Patents by Inventor Keith M. Maclin
Keith M. Maclin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 6635642Abstract: 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 endotoxicType: GrantFiled: September 1, 1998Date of Patent: October 21, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Jia-He Li, Keith M. Maclin, Jie Zhang
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Publication number: 20030083374Abstract: The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.Type: ApplicationFiled: June 10, 2002Publication date: May 1, 2003Inventors: Paul F. Jackson, Keith M. Maclin, Eric Wang, Barbara S. Slusher, Rena S. Lapidus, Pavel Majer
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Patent number: 6514983Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, wherein Y is alkylhalo, alkyl-CO—G, COG, a direct bond, C═O, O, NR11, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is NR16, O, S, CR12R13, C═O, a bond, —CR12═CR13—, —C(R12R13)C(R14R15)—, or; Rhd 1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylhaType: GrantFiled: September 1, 1998Date of Patent: February 4, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang, Paul F. Jackson, Keith M. Maclin
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Patent number: 6479471Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: December 17, 1999Date of Patent: November 12, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher, Kevin L. Tays, Keith M. Maclin
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Publication number: 20020151503Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: ApplicationFiled: January 28, 2002Publication date: October 17, 2002Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Patent number: 6458775Abstract: The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.Type: GrantFiled: July 2, 1999Date of Patent: October 1, 2002Assignee: Guilford Pharmaceutical Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Eric Wang, Barbara S. Slusher, Rena S. Lapidus, Pavel Majer
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Patent number: 6426415Abstract: A compound of formula I: or a pharmaceutically acceptable salt, prodrug, metabolite, optical isomer or stereoisomer thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH-(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iiiType: GrantFiled: May 15, 1998Date of Patent: July 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6413948Abstract: The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.Type: GrantFiled: September 2, 1999Date of Patent: July 2, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Patent number: 6380211Abstract: A compound, compositions, methods of use, and processes of making formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH—(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-memberType: GrantFiled: November 15, 2000Date of Patent: April 30, 2002Assignee: Guilford Pharmaceutical Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6372726Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: September 27, 1999Date of Patent: April 16, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Publication number: 20020028813Abstract: A compound of formula I: 1Type: ApplicationFiled: September 1, 1998Publication date: March 7, 2002Inventors: PAUL F. JACKSON, KEITH M. MACLIN, JIE ZHANG
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Patent number: 6346536Abstract: Poly(ADP-ribose) polymerase (“PARP”) inhibitors and methods for treating neurodegenerative diseases, neural tissue damage related to cerebral ischemia and reperfusion injury, and cardiovascular in an animal.Type: GrantFiled: September 3, 1997Date of Patent: February 12, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Publication number: 20010044459Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: ApplicationFiled: June 15, 2001Publication date: November 22, 2001Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. Maclin, Barbara S. Slusher
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Patent number: 6306889Abstract: 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.Type: GrantFiled: March 25, 1998Date of Patent: October 23, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang, Paul F. Jackson, Keith M. Maclin
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Patent number: 6288046Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: GrantFiled: April 26, 1999Date of Patent: September 11, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Kevin L. Tays, Barbara S. Slusher
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Patent number: 6271245Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: GrantFiled: June 1, 1999Date of Patent: August 7, 2001Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. MacLin, Barbara S. Slusher
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Patent number: 6265609Abstract: The present invention relate to thio-substituted pentanedioic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders and prostate diseases.Type: GrantFiled: January 12, 1999Date of Patent: July 24, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Eric Wang, Barbara S. Slusher, Rena Lapidus
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Patent number: 6197785Abstract: A compound, compositions, methods of use, and processes of making formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH—(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membereType: GrantFiled: September 1, 1998Date of Patent: March 6, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6121278Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.Type: GrantFiled: September 1, 1998Date of Patent: September 19, 2000Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6071965Abstract: The present invention relate to phosphinic alkanoic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.Type: GrantFiled: December 31, 1997Date of Patent: June 6, 2000Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Weixing Li, Keith M. Maclin, Kevin L. Tays, Takashi Tsukamoto, Barbara S. Slusher