80253-36-7

Upstream product

• 2843-19-8 3-amino-2,2-dimethylpropanoic acid, hydrochloride salt 
• 501-53-1 benzyl chloroformate 
• 19036-43-2 aminopivalic acid 
• 26734-09-8 3-amino-2,2-dimethylpropan-1-ol 
• 666844-60-6 benzyl (3-hydroxy-2,2-dimethylpropyl)carbamate 
• 259794-51-9 methyl 2,2-dimethyl-3-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)propanoate 
• 14002-80-3 Methyl 2,2-dimethyl-3-hydroxypropionate 

Downstream Products

• 666844-61-7 (2-carbamoyl-2-methylpropyl)carbamic acid benzyl ester 
• 1201096-13-0 C₂₃H₃₅NO₆ 
• 80253-41-4 β-benzyloxycarbonylaminopivaloyl-β-aminopivaloyl-β-aminopivalic acid 
• 80253-44-7 β-benzyloxycarbonylaminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivalic acid ethyl ester 
• 80253-45-8 β-benzyloxycarbonylaminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivaloyl-β-aminopivalic acid 
• 80253-40-3 β-benzyloxycarbonylaminopivaloyl-β-aminopivaloyl-β-aminopivalic acid ethyl ester 
• 80253-39-0 β-benzyloxycarbonylaminopivaloyl-β-aminopivalic acid 
• 259794-60-0 (+/-)-methyl 2-[({[2-(tert-butoxycarbonyl)-2,2-dimethylethyl]amino}sulfonyl)amino]-4-phenylbutanoate 
• 259794-64-4 (+/-)-tert-butyl 2,2-dimethyl-3-[4-(2-phenylethyl)-1,1,3-trioxo-1λ⁶,2,5-thiadiazolan-2-yl]propanoate 
• 259794-53-1 3-amino-2,2-dimethylpropionic acid tert-butyl ester 
• 259794-52-0 tert-butyl 3-{[(benzyloxy)carbonyl]amino}-2,2-dimethylpropanoate 

Relevant academic research and scientific papers

SGC STIMULATORS

Compounds of Formulae (I') and (I) are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

CYCLIC AMINE COMPOUND

The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, -(CH2)a-X1-(CH2)b- (X1: the formula -NH-, -O- or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].

PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF

The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents -RB, -CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.,; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity, and a disease associated with the increase of blood galactose level such as galactosemia, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

Synthesis of 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives and evaluation of their affinity for MHC class-II proteins

1,2,5-Thiadiazolidin-3-one 1,1-dioxide derivatives (±)-1a-d and (±)-2 were designed by molecular modeling as MHC (major histocompatibility complex) class-II inhibitors. They were prepared from the unsymmetrically N,N'- disubstituted acyclic sulfamides (±)

Benzo-fused lactams that promote the release of growth hormone

There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Peptidylaminodiols

A renin inhibiting compound of the formula: STR1 wherein A is a substituent; W is C=O or CHOH; U is CH2 or NR2, provided that when W is CHOH then U is CH2 ; R1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R4 is loweralkyl, cycloalkylmethyl or benzyl; R5 is vinyl, formyl, hydroxymethyl or hydrogen; R7 is hydrogen or loweralkyl; R8 and R9 are independently selected from OH and NH2 ; and R6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R5 and R7 are both hydrogen and R8 and R9 are OH, the carbon bearing R5 is of the "R" configuration and the carbon bearing R6 is of the "S" configuration, or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

RENIN INHIBITING COMPOUNDS

The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; Or 10 wherein R 10 is hydrogen or loweralkyl; NR 11 R 12 wherein R. sub.11 and R 12 are independently selected from hydrogen and loweralkyl; or R 13--CO--B wherein B is NH, O, CH 2, HNCH 2 and R 13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H, H; or when taken together as O represents a carbonyl with the provisos that if U,V=H, OH, then W=CH, and if U,V=O then W=N; R 1 , R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2, R 4, R 7, R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO, SO 2, or CH 2 ; and R 6 is loweralkyl cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R 6 may be an N-protecting group when X is NH.

Angiotensinogen analogs

The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; OR10 or SR10 wherein R10 is hydrogen, loweralkyl or aminoalkyl; NR11 R12 wherein R11 and R12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; STR2 wherein B is NH, alkylamino, S, O, CH2 or CHOH and R13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH2 or NR2 with the proviso that when W is CHOH then U is CH2 ; R1 is loweralkyl, cycloaklylmethyl, benzyl, α,α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)-methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R1 is phenoxy, thiophenoxy or anilino, B is CH2 or CHOH or A is hydrogen, R3 is loweralkyl, vinylloweralkyl, benzyl or heterocyclic ring substituted methyl, R5 is loweralkyl, cycloalkylmethyl or benzyl; R2 and R4 are independently selected from hydrogen and loweralkyl; R6 is CHOH or CO; R7 is CH2, CF2 or CF with the proviso that when R6 is CO, R7 is CF2 ; R8 is CH2, CHR14 wherein R14 is lower-alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or R7 and R8 taken together can be STR3 with the proviso that when R7 is CF2, R8 is CH2 ; E is O, S, SO, SO2, NR15 wherein R15 is hydrogen or loweralkyl or NR16 CO wherein R16 is hydrogen or loweralkyl; R9 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protected group, or E and R9 taken together can be N3, with the proviso that when E is NH, R9 is an N-protecting group; and pharmaceutically acceptable salts thereof.

Synthesis of β-Amino-acid Peptides. Part 2. Preparation of Peptides of 2-Amino-2,2-dimethylpropionic Acid by Means of Conventional Coupling Reagents and with Oxazin-6-one Derivatives

Side reactions were encountered during the coupling of 3-amino-2,2-dimethylpropionic acid (β-Api) derivatives, some of which could be directly ascribed to steric hindrance at the carboxy-group.Protected and deprotected tri- and hexa-peptides were prepared