Chalcogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/252)
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Publication number: 20110152291Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: March 1, 2011Publication date: June 23, 2011Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. AYDT, Remo Kranich, Anke S. Busemann
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Patent number: 7960422Abstract: Compounds of formula (I) wherein R1 is as well as pharmaceutically acceptable salts, hydrates and/or enantiomers thereof are useful as compounds that exhibit activity at metabotropic glutamate receptors.Type: GrantFiled: October 17, 2008Date of Patent: June 14, 2011Assignee: AstraZeneca ABInventors: Erwan Arzel, Louise Edwards, Methvin Isaac, Donald A. McLeod, Abdelmalik Slassi, Tao Xin
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Patent number: 7960417Abstract: The present invention is directed to benzazole compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: February 17, 2006Date of Patent: June 14, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Steven P. Govek, Jean-Michel Vernier, Theodore Kamenecka, John H. Hutchinson, Richard Pracitto
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Publication number: 20110136881Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 9, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 7947842Abstract: The invention relates to hydrates of pharmaceutically acceptable alkaline-earth salts of irbesartan and to their preparation in an aqueous medium.Type: GrantFiled: December 5, 2007Date of Patent: May 24, 2011Assignee: Sanofi-AventisInventors: Alain Aulombard, Philippe Mercey
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Publication number: 20110105460Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Publication number: 20110105749Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 14, 2010Publication date: May 5, 2011Inventors: Weiwen YING, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
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Publication number: 20110105539Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.Type: ApplicationFiled: March 19, 2009Publication date: May 5, 2011Applicant: LEK Pharmaceuticals D.D.Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
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Publication number: 20110098481Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.Type: ApplicationFiled: November 2, 2010Publication date: April 28, 2011Applicants: ASAHI GLASS COMPANY, LIMITED, KAKEN PHARMACEUTICAL CO., LTD.Inventors: Takahiko MURATA, Masahiro AMAKAWA, Shin TERADAIRA, Yasushi MATSUMURA, Katsuhiko KONISHI
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Patent number: 7923566Abstract: The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.Type: GrantFiled: December 21, 2005Date of Patent: April 12, 2011Assignee: Suven Life Sciences LimitedInventors: Arava Veera Reddy, Siripalli Udaya Bhaskara Rao, Chinnapillai Rajendiran, Venkateswarlu Jasti
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Patent number: 7919506Abstract: Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: April 5, 2011Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry, Dongxiang Zeng
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Publication number: 20110077273Abstract: The present invention relates to compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A, B, R1, R2, R3, R4, R5, n, m and p have the significance defined herein.Type: ApplicationFiled: September 20, 2010Publication date: March 31, 2011Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Markus Rudolph, Sven Taylor
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Patent number: 7915425Abstract: The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.Type: GrantFiled: December 21, 2005Date of Patent: March 29, 2011Assignee: Suven Life Sciences LimitedInventors: Arava Veera Reddy, Siripalli Udaya Bhaskara Rao, Chinnapillai Rajendiran, Venkateswarlu Jasti
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Publication number: 20110053901Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.Type: ApplicationFiled: February 13, 2009Publication date: March 3, 2011Applicants: SIGNUM BIOSCIENCES, INC., Signum Biosciences, Inc.Inventors: Seung-Yub Lee, Michael Voronkov, Peter Wolanin
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Patent number: 7897784Abstract: The present invention provides processes for preparing a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein A is a pyrrole, tetrazole or triazole ring.Type: GrantFiled: November 24, 2009Date of Patent: March 1, 2011Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 7884211Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: July 24, 2009Date of Patent: February 8, 2011Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Publication number: 20100311789Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.Type: ApplicationFiled: June 3, 2009Publication date: December 9, 2010Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Patent number: 7816538Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: July 24, 2009Date of Patent: October 19, 2010Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20100261772Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.Type: ApplicationFiled: May 24, 2010Publication date: October 14, 2010Inventors: Jing Fang, Dennis Heyer, Subba Reddy Katamreddy, Kenneth William Batchelor, Richard Dana Caldwell
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Publication number: 20100222597Abstract: The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.Type: ApplicationFiled: December 21, 2005Publication date: September 2, 2010Applicant: Suven Life Sciences LimitedInventor: Arava Veera Reddy
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Patent number: 7776896Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: GrantFiled: March 27, 2008Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: William Guilford, Werner Skuballa, Daryl H. Faulds, Monica Kochanny, Wheeseong Lee, Bernd Radüchel
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Publication number: 20100190996Abstract: The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.Type: ApplicationFiled: December 21, 2005Publication date: July 29, 2010Applicant: Suven Life Sciences, LtdInventors: Arava Veera Reddy, Siripalli Udaya Bhaskara Rao, Chinnapillai Rajendrian, Vankateswarlu Jasti
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Patent number: 7741352Abstract: This invention relates to novel compounds useful as modulators of the KCNQ channel, to pharmaceutical compositions comprising these compounds, and to methods of treatment herewith.Type: GrantFiled: March 11, 2004Date of Patent: June 22, 2010Assignee: Neurosearch A/SInventors: William Dalby Brown, Lene Teuber, Bjarne H. Dahl
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Publication number: 20100152260Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: January 12, 2010Publication date: June 17, 2010Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20100152458Abstract: The present invention relates to a process for the manufacture of intermediates that may be used for the manufacture of ARBs (also called angiotension II receptor antagonists or AT1 receptor antagonists) comprising as a common structural feature a tetrazole ring.Type: ApplicationFiled: March 2, 2010Publication date: June 17, 2010Inventors: Christoph Krell, Hans Hirt
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Publication number: 20100144809Abstract: This invention relates to novel benzamidine derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. A stereoisomer or a mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically-acceptable addition salt thereof, wherein B may be absent (i.e. no heterocyclic ring is formed); and when absent, the nitrogen next to B holds a hydrogen (i.e. “NH”), and A represents NH2 or OH; or B may be present (i.e. forms part of a heterocyclic ring); and when present, B represents C?O or C?S; and A represents NH or O; and wherein the rest of variables are as specified in claim 1.Type: ApplicationFiled: May 7, 2008Publication date: June 10, 2010Applicant: Neuro Search A/SInventors: Antonio Nardi, Joachim Demnitz, Morten Grunnet, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Publication number: 20100137347Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: January 21, 2008Publication date: June 3, 2010Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100113449Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Publication number: 20100105689Abstract: This invention relates to novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazole derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.Type: ApplicationFiled: January 17, 2008Publication date: April 29, 2010Inventors: Antonio Nardi, Morten Grunnet, Joachim Demnitz, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Patent number: 7700784Abstract: The present invention relates to a process for the manufacture of intermediates that may be used for the manufacture of ARBs (also called angiotension II receptor antagonists or AT1 receptor antagonists) comprising as a common structural feature a (1H-tetrazol-5-yl)-biphenyl ring.Type: GrantFiled: February 1, 2005Date of Patent: April 20, 2010Assignee: Novartis AGInventors: Christoph Krell, Hans Hirt
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Publication number: 20100087496Abstract: This invention relates to novel cinnamic amide derivatives that are found to be potent modulators of ion channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of ion channels.Type: ApplicationFiled: December 17, 2007Publication date: April 8, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Morten Grunnet, Joachim Demnitz, Thomas Diness Jensen, Palle Christophersen, David Spencer Jones, Elsebet Ostergaard Nielsen, Dorte Strobaek, Lars Siim Madsen
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Publication number: 20100081643Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: September 21, 2009Publication date: April 1, 2010Inventors: BRETT C. BOOKSER, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Publication number: 20100048664Abstract: Disclosed herein is a compound represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 17, 2009Publication date: February 25, 2010Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20100029735Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.Type: ApplicationFiled: January 22, 2008Publication date: February 4, 2010Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20100016383Abstract: Compounds of formula wherein A0 is a bond or a C1-C6alkylene bridge; A1, A2 and A3 are a C1-C6alkylene bridge; D is CH or N; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is a bond or, for example, O, NH, S, SO or SR2; Q is, for example, O, S, SO or SO2; Y is, for example, O, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN or nitro; R4 is, for example, H, halogen, OH, SH, CN, nitro or C1-C6alkyl; R5 is, for example, H, CN, OH, C1-C6alkyl or C3-C8cycloalkyl; k is 1, 2 or 3 when D is nitrogen; or is 1, 2, 3 or 4 when D is CH; m is 1 or 2; E is heteroaryl which is unsubstituted or substituted—depending upon the substitutions possible on the ring—by from one to four identical or different substituents selected from R10; and R10 is, for example, halogen, CN, NO2, OH, SH or C1-C6alkyl; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free formType: ApplicationFiled: September 23, 2009Publication date: January 21, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Arthur Steiger, Peter Renold, Stephan Trah, Roger Graham Hall
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Publication number: 20100008956Abstract: Compositions comprising a Carboxylic Acid Losartan in a dosage form are provided. Such compositions may be employed for treatment of hypertension, congestive heart failure, diabetic nephropathy, and myocardial infarction. The compositions may further include one or more additional therapeutic agents based on the condition to be treated.Type: ApplicationFiled: July 8, 2008Publication date: January 14, 2010Inventor: Jie Du
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Patent number: 7638541Abstract: Compounds, compositions, and methods relating to 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine or a pharmaceutically acceptable salt thereof are provided for the treatment of Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: December 26, 2007Date of Patent: December 29, 2009Assignee: Metabolex Inc.Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christoper J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
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Publication number: 20090306397Abstract: The novel process for preparing substituted azoles allows compounds of the general formula (I) and/or their salts and/or their acid addition compounds in which the substituents R1 and R2, A and B are as defined in the description to be prepared in good yield and in a simple, economically favourable manner.Type: ApplicationFiled: May 27, 2006Publication date: December 10, 2009Inventors: Rainer Bruns, Hermann Uhr, Erasmus Vogl
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Publication number: 20090270367Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: ApplicationFiled: March 3, 2009Publication date: October 29, 2009Inventors: Varghese JOHN, Michel MAILLARD, John TUCKER, Jose AQUINO, Barbara JAGODZINSKA, Louis BROGLEY, Jay TUNG, Simeon BOWERS, Darren DRESSEN, Gary PROBST, Neerav SHAH
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Publication number: 20090247510Abstract: The present invention relates to the use of irbesartan for the preparation of medicinal products that are useful for preventing or treating pulmonary arterial hypertension or pulmonary hypertension.Type: ApplicationFiled: June 3, 2009Publication date: October 1, 2009Inventors: Sylvie Cosnier-Pucheu, Dino Nisato, Alain Roccon
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Publication number: 20090240060Abstract: A process for the manufacturing of a pure irbesartan comprising converting irbesartan or a protected derivative thereof into an isolated hydrohalide acid addition salt, whereupon said hydrohalide acid addition salt is converted into the irbesartan is described.Type: ApplicationFiled: April 4, 2007Publication date: September 24, 2009Inventor: Lovro Selic
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Publication number: 20090215756Abstract: The invention relates, in general, to new formulations and dosage units containing losartan and/or its salts (e.g., losartan potassium) that are useful for the therapeutic treatment (including prophylactic treatment) of mammals, including humans, and a process for making the same. The process generally includes (i) mixing and blending losartan potassium and a first portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the mixture of step (i); (ii) compacting the mixture obtained in step (i) to form an agglomerate; (iii) breaking apart the agglomerate in order to obtain a granulate; (iv) adding lactose monohydrate and a second portion of at least one of pre-gelatinized starch, microcrystalline cellulose and magnesium stearate to the granulate and blending; and (v) tableting the granulate mixture into tablets. The process can further include coating the prepared tablets with a suitable coating material.Type: ApplicationFiled: May 17, 2006Publication date: August 27, 2009Applicant: COMBINO PHARM, S.L.Inventor: Sergio Lloret Perez
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Patent number: 7576112Abstract: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.Type: GrantFiled: February 17, 2009Date of Patent: August 18, 2009Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7572753Abstract: The use of certain tetrazole compounds as fungicides is disclosed wherein said compounds are of the structural formula: wherein: R is selected from the group consisting of phenyl groups of the structural formula: and thienyl groups of the structural formula: and X and Y are each selected from the group consisting of hydrogen, haloalkyl, halogen, and nitro. Novel compounds wherein X is selected from the group consisting of haloalkyl, halogen, and nitro and Y is selected from the group consisting of hydrogen, haloalkyl, halogen, and nitro are also disclosed.Type: GrantFiled: September 15, 2005Date of Patent: August 11, 2009Assignee: Chemtura CorporationInventors: Mark A. Dekeyser, Ahmad Ghavami, Robert G. Davis, Sheldon B. Park, Steven J. Hobbs, Clifford Pratt, Gaik-Lean Chee, Daniel Walther
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Publication number: 20090192318Abstract: From the starting 4-bromomethyl-2?-(1-triphenylmethyltetrazol-5-yl)biphenyl, N-[(2?(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester of formula 7 is obtained via a reaction with L-valine benzyl ester, and is converted to valsartan of formula I via a reaction with valeryl chloride and removing of protective groups. The method consists in converting, with hydrochloric acid, N-[(2?-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester of formula 7, obtained in the first stage, to N-[(2?-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester hydrochloride of formula III, which is optionally re-crystallized.Type: ApplicationFiled: May 14, 2004Publication date: July 30, 2009Applicant: Zentiva, A.S.Inventors: Stanislav Radl, Jan Stach, Eva Dedinova
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Patent number: 7550448Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 11, 2007Date of Patent: June 23, 2009Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: RE40861Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: November 30, 2006Date of Patent: July 21, 2009Assignee: Sigma-Tau Industrie Farmaceutiche Reunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria O. Tinti, Piero Chiodi, Arduino Arduini
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Patent number: RE41226Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: December 1, 2006Date of Patent: April 13, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini