Patents Examined by Robert Gerstl
  • Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
    Patent number: 6518292
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably,  and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: February 11, 2003
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, James J. Li, Jun Li, Stephen G. Swartz
  • 1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders
    Patent number: 6518289
    Abstract: Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: February 11, 2003
    Assignee: Pfizer, Inc.
    Inventors: Justin Stephen Bryans, Thomas Capiris, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
  • Compounds and compositions for treating C1s-mediated diseases and conditions
    Patent number: 6515002
    Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: February 4, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Roger F. Bone, Scott L. Klein, Troy L. Randle
  • Method of preparing retroviral protease inhibitor intermediates
    Patent number: 6515162
    Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: February 4, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John S Ng, Claire S. Przybyla, Shu-Hong Zhang
  • Heterocyclic derivatives for the treatment of diabetes and other diseases
    Patent number: 6515003
    Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: February 4, 2003
    Assignee: Maxia Pharmaceuticals, Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
  • Thiophene substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Patent number: 6515014
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: February 4, 2003
    Assignee: G. D. Searle & Co.
    Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Lu Hwang-Fun
  • Substituted azole derivatives as inhibitors of corticotropin releasing factor
    Patent number: 6515005
    Abstract: The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor (“CRF receptor”) and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: February 4, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gene M. Dubowchik, Dmitry S. Zuev
  • N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
    Patent number: 6515004
    Abstract: The present invention describes compounds of formula I: and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: February 4, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Raj N. Misra, Hai-Yun Xiao
  • Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
    Patent number: 6512121
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: January 28, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
  • Small molecule inhibitors of rotamase enzyme activity
    Patent number: 6509477
    Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: January 21, 2003
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner
  • Process for producing 4-thiazolylmethyl derivative
    Patent number: 6506903
    Abstract: A process for the production of 4-thiazolylmethyl derivatives are provided. A process for the production of the compound represented by the formula (I): wherein R1 is hydrogen or halogen and Hal is halogen, which comprises reacting 4-methylthiazole with N-halosuccinimide in a solvent in the presence of a radical initiator.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: January 14, 2003
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masaaki Uenaka, Masahiko Nagai, Naotake Kobayashi
  • N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of c-proteinase and for treating or preventing disorders related to unregulated collagen production
    Patent number: 6506936
    Abstract: The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: January 14, 2003
    Assignee: FibroGen, Inc.
    Inventor: Wen-Bin Ho
  • Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
    Patent number: 6506782
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: January 14, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly Company
    Inventors: Eugene D. Thorsett, Warren J. Porter, Jeffrey S. Nissen, Lee H. Latimer, James E. Audia, James Droste
  • Substituted thiadiazolesulfonamides
    Patent number: 6503934
    Abstract: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: January 7, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Klaus-Ulrich Weithmann, Swen Hölder
  • Use of spiro compounds as materials in non-linear optics
    Patent number: 6504042
    Abstract: Spiro compounds of the formula I in which &psgr; is C, Si, Ge or Sn and K1 and K2 independently of one another are conjugated systems, are suitable as materials in nonlinear optics.
    Type: Grant
    Filed: October 10, 1996
    Date of Patent: January 7, 2003
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Donald Lupo, Josef Salbeck
  • Pyrrolidine derivatives and processes for preparing same
    Patent number: 6500959
    Abstract: This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: December 31, 2002
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner
  • Bicyclic amino derivatives and PGD2 antagonist containing the same
    Patent number: 6498190
    Abstract: A compound of the formula (I): wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1—X2—X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: December 24, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Akinori Arimura, Tatsuo Tsuri, Junji Kishino, Tsunetoshi Honma
  • Oxazole derivatives, their production and use
    Patent number: 6498179
    Abstract: A novel compound of the formula: wherein R1 is a halogen atom, an optionally substituted heterocyclic, hydroxy, thiol or amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, or an optionally esterified or amidated carboxy group; B is an optionally substituted aromatic group; Y is a divalent aliphatic hydrocarbon group, or a salt thereof, which have an excellent insulin secertion-promoting and blood sugar-depressing effect, and useful in agents for diabetes.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: December 24, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yu Momose, Hiroyuki Odaka
  • Method of preparing a carbamate- or urea-functional compound
    Patent number: 6498266
    Abstract: A method of preparing a carbamate or urea-functional compound is described comprising the step of reacting a lactone or hydroxy carboxylic acid with a compound (A) comprising a carbamate or urea group or a group that can be converted to a carbamate or urea group, and an active hydrogen group capable of reacting with the hydroxy carboxylic acid or in a ring-opening reaction with a lactone. The compound thus prepared is useful in curable compositions.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: December 24, 2002
    Assignee: BASF Corporation
    Inventors: Brian D. Bammel, John D. McGee, Walter H. Ohrbom, Todd A. Seaver, Gregory G. Menovcik, Paul J. Harris, John W. Rehfuss
  • Method for induction of L-selectin shedding
    Patent number: 6498189
    Abstract: The invention provides anti-thiol reagents which inhibit enzyme activity of cell-associated protein disulfide isomerase (PDI) by oxidizing or blocking PDI active site vicinal thiol groups which normally participate in disulfide bond rearrangement of PDI substrates. Inhibition of this PDI function is particularly useful in blocking PDI-mediated entry of HIV or other virions into a host cell, as well as inhibiting lymphocyte traffic through the lymph nodes. The invention further provides an assay for the identification of such PDI inhibitors based on the discovery that inhibitors of the invention also induce shedding of the leucocyte L-selectin adhesion molecule. The invention additionally provides for suppression of inflammation and of lymph node entry by calmodulin antagonists that, like PDI inhibition, cause leukocyte L-selectin shedding.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: December 24, 2002
    Assignee: University of New Mexico
    Inventors: Snezna Rogelj, Teresa A. Bennett, Larry A. Sklar