Patents Assigned to Allelix Biopharmaceuticals Inc.
  • Patent number: 5834459
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, 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. and C(O);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 D4 receptor stimulation is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: November 10, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventor: Jian-Min Fu
  • Patent number: 5830712
    Abstract: A novel method for inactivating undesirable members in a nucleic acid sample which comprises undesirable and desirable members of a nucleic acid family. The method includes the step of adding a blocker to the sample which selectively associates with the undesirable members such that they are unable to participate in any further processing of the sample. The method advantageously provides a means whereby desirable members of the nucleic acid family can be processed, i.e. identified, amplified and/or isolated, without interference from undesirable sequence-related members.
    Type: Grant
    Filed: February 6, 1996
    Date of Patent: November 3, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Vikarna Rampersad, Roman Zastawny, Rajender Kamboj
  • Patent number: 5831001
    Abstract: Described herein are oligopeptides useful to inhibit replication of herpesviruses, especially herpes simplex viruses. In a preferred embodiment of the invention, the oligopeptide is a D-arginine nonamer having N- and C-terminal protecting groups, which, at a 5 uM concentration, exhibits greater than 95% inhibition of HSV-1 replication, in a standard assay.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: November 3, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Michael Twist, Richard W. Barnett, Lorne S. Reid, Martin Sumner-Smith
  • Patent number: 5824676
    Abstract: 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: Grant
    Filed: December 10, 1996
    Date of Patent: October 20, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Ashok Tehim, Jian-min Fu, Sumanas Rakhit
  • Patent number: 5814628
    Abstract: 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.CHCI, 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: Grant
    Filed: December 10, 1996
    Date of Patent: September 29, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
  • Patent number: 5798350
    Abstract: 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: Grant
    Filed: May 3, 1996
    Date of Patent: August 25, 1998
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5789379
    Abstract: Analogs of glucagon-like peptide 2, a product of glucagon gene expression, have been identified as intestinal tissue growth factors. Their formulation as pharmaceutical, and therapeutic use in treating disorders of the small bowel, are described.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: August 4, 1998
    Assignees: Allelix Biopharmaceutical Inc., 1149336 Ontario Inc.
    Inventors: Daniel J. Drucker, Anna E. Crivici, Martin Sumner-Smith
  • Patent number: 5770742
    Abstract: 5-Thiophene-substituted tryptamine analogs are provided, which exhibit selectivity towards 5-HT.sub.D1 receptors and consequently show potential in alleviation of the symptoms of migraine. The analogs are represented by the following general chemical formula: ##STR1## in which X represents H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or halogen, at the 4- or 5-position of the thiophene nucleus; Y represents a direct bond or a C.sub.1 -C.sub.3 alkylene group optionally substituted with hydroxyl: and Z represents amino, mono- or di-N-lower alkyl-substituted amino, or optionally N-lower alkyl-substituted pyrrolidine.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: June 23, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Qingchang Meng, Abdelmalik Slassi, Sumanas Rakhit
  • Patent number: 5700445
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein X.sub.1 is selected from CH.sub.2, NH, O and S;X.sub.2 - - is selected from CH.dbd., CH.sub.2 13 , and N.dbd.;R.sub.1 to R.sub.8 are each independently selected from H, C.sub.1-4 alkyl, halo, cyano, nitro and halo-substituted C.sub.1-4 alkyland 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: Grant
    Filed: December 12, 1994
    Date of Patent: December 23, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5674877
    Abstract: 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: Grant
    Filed: April 24, 1996
    Date of Patent: October 7, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Ashok Tehim, Sumanas Rakhit
  • Patent number: 5674849
    Abstract: An anti-viral composition includes a synergistic combination of an anti-viral nucleoside analogue, which may inhibit a virus-specific enzyme, such as viral thymidine kinase and reverse transcriptase, an anti-viral oligonucleotide compound having from 6 to 12 amino acid residues substantially all of which are D-arginine residues, and a pharmaceutically acceptable carrier. A method for treating a viral infection is also described.
    Type: Grant
    Filed: January 9, 1995
    Date of Patent: October 7, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Michael Twist, Martin Sumner-Smith
  • Patent number: 5646120
    Abstract: Described herein are oligopeptides useful to inhibit replication in virally infected individuals. In a preferred embodiment of the invention, the oligopeptide is a D-arginine nonamer having N- and C-terminal protecting groups, which, at a 5 uM concentration, exhibits greater than 95% inhibition of HIV replication, in a standard assay.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: July 8, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Martin Sumner-Smith, Richard W. Barnett, Lorne S. Reid, Nahum Sonenberg
  • Patent number: 5643785
    Abstract: Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR4B receptor. The receptor is characterized structurally and the construction and use of cell lines expressing the receptor is disclosed.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: July 1, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Rajender Kamboj, Candace E. Elliott, Stephen L. Nutt
  • Patent number: 5633230
    Abstract: Described herein are anti-cytomegalovirus peptides. In a preferred embodiment, the peptide is acetyl-[D-Arg].sub.9 -NH.sub.2. The use of these peptides, either per se or in combination with other anti-CMV compounds, is disclosed as an effective method for controlling CMV infection.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: May 27, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Michael Twist, deceased, Martin Sumner-Smith
  • Patent number: 5629205
    Abstract: The present invention provides a novel expression system for the production of protein in bacterial hosts. The system utilizes novel promoters that are highly efficient in initializing transcription and therefore enhance protein yield. The promoters comprise the -35 region of the consensus E. coli promoter, the -10 region of the lppP-5 promoter and a spacer between these two regions derived from either the lpp or lacUV5 promoters.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 13, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventor: Peter A. Lagosky
  • Patent number: 5627194
    Abstract: Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: May 6, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Sumanas Rakhit, Abdelmalik Slassi
  • Patent number: 5616481
    Abstract: 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: Grant
    Filed: April 3, 1995
    Date of Patent: April 1, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
  • Patent number: 5614406
    Abstract: 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: Grant
    Filed: February 28, 1994
    Date of Patent: March 25, 1997
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Rajender Kamboj, Stephen L. Nutt, Lee Shekter, Michael A. Wosnick
  • Patent number: 5610032
    Abstract: 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: Grant
    Filed: June 6, 1994
    Date of Patent: March 11, 1997
    Assignee: Allelix Biopharmaceutical Inc.
    Inventors: Rajender Kamboj, Candace E. Elliott, Stephen L. Nutt
  • Patent number: 5602120
    Abstract: 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: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby