Patents Represented by Attorney, Agent or Law Firm John B. Alexander
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Patent number: 8343966Abstract: 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: GrantFiled: January 2, 2009Date of Patent: January 1, 2013Assignee: Novartis AGInventors: Claire Adcock, Urs Baettig, Peter Hunt, Catherine Leblanc, Maude Nadine Pierrette Pipet, Robert Alexander Pulz, Katrin Spiegel, Nikolaus Johannes Stiefl
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Patent number: 8314112Abstract: 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: GrantFiled: January 9, 2009Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
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Patent number: 8309596Abstract: 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: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 8242117Abstract: 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: GrantFiled: November 19, 2010Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
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Patent number: 8242125Abstract: 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: GrantFiled: December 7, 2009Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Gerald David Artman, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
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Patent number: 8211932Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: September 10, 2010Date of Patent: July 3, 2012Assignee: Novartis AGInventors: 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
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Patent number: 8183341Abstract: This invention relates to a novel antibiotic compounds, pharmaceutically acceptable salts and derivatives thereof, and to methods for obtaining such compounds.Type: GrantFiled: December 19, 2007Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Matthew J. Lamarche, Jennifer A. Leeds, Phillipp Krastel, Hans-Ulrich Naegeli
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Patent number: 8143253Abstract: 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: GrantFiled: July 24, 2008Date of Patent: March 27, 2012Assignee: Novartis AGInventors: Dimitrios Lizos, Sven Weiler, Nikolaus Johannes Stiefl
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Patent number: 8119666Abstract: 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: GrantFiled: December 6, 2006Date of Patent: February 21, 2012Assignee: Novartis AGInventors: David Barnes, Gregory Raymond Bebernitz, Gary Mark Coppola, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
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Patent number: 8097617Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: GrantFiled: March 29, 2007Date of Patent: January 17, 2012Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Nils Ostermann, Francois Gessier, Finton Sirockin, Kenji Namoto
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Patent number: 8084448Abstract: 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: GrantFiled: March 29, 2007Date of Patent: December 27, 2011Assignee: Novartis AGInventors: 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
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Patent number: 8058276Abstract: 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: GrantFiled: March 9, 2007Date of Patent: November 15, 2011Assignee: Novartis AGInventors: Guido Bold, Andrea Vaupel, Marc Lang
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Patent number: 8034810Abstract: ?-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: GrantFiled: October 16, 2006Date of Patent: October 11, 2011Assignee: Novartis AGInventors: Werner Breitenstein, Kenji Hayakawa, Genji Iwasaki, Takanori Kanazawa, Tatsuhiko Kasaoka, Shinichi Koizumi, Shinichiro Matsunaga, Motowo Nakajima, Junichi Sakaki
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Patent number: 8030497Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.Type: GrantFiled: January 13, 2005Date of Patent: October 4, 2011Assignee: Novartis AGInventors: Marc Gerspacher, Sven Weiler
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Patent number: 8008479Abstract: 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: GrantFiled: April 11, 2007Date of Patent: August 30, 2011Assignee: Novartis AGInventor: Robert Portman
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Patent number: 7288537Abstract: 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: GrantFiled: March 14, 2003Date of Patent: October 30, 2007Assignee: Novartis AGInventors: Darren Mark Le Grand, Clive McCarthy, Clive Victor Walker, John James Woods
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Patent number: 6830889Abstract: 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: GrantFiled: July 22, 2002Date of Patent: December 14, 2004Assignee: Japan Science and Technology AgencyInventors: Kazuko Matsumoto, Shinji Sueda
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Patent number: 6831190Abstract: 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: GrantFiled: November 22, 2000Date of Patent: December 14, 2004Assignee: Teikoku Chemical Industries Co., Ltd.Inventors: Osamu Kamoda, Hiromichi Fujiwara, Toshiharu Yanagi
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Patent number: 6825223Abstract: 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: GrantFiled: February 21, 2001Date of Patent: November 30, 2004Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
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Patent number: 6825379Abstract: 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: GrantFiled: January 14, 2002Date of Patent: November 30, 2004Assignee: Chemaxz International CorporationInventors: Sien-Chun Chou, Edward K. S. Wang, Chung Ho Wu, Yaw Jong Liu, Ping Chiang