183549-97-5

Upstream product

• 98-80-6 phenylboronic acid 
• 544671-80-9 5-[3,5-bis(trifluoromethyl)benzyl]-7-iodo-3,4,5,6-tetrahydro-2H-pyrido[2,3-b]-1,5-oxazocin-6-one 
• 183551-09-9 N-[3,5-Bis(trifluoromethyl)benzyl]-2-chloro-N-(3-hydroxypropyl)-4-phenyl-3-pyridinecarboxamide 
• 183551-10-2 N-[3,5-bis (trifluoromethyl)-benzyl]-N-(3-hydroxypropyl)amine 
• 153034-86-7 2-chloro-4-iodopyridine 
• 183551-51-1 3,5-bis(trifluoromethyl)benzyl methanesulfonate 
• 32707-89-4 3,5-bis(trifluoromethyl)benzenemethanol 
• 544671-79-6 N-[3,5-bis(trifluoromethyl)benzyl]-2-chloro-N-(3-hydroxypropyl)-4-iodo-3-pyridinecarboxamide 
• 544671-78-5 2-chloro-4-iodo-3-pyridinecarboxylic acid 
• 78607-36-0 2-chloro-3-iodopyridine 

Downstream Products

• 544671-86-5 5-[3,5-bis(trifluoromethyl)benzyl]-10-oxo-7-phenyl-3,4,5,6-tetrahydro-2H-pyrido[2,3-b]-1,5-oxazocin-6-one 
• 544671-92-3 5-[3,5-bis(trifluoromethyl)benzyl]-9-chloro-7-phenyl-3,4,5,6-tetrahydro-2H-pyrido[2,3-b]-1,5-oxazocin-6-one 
• 544671-66-1 9-(4-aminopiperidine-1-yl)-5-[3,5-bis(trifluoromethyl)benzyl]-6-oxo-7-phenyl-2,3,4,5-tetrahydro-6H-pyrido[2,3-b][1,5]oxazocine 

Relevant academic research and scientific papers

Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9- tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists

A series of novel bicyclic pyrimidine derivatives was prepared as part of a search for NK1 antagonist aimed at the treatment of urinary incontinence. Among them, 3g, a pyrimido[4,5-b][1,5]oxazocine derivative, bearing a 4-acetylpiperazinyl grou

Convenient synthesis of 7-aryl-3,4,5,6-tetrahydro-2H-pyrido[4,5-b]- and [2,3-b]-1,5-oxazocine-6-ones

A convenient and diversity-oriented method for synthesis of the novel 7-aryl-3,4,5,6-tetrahydro-2H-pyrido[4,5-b]-1,5-oxazocine-6-one skeleton 1 and the very rarely described 7-aryl-3,4,5,6-tetrahydro-2H-pyrido[2,3-b]-1,5- oxazocine-6-one skeleton 2, featu

Amide-based atropisomers in tachykinin NK1-receptor antagonists: Synthesis and antagonistic activity of axially chiral N-benzylcarboxamide derivatives of 2,3,4,5-tetrahydro-6H-pyrido[2,3-b][1,5]oxazocin-6-one

A series of novel N-benzylcarboxamide derivatives of bicyclic compounds, 3,4-dihydropyrido[3,2-f][1,4]oxazepin-5(2H)-one and 2,3,4,5-tetrahydro-6H- pyrido[2,3-b][1,5]oxazocin-6-one, were synthesized by cyclization of N-benzyl-2-chloro-N-(2-hydroxyethyl)-

FUSED BICYCLIC PYRIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS

A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): ???wherein the rings A and B are each a benzene'r

FUSED BICYCLIC PYRIDINE DERIVATIVE AS TACHYKININ RECEPTOR ANTAGONIST

A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: ???wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to fo

PREVENTIVES/REMEDIES FOR EMOTIONAL DISORDERS

An agent for the prophylaxis or treatment of an emotional disorder, which contains the NK-1 receptor antagonist having particular properties of (1) having no serotonin uptake inhibitory effect, (2) being capable of migrating into the hypothalamus, or (3) having an inhibitory effect on micturition reflex, an agent for the prophylaxis or treatment of depression accompanied by urinary frequency, urinary incontinence and/or irritable bowel syndrome, which contains an NK-1 receptor antagonist, an agent for the prophylaxis or treatment of a mood disorder of patients with urinary frequency and urinary incontinence, and a circadian rhythm controller for the hypothalamic endocrine system are provided.

COMBINATION DRUGS

A pharmaceutical agent containing an NK-1 receptor antagonist, an NK-2 receptor antagonist and/or an anti-cholinergic drug in combination is provided, which is useful as a prophylactic or therapeutic agent of urinary frequency, urinary incontinence, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, osteoarthritis, pain, cough, irritable bowel syndrome, emesis, depression, anxiety, manic depressive psychosis or schizophrenia. More particularly, a pharmaceutical agent is provided, which contains a compound represented by the formula (I), wherein M ring is a heterocyclic ring having -N=Ca and Rb are bonded to each other to form ring A, or the same or different and each is a hydrogen atom or a substituent for ring M; ring A and ring B are each a homocyclic or heterocyclic ring optionally having substituents and at least one of them is a heterocyclic ring optionally having substituents; ring C is a homocyclic or heterocyclic ring optionally having substituents; ring Z is an optionally substituted heterocyclic ring containing nitrogen; and n is an integer of 1 to 6, or a salt thereof or a prodrug thereof, and an NK-2 receptor antagonist and/or an anti-cholinergic drug in combination.

HETEROCYCLIC COMPOUNDS, THEIR PRODUCTION AND USE

A compound represented by the formula: wherein ring M is a heterocyclic ring wherein--X=Yis one of--N=C,--CO--N or--CS--N; Ra and Rb are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, with the proviso that at least one of them is an optionally substituted heterocyclic ring; Ring C is an optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted nitrogen-containing heterocyclic ring; and n is an integer from 1 to 6, or a salt thereof has a tachykinin receptor antagonistic activity in vitro, and is useful for preventing or treating depression, anxiety, manic-depressive illness or psychopathy.

CYCLIC COMPOUNDS, THEIR PRODUCTION AND USE

Novel compounds of the following general formula or salts thereof. STR1 wherein Ring M is a heterocyclic ring having--N=C ,--CO--N or--CS--N as the partial structure--X . . . Y ; R. sup.a and R. sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.