31366-49-1

Upstream product

• 20143-58-2 (3-methyl-2-nitro-phenoxy)-acetic acid 
• 2835-97-4 2-amino-3-methylphenol 
• 79-04-9 chloroacetyl chloride 
• 1154696-12-4 C₁₀H₁₁NO₅ 
• 888731-57-5 2-chloro-N-(2-hydroxy-6-methylphenyl)-acetamide 
• 4920-77-8 3-methyl-2-nitrophenol 

Downstream Products

• 141068-94-2 6-amino-5-methyl-4H-benzo[1,4]oxazin-3-one 
• 179863-45-7 8-Amino-5-methyl-4H-benzo[1,4]oxazin-3-one 
• 888731-58-6 5-methyl-3,4-dihydro-2H-benzo[1,4]oxazine 
• 1221503-81-6 6-{1-[3-(benzyloxy)-2,2-difluoropropyl]-5-(4-fluorophenyl)-3-methyl-1H-pyrazol-4-yl}-5-methyl-2H-1,4-benzoxazin-3(4H)-one 
• 1221501-59-2 6-[1-(2,2-Difluoro-3-hydroxypropyl)-5-(4-fluorophenyl)-3-methyl-1H-pyrazol-4-yl]-5-methyl-2H-1,4-benzoxazin-3(4H)-one 
• 1221501-60-5 6-[1-(2,2-Difluoropropyl)-5-(4-fluorophenyl)-3-methyl-1H-pyrazol-4-yl]-5-methyl-2H-1,4-benzoxazin-3(4H)-one 
• 1221500-34-0 6-[5-(4-Fluorophenyl)-1,3-dimethyl-1H-pyrazol-4-yl]-5-methyl-2H-1,4-benzoxazin-3(4H)-one 

Relevant academic research and scientific papers

A simple and facile route for the synthesis of 2H-1,4-benzoxazin-3-(4H)- ones via reductive cyclization of 2-(2-nitrophenoxy)acetonitrile adducts in the presence of Fe/acetic acid

A simple route for the synthesis of 1,4-benzoxazin-3-(4H)-ones is described herein. This method involves the reductive cyclization of 2-(2-nitrophenoxy) acetonitrile adducts in the presence of Fe/acetic acid in good to excellent yields. This system was compatible with various other functional groups.

PYRAZOLE COMPOUNDS

The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineralocorticoid receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of a disease or condition mediated by the mineralocorticoid receptor activation.

Production Method of Nitrogen-Containing Fused Ring Compounds

[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.

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.

Nitrogen-containing fused ring compounds and use thereof

A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]: wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.

Imidiazoles having reduced side effects

Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.

Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors

Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.

NOVEL METHODS AND COMPOSITIONS FOR ALLEVIATING PAIN

The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic α-adrenergic receptor in the absence of α-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic α-adrenergic receptor can be, for example, the α-2B receptor.

Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B / 2C adrenergic receptors

Compounds having adrenergic activity which are a selective agonists for one or both of the α2B and α2c adrenoceptor receptor subtypes in preference to the α2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having the formula 1wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, but R1 is absent when the bond between X and the ring represented by 2is a double bond; Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, —CH=CH— or —Y1CH2—, wherein Y1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R2, R3 or R4 is bound to an unsaturated carbon atom and x is 2 when R2, R3 or R4 is bonded to a saturated carbon atom; R2 is H, lower alkyl, halogen, hydroxy, lower alkoxy, lower alkenyl, acyl or lower alkynyl, or, when attached to a saturated carbon atom, R2 may be oxo; R3 and R4 are, each, H, lower alkyl, halogen, lower alkenyl, acyl, lower alkynyl, aryl, heteroaryl, or sub stituted aryl or heteroaryl, wherein said substituent is halogen, lower alkyl, lower alkoxy, lower alkenyl, acyl, lower alkynyl, nitro, cyano, trifluoromethyl, hydroxy, or phenyl or, together, are —(C(R2)x)z—; —Y1(C(R2)x)z′—; —Y1(C(R2)x)y Y1—; —(C(R2)x)—Y1—(C(R2)x)—; —(C(R2)x)—Y1—(C(R2)x)—(C(R2)x)— and —Y1—(C(R2)x)—Y1—(C(R2)x)— wherein z is an integer of from 3 to 5, z′ is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects.

Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6- yl)imino]imidazoline, a potent, peripherally acting α2 adrenoceptor agonist

We have synthesized 2-[(5-methylbenz-1-ox-4-azin-6- yl)imino]imidazoline, 3, a potent, peripherally acting α2 adrenoceptor agonist. The agent is conveniently prepared in five steps from 2-amino-m- cresol. The agent has demonstrated good selectivity for α2 adrenoceptors in binding and functional studies. When applied topically to eyes, the agent is efficacious for the reduction of intraocular pressure. The agent does not penetrate the blood-brain barrier and, as a consequence, does not lower blood pressure or induce sedation when administered topically or intravenously. We have determined the pK(a) and log P in water versus both octanol and dodecane of 3 and a set of related agents. The best physical parameter to explain its lack of central nervous system penetration appears to be log P measured in octanol versus water.