52117-00-7

Upstream product

• 28188-41-2 m-(bromomethyl)benzonitrile 
• 1068-90-2 2-acetylaminomalonic acid diethyl ester 

Downstream Products

• 80852-49-9 3-(3-Cyano-phenyl)-2-(toluene-4-sulfonylamino)-propionyl chloride 
• 80852-50-2 3-(3-Cyano-phenyl)-2-(naphthalene-1-sulfonylamino)-propionyl chloride 
• 80852-52-4 N^α-(2-naphthylsulfonyl)-3-cyano-DL-phenylalanyl chloride 
• 80852-55-7 N-[1-(3-Cyano-benzyl)-2-oxo-2-pyrrolidin-1-yl-ethyl]-4-methyl-benzenesulfonamide 
• 84792-43-8 N_α-(Tosylglycyl)-3-cyanphenylalanin 
• 80852-62-6 N-Butyl-3-(3-cyano-phenyl)-2-(toluene-4-sulfonylamino)-propionamide 
• 80852-93-3 3-[3-Oxo-3-pyrrolidin-1-yl-2-(toluene-4-sulfonylamino)-propyl]-thiobenzamide 
• 80852-53-5 N-[1-(3-Cyano-benzyl)-2-oxo-2-piperidin-1-yl-ethyl]-4-methyl-benzenesulfonamide 
• 92740-40-4 N_α-(Tosylglycyl)-3-amidinophenylalanin 
• 80852-99-9 N-Butyl-3-(3-thiocarbamoyl-phenyl)-2-(toluene-4-sulfonylamino)-propionamide 
• 109062-58-0 3-(3-Thiocarbamoyl-phenyl)-2-[2-(toluene-4-sulfonylamino)-acetylamino]-propionic acid 
• 80852-57-9 N-[1-(3-Cyano-benzyl)-2-morpholin-4-yl-2-oxo-ethyl]-4-methyl-benzenesulfonamide 
• 80852-83-1 Naphthalene-2-sulfonic acid [1-(3-cyano-benzyl)-2-oxo-2-pyrrolidin-1-yl-ethyl]-amide 
• 80852-91-1 3-[3-Oxo-3-piperidin-1-yl-2-(toluene-4-sulfonylamino)-propyl]-thiobenzamide 

Relevant academic research and scientific papers

AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND PROCESSES FOR PREPARING THEM

The invention relates to new amino acid derivatives of general formula (I), wherein B, T, Z, Y, V and n are defined as in claim 1, the tautomers, diastereomers and enantiomers thereof, the mixtures thereof and the salts thereof, particularly their physiologically acceptable salts with inorganic or organic acids or bases which have valuable pharmacological properties, particularly selective NPY-antagonist properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.

Aromatic heterocyclic derivatives as enzyme inhibitors

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Use of 2-aminothiazoline derivatives as inhibitors of inducible no-synthase

The present invention relates to the use of 2-aminothiazoline derivatives of formula: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S

Inhibitors of urokinase and blood vessel formation

Novel compounds having activity inhibitors of urokinase and in reducing or inhibiting blood vessel formation are provided. These compounds have an arginine or arginine mimic aldehyde or an arginine ketoamide group at P1. These compounds are useful in vitr

Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases

There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9; or is a member selected from the group consisting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)r-A2-, where A1 and A2 are each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9; B is a member independently selected from the group consisting of the following: E is a single bond; —O—; —NR10—; —CH═CH—; —CC—; —S(═)q; —CR11R12NR10—; or —CR11R12; X is —O—; —C(═O)—; —S(═O)q—; or —NR10—; X1, X2 and X3 are each independently selected from the group consisting of CH, CR9 or N; Y is a single bond; —C(═O)—; —C(═S)—; or —S(═O)2—; R7 is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(═O)R5; (CH2)kNR6C(═O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with 0 to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R9; or R7 may be taken together with R8 to form a cycloalkyl or heterocyclyl ring; or R7 may be taken together with R11 to form a cycloalkyl or heterocyclyl ring; and R8 is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy.

Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors

The present invention provides peptide aldehydes having a 3-amino-2-hydroxyphyenyl-acetamide group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having inhibitory activity toward proteases of the trypsin/chymotrypsin class.

Aromatic heterocyclic derivatives as enzyme inhibitors

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

ARGININE MIMIC DERIVATIVES AS ENZYME INHIBITORS

The present invention provides peptide aldehydes having an azetidinyl, prolyl or pipecolyl group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibi

3-AMINO-2-OXO-1-PIPERIDINEACETIC DERIVATIVES CONTAINING AN ARGININE MIMIC AS ENZYME INHIBITORS

The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin,

AROMATIC HETEROCYCLIC DERIVATIVES AS ENZYME INHIBITORS

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.