Patents by Inventor William Pendergast
William Pendergast 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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Publication number: 20020052007Abstract: Diarylmethylbenzylpiperazine compounds, optionally substituted on an aromatic ring of the benzyl substituent with one or more halo substituents, and pharmaceutically acceptable esters and salts of such compounds. Such compounds are usefully employed in therapeutic intervention for treatment or prophylaxis of disease states and conditions such as drug addiction, alcohol addiction, drug overdose, mental illness, cough, lung edema, gastro-intestinal disorders, arthritis, psoriasis, asthma, inflammatory bowel disease, disorders of respiratory function, functional bowel disease, irritable bowel syndrome, diarrhea, functional distension, pain (e.g., functional pain, trauma pain, etc.), non-ulcerogenic dyspepsia, urogenital tract disorders, organ transplant rejection, skin graft rejection, mental disorders, cognitive disorders, emesis, respiratory depression, acne and skin lesions.Type: ApplicationFiled: September 21, 2001Publication date: May 2, 2002Inventors: Kwen Jen Chang, William Pendergast, Kestutis P. Biciunas, Edwin Shen-Chou Wu
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Patent number: 6348589Abstract: The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment.Type: GrantFiled: July 10, 1998Date of Patent: February 19, 2002Assignee: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Benjamin R. Yerxa, Janet L. Rideout, Suhaib M. Siddiqi
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Publication number: 20020013289Abstract: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.Type: ApplicationFiled: November 25, 1998Publication date: January 31, 2002Inventors: WILLIAM PENDERGAST, SAMMY R. SHAVER, DAVID J. DRUTZ, JANET L. RIDEOUT
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Patent number: 6323187Abstract: The present invention relates to P1-(cytidine 5′-)-P-(uridine 5′-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.Type: GrantFiled: May 21, 1999Date of Patent: November 27, 2001Assignees: Inspire Pharmaceuticals, Inc., University of North Carolina at Chapel HillInventors: Benjamin R. Yerxa, William Pendergast, Janet L. Rideout, Maryse Picher, Richard C. Boucher, Jr., M. Jackson Stutts
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Patent number: 6319908Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture, wherein: X is Na, NH4 or H, provided that all X groups are not H.Type: GrantFiled: July 24, 1998Date of Patent: November 20, 2001Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, William Pendergast
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Patent number: 6306865Abstract: Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacologicType: GrantFiled: June 6, 2000Date of Patent: October 23, 2001Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
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Publication number: 20010011079Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture.Type: ApplicationFiled: March 13, 2001Publication date: August 2, 2001Inventors: Benjamin R. Yerxa, William Pendergast
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Patent number: 6143279Abstract: Compounds of Formula I: ##STR1## wherein: X.sub.1, and X.sub.2 are each independently either O.sup.- or S.sup.- ;X.sub.3 and X.sub.4 are each independently either --H or --OH, with the proviso that X.sub.3 and X.sub.4 are not simultaneously --H;R.sub.1 is selected from the group consisting of O, imido, methylene and dihalomethylene;R.sub.2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido;R.sub.3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; andR.sub.4 is selected from the group consisting of --OR', --SR', --NR', and --NR'R", wherein R' and R" are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R.sub.Type: GrantFiled: August 28, 1998Date of Patent: November 7, 2000Assignees: The University of North Carolina at Chapel Hill, Inspire Pharmaceuticals, Inc.Inventors: Richard C. Boucher, Jr., Sammy Ray Shaver, William Pendergast, Benjamin Yerxa, Janet L. Rideout, Robert Dougherty, Dallas Croom
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Patent number: 6090941Abstract: Compounds of the formula (I) or salts thereof, ##STR1## wherein the dotted line represents a single or double bond, R.sup.1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group: R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O).sub.n R.sup.8 wherein n is the integer 0, 1 or 2 and R.sup.8 is halo or alkyl or a group NR.sup.9 R.sup.10 are both hydrogen, a group NR.sup.11 R.sup.12 wherein R.sup.11 and R.sup.12 are the same or different and each is hydrogen or alkyl, a group OR.sup.13 wherein R.sup.13 is hydrogen or C.sub.1-4 alkyl substituted by halo; a C.sub.1-4 aliphatic group optionally substituted by a group OR.sup.14 or NR.sup.14 R.sup.15 wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen or alkyl; ot two of R.sup.2 to R.sup.5 are linked together to form a benzp group, one of R.sup.2 to R.sup.3 is a group X--Y--R.sup.16 wherein X is CH.sub.2, NR.sup.17, CO, or S(O).sub.Type: GrantFiled: January 13, 1993Date of Patent: July 18, 2000Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
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Patent number: 6022527Abstract: Compounds of Formula I: ##STR1## wherein: X.sub.1, and X.sub.2 are each independently either O.sup.- or S.sup.- ;X.sub.3 and X.sub.4 are each independently either --H or --OH, with the proviso that X.sub.3 and X.sub.4 are not simultaneously --H;R.sub.1 is selected from the group consisting of O, imido, methylene and dihalomethylene;R.sub.2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido;R.sub.3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; andR.sub.4 is selected from the group consisting of --OR', --SR', --NR', and --NR'R", wherein R' and R" are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R.sub.Type: GrantFiled: July 13, 1999Date of Patent: February 8, 2000Assignees: The University of North Carolina at Chapel Hill, Inspire Pharmaceuticals, Inc.Inventors: Richard C. Boucher, Jr., Sammy Ray Shaver, William Pendergast, Benjamin Yerxa, Janet L. Rideout, Robert Dougherty, Dallas Croom
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Patent number: 5981506Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: January 9, 1998Date of Patent: November 9, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5972904Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: January 9, 1998Date of Patent: October 26, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5968913Abstract: Novel pharmaceutical compositions of uridine 5'-triphosphate (UTP) for use in promoting increased mucociliary clearance of retained mucous secretions of the human airways, middle/inner ears or sinuses are disclosed. Novel Formulation I comprises UTP and aqueous solution having a therapeutic concentration between 5 and 45 mg/mL, a controlled tonicity within the range of 250 to 100 mOsM, a pH between 7.0 and 7.5, and is sterile. The pH-adjusted composition is capable of long-term storage in the refrigerated state with a shelf life of up to 30 months. Formulation I may be delivered therapeutically either in a nebulized form or in a liquid form. Novel Formulation II comprises UTP in an aqueous solution or suspension having a therapeutic concentration approaching the limit of UTP's solubility at ambient temperature. This high concentration allows delivery of a therapeutic amount of UTP in very small volumes (50 to 100 .mu.L) suitable for administration via portable hand-held devices such as metered dose inhalers.Type: GrantFiled: December 23, 1997Date of Patent: October 19, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karol K. LaCroix, Christy L. Shaffer, Karla M. Jacobus, Janet L. Rideout, David J. Drutz, Richard C. Evans, William Pendergast
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Patent number: 5958897Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: January 9, 1998Date of Patent: September 28, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5900407Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5'-triphosphate ?UTP!, dinucleotides, cytidine 5'-triphosphate ?CTP!, adenosine 5'-triphosphate ?ATP!, or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: February 6, 1997Date of Patent: May 4, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 5837861Abstract: The present invention encompasses structures of the formula ##STR1## wherein: X is oxygen, methylene, or difluoromethylene;n=0 or 1;m=0 or 1;n+m=0, 1 or 2; andB and B' are each independently a purine residue or a pyrimidine residue linked through the 9- or 1-position, respectively, provided that compounds disclosed in Table I are excluded. In the instance where B and B' are uracil, attached at the N-1 position to the ribosyl moiety, then the total of m+n may equal 3 or 4 when X is oxygen.The compounds of the present invention are highly selective agonists of the P2Y.sub.2 purinergic receptor, thus, they are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.Type: GrantFiled: February 10, 1997Date of Patent: November 17, 1998Assignee: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Benjamin R. Yerxa, Janet L. Rideout, Suhaib M. Siddiqi
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Patent number: 5789391Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: July 3, 1996Date of Patent: August 4, 1998Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5663337Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.Type: GrantFiled: May 25, 1995Date of Patent: September 2, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5661155Abstract: The present invention relates to bezoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.Type: GrantFiled: May 26, 1995Date of Patent: August 26, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5405851Abstract: The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.Type: GrantFiled: April 16, 1992Date of Patent: April 11, 1995Assignee: Burroughs Wellcome Co.Inventors: William Pendergast, Scott H. Dickerson, Julius V. Johnson, Robert Ferone