Patents Represented by Attorney, Agent or Law Firm John B. Alexander
  • Patent number: 8343966
    Abstract: Compounds of formula I in free or salt or solvate form, where T1, T2, X, Ra, Rb, R8 and R9 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: January 2, 2009
    Date of Patent: January 1, 2013
    Assignee: Novartis AG
    Inventors: Claire Adcock, Urs Baettig, Peter Hunt, Catherine Leblanc, Maude Nadine Pierrette Pipet, Robert Alexander Pulz, Katrin Spiegel, Nikolaus Johannes Stiefl
  • Patent number: 8314112
    Abstract: Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: November 20, 2012
    Assignee: Novartis AG
    Inventors: Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
  • Patent number: 8309596
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: November 13, 2012
    Assignee: Novartis AG
    Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
  • Patent number: 8242117
    Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Novartis AG
    Inventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
  • Patent number: 8242125
    Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: August 14, 2012
    Assignee: Novartis AG
    Inventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
  • Patent number: 8211932
    Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: July 3, 2012
    Assignee: Novartis AG
    Inventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
  • Patent number: 8183341
    Abstract: This invention relates to a novel antibiotic compounds, pharmaceutically acceptable salts and derivatives thereof, and to methods for obtaining such compounds.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: May 22, 2012
    Assignee: Novartis AG
    Inventors: Matthew J. Lamarche, Jennifer A. Leeds, Phillipp Krastel, Hans-Ulrich Naegeli
  • Patent number: 8143253
    Abstract: Compounds of formula I in free or salt or solvate form, where R1, R2 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: March 27, 2012
    Assignee: Novartis AG
    Inventors: Dimitrios Lizos, Sven Weiler, Nikolaus Johannes Stiefl
  • Patent number: 8119666
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: February 21, 2012
    Assignee: Novartis AG
    Inventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Patent number: 8097617
    Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: January 17, 2012
    Assignee: Novartis AG
    Inventors: Daniel Kaspar Baeschlin, Nils Ostermann, Francois Gessier, Finton Sirockin, Kenji Namoto
  • Patent number: 8084448
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: December 27, 2011
    Assignee: Novartis AG
    Inventors: Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Patent number: 8058276
    Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
    Type: Grant
    Filed: March 9, 2007
    Date of Patent: November 15, 2011
    Assignee: Novartis AG
    Inventors: Guido Bold, Andrea Vaupel, Marc Lang
  • Patent number: 8034810
    Abstract: ?-Amino hydroxamic acid derivative of the formula I, in which R is C2-C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cycloalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3-C7-alkenyl or C3-C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cycloalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: October 11, 2011
    Assignee: Novartis AG
    Inventors: Werner Breitenstein, Kenji Hayakawa, Genji Iwasaki, Takanori Kanazawa, Tatsuhiko Kasaoka, Shinichi Koizumi, Shinichiro Matsunaga, Motowo Nakajima, Junichi Sakaki
  • Patent number: 8030497
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: October 4, 2011
    Assignee: Novartis AG
    Inventors: Marc Gerspacher, Sven Weiler
  • Patent number: 8008479
    Abstract: A process for preparing compounds of formula (I) or a solvate or hydrate thereof, where R, R1, R2, R3 and R5 have the meanings as indicated in the specification. Such compounds are useful in the treatment of a number of conditions associated with substance P and neurokinin.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: August 30, 2011
    Assignee: Novartis AG
    Inventor: Robert Portman
  • Patent number: 7288537
    Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y, R1, R2, R3, R5, m, n, p and q have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: March 14, 2003
    Date of Patent: October 30, 2007
    Assignee: Novartis AG
    Inventors: Darren Mark Le Grand, Clive McCarthy, Clive Victor Walker, John James Woods
  • Patent number: 6830889
    Abstract: A practically usable DNA detection method by a DNA hybridization method with the use of fluorescent resonance energy transfer wherein the background luminescence based on the luminescence of a donor and the direct excitation of an acceptor) affecting the sensitized luminescence of the acceptor is minimized so that a target DNA strand can be conveniently and very easily detected in a homogeneous solution. In this DNA detection method, a DNA is detected by the DNA hybridization method by using, as detection reagents, streptoavidin labeled with a fluorescent rare earth metal complex, a nucleic acid probe modified with biotin and a nucleic acid probe labeled with an organic cyanine pigment and taking advantage of florescent resonance energy transfer.
    Type: Grant
    Filed: July 22, 2002
    Date of Patent: December 14, 2004
    Assignee: Japan Science and Technology Agency
    Inventors: Kazuko Matsumoto, Shinji Sueda
  • Patent number: 6831190
    Abstract: The invention relates to novel and valuable intermediate compounds of the general formula (VIII) which can be used for the preparation of novel compounds comprising an antibacterial action, especially with a strong antibacterial action against helicobacter pylori, and pharmaceutically acceptable salts thereof. In the general formula (VIII) X is hydrogen or halogen, Y is hydrogen or a substituted or unsubstituted aralkyloxycarbonyl group having 8-19 carbon atoms, Z is hydrogen, a substituted aralkyloxycarbonyl group having 8-19 carbon atoms or a substituted alkoxycarbonyyl group having 2-19 carbon atoms, except that X, Y and Z are all hydrogen.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 14, 2004
    Assignee: Teikoku Chemical Industries Co., Ltd.
    Inventors: Osamu Kamoda, Hiromichi Fujiwara, Toshiharu Yanagi
  • Patent number: 6825223
    Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: November 30, 2004
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
  • Patent number: 6825379
    Abstract: The present invention relates to a method for recovering and producing C4-C6 dicarboxylates from an alkaline waste solution generated in a caprolactam preparation process, in which the alkaline waste solution is treated with sulfuric acid to separate into an aqueous phase and an organic phase, allowing valuable substances contained in the organic phase to be firstly oxidized and converted into dicarboxylic acids. The dicarboxylic acids then undergo concentration, esterification and distillation processes, so as to obtain desirable C4-C6 dicarboxylates with high purity. This therefore provides an efficient and improved method for effectively recovering most valuable substances from the alkaline waste solution, so that economic benefits in recovery are greatly raised.
    Type: Grant
    Filed: January 14, 2002
    Date of Patent: November 30, 2004
    Assignee: Chemaxz International Corporation
    Inventors: Sien-Chun Chou, Edward K. S. Wang, Chung Ho Wu, Yaw Jong Liu, Ping Chiang