- Pyrrole compounds as granzyme B inhibitors
-
Pyrrole compounds as Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Method for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.
- -
-
Page/Page column 46
(2016/10/24)
-
- Covalent granzyme B inhibitors
-
Covalent Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. A method for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are pr
- -
-
Page/Page column 42
(2016/10/27)
-
- COSMETIC USES AND METHODS FOR INDOLINE GRANZYME B INHIBITOR COMPOSITIONS
-
Cosmetic uses and methods for indoline granzyme B inhibitor compounds in compositions with a cosmetically acceptable carrier. Uses and methods for treating, reducing or inhibiting the appearance of ageing in the skin are provided. Also provided are compositions and formulation for cosmetic uses and methods of maintaining a youthful appearance, reducing an appearance of ageing, inhibiting an appearance of ageing, reducing a rate of an appearance of ageing, reducing a skin inelasticity, reducing a rate of increasing skin inelasticity, maintaining a skin elasticity, and increasing the density of hair follicles of a skin of a subjecl. The uses and methods comprise applying/administering an indoline granzyme B inhibitor to a skin, or a portion of a skin of the subject.
- -
-
Page/Page column 67
(2014/10/15)
-
- NOVEL COMPOUNDS
-
The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.
- -
-
Page/Page column 88
(2011/08/22)
-
- TETRAPEPTIDE ANALOGS
-
Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.
- -
-
Page/Page column 141
(2010/10/20)
-
- ANTITHROMBOTIC AGENTS
-
This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
- -
-
-
- ANTITHROMBOTIC AGENTS
-
This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
- -
-
-
- ANTITHROMBOTIC AGENTS
-
This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
- -
-
-
- ANTITHROMBOTIC AGENTS
-
This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
- -
-
-
- ANTITHROMBOTIC AGENTS
-
This invention relates to thrombin inhibiting compounds having the FormulaIX--Y--NH--(CH 2) r--G I where X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
- -
-
-
- Benzo-fused lactams
-
Compounds of the formula STR1 wherein A is STR2 are useful as ACE and NEP inhibitors and those wherein A is STR3 are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.
- -
-
-
- PHOSPHONYL HYDROXYACYL AMINO ACID DERIVATIVES AS ANTIHYPERTENSIVE
-
Phosphonyl hydroxyacyl amino acids of the formula STR1 wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
- -
-
-
- 1-(carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives
-
1-(Carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives of the formula STR1 where each R1 is independently alkyl, alkoxy, acyloxy, hydroxy, halo or trifluoromethyl, n is 0, 1, 2 or 3, R2 and R3 are independently hydroxy, alkoxy, amino or substituted amino, R4 and R5 are independently hydrogen, alkyl or substituted alkyl, R6 is hydrogen, alkyl or substituted alkyl, and Y is O, S or N--R7 where R7 is hydrogen, alkyl, cyano or substituted alkyl, and salts thereof, which are useful as antihypertensive and cardioactive agents, methods of preparing the same, and pharmaceutical compositions thereof, are provided.
- -
-
-
- 1-mercaptoalkanoylindoline-2-carboxylic acids
-
1-Mercaptoalkanoylindoline-2-carboxylic acids, e.g., those of the formula STR1 and functional derivatives thereof, are antihypertensive and cardioactive agents.
- -
-
-
- Substituted iminodiacids, their preparation and pharmaceutical compositions containing them
-
Compounds of the general formula: STR1 wherein: the ring A is saturated and n=0 or 1, or the ring A is a benzene ring and n=1, R1 represents a lower alkyl group which can carry an amino group, R2 represents a hydrogen atom or a lower alkyl group, R3 represents a straight or branched alkyl group, a mono- or di-cycloalkylalkyl or phenylalkyl group having no more than a total of 9 carbon atoms, or a substituted alkyl group, and also the salts thereof. These compounds are useful as therapeutic drugs.
- -
-
-
- 1-Carboxyalkanoylindoline-2-carboxylic acids
-
1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula STR1 R=H, alkyl, alkoxy, halogeno or CF3 ; R'=H or R-phenyl; m=0 or 1; p,q=0 to 2; and derivatives thereof, are antihypertensive and cardioactive agents.
- -
-
-
- Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives
-
The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.
- Stanton,Gruenfeld,Babiarz,Ackerman,Friedmann,Yuan,Macchia
-
p. 1267 - 1277
(2007/10/02)
-
- 1-CARBOXYALKANOYLINDOLINE-2-CARBOXYLIC ACIDS
-
1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula STR1 R=H, alkyl, alkoxy, halogeno or CF. sub.3 ; R'=H or R-phenyl;m=0 or 1;p, q=0 to 2; and functional derivatives thereof, are antihypertensive a
- -
-
-