10/6, V/V) was added Pd(PPh3)4 (200 mg). The mixture was purged with N2 for 30 min and heated to 80 C for 3 h. The reaction mixture was cooled followed by a standard aqueous/EtOAc workup and purified by prep- TLC (EA : PE = 1 : 5) to give Intermediate 46 (12 mg, 1.5%).

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Reference£º
Patent; N30 PHARMACEUTICALS, LLC; SUN, Xicheng; QIU, Jian; WO2011/38204; (2011); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

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Isopropyl magnesium chloride lithium chloride complex (2.62 ml, 3.41 mmol) was addeddropwise to 4-iodoisoxazole (0.609 g, 3.12 mmol) in THF (10 mL) at 0C and the mixture wasstirred for 1 h, during which time the temperature rose to 18C. A solution of methyl 3,3- dicyano-2-cyclopropylacrylate (see Step A of 1-19) (0.5 g, 2.84 mmol) in THF (3 mL) was added at 0C. The resulting mixture was allowed to rise to RT slowly and stirred for 4 h, then was quenched with ice-cold saturated aq. NH4C1 and extracted with EtOAc. The organic layer wasdried with Mg504, filtered, and concentrated in vacuo. Purification by silica gel column chromatography using a hexanes/EtOAc gradient (0-1 00%EtOAc/Hexane) afforded the title product. 1H NMR (500 MHz, CDC13): oe 8.74 (1H, s), 8.53 (1H, s), 4.59 (1H, s), 3.89 (3H, s),1.08 (1H, m), 0.91(2H, m), 0.61 (1H, m), 0.52 (1H, m), m/z=246.13 (M+1).

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Reference£º
Patent; MERCK SHARP & DOHME CORP.; HAN, Xiaoqing; WHITEHEAD, Alan; RAGHAVAN, Subharekha; GROEPER, Jonathan; GUO, Jian; ZHANG, Yong; WO2015/88885; (2015); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem