Patents Issued in April 6, 2010
  • Modulation of cell fates and activities by phthalazinediones
    Patent number: 7691819
    Abstract: Phthalazinediones that function as intracellular redox modulators are useful in treating cells in various disease states where intracellular redox status is impaired. By buffering aberrant redox states, phthalazinediones enable cellular processes essential for survival and augment medical treatments. The phthalazinediones of the invention can modulate functions related to cell growth, differentiation, activity, or death, to correct aberrations and restore homeostasis, and can serve as adjunctive therapy in treating various disease conditions.
    Type: Grant
    Filed: February 4, 2008
    Date of Patent: April 6, 2010
    Assignee: Bach Pharma, Inc.
    Inventors: Mark O. Henry, William S. Lynn
  • Preparation of thioarabinofuranosyl compounds and use thereof
    Patent number: 7691820
    Abstract: Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: April 6, 2010
    Assignee: Southern Research Institute
    Inventors: John A. Secrist, III, Kamal N. Tiwari, John A. Montgomery, William L Hinds, Jr., legal representative
  • Inhibition of SHIP to enhance stem cell harvest and transplantation
    Patent number: 7691821
    Abstract: The instant invention teaches the inhibition of SHIP expression, or function, for the increased efficacy of autologous stem cell transplants. In another embodiment, interference with SHIP function can be used to temporarily expand and mobilize the hematopoietic stem cell compartment to assist with leukapheresis, to promote hematopoietic recovery after myeloablation treatments, to deplete target stem cell clones (such a leukemic clones and other tumor stem cell types), and to deplete, or damage, the repopulating ability of the endogenous hematopoietic stem cell pool in order to allow transplanted hematopoietic stem cells to better home and engraft and to promote in vivo expansion and mobilization of other organ-specific stem cell populations (e.g., mesenchymal, mammary).
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: April 6, 2010
    Assignee: University of South Florida
    Inventors: Caroline Desponts, Joseph Wahle, John Ninos, William G. Kerr
  • Methods and compositions for treatment of interferon-resistant tumors
    Patent number: 7691822
    Abstract: The present invention provides a method for the treatment of interferon resistant tumors through the use of recombinant vectors encoding interferon species. In particular it is noted that interferon species provided by recombinant vectors possesses properties not associated with the recombinantly produced interferon proteins. The present invention further provides compositions useful in the treatment of interferon resistant tumors using recombinant vectors encoding interferons.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: April 6, 2010
    Assignee: Canji, Inc.
    Inventor: William F. Benedict
  • RIP140 regulation of glucose transport
    Patent number: 7691823
    Abstract: Inhibition of RIP140 increases glucose transport. Compounds that inhibit RIP140 expression or activity are useful for treating disorders associated with aberrant glucose transport (e.g., diabetes), treating obesity, increasing metabolism (e.g., fatty acid metabolism), and increasing brown fat.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: April 6, 2010
    Assignee: University of Massachusetts
    Inventors: Michael P. Czech, Aimee Powelka, Adilson L. Guilherme, Andrew D. Cherniack
  • Compositions and methods for inhibiting expression of a gene from the JC virus
    Patent number: 7691824
    Abstract: The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the JC Virus (JC virus genome), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a gene from the JC Virus. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by JC virus expression and the expression of a gene from the JC Virus using the pharmaceutical composition; and methods for inhibiting the expression of a gene from the JC Virus in a cell.
    Type: Grant
    Filed: April 27, 2007
    Date of Patent: April 6, 2010
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Pamela Tan, Dinah Sah, Birgit Bramlage
  • Adenosine Areceptor agonists
    Patent number: 7691825
    Abstract: The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: April 6, 2010
    Assignee: King Pharmaceuticals Research and Development, Inc.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan R. Moorman, Delia Preti
  • Polysialic acid derivatives
    Patent number: 7691826
    Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: April 6, 2010
    Assignee: Lipoxen Technologies Limited
    Inventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
  • Amide prodrug of gemcitabine, compositions and use thereof
    Patent number: 7691827
    Abstract: The present invention relates to the gemcitabine prodrug 1-(2,2-difluoro-2-deoxy-?-D -ribofuranosyl)-4-(2-propyl-1-oxopentyl)aminopyrimidin-2-one useful as an oral drug for the treatment of cancer.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: April 6, 2010
    Assignee: Eli Lilly and Company
    Inventors: David Michael Bender, David Michael Remick
  • Compositions for ameliorating fecal properties
    Patent number: 7691828
    Abstract: Provided is a fecal condition improving composition containing (a) a compound selected from the group consisting of caffeic acid, chlorogenic acid and ferulic acid, esters thereof, and pharmaceutically acceptable salts thereof, (b) a water-soluble and hardlyfermentable dietary fiber, and (c) a water-soluble and fermentable dietary fiber. The composition of the present invention is useful as a food or beverage, or a pharmaceutical for improving the fecal condition of humans or animals, more specifically, inhibiting intestinal clamping due to imbalance of the autonomic nervous system caused by psychological stress or dietary change, suppressing abdominal pain or discomfort, improving the fecal condition, and ameliorating constipation.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: April 6, 2010
    Assignee: Kao Corporation
    Inventors: Yasushi Shioya, Wataru Okawa, Yasushi Kajihara
  • Composition and method for healing tissues
    Patent number: 7691829
    Abstract: The composition and method for healing tissues is a medicinal composition for facilitating the growth, protection and healing of tissues and cells in animals and humans. The composition is formulated as a either a powder, gel, paste, film, fluid injectable, rehydratable freeze-dried paste or sponge, sprayable solution, topically applied patch with adhesive and reservoir system, an intermediate for coatables such as films and bandages, a matrix for membranes, or as a matrix of flexible polymer(s), or delivered as either an orally ingestible liquid, tablet or capsule. The main ingredient of the formulated compositions is hydrolyzed collagen, which can be combined with polysulfated glycosaminoglycans, hyaluronic acid or salts thereof, or a glucosamine salt, and mixtures thereof. The composition may be formulated as an aqueous eye drop solution.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: April 6, 2010
    Inventors: George D. Petito, Anita M. Petito
  • Method and composition for treatment of a mucosal tissue disorder
    Patent number: 7691830
    Abstract: Methods of treating a subject suffering from a disorder in a mucosal tissue, such as interstitial cystitis; cancer in a mucous membrane such as bladder or vaginal cancer; Crohn's disease; inflammatory bowel disease or colitis, by administering a medicament containing a sulfated chitinous polymer administered topically are described. Pharmaceutical compositions containing the sulfate chitinous polymer are also disclosed.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: April 6, 2010
    Inventors: Clive Elson, Agis Kydonieus, Susan Elizabeth Henderson
  • Pharmaceutical combination and method for treatment of reactive arthritis or bursitis
    Patent number: 7691831
    Abstract: A method for treatment for conditions in human beings associated with either or both reactive arthritis or bursitis comprising administering a combination of a member from each of the following groups of medications: (1) synthetic purine nucleoside analog antiviral drugs, (2) antibiotic drugs, and (3) imidazole drugs. Alternate embodiments of the invention include dual combinations of (A) a member of the synthetic purine nucleoside analog group of antiviral drugs and a member of the antibiotic group of drugs, (B) a member of the antibiotic group of drugs and a member of the imidazole family of drugs, and (C) a member of the synthetic purine nucleoside analog group of antiviral drugs and a member of the imidazole group of drugs.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: April 6, 2010
    Inventors: Ernest L. Bonner, Jr., Robert Hines
  • Methods of treatment of inflammatory diseases
    Patent number: 7691832
    Abstract: Inflammatory bowel diseases are represented by two idiopathic disorders, which include ulcerative colitis and Crohn's disease. Ulcerative colitis is restricted to the colon and involves uncertain and inflammation of the lining (mucosa) of the large intestine. Crohn's disease, on the other hand, can involve the mucosa of the small and/or large intestine and may involve deeper layers of the bowel wall. The present invention contains N-acetylcysteine disposed in a pharmaceutically acceptable carrier for oral or rectal delivery for treating such inflammatory bowel diseases by topical application within the colon.
    Type: Grant
    Filed: February 2, 2006
    Date of Patent: April 6, 2010
    Assignee: The Board of Regents of the University of Oklahoma
    Inventor: Richard F. Harty
  • Compositions and methods for preventing sporadic neoplasia in colon
    Patent number: 7691833
    Abstract: Compositions and methods for preventing sporadic neoplasia of the colon are provided. The compositions provided are based on administration of acetylsalicylic acid.
    Type: Grant
    Filed: March 3, 2003
    Date of Patent: April 6, 2010
    Assignee: Trustees of Dartmouth College
    Inventor: John A. Baron
  • Substance for lowering high cholesterol level in serum and methods for preparing and using the same
    Patent number: 7691834
    Abstract: The invention relates to a substance which lowers LDL cholesterol levels in serum and which is fat soluble ?-sitostanol fatty acid ester, and to a method for preparing and using the same. The substance can be taken orally as a food additive, food substitute or supplement. A daily consumption of the ?-sitostanol ester in an amount between about 0.2 and about 20 g/day has been shown to reduce the absorption of biliary and endogenic cholesterol.
    Type: Grant
    Filed: August 11, 2005
    Date of Patent: April 6, 2010
    Assignee: Raisio Nutrition Ltd.
    Inventors: Tatu Miettenen, Hannu Vanhanen, Ingmar Wester
  • Formulations
    Patent number: 7691835
    Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: April 6, 2010
    Assignee: Hollis-Eden Pharmaceuticals, Inc.
    Inventor: James M. Frincke
  • Progesterone receptor modulators
    Patent number: 7691836
    Abstract: The subject invention provides a compound according to Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: April 6, 2010
    Assignee: N.V. Organon
    Inventors: Johannes Antonius Maria Hamersma, Johannes Bernardus Maria Rewinkel
  • Pyrrole derivatives as antimycobacterial compounds
    Patent number: 7691837
    Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: April 6, 2010
    Assignee: Lupin Limited
    Inventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
  • Method for treating diseases using HSP90-inhibiting agents in combination with antimitotics
    Patent number: 7691838
    Abstract: The present invention provides a method for treating cancer. The method involves the administration of an HSP90 inhibitor and an antimitotic, where the combined administration provides a synergistic effect. In one aspect of the invention, a method of treating cancer is provided where a subject is treated with a dose of an HSP90 inhibitor in one step and a dose of an antimitotic in another step. In another aspect of the invention, a method of treating cancer is provided where a subject is first treated with a dose of an HSP90 inhibitor and subsequently treated with a dose of an antimitotic. In another aspect of the invention, a method of treating cancer is provided where a subject is first treated with a dose of an antimitotic and subsequently treated with a dose of an HSP90 inhibitor.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: April 6, 2010
    Assignee: Kosan Biosciences Incorporated
    Inventors: Robert Johnson, Jr., Yiqing Zhou, Thomas Müller
  • Methods and compositions for blocking platelet and cell adhesion, cell migration and inflammation
    Patent number: 7691839
    Abstract: The present invention provides compositions of saratin and methods of use thereof. One aspect of the invention is a method of prevention or mitigation of the development of adhesions, keloids and scars. The adhesions, keloids and scars can be due to surgery, such as plastic surgery or orthopedic surgery, or can be pre-existing scars. Another aspect of the invention is a method for treatment of flexor tendon injuries.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: April 6, 2010
    Assignee: Biovascular, Inc.
    Inventor: Paul F. Glidden
  • Analogs of benzoquinone-containing ansamycins and methods of use thereof
    Patent number: 7691840
    Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: April 6, 2010
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright
  • Azetidine derivatives as CCR-3 receptor antagonist
    Patent number: 7691841
    Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: April 6, 2010
    Assignee: Novartis AG
    Inventor: Darren M Legrand
  • Tricyclic 6-alkylidene-penems as ?-lactamase inhibitors
    Patent number: 7691842
    Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof, wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is O.
    Type: Grant
    Filed: August 7, 2008
    Date of Patent: April 6, 2010
    Assignee: Wyeth LLC
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
  • N-hydroxyamide derivatives possessing antibacterial activity
    Patent number: 7691843
    Abstract: Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: April 6, 2010
    Assignee: Pfizer Inc.
    Inventors: Bore G. Raju, Hardwin O'Dowd, Hongwu Gao, Dinesh V. Patel, Jaoquim Trias
  • Nonpeptide substituted spirobenzoazepines as vasopressin antagonists
    Patent number: 7691844
    Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: April 6, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. K. Chen, Min A. Xiang
  • Anti-inflammatory agents
    Patent number: 7691845
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or (I?), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.
    Type: Grant
    Filed: August 10, 2005
    Date of Patent: April 6, 2010
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
    Patent number: 7691846
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: March 10, 2009
    Date of Patent: April 6, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Method of treating neurological diseases and disorders
    Patent number: 7691847
    Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.
    Type: Grant
    Filed: October 17, 2003
    Date of Patent: April 6, 2010
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Gideon Dreyfuss, Jin Wang
  • Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists
    Patent number: 7691848
    Abstract: This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment utilizing these compounds.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: April 6, 2010
    Assignee: Wyeth
    Inventors: Amedeo A. Failli, Dominick Quagliato, Patrick Andrae, Gavin D. Heffernan, Richard D. Coghlan, Emily S. Shen
  • Carboxamidine derivatives and their use in the treatment of vascular diseases
    Patent number: 7691849
    Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions comprising the same, and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: April 6, 2010
    Assignee: CytRx Corporation
    Inventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
  • Antibacterial agents
    Patent number: 7691850
    Abstract: Compounds of formula (I) and derivatives thereof: compositions containing them, their preparation and their use as antibacterials.
    Type: Grant
    Filed: June 15, 2005
    Date of Patent: April 6, 2010
    Assignee: Glaxo Group Limited
    Inventors: William Henry Miller, Israil Pendrak, Mark Andrew Seefeld
  • Metalloprotease inhibitors containing a heterocyclic moiety
    Patent number: 7691851
    Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a modified benzoxazine moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: April 6, 2010
    Assignee: Alantos Pharmaceuticals Holding, Inc.
    Inventors: Christian Gege, Arthur Taveras
  • Compounds for enzyme inhibition
    Patent number: 7691852
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: April 6, 2010
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Pyrazole compounds useful as protein kinase inhibitors
    Patent number: 7691853
    Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: April 6, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies, Pan Li, Marion W. Wannamaker, Cornelia J. Forster, Albert C. Pierce
  • Dihydropyridine derivatives for use as human neutrophil elastase inhibitors
    Patent number: 7691854
    Abstract: The invention relates to novel dihydropyridine derivatives, of Formula (I) processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
    Type: Grant
    Filed: August 18, 2003
    Date of Patent: April 6, 2010
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
  • Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives
    Patent number: 7691855
    Abstract: The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: April 6, 2010
    Assignee: Novartis AG
    Inventors: Pascal Furet, Patricia Imbach, Timothy Michael Ramsey, Achim Schlapbach, Dieter Scholz, Giorgio Caravatti
  • Thiadiazoledioxides and thiadiazoleoxides as CXC- and CC-chemokine receptor ligands
    Patent number: 7691856
    Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: April 6, 2010
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Arthur G. Taveras, Jianhua Chao, Purakkattle J. Biju, Younong Yu, Cynthia J. Aki, J. Robert Merritt, Ge Li, John J. Baldwin, Gaifa Lai, Minglang Wu, Evan A. Hecker
  • Muscarinic agents as therapeutic compounds
    Patent number: 7691857
    Abstract: Muscarinic agonists of the formula (I) with M1 selectivity which are useful as agents for stimulating the cognitive functions of the brain.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: April 6, 2010
    Assignee: Muscagen Limited
    Inventors: Maxime Buffat, James Eric Thomas, Harvard Robin Davies
  • Kinase inhibitors and methods of use thereof
    Patent number: 7691858
    Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as uveitis, retinopathies or macular degeneration, macular edema or other vitreoretinal diseases, inflammatory diseases such as autoimmune diseases, vascular leakage syndrome, edema, or diseases involving leukocyte activation, transplant rejection, respiratory diseases such as asthma, adult or acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease, and the like.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: April 6, 2010
    Assignee: TargeGen, Inc.
    Inventors: John Doukas, Chi Ching Mak, Elena Dneprovskaia, Glenn Noronha
  • Prenyl transferase inhibitors
    Patent number: 7691859
    Abstract: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: April 6, 2010
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Thomas D. Gordon, Barry A. Morgan
  • Sulfonamide derivatives
    Patent number: 7691860
    Abstract: The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substituent(s) with at least one of them meaning the methine group; E means a group represented by the following formulae (E1): R1 means a lower alkyl group or an aryl group optionally having a substituent(s) or means a lower alkylene group linked to arbitrary, linkable position(s) of E, and others. The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.
    Type: Grant
    Filed: February 15, 2005
    Date of Patent: April 6, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Norikazu Otake, Yoshio Ogino, Akio Kanatani
  • Indolymaleimide derivatives
    Patent number: 7691861
    Abstract: A compound of formula I wherein R, Ra, Rb, Rc, Rd and Re are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 19, 2005
    Date of Patent: April 6, 2010
    Assignee: Novartis AG
    Inventors: Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou
  • Method and composition for treating periodontal disease
    Patent number: 7691862
    Abstract: The present invention is directed to a pharmaceutical composition comprising a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. A suitable antibiotic is selected from the group consisting of doxycycline, gentamicin, tobramicin, ciprofloxacin, clindamycin, clarithromycin, azithromycin and metronidazole. Preferred antibiotics are doxycycline and ciprofloxacin. More preferably, the antibiotic is doxycycline. In its second aspect, the present invention is directed to a method for treating periodontal disease in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. Typically, the mammalian patient is a human.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: April 6, 2010
    Assignee: Regena Therapeutics LC
    Inventors: Frank Wingrove, Rex McKee
  • Pyrazine-2-carboxamide derivatives as CB2 receptor modulators
    Patent number: 7691863
    Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB2 receptors.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: April 6, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michel Dietz, Sabine Gruener, Paul Hebeisen, Sylvie C. Meyer Reigner, Matthias Nettekoven, Bernd Puellmann, Stephan Roever, Christoph Ullmer
  • Anti-hypertensive composition and methods of treatment
    Patent number: 7691864
    Abstract: Pharmaceutical compositions for the treatment of hypertension comprising an effective anti-hypertensive amount of at least one compound in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound having one of the formulae (I), (II), (III) or (IV), and methods for the treatment of hypertension or effecting anti-hypertensive action which comprises administering to a patient requiring anti-hypertensive therapy or effect at least one of the above-described compounds.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: April 6, 2010
    Assignee: University of Florida
    Inventor: Raymond J. Bergeron, Jr.
  • Pyrazolopyridines and methods of making and using the same
    Patent number: 7691865
    Abstract: Compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: April 6, 2010
    Assignee: Biogen Idec MA Inc.
    Inventors: Wen-Cherng Lee, Mary Beth Carter, Lihong Sun, Paul Lyne, Claudio Chuaqui, Zhongli Zheng, Juswinder Singh, Paula Boriack-Sjodin
  • 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines and methods of their use as inhibitors of Raf kinase
    Patent number: 7691866
    Abstract: New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: April 6, 2010
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian
  • Chemical compounds
    Patent number: 7691867
    Abstract: Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to process for their preparation, as well as pharmaceutical compositions containing them as active ingredient.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: April 6, 2010
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Georges Rene Pasquet, Andrew Austen Mortlock, Frederic Henri Jung
  • Thiazolyl-dihydro-quinazoline
    Patent number: 7691868
    Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: April 6, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Trixi Brandl, Udo Maier, Matthias Hoffmann, Stefan Scheuerer, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Christoph Hoenke, Klaus Erb, Michael Pieper, Ingo Pragst