Abstract: The present invention is directed to a compound according to formula, (R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1, that act as ligands for one or more of the melanocortin receptors, the pharmaceutically-acceptable salts thereof, to methods of using such peptides to treat mammals and to pharmaceutical compositions useful therefore comprising said peptides.
Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.
Type:
Grant
Filed:
October 7, 2009
Date of Patent:
December 4, 2012
Assignee:
IPSEN Pharma S.A.S.
Inventors:
Michael D. Culler, Zheng Xin Dong, Sun H. Kim, Jacques-Pierre Moreau
Abstract: The present invention provides a novel pyrazolo[3,4-d]pyrimidin-4-one, specifically a derivative of 1-(pyridine-4-yl)-pyrazolo[3,4-d]pyrimidin-4-one. This compound is a kinase inhibitor that shows unexpected anti-proliferative activity against cells, including against tumor cells, and anti-tumor activity in xenograft tumor models. The compound or a suitable salt or prodrug thereof is useful for the treatment of individuals suffering from a cancer or another proliferative disorder or disease.
Abstract: The invention comprises peptidyl analogs of ghrelin having greater stability which are active at the GHS receptor according to formulae depicted below: (R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1 wherein the definitions of A1 to A28, R1 and R2 are provided for in the specification, with the exception that the N-terminal amino acid must be selected from the group consisting of Inp, 1-Apc and 4-Apc, the pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of said compound together with therapeutic and non-therapeutic uses thereof.
Abstract: Oral immunogenic compositions imparting dual protection against enterotoxigenic labile toxin (LT)-expressing Escherichia coli (ETEC) and Vibrio cholerae based on the delivery of recombinant cholera toxin B antigen by attenuated, live bacterial vectors derived from Vibrio cholerae are disclosed. The compositions exhibit dual immunogenicity and retain the ability to colonize gastrointestinal mucosa-associated lymphoid tissues.
Type:
Grant
Filed:
April 24, 2008
Date of Patent:
October 16, 2012
Assignee:
Celldex Therapeutics, Inc.
Inventors:
Kevin P. Killeen, Kenneth L. Roland, Lawrence J. Thomas
Abstract: ADAMTS4 is found to be useful as a blood biomarker for chronic renal failure and also as a therapeutic target for treating chronic renal failure in a human individual. A change in the level of expression of selected genes as disclosed herein in kidney tissue of an individual may also be used to diagnose chronic renal failure in an individual.
Abstract: The invention comprises peptidyl analogs according to formulae (I) or (II) as depicted below: (R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13- A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25- A-26-A27-A28-R1 wherein the definitions of A1 to A28 and R1 to R3 are provided for in the specification for each of formulae (I) and (II), pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of a compound of formula (I), that possess agonist or antagonist ghrelin activity, along with therapeutic and non-therapeutic uses thereof.
Type:
Grant
Filed:
March 28, 2008
Date of Patent:
September 4, 2012
Assignee:
IPSEN Pharma S.A.S.
Inventors:
Zheng Xin Dong, Michael DeWitt Culler, Yeelana Shen, Jeanne Mary Comstock
Abstract: The present invention relates to engineered multivalent and multispecific binding proteins, methods of making, and specifically to their uses in the prevention and/or treatment of acute and chronic inflammatory and other diseases.
Type:
Grant
Filed:
July 2, 2009
Date of Patent:
September 4, 2012
Assignee:
Abbott Laboratories
Inventors:
Chengbin Wu, Tariq Ghayur, Richard W. Dixon, Jochen G. Salfeld
Abstract: The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.
Type:
Grant
Filed:
October 17, 2007
Date of Patent:
August 7, 2012
Assignee:
IPSEN Pharma S.A.S.
Inventors:
Zheng Xin Dong, Yeelana Shen, Michael DeWitt Culler, Christophe Alain Thurieau, Jundong Zhang, Sun Hyuk Kim
Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
Type:
Grant
Filed:
July 15, 2011
Date of Patent:
July 31, 2012
Assignees:
Wayne State University, The Regents of the University of Michigan
Inventors:
Jiri Zemlicka, Shaoman Zhou, John C. Drach
Abstract: Blood biomarkers are described for use in methods and compositions to determine whether an individual has sustained a bone fracture or a cartilage injury.
Type:
Grant
Filed:
April 28, 2008
Date of Patent:
May 22, 2012
Assignee:
Genera Istrazivanja d.o.o.
Inventors:
Lovorka Grgurevic, Boris Macek, Slobodan Vukicevic
Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.
Type:
Grant
Filed:
June 22, 2009
Date of Patent:
May 15, 2012
Assignee:
IPSEN Pharma, S.A.S.
Inventors:
Michael D. Culler, Zheng Xin Dong, Sun H. Kim, Jacques-Pierre Moreau
Abstract: A family of peptides and peptidomimetic compounds useful as GHS analogs according to either formula (I) or (II) as depicted below: or a pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification.
Type:
Grant
Filed:
July 24, 2006
Date of Patent:
March 20, 2012
Assignee:
Ipsen Pharma S.A.S.
Inventors:
Zheng Xin Dong, John S. Eynon, Yeelana Shen
Abstract: Methods and compositions are described to regenerate cartilage in a partial thickness defect or area of reduced volume of articular cartilage comprising an infiltration suppressor agent and a columnar growth promoting agent.
Abstract: The present invention is a novel cytokine protein called IL-12 or Cytotoxic Lymphocyte Maturation Factor (CLMF) which is produced and synthesized by human NC-37 B lymphoblastoid cells (American Type Culture Collection, Rockville, Md.). CLMF synergistically induces with low concentrations of IL-2 the cytolytic activity of Lymphokine Activated Killer (LAK) cells, and CLMF is capable of stimulating T-cell growth. Also claimed are the cloned gene for CLMF, its recombination in a suitable vector, the transformed cells containing said vector, the recombinant protein produced by the transformed cells and antibodies to CLMF.
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
February 7, 2012
Assignee:
Hoffman-La Roche Inc.
Inventors:
Maurice Kent Gately, Ulrich Andreas Gubler, Jeffrey David Hulmes, Frank John Podlaski, Alvin Seth Stern, Richard Anthony Chizzonite, Yu-Ching Eugene Pan
Abstract: The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, untimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.
Type:
Grant
Filed:
December 21, 2004
Date of Patent:
January 17, 2012
Assignee:
Agennix USA Inc.
Inventors:
Nicholas Bockovich, Arthur F. Kluge, Chris Oalmann, Krishna K. Murthi, Siya Ram, Zhongguo Wang, Jianxing Huang
Abstract: A method and pharmaceutical composition for inhibiting the effect of glucocorticoids, particularly dexamethasone, which suppress growth hormone secretion, by administering ghrelin or a ghrelin analogue, for example, [Aib2, Glu3(NH-hexyl)]hGhrelin(1-28)-NH2 (SEQ ID NO:2) or other suitable ghrelin agonist, to counteract the catabolic effects of said dexamethasone and other natural glucocorticoids.
Type:
Grant
Filed:
September 10, 2008
Date of Patent:
December 13, 2011
Assignee:
IPSEN Pharma, S.A.S.
Inventors:
Giovanni Tulipano, Andrea Giustina, Zheng Xin Dong, Michael DeWitt Culler
Abstract: The present invention describes a method or uses of prevention and/or treatment of a cancer or a tumor, and in particular to a combination therapy, methods, compositions and pharmaceutical packages comprising an inhibitor of receptors of the EGFR family or a chemotherapeutically active pyrimidine analogue and certain platinum-based chemotherapeutic agents.
Type:
Grant
Filed:
November 13, 2006
Date of Patent:
November 1, 2011
Assignee:
Agennix AG
Inventors:
Katja Wosikowski-Buters, Christoph Schaab, Marino Schuhmacher, Franz Obermayr, Igor Ivanov
Abstract: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.