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Attorney: Daniel; Mark R., DiPrima; Joseph F.


Number of patents: 32
Last date: October 04, 1994

NumberTitleIssue Date
5352705Inhibitors of farnesyl protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
10/04/1994
5326773Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
07/05/1994
5324726Benzodiazepine analogs
Benzodiazepine analogs of the formula: ##STR1## wherein: R3 is ##STR2## --NH(CH2)2 --3 NHCOR7, ##STR3## or --X11 NR18 SO2 (CH2)q...
06/28/1994
5314900Aryl thiopyrano[2,3,4-C,D]indoles as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of 5-lipoxygenase and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in ...
05/24/1994
5310884LTD4 receptor and photoaffinity probe
The LTD4 receptor has been defined by radioligand binding studies as a member of the family of G-protein coupled receptors. A photoactivable azido derivative of LTD4 ([125 I]Azido-LTD4) has been synthesized for ...
05/10/1994
5308852Heteroarylnaphthalenes as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, ...
05/03/1994
5298655Farnesyl pyrophosphate analogs
The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the com...
03/29/1994
5292879Intermediates for preparing cationic-2-heteroaryl-phenyl-carbapenem antibacterial agents
Carbapenem compounds of the formula ##STR1## are useful intermediates for preparing antibacterial agents....
03/08/1994
5290798(hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, a...
03/01/1994
5281720Pyranylphenyl hydroxyalkylnaphthoic acids as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, ...
01/25/1994
5274096Hydrazine synthesis
An improved synthesis is described for producing a quinolinylmethoxyphenyl hydrazine which is an intermediate in the preparation of quinolinylmethoxyindoles useful as inhibitors of leukotriene biosynthesis. The improved process eliminates two isolation st...
12/28/1993
5266568Hydroxyalkylquinoline ether acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in t...
11/30/1993
5254682Cyclic renin inhibitors containing 3(S)-amino-4-cyclohexyl-2(R)-hydroxy-butanoic acid or 4-cyclo-hexyl-(2R, 3S)-dihydroxybutanoic acid or related analogs
Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteroni...
10/19/1993
5252585Fluorinated quinoline indoles as inhibitors of the biosynthesis of leukotrienes
This invention relates to compounds having the formula I: ##STR1## wherein R1 is H, F or MeO, which are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotect...
10/12/1993
5245069Process for the preparation of bis(aryl)-phosphorohalidates
This invention relates to a novel process for preparing bis(aryl)phosphorohalidates which are useful in the synthesis of various enol phosphates. The process of this invention provides a means of producing a high-yield, high-purity product without the nee...
09/14/1993
5242680Thiol-reactive maleimido-based radiolabeling reagents
Novel thiol-reactive maleimido-based radiolabeling reagents are disclosed which are useful for binding and receptor studies and assays. The reagents are also useful as diagnostic imaging agents, and as radiotherapeutic drugs....
09/07/1993
5238922Inhibitors of farnesyl protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
08/24/1993
5223509ଲ-carbolines as cholecystokinin and gastrin antagonists
This invention relates to certain ଲ-carbolines, which are antagonists of the functions of cholecystokinin (CCK) and gastrin, to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the prevention and treatment...
06/29/1993
5220018Cholecystokinin antagonists
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
06/15/1993
5220017Cholecystokinin antagonists
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
06/15/1993
5218115Cholecystokinin antagonists
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
06/08/1993
5218114Cholecystokinin antagonists
Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK)....
06/08/1993
5215989Nitrogen-containing heterocyclic compounds as class III antiarrhythmic agents
Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R2 and R3 are H, substituted or unsu...
06/01/1993
52100822-benzazepines with 5- and 6-membered heterocyclic rings to treat pain and anxiety disorders
Pharmaceutical compositions containing aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder....
05/11/1993
5206240Nitrogen-containing spirocycles
Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents....
04/27/1993
5206237Benzodiazepine analogs
Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder....
04/27/1993
5194605Cyclic renin inhibitors containing 2-substituted (3S,4S)-4-amino-5-cyclohexyl-3-hydroxy pentanoic acid, 2-substituted (3S,4S)-5-cyclohexyl-3,4-di-hydroxy pentanoic acid or 2-substituted (4S,5S)-5-amino-6-cyclohexyl-4-hydroxyhexanoic acid or its analogs
Compounds of the formula ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, ...
03/16/1993
5189050Fermentation analogs of Virginiamycin M1 to treat panic and anxiety disorder
Pharmaceutical compositions containing Virginiamycin M1 having the Formula: ##STR1## and Virginiamycin M1 analogs having the Formulae I-IV: ##STR2## are disclosed which are useful in the treatment of panic disorder or ...
02/23/1993
5185331Triazolobenzodiazepines
Pharmaceutical compositions containing Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder....
02/09/1993
51770711,4-benzodiazepines with 6-membered heterocyclic rings to treat panic and anxiety disorder
Pharmaceutical compositions containing 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder....
01/05/1993
5171860Diamino isothiazole-1-oxides and 1,1 dioxides as gastric secretion inhibitors
This invention is directed to diamino isothiazole -1-oxides and -1,1-dioxides and related compounds as well as pharmaceutical compositions and methods useful in the treatment of gastric secretion in mammals....
12/15/1992
51661512-Benzazepines with 5- and 6-membered heterocyclic rings, compositions and medical methods of use thereof
Aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central...
11/24/1992
 
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