Patents Assigned to Allelix Biopharmaceuticals
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Patent number: 5616481Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: April 3, 1995Date of Patent: April 1, 1997Assignee: Allelix Biopharmaceuticals Inc.Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
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Patent number: 5614406Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: February 28, 1994Date of Patent: March 25, 1997Assignee: Allelix Biopharmaceuticals Inc.Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
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Patent number: 5610032Abstract: Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR1B receptor. The receptor is characterized structurally and the construction and use of cell lines expressing the receptor is disclosed.Type: GrantFiled: June 6, 1994Date of Patent: March 11, 1997Assignee: Allelix Biopharmaceutical Inc.Inventors: Rajender Kamboj, Candace E. Elliott, Stephen L. Nutt
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Patent number: 5602120Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
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Patent number: 5602124Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5602121Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 . . . is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventor: Jian-Min Fu
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Patent number: 5599792Abstract: Described herein are Met.sup.8 -substituted variants of parathyroid hormone that retain bone stimulating activity yet, unlike their native counterparts, have substantially no vasoactivity. Their production using recombinant DNA-based techniques is also described, as is their therapeutic use, e.g. in the treatment of osteoporosis.Type: GrantFiled: October 31, 1994Date of Patent: February 4, 1997Assignee: Allelix Biopharmaceuticals Inc.Inventors: K. Anne Kronis, Richard P. Bozzato
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Patent number: 5595969Abstract: A novel steroid-binding variant of human corticosteroid binding globulin in which one or more of the glycosylation sites, other than the glycosylation site at amino acid position 238, has been functionally disrupted is complexed with an anti-inflammatory ligand in the treatment of inflammation in mammals.Type: GrantFiled: April 14, 1995Date of Patent: January 21, 1997Assignee: Allelix Biopharmaceutical Inc.Inventors: Geoffrey L. Hammond, George V. Avvakumov
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Patent number: 5576205Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: January 24, 1994Date of Patent: November 19, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
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Patent number: 5576314Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2;R.sub.1 is selected from H and an amino acid side chain;R.sub.2 is selected from H, OH, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, and benzyloxy; andR.sub.3 is selected from H, OH, halo, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenoxy, benzyloxy, .dbd.O, .dbd.S, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylthio, amino, and aminocarbonyl;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: December 12, 1994Date of Patent: November 19, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Patricia L. Power, Sumanas Rakhit
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Patent number: 5574144Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors of the kainate-binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: June 24, 1992Date of Patent: November 12, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Rajender Kamboj, Candace E. Elliott, Stephen L. Nutt
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Patent number: 5561127Abstract: Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 19, 1994Date of Patent: October 1, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Sumanas Rakhit
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Patent number: 5547855Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of the kainate-binding type of EAA receptor, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Disclosed is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: March 15, 1995Date of Patent: August 20, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Rajender Kamboj, Candace E. Elliott, Stephen L. Nutt
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Patent number: 5538965Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 -- is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: December 12, 1994Date of Patent: July 23, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5504101Abstract: Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1D.beta. receptor, of the formula: ##STR1## wherein R.sup.1 is a group selected from aryl-C.sub.1-7 alkyl; aryl-C.sub.2-7 alkoxy; aryl-C.sub.2-7 alkanoyl and aryl-C.sub.1-7 alkanoyloxy, wherein said alkyl, alkoxy, alkanoyl and alkanoyloxy groups are optionally substituted by a C.sub.1-4 alkyl substituent and wherein said aryl group is optionally substituted by one or more substituent selected from hydroxyl, halogen, mercapto, linear or branched C.sub.1-4 alkyl, linear or branched C.sub.1-4 alkoxy, linear or branched C.sub.1-4 alkylthio, thiol substituted C.sub.1-4 alkyl and nitro substituted C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected independently from H and C.sub.1-4 alkyl; andR.sup.4 is selected from H, C.sub.1-4 alkyl, aryl and arylC.sub.1-4 alkyl.Type: GrantFiled: May 6, 1994Date of Patent: April 2, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventor: Richard A. Glennon
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Patent number: 5496801Abstract: Described herein are preparations containing parathyroid hormone that has been stablized with an excipient and buffering agent. Preferred preparations incorporate human PTH(1-84), mannitol as excipient and citrate as buffering agent, and are incorporated in vials as a freeze-dried powder for reconstitution to treat osteoporosis.Type: GrantFiled: December 23, 1993Date of Patent: March 5, 1996Assignee: Allelix BioPharmaceuticals Inc.Inventors: Josephus J. M. Holthuis, Albert Mekking, Alwinus A. Voetman
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Patent number: 5494792Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commerical significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.Type: GrantFiled: July 15, 1993Date of Patent: February 27, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
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Patent number: 5495006Abstract: The herpes simplex virus encodes ICP4, a DNA binding protein. ICP4-binding duplexed structures having significantly enhanced stability under physiological conditions are described. The structures are provided in the form of polynucleotide conjugates capable of adopting a duplexed structure, in which annealable polynucleotide strands are coupled covalently at one or both ends through a chemical linker which establishes a stabilizing bridge between strands. The present polynucleotide conjugates have therapeutic utility against viral infection as the polynucleotide strands thereof define a binding site for a viral regulatory protein, thereby inactivating the protein and preventing viral replication from occurring.Type: GrantFiled: March 1, 1993Date of Patent: February 27, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Shane Climie, Michael Ma
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Patent number: 5432080Abstract: A novel steroid-binding variant of human corticosteroid binding globulin in which one or more of the glycosylation sites, other than the glycosylation site at amino acid position 238, has been functionally disrupted is complexed with an anti-inflammatory ligand in the treatment of inflammation in mammals.Type: GrantFiled: December 16, 1992Date of Patent: July 11, 1995Assignee: Allelix Biopharmaceuticals Inc.Inventors: Geoffrey L. Hammond, George V. Avvakumov
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Patent number: 5403825Abstract: Described is a purified osteogenic factor that when delivered to bone in association with a physiologically acceptable delivery vehicle is capable of inducing new bone growth at the bone surface. The osteogenic factor is water soluble, and is characterized physically by a molecular weight of about 2.5 kD when measured by gel filtration under dissociating conditions and an isoelectric point in the pH range from about 4.6 to 7.2. Use of the purified factor in treating bone defects is described. Also described is a method for obtaining the purified factor from mammalian bone.Type: GrantFiled: September 1, 1992Date of Patent: April 4, 1995Assignee: Allelix Biopharmaceuticals Inc.Inventors: Alain E. Lagarde, Abdulwahid Abdulwajid, Donna Bueschkens, Deanna Byrne