Patents Examined by Sabiha N. Qazi
  • Active ingredient combinations having insecticidal and acaricidal properties
    Patent number: 8841294
    Abstract: The invention relates to insecticidal and acaricidal mixtures comprising certain cyclic ketoenols and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.
    Type: Grant
    Filed: January 6, 2005
    Date of Patent: September 23, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Glucocorticoid receptor agonists
    Patent number: 8822439
    Abstract: This invention relates to novel glucocorticoid receptor agonists of formula (I): and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: September 2, 2014
    Assignee: Pfizer Inc.
    Inventors: Paul Alan Glossop, David Simon Millan, David Anthony Price
  • Oligomer-corticosteroid conjugates
    Patent number: 8796248
    Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: August 5, 2014
    Assignee: Nektar Therapeutics
    Inventors: Wen Zhang, Jennifer Riggs-Sauthier, J. Milton Harris, Michael D. Bentley
  • 9, 10-secopregnane derivative and pharmaceutical
    Patent number: 8796246
    Abstract: A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: August 5, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Hiroki Fujieda, Hironori Otsu, Shoji Yasufuku, Masaaki Shirai
  • Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
    Patent number: 8796278
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: August 5, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • 11?-hydroxyandrosta-4-ene-3-ones
    Patent number: 8785425
    Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 22, 2014
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Samir Rameshchandra Shah, Sanjay Nandlal Mandhane, Trinadha Rao Chitturi, Rajamannar Thennati
  • A-ring modified 19-nor-vitamin D analogs and their uses
    Patent number: 8785422
    Abstract: Disclosed are 19-nor-vitamin D compounds, and specifically seco-A-2,19-dinor-1,25-dihydroxyvitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high activity in vivo, specifically in intestinal tissues, but relatively low VDR binding activity, cell differentiation activity and gene transcription activity. There is thus potential for these compounds to have strong cell selectivity for use as therapeutic agents against some cancers, such as colon cancer or polyps, as well as hyperplastic intestinal disorders, such as Crohn's disease, ulcerative colitis and celiac disease. These compounds also have relatively high intestinal calcium transport activity evidencing potential in the treatment of bone diseases.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 22, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Agnieszka Glebocka
  • Betulinic acid derivatives and methods of use thereof
    Patent number: 8778990
    Abstract: This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: July 15, 2014
    Assignees: Trustees of Dartmouth College, Reata Pharmaceuticals, Inc.
    Inventors: Tadashi Honda, Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Robert M. Kral, Jr., Melean Visnick
  • Ship 1 modulators
    Patent number: 8765994
    Abstract: The present invention includes the use of pelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIP 1 activity. This invention also provides novel terpene compounds capable of modulating SHIP 1 activity and methods of synthesis thereof.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: July 1, 2014
    Assignee: The University of British Columbia
    Inventors: Raymond Andersen, David E. Williams, Alice Mui, Christopher Ong, Gerald Krystal, Lu Yang
  • Once-a-week administration of 25-hydroxy vitamin Dto sustain elevated steady-state pharmacokinetic blood concentration
    Patent number: 8759328
    Abstract: An oral dosage form comprising a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days and a pharmaceutically suitable oral carrier system, wherein subsequent single doses at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 24, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. Deluca, Lori A. Plum, Margaret Clagett-Dame
  • Stereoselective synthesis of vitamin D analogues
    Patent number: 8759555
    Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: June 24, 2014
    Assignee: Leo Pharma A/S
    Inventors: Thomas Peter Sabroe, Martin John Calverley
  • Substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives, preparation and therapeutic use thereof
    Patent number: 8754095
    Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: June 17, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Anti-diabetic compounds
    Patent number: 8741882
    Abstract: The preset invention relates to a new oral anti-diabetic compound prepared by synthesizing a steroid and a guanide or biguanide, which is eliminated via the hepatic route, instead of the renal route, to avoid adverse effects of administering metformin in diabetic patients with renal dysfunction. A pharmaceutical composition comprising the compound of the invention and the method for treating diabetes using the compound are also provided.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: June 3, 2014
    Assignee: Sen Capital, LLC.
    Inventor: John Soong
  • Substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides, preparation and therapeutic use thereof
    Patent number: 8735385
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • 3-desoxy-2-methylene-vitamin D analogs and their uses
    Patent number: 8729054
    Abstract: This invention discloses 3-desoxy-2-methylene-vitamin D analogs, and specifically (20S)-3-desoxy-1?,25-dihydroxy-2-methylene-vitamin D3 and (20R)-3-desoxy-1?,25-dihydroxy-2-methylene-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: May 20, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Rafal R. Sicinski, Izabela Sibilska
  • N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same
    Patent number: 8648096
    Abstract: This invention relates to N-methylaminomethyl isoindole compounds. Pharmaceutical compositions comprising the compounds and methods for treating, preventing and managing various disorders are also disclosed.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: February 11, 2014
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Roger Shen-Chu Chen
  • 1-desoxy-2-methylene-19-nor-vitamin D analogs and their uses
    Patent number: 8642579
    Abstract: This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 4, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Katarzyna M. Barycka, Izabela Sibilska, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki, Rafal R. Sicinski, Katarzyna Plonska-Ocypa
  • 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin Dand their uses
    Patent number: 8614202
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: December 24, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
  • Sulfonamide derivatives of polycyclic dyes used for analytical applications
    Patent number: 8614317
    Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: December 24, 2013
    Assignee: Atto-Tec GmbH
    Inventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
  • 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs
    Patent number: 8609643
    Abstract: This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-19,26-dinor-1?,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: December 17, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Margaret Clagett-Dame, Lori A. Plum, Grazia Chiellini, Pawel Grzywacz