Abstract: The present invention relates to a new process for the preparation of new crystal modifications of esomeprazole non-salt form. Further, the present invention also relates to the use of said new crystal modifications for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the crystal modifications, as such.
Abstract: The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Type:
Grant
Filed:
September 8, 2008
Date of Patent:
February 21, 2012
Assignee:
AstraZeneca AB
Inventors:
Yun-Xing Cheng, Xuehong Luo, Vijayaratnam Santhakumar, Miroslaw Jerzy Tomaszewski
Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.
Type:
Grant
Filed:
June 23, 2009
Date of Patent:
February 21, 2012
Assignee:
AstraZeneca AB
Inventors:
Jonas Brånalt, David Gustafsson, Ingemar Nilsson, Magnus Polla
Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.
Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
Type:
Grant
Filed:
May 7, 2007
Date of Patent:
February 14, 2012
Assignee:
AstraZeneca AB
Inventors:
Peter Hansen, Marianne Ivarsson, Karolina Lawitz, Hans Lönn, Antonios Nikitidis, Asim Ray
Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
Type:
Application
Filed:
August 5, 2011
Publication date:
February 9, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Robert Bruce DIEBOLD, Thomas GERO, Paul GROVER, Shan HUANG, Stephanos IOANNIDIS, Claude Afona OGOE, Jamal Carlos SAEH, Jeffrey Gilbert VARNES
Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.
Type:
Application
Filed:
October 14, 2011
Publication date:
February 9, 2012
Applicant:
AstraZeneca AB
Inventors:
Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
Abstract: (5R)-3-[4-[1-[(2S)-2,3-dihydroxypropanoyl]-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluoro-phenyl]-5-(isoxazol-3-yloxymethyl)oxazolidin-2-one, or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, for use in the treatment of Mycobacterium tuberculosis.
Type:
Application
Filed:
March 16, 2010
Publication date:
February 9, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Kaveri Das, David Alan Melnick, Shandil Radha
Abstract: 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described.
Abstract: Disclosed herein are compounds of formula I in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
Type:
Grant
Filed:
April 30, 2010
Date of Patent:
February 7, 2012
Assignee:
AstraZeneca AB
Inventors:
Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Bjorn Christian Ingvar Lofberg, Joachim Persson
Abstract: The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.
Type:
Application
Filed:
August 2, 2011
Publication date:
February 2, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Brian AQUILA, Victor KAMHI, Bo PENG, Timothy PONTZ, Jamal Carlos SAEH, Kumar THAKUR, Bin YANG
Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.
Abstract: A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer.
Type:
Grant
Filed:
July 24, 2009
Date of Patent:
January 31, 2012
Assignee:
AstraZeneca AB
Inventors:
Mark Ebden, Premji Meghani, Colin Bennion, Anthony Ronald Cook, Roger Victor Bonnert
Abstract: A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.
Type:
Application
Filed:
July 19, 2011
Publication date:
January 26, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Armelle Marie-Laudine JANIN, Philip Alexander MACFAUL, Rachel Marie PUGH, Emily Jane ROBERTS, Ian Alun NASH
Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
Type:
Application
Filed:
December 11, 2009
Publication date:
January 26, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Shahul Hameed Peer Mohamed, David Waterson
Abstract: The invention concerns pyrazine derivatives of the Formula I or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions.
Type:
Application
Filed:
January 18, 2011
Publication date:
January 26, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Tao FENG, Hitesh Jayantilal SANGANEE, Hiroki WADA
Abstract: The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, and to new intermediates prepared in said process suitable for large scale manufacturing of said compound.
Type:
Grant
Filed:
April 17, 2008
Date of Patent:
January 24, 2012
Assignee:
AstraZeneca AB
Inventors:
Vern Delisser, Martin Hedberg, Annette Jansson, Andreas Rådevik, Per Ryberg, Swantje Thiering
Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I), methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
Type:
Grant
Filed:
October 10, 2008
Date of Patent:
January 24, 2012
Assignee:
AstraZeneca AB
Inventors:
Richard William Arthur Luke, Zbigniew Stanley Matusiak