The Additional Hetero Ring Also Contains Nitrogen Patents (Class 548/518)
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Publication number: 20130158004Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
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Publication number: 20130150578Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 1, 2011Publication date: June 13, 2013Applicant: CADILA PHARMACEUTICALS LIMITEDInventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
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Patent number: 8455222Abstract: Methods for producing biliverdin in a microorganism, methods for producing biliverdin from a non-animal source, cells for producing biliverdin and methods for producing cells for producing biliverdin are disclosed.Type: GrantFiled: November 4, 2010Date of Patent: June 4, 2013Assignee: Utah State UniversityInventors: Jon Y Takemoto, Dong Chen
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Patent number: 8455867Abstract: A heterocyclic compound represented by a general Formula 1 and an organic light-emitting device including the heterocyclic compound. In some embodiments the heterocyclic compound of Formula 1 may be used as a light-emitting material, a hole transporting material, or an electron transporting material. The heterocyclic compound of Formula 1 having a heterocyclic group in the molecules thereof has a high glass transition temperature (Tg) or a high melting point due to the inclusion of the heterocyclic group. Thus, the heterocyclic compound has high heat resistance against Joule's heat generated in an organic layer, between organic layers, or between an organic layer and a metal electrode when light emission occurs, and has high durability in high-temperature environments. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1 has high durability when stored or operated.Type: GrantFiled: April 1, 2011Date of Patent: June 4, 2013Assignee: Samsung Display Co., Ltd.Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Yoon-Hyun Kwak, Sun-Young Lee, Jong-Hyuk Lee, Sung-Chul Kim
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Patent number: 8450335Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.Type: GrantFiled: June 26, 2009Date of Patent: May 28, 2013Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Patent number: 8445683Abstract: Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.Type: GrantFiled: October 3, 2008Date of Patent: May 21, 2013Inventors: Robert E. Connors, Chuchawin Changtong, John L. Lombardi
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Publication number: 20130116230Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
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Patent number: 8431580Abstract: 4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.Type: GrantFiled: December 18, 2008Date of Patent: April 30, 2013Assignee: Palau Pharma, S.A.Inventors: Elena Carceller González, Eva Maria Medina Fuentes, Robert Soliva Soliva, Marina Virgili Bernadó, Josep Martí Via
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Publication number: 20130090362Abstract: Polyamide compositions containing guanidinyl radicals, including tetramethylguanidinyl radicals, are described. These polyamides are useful for medical applications, for example, for treating human papilloma virus infections.Type: ApplicationFiled: October 10, 2012Publication date: April 11, 2013Applicant: NANOVIR, LLCInventor: NANOVIR, LLC
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Publication number: 20130090472Abstract: The invention provides compounds of the Formula (I), in which W is independently selected from W1, W2, W3, W4, W5, or W represents a pair of substituents independently selected from H, alkyl, aryl or amide in which the amide is optionally part of a linking chain, and the Zn—Zn bonds (n=4-17; n?=n+1) are optionally of any whole or partial bond order, Y is Y1 or Y represents a pair of substituents independently selected from H, C-1-C6 alkyl, Z5 or Z6 aryl, or Y is optionally a bridging structure that may comprise one or more C-1-C6 amide, C-1-C6 ether, or C-1-C6 ester groups, R-R39 are independently selected from no substituent, a lone pair of electrons, H, halogen, C5-C6 aryl, C1- C-12 alkyl, amine, C-1-C6 alkylamine, C-1-C6 amide, nitro, cyano, carboxyl, C-1-C6 ester, phosphane, thiol, C-1-C6 thioether, OR?, and suitable pairs of adjacent R groups (R-R39) may optionally together form part of a C5 or C6 aryl ring, a Z5 or Z6 ring, R? is independently selected from H, C-1-C6 alkyl, Z5 or Z6 aryl, C-1-C6 ester,Type: ApplicationFiled: June 14, 2011Publication date: April 11, 2013Applicant: UNIVERSITY OF KWAZULU-NATALInventors: Orde Quentin Munro, Kate Julie Akerman, Piers Akerman
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Patent number: 8410141Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: GrantFiled: May 18, 2010Date of Patent: April 2, 2013Assignee: Bayer Cropscience AGInventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
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Publication number: 20130079528Abstract: A method of making a compound of Formula I? comprises reacting a compound of the formula DLCHO, with a compound of the formula to produce the compound of Formula I?. Methods of using the compounds are also described, particularly as intermediates for the synthesis of porphyrin rods, which porphyrin rods are in turn useful for (among other things) the production of molecular memory devices.Type: ApplicationFiled: August 31, 2012Publication date: March 28, 2013Inventors: Jonathan S. Lindsey, Lianhe Yu, Patchanita Thamyongkit, Anil D. Bhise
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Patent number: 8404719Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: December 12, 2011Date of Patent: March 26, 2013Assignee: AbbVie Inc.Inventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
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Patent number: 8405074Abstract: A heterocyclic compound represented by a general Formula 1 and an organic light-emitting device including the heterocyclic compound. In some embodiments the heterocyclic compound of Formula 1 may be used as a light-emitting material, a hole transporting material, or an electron transporting material. The heterocyclic compound of Formula 1 having a heterocyclic group in the molecules thereof has a high glass transition temperature (Tg) or a high melting point due to the inclusion of the heterocyclic group. Thus, the heterocyclic compound has high heat resistance against Joule's heat generated in an organic layer, between organic layers, or between an organic layer and a metal electrode when light emission occurs, and has high durability in high-temperature environments. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1 has high durability when stored or operated.Type: GrantFiled: April 1, 2011Date of Patent: March 26, 2013Assignee: Samsung Display Co., Ltd.Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Yoon-Hyun Kwak, Sun-Young Lee, Jong-Hyuk Lee, Sung-Chul Kim
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Patent number: 8399256Abstract: The present invention provides a method for transferring a gene into cells, which is practically useful and can achieve high transfer efficiency, and also a composition for use in the method. By bringing a mixture of a composition comprising a diallylamine sulfur dioxide copolymer having a repeating unit represented by the formula (1) or a salt thereof and a gene into contact with a cell, a gene such as DNA and RNA can be transferred into a target cell safely and conveniently, and into a cell at a specific site with high gene transfer efficiency.Type: GrantFiled: October 13, 2009Date of Patent: March 19, 2013Assignee: Mitsubishi Gas Chemical Company, Inc.Inventor: Kazuto Ikemoto
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Publication number: 20130065925Abstract: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a C3-8 cycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a C3-8 cycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a C1-6 alkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Ichiro YOSHIDA, Tadashi OKABE, Yasunobu MATSUMOTO, Nobuhisa WATANABE, Yuji ONIZAWA, Yoshiaki OHASHI, Hitoshi HARADA
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Publication number: 20130065882Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxyType: ApplicationFiled: October 3, 2012Publication date: March 14, 2013Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Patent number: 8394806Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: GrantFiled: July 14, 2011Date of Patent: March 12, 2013Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Publication number: 20130059891Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130059873Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: April 3, 2012Publication date: March 7, 2013Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Publication number: 20130053378Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: July 30, 2012Publication date: February 28, 2013Applicant: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
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Patent number: 8383625Abstract: Compounds of formula (I) in salt or zwitterionic form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: December 22, 2005Date of Patent: February 26, 2013Assignee: Novartis AGInventors: Neil J Press, Collingwood P Stephen
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Patent number: 8383624Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: GrantFiled: July 15, 2010Date of Patent: February 26, 2013Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Virajkumar B. Gandhi, Gui-Dong Zhu, Yunsong Tong, Keith W. Woods, Chunqiu Lai, Jane Gong, Alan S. Florjancic
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Publication number: 20130023503Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: September 24, 2012Publication date: January 24, 2013Applicant: OPKO Health, Inc.Inventor: OPKO Health, Inc.
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Publication number: 20130023563Abstract: Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoaniline derivative represented by the following formula (1-1) or a pharmaceutically acceptable salt thereof: <in the formula (1-1), each symbol is as defined in the Description>, and a pharmaceutical composition containing the amidinoaniline derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: AJINOMOTO CO., INC.Inventor: AJINOMOTO CO., INC.
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Patent number: 8354545Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 10, 2008Date of Patent: January 15, 2013Assignees: Merck, Sharp & Dohme, Corp., Istituto di Ricerche di Biologia Molecolare P Angeletti SPAInventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
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Publication number: 20130004518Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: Merck, Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: 8343963Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.Type: GrantFiled: January 29, 2010Date of Patent: January 1, 2013Assignee: 4SC AGInventor: Stefano Pegoraro
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Patent number: 8329699Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: May 18, 2011Date of Patent: December 11, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
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Patent number: 8329705Abstract: The present invention relates to substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: December 11, 2012Assignee: ArQule, Inc.Inventor: Neil Westlund
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Patent number: 8329700Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: March 7, 2011Date of Patent: December 11, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Matthew Paul Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Patent number: 8318793Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 29, 2010Date of Patent: November 27, 2012Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Wilfried Hornberger, Falko Ernst Wolter
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Patent number: 8318750Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Patent number: 8309725Abstract: The present subject matter relates to perhydroquinoxaline derivates, processes for their preparation, their use for the preparation of a medicament and medicaments containing perhydroquinoxaline derivates.Type: GrantFiled: December 19, 2008Date of Patent: November 13, 2012Assignee: Dr. August Wolff GmbH & Co. KG—ArzneimittelInventors: Bernhard Wünsch, Dirk Schepmann, Christian Bourgeois
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Patent number: 8304561Abstract: A method of making a metalloporphyrin is carried out by reacting (i) a linear tetrapyrrole, said linear tetrapyrrole having a 19-acyl group and a 1-protecting group, with (ii) a metal salt under basic conditions to produce the metalloporphyrin. Products produced by such methods and intermediates useful for carrying out such methods are also described.Type: GrantFiled: April 26, 2012Date of Patent: November 6, 2012Assignee: North Carolina State UniversityInventors: Jonathan S. Lindsey, Dilek Dogutan Kiper
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Patent number: 8304371Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.Type: GrantFiled: January 29, 2009Date of Patent: November 6, 2012Assignee: Bayer Cropscience AGInventors: Ulrich Görgens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Publication number: 20120277405Abstract: The present application provides a copolymer including one or more units of pyrene and one or more units of pyrrole. The present application also provides a method of producing a copolymer, including incubating pyrene monomer and pyrrole monomer with an oxidant in the presence of a reaction solvent. Uses of the copolymers are also provided.Type: ApplicationFiled: June 4, 2010Publication date: November 1, 2012Applicant: TONGJI UNIVERSITYInventors: Xin-Gui Li, Mei-rong Huang, Zhenzhong Hou
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Publication number: 20120277420Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.Type: ApplicationFiled: June 5, 2012Publication date: November 1, 2012Inventors: Jonathan S. Lindsey, Masahiko Taniguchi, Doyoung Ra, Guoning Mo, Thiagarajan Balasubramanian
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Patent number: 8299115Abstract: Pyrrole-2-carboxamide derivatives, their polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, beneficial for prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these pyrrole-2-carboxamides.Type: GrantFiled: June 5, 2008Date of Patent: October 30, 2012Inventors: Debnath Bhuniya, S. Gobind Kapkoti, S. Jayakumar Warrier, Gagan Kukrejka, N. Jagadeesh Mavinahalli, P. Venkata Palle, A. Kasim Mookhtiar
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Patent number: 8299096Abstract: This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.Type: GrantFiled: June 26, 2009Date of Patent: October 30, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Tomas Navratil, Ward M. Peterson, John W. Lampe, Emilee H. Fulcher, Scott D. Sorensen
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Patent number: 8293957Abstract: Described are oligotetracenes of formula I which may either be unsubstituted or carry one or more substituents R and R? which are selected from the group comprising halogen, CN, alkyl or alkoxy radicals containing 1 to 18 carbon atoms, aryl radicals containing up to 10 carbon atoms which may also contain one or more heteroatoms, and/or fluorinated or perfluorinated alkyl or alkoxy radicals containing 1 to 18 carbon atoms, where n is an integer from 1 to 20, preferably 1 to 6, very particularly preferably 1 or 2, and X stands for a single bond, an alklyene group containing 1 to 6 carbon atoms, a hydrocarbon chain having one or more conjugated double bonds, an aryl group, or a system composed of one or more condensed aromatic rings. In the oligotetracenes according to the invention, one or more of the condensed aromatic six-atom rings may be substituted by a five-atom ring which may also contain a heteroatom.Type: GrantFiled: June 21, 2006Date of Patent: October 23, 2012Assignee: Dritte Patentportfolio Beteiligungsgesellschaft mbH & Co. KGInventors: Matthias Rehahn, Michael Roth, Heinz Von Seggern, Roland Schmechel, Marcus Ahles
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20120258963Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8283363Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: November 5, 2010Date of Patent: October 9, 2012Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20120253052Abstract: A method of making a porphyrin is carried out by: (a) condensing (i) a 1,9-bis(N,N-)dialkylaminomethyl)dipyrromethane of Formula II: with (ii) a dipyrromethane to produce a reaction product; then (b) oxidizing the reaction product; and then (c) optionally demetallating said reaction product to produce the porphyrin. The reaction is particularly useful for making substituted porphyrins with a wide range of substituents at the A and/or B (the 5 and/or 15) positions.Type: ApplicationFiled: June 5, 2012Publication date: October 4, 2012Inventors: Jonathan S. Lindsey, Masahiko Taniguchi, Dazhong Fan
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Publication number: 20120252063Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.Type: ApplicationFiled: April 4, 2012Publication date: October 4, 2012Applicant: Biotium, IncInventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung, Lori Michelle Roberts
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Patent number: 8278334Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: December 18, 2009Date of Patent: October 2, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20120238752Abstract: Provided is a colored photosensitive curing composition useful for color filters in primary colors, including blue, green, and red, having a high molar absorption coefficient and allowing a reduction in film thickness and superior color purity and fastness. A colored photosensitive curing composition, comprising, as its colorant, a dipyrromethene-based metal complex compound obtained from a metal or metal compound and a dipyrromethene-based compound represented by the following Formula (I): wherein in Formula (I), R1 to R6 each independently represent a hydrogen atom or a substituent group; and R7 represents a hydrogen or halogen atom, or an alkyl, aryl or heterocyclic group.Type: ApplicationFiled: May 23, 2012Publication date: September 20, 2012Applicant: FUJIFILM CORPORATIONInventors: Yuki MIZUKAWA, Ryoji GOTO, Hideki TAKAKUWA, Masashi OGIYAMA, Toru FUJIMORI
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Publication number: 20120238551Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: December 22, 2011Publication date: September 20, 2012Applicants: Cephalon France, Cephalon, Inc.Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allizon L. Zulli, Christophe Yue