Abstract: The present invention provides the inhibitors of dipeptidyl peptidase IV based upon or including proline or similar moieties. The inhibitors are useful for treating various disorders, including those of the central nervous system and the prostate. Many of the inhibitors can be reversible, and can cross the blood-brain barrier. Methods of making and using the inhibitors and treatment methods also are provided.
Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.
Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.
Type:
Application
Filed:
June 24, 2003
Publication date:
April 29, 2004
Applicant:
Guilford Pharmaceuticals Inc.
Inventors:
Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
Abstract: This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.
Abstract: Symmetrically disubstituted aromatic compounds and pharmaceutical compositions containing such compounds that inhibit and/or modulate the activity of poly(ADP-ribose) glycohydrolase, also known as PARG, are described. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
Type:
Application
Filed:
August 28, 2003
Publication date:
April 1, 2004
Applicant:
Guilford Pharmaceuticals, Inc.
Inventors:
Jia-He Li, Dana Victor Ferraris, Paul W. Kletzly, Weixing Li, Eric Yanjun Wang, Amy D. Xing, Weizheng Xu, Jie Zhang
Abstract: The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the growth or regeneration of neuronal cells. In part, the invention provides compounds that interact with or bind to a cyclophilin and compounds that have activity towards neuronal cells. Methods for using the compounds, such as administering them to cells or animals or using them to treat neurodegenerative conditions, are specifically included.
Type:
Grant
Filed:
September 7, 2000
Date of Patent:
January 13, 2004
Assignee:
Guilford Pharmaceuticals, Inc.
Inventors:
Gregory S. Hamilton, Joseph P. Steiner, Mark J. Vaal, Chi Choi, Ling Wei
Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.
Type:
Grant
Filed:
January 25, 2002
Date of Patent:
December 2, 2003
Assignee:
Guilford Pharmaceuticals Inc.
Inventors:
Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
Type:
Application
Filed:
May 8, 2003
Publication date:
November 20, 2003
Applicant:
GUILFORD PHARMACEUTICALS INC.
Inventors:
Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
Abstract: Biodegradable polymer compositions suitable for intraperitoneal administration to treat a mammalian subject having ovarian cancer are described, wherein the polymer compositions provide extended release of the antineoplastic agent into the peritoneum of the subject. The subject compositions can increase the median survival rate from the cancer by at least about 10%, as compared with the median survival rate obtained by administration of a composition comprising the same dosage of the antineoplastic agent without the biodegradable polymer. Solid articles and methods for treating ovarian cancer are also described.
Abstract: Symmetrically disubstituted aromatic compounds and pharmaceutical compositions containing such compounds that inhibit and/or modulate the activity of poly(ADP-ribose) glycohydrolase, also known as PARG, are described. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
Type:
Grant
Filed:
April 10, 2001
Date of Patent:
October 21, 2003
Assignee:
Guilford Pharmaceuticals, Inc.
Inventors:
Jia-He Li, Dana Victor Ferraris, Paul W. Kletzly, Weixing Li, Eric Yanjun Wang, Amy D. Xing, Weizheng Xu, Jie Zhang
Abstract: The present invention relates to PARP inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat tissue damage resulting from cell damage or death due to necrosis or apoptosis, effect neuronal activities not mediated by NMDA toxicity; to treat neural tissue damage resulting from ischemia and reperfusion injury, neurological disorders and neurodegenerative diseases; to prevent or treat vascular stroke; to treat or prevent cardiovascular disorders; to treat other conditions and/or disorders such as age-related macular degeneration, AIDS and other immune senescence diseases, arthritis, atherosclerosis, cachexia, cancer, degenerative diseases of skeletal muscle involving replicative senescence, diabetes, head trauma, immune senescence, inflammatory bowel disorders (such as colitis and Crohn's disease), muscular dystrophy, osteoarthritis, osteoporosis, chronic and/or acute pain (such as neuropathic pain), renal failure, retinal ischemia, septic shock (such as endotoxic
Type:
Grant
Filed:
September 1, 1998
Date of Patent:
October 21, 2003
Assignee:
Guilford Pharmaceuticals Inc.
Inventors:
Paul F. Jackson, Jia-He Li, Keith M. Maclin, Jie Zhang
Abstract: Biodegradable terephthalate polymers are described comprising the recurring monomeric units shown in formula I:
wherein R is a divalent organic moiety;
R′ is an aliphatic, aromatic or heterocyclic residue;
x is ≧1; and
n is 0-5,000,
wherein the biodegradable polymer is biocompatible before and upon biodegradation. Processes for preparing the polymers, compositions containing the polymers and biologically active substances, articles useful for implantation or injection into the body fabricated from the compositions, and methods for controllably releasing biologically active substances using the polymers, are also described.
Type:
Grant
Filed:
August 2, 2001
Date of Patent:
July 29, 2003
Assignees:
Guilford Pharmaceuticals, Inc., John Hopkins University
Inventors:
Hai-Quan Mao, Kam W. Leong, Wenbin Dang, Hungnan Lo, Zhong Zhao, David P. Nowotnik, James P. English
Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.
Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
Type:
Grant
Filed:
January 17, 2002
Date of Patent:
July 1, 2003
Assignee:
Guilford Pharmaceuticals Inc.
Inventors:
Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
Abstract: Compounds, compositions containing compounds, methods of sing compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: 1
Type:
Application
Filed:
April 1, 2002
Publication date:
June 5, 2003
Applicant:
Guilford Pharmaceuticals Inc.
Inventors:
Jia-He Li, Kevin Leonard Tays, Jie Zhang
Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
Type:
Application
Filed:
January 17, 2002
Publication date:
June 5, 2003
Applicant:
GUILFORD PHARMACEUTICALS INC.
Inventors:
Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
Abstract: This invention is related to methods of effecting neuronal activity with non-immunosuppressive neurotrophic low molecular weight, small molecule cyclophilin inhibitor compounds having an affinity for cyclophilin-type immunophilins. The methods of this invention are useful in the stimulation of damaged neurons, promotion of neuronal regeneration, prevention of neurodegeneration, and treatment of neurological disorders.
Type:
Application
Filed:
September 7, 2001
Publication date:
April 10, 2003
Applicant:
Guilford Pharmaceuticals, Inc.
Inventors:
Gregory S. Hamilton, Ling Wei, Joseph P. Steiner
Abstract: A biodegradable polymer composition comprising:
(a) a poly(phosphoester) biodegradable polymer and
(b) at least one antineoplastic agent in an amount effective to inhibit the growth of a solid tumor, which
is suitable for intratumoral administration to treat a mammal having a solid tumor.