8013-43-2

Downstream Products

• 139679-40-6 N-Butyl-N'-[1-[4-(1H-imidazol-1-yl)benzoyl]-4-piperidinyl]N'-methylurea methanesulfonic acid salt 
• 139679-38-2 4-(1-Hydroxyhexyl)-1-[4-(1H-imidazol-1-yl)benzoyl]piperidine, methanesulfonic acid salt 
• 101477-54-7 KB-2796 dihydrochloride 
• 84231-36-7 6-Chloro-3{1-[4,4-bis(4-fluorophenyl)-1-butyl]-4-piperidyl}-1,2-benzisoxazole hydrochloride 
• 84162-97-0 1-acetyl-4-(5-fluoro-2-hydroxybenzoyl)piperidine oxime 
• 71064-21-6 1-amino-3-furfurylguanidine hydriodide 
• 61608-75-1 3-(N-benzyl-N-methylamino)-1,1-diphenyl-propan-2-one 
• 167621-46-7 4-[N-methyl-N-(2-phenylethyl)amino]-1-[3-(2-oxo-1-piperidin-yl)benzoyl]piperidine hydrochloride 

Relevant academic research and scientific papers

Thermogenic composition and benzazepine thermogenics

The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.

Thienopyridine compounds, their production and use

The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.

Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials

This invention relates to a N1 -(halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by the following formula (I): STR1 wherein X1 is a halogen atom or a hydrogen atom; X2 is a halogen atom; R1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R2 is a group represented by the following formula (II): STR2 wherein R3 and R4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): STR3 wherein X3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidynyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.

Benzazepine derivative, pharmaceutical composition thereof, and intermediate thereof

Benzazepine derivatives represented by the following general formula (I) useful as arginine vasopressin antagonists or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and difluorobenzazepinone derivatives represented by the following general formulae (II) and (III) which are useful as production intermediates of the compound (I). STR1

NOVEL CARBAMATE DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THE SAME

Carbamate derivatives represented by the general formula (I), salts thereof, hydrates thereof or solvates thereof wherein each symbol has the following meaning: A ring: a benzene ring or a pyridine ring,B ring: a nitrogen-containing saturated hetero-ring which may have a substituent on the nitrogen atom and which may have a cross-linking,R1: a phenyl group which may have a substituent, a cycloalkyl or cycloalkenyl group having 3 to 8 carbon atoms or a five-or six-membered nitrogen-containing heterocyclic group,X: a single bond or a methylene group,Y: a single bond, a carbonyl group, a methylene group which may be substituted with a hydroxyl group or a group represented by the formula-S(O)?-, and?: an integer of 0, 1 or 2.They have muscarinic M3 receptor antagonism and are useful as an agent for the prevention and treatment of gastrointestinal diseases, respiratory diseases or urinary diseases.

Azole-fused peptides and processes for preparation thereof

Azole-fused peptides useful as Substance P antagonists and analgesics, for example STR1 wherein STR2 represents STR3 wherein X is O, S or NH and * is D, or as intermediates therefor are prepared by azole and peptide forming methods.

PHARMACEUTICAL COMPOUNDS

Compounds of the formula: STR1 in which each R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R 2 is hydrogen, C 1-4 alkyl or C 2-4 alkenyl, R. sup.3 and R. sup.4 are each hydrogen, C 1-4 alkyl, optionally substituted phenyl or C. sub.6-9 cycloalkyl optionally substituted by 1 to 4 C 1-4 alkyl groups, R 5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C 6-10 cycloalkyl optionally substituted with 1 to 4 C. sub.1-4 alkyl groups or a phenyl group, or C. sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.

3-hydroxy-pyridin-4-ones useful for treating parasitic infections

3-Hydroxypyridin-4-ones of formula (I) STR1 in which R1 is a C3 or C4 hydroxyalkyl group in which the hydroxy group is terminally substituted on the alkyl group, R2 is methyl or ethyl and R3 and R4 are each separately hydrogen, methyl or ethyl but with the proviso that the total number of carbon atoms in R1 to R4 is no more than six, the compound optionally being in the form of a physiologically acceptable salt and/or pro-drug thereof, are of value for the treatment of conditions caused by iron dependent parasites, particularly malaria.

1,9-ALKANO-BRIDGED-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINES

1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: STR1 wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R 1, R 2 and R 3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.

SUBSTITUTED 6H-7,8-DIHYDROTHIAPYRANO(3,2-D)-PYRIMIDINES AS HYPOGLYCEMIC AGENTS

There are disclosed certain 2-substituted-4-substituted 6H-7,8-dihydrothiapyrano[3,2-d]pyrimidines which have oral hypoglycemic activity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed. The compounds are also β-adrenergic blocking agonists or . alpha.-adrenergic blocking agents and act as ocular antihypertensives and are useful for the treatment of glaucoma and other eye disorders.