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Browse by: INVENTOR PATENT HOLDER PATENT NUMBER DATE
 
 
Inventor:
Veber; Daniel F.
Address:
Ambler, PA
No. of patents:
64
Patents:


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Patent Number Title Of Patent Date Issued
7563784 Protease inhibitors July 21, 2009
The present invention provides C.sub.1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compo
7071184 Protease inhibitors July 4, 2006
The present invention provides C.sub.1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compo
6566373 Protease inhibitors May 20, 2003
The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bon
6369077 Protease inhibitors April 9, 2002
This invention relates to compounds of formula (I): ##STR1##wherein:Y is Ar or NR.sup.1 R.sup.2 ;R.sup.1 is R", R"C(O), R"C(S), R"SO.sub.2, R"OC(O), R"R'NC(O), or R"R'NC(S);R.sup.2 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, Ar-C.sub.0-6 alkyl, or Het-C.sub.0-6 alkyl;R.sup.3 is H, C.sub.2-
5693643 Hydantoin and succinimide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antago December 2, 1997
Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea, and for the stoppage of labor preparatory to Cesarean delivery. ##STR1##
5681926 Thrombin receptor binding peptides October 28, 1997
Peptides having the general sequence A-B-C-D-E-F-Z wherein A is Ala, B is pFPhe, C is, for example, Arg, D is Cha, E is, for example, hArg, F is, for example, Tyr, and Z is, for example NH.sub.2. The peptides are useful for promoting wound healing and arresting bleeding in a patient.
5672582 Thrombin inhibitors September 30, 1997
4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability. They have the formula ##STR1## for example
5648352 Piperazinylcamphorsulfonyl oxytocin antagonists July 15, 1997
The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in
5492917 Endothelin antagonists incorporating a cyclobutane February 20, 1996
Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myo
5457177 Thrombin receptor radioligands October 10, 1995
The radioligands are six amino acid peptides having iodinated tyrosine at amino acid position six, including Ala-pFPhe-hArg-Cha-hArg-Tyr(I)-NH.sub.2, which mimic the activated form of the thrombin receptor protein. Thrombin receptor radioligands of the present invention are useful fo
5420133 Quinazolinones substituted with phenoxyphenylacetic acid derivatives May 30, 1995
Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial
5374638 Six membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives used to December 20, 1994
Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and ca
5374622 Fibrinogen receptor antagonists December 20, 1994
A fibrinogen receptor antagonist of the formulaor
5340798 Fibrinogen receptor antagonists August 23, 1994
The present invention comprises fibrinogen receptor antagonist compounds, compositions containing them and methods for using them to inhibit fibrinogen binding to blood platelets. Compounds of the invention have the following formula ##STR1## wherein Z is ##STR2## X is C
5338723 Fibrinogen receptor antagonists August 16, 1994
A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
5225528 Cyclic hexapeptide oxytocin antagonists July 6, 1993
Disclosed are cyclic hexapeptides of the formula: ##STR1## These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarian delivery. Also disclosed are pharmaceutical compositions cont
5204328 Peptides having atrial natriuretic factor activity April 20, 1993
Atrial natriuretic factor analogs containing N-alkylated amino acids and showing enhanced potency and increased metabolic stability. These analogs have natriuretic, diuretic and vasorelaxant activity, making them suitable for treating congestive heart failure and renal hypertension.
5091366 Peptides having ANF activity February 25, 1992
Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid
5061693 Fibrinogen receptor antagonists October 29, 1991
A fibrinogen receptor antagonist compound of the structure:wherein A, B, C, D and E are preferably defined as follows:A is L-asparagine, D-asparagine or acylated asparagineB is an L-or D-isomer of proline, thioproline, .beta.,.beta.-dimethylthioproline, or N-methylalanine;C is arginine;D is phen
5057603 Peptides having ANF activity October 15, 1991
Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein X is L-Ile, D-Ile, D-allo-Ile, L-Met or D-Met, Y is Gly, L-Ala or D-Ala, A is optionally absent or is Ser, Ser-Ser, Arg-Ser-Ser, Arg-Arg-Ser-Ser, Leu-Arg-Arg-S
5023233 Fibrinogen receptor antagonists June 11, 1991
A fibrinogen receptor antagonist of the formula: ##STR1## wherein A, B, C, D, E, R, R.sup.1 and X-Y are preferably defined as follows:A is acylamido;R and R.sup.1 are H;X-Y is S--S;B is L-asparagine;C is proline or thioproline or .beta., .beta.-dimethylthroprolineD is arginine; andE is C
5006511 Di- or tripeptide renin inhibitors containing lactam conformational restriction in achpa April 9, 1991
Enzyme di- or tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optiona
4782043 Renin inhibitors containing a C-terminal amide cycle November 1, 1988
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4748153 Compounds having somatostatin-like activity useful as local anti-inflammatory agents May 31, 1988
Compounds having somatostatin-like activity have been found to be useful as local anti-inflammatory agents in the treatment of such conditions as, for example, psoriasis, eczema, seborrhea, and other localized inflammatory and allergic conditions. Particularly useful are cyclic and bridg
4680283 Analogs of substance P and eledoisin July 14, 1987
Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, a
4668770 Renin inhibitory tripeptides May 26, 1987
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4663310 Renin inhibitors containing 2-substituted statine May 5, 1987
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4659691 Novel cyclic Hexapeptide LHRH antagonists April 21, 1987
Novel peptides of the formula: ##STR1## where R.sup.1 through R.sup.8 are various radicals derived from L- and D- amino acids; having LHRH antagonist activity; useful in reducing fertility.Pharmaceutical compositions and methods for use in reducing fertility.
4656188 Ace inhibitors in macular degeneration April 7, 1987
Angiotensin converting enzyme inhibitors are useful in the treatment of senile macular degeneration.
4628084 Process for 3-acylamino benzodiazepines December 9, 1986
The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl;R' is hydrogen, l
4493934 2(3-Amino-2-oxopyrrolidin-1-yl) acetic acid and n-acylated derivatives thereof January 15, 1985
Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
4485099 Renin inhibitors containing a C-terminal amide cycle November 27, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4479941 Renin inhibitory peptides having PHE.sup.13 delection October 30, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperalaosteronism.
4478826 Renin inhibitory peptides October 23, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4477441 Renin inhibitors containing a C-terminal disulfide cycle October 16, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4477440 Renin inhibitors containing an n-terminal disulfide cycle October 16, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4470971 Renin inhibitory peptides having His.sup.13 September 11, 1984
Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4439359 Cyclic octapeptide analogs of neurotensin March 27, 1984
There are disclosed cyclic octapeptide analogs of the tridecapeptide, neurotensin.
4384994 Renin inhibitory peptides May 24, 1983
Renin inhibitory peptides of the formula:and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
4377515 Long lasting agonists and antagonists of LH-RH March 22, 1983
Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
4360516 Modified D-retro cyclic hexapeptide somatostatin analogs November 23, 1982
Highly active and long lasting cyclic hexapeptide analogs of somatostatin are prepared. A single amino acid of D-configuration, functioning as a spacer for the remaining amino acids, replaces seven of the ring amino acids of somatostatin. The amino acid adjacent to this spacer amino acid
4310518 Cyclic hexapeptide somatostatin analogs January 12, 1982
Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity
4301151 Long-lasting agonists of enkephalin November 17, 1981
Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.
4254107 Long-lasting agonists of enkephalin March 3, 1981
Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.
4235886 Cyclic hexapeptide somatostatin analogs November 25, 1980
Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synethesize, have a longer duration of activity, and many have a greater level of activity
4192875 Cyclic hexapeptide March 11, 1980
Synthetic novel cyclic hexapeptide having the structure: ##STR1## and the dipeptide ##STR2## are prepared. Oral administration of these peptides improves the digestive efficiency of certain herbivorous animals.
4191754 Bicyclic somatostatin analogs March 4, 1980
Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by a combination of the solid phase method and the solution method. These analogs have the property of inhibiting the release of insulin, glucagon and growth hormone in humans
4190648 Peptides having somatostatin activity February 26, 1980
Peptides having the structural formula: ##STR1## wherein A is D-Thr, D-Val;B is D-Phe, D-Tyr;C is D-Phe, D-Tyr, O-Me-D-Tyr;wherein the ring formed by the peptide backbone contains 26 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid
4162248 Somatostatin analogs July 24, 1979
Somatostatin analogs having the structural formula:Cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ]WhereinX is ##STR1## and n=0 to 4; A is Lys, (.epsilon.-INOC) Lysine;B is Asn, Ala, .alpha.-aminobutyric acid;C is Ser, Gly;J, k, l and m are 0 to
4161521 Somatostatin analogs July 17, 1979
Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release
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