The Nitrogen Is Bonded Directly At The 2-position Of The Diazole Ring Patents (Class 548/331.5)
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Patent number: 11891392Abstract: There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein.Type: GrantFiled: July 12, 2021Date of Patent: February 6, 2024Assignee: The Scripps Research InstituteInventors: Kim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Patent number: 10377721Abstract: Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction.Type: GrantFiled: August 21, 2018Date of Patent: August 13, 2019Assignee: Lumos Pharma, Inc.Inventors: William R. Cantrell, Jr., William E. Bauta
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Patent number: 10010631Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: GrantFiled: June 12, 2013Date of Patent: July 3, 2018Assignee: Lantheus Medical Imaging, Inc.Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Patent number: 8865709Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: September 24, 2013Date of Patent: October 21, 2014Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20140221383Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: April 14, 2014Publication date: August 7, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Publication number: 20140094436Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: ApplicationFiled: December 11, 2013Publication date: April 3, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Publication number: 20140030189Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: ApplicationFiled: June 12, 2013Publication date: January 30, 2014Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Patent number: 8551992Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: May 23, 2012Date of Patent: October 8, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20130217739Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 29, 2013Publication date: August 22, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130217632Abstract: This invention relates in one aspect to non-natural desamino alkyl amino acid compounds, methods of making these compounds, and peptides containing these compounds. In one embodiment, the peptide is neurotensin (8-13) in which the N-terminus is an alpha-desamino, alpha-methyl-N,N-dimethyl-homolysine residue of the invention.Type: ApplicationFiled: March 4, 2013Publication date: August 22, 2013Applicant: MUSC Foundation for Research DevelopmentInventor: MUSC Foundation for Research Development
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Publication number: 20130029981Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.Type: ApplicationFiled: June 18, 2012Publication date: January 31, 2013Applicant: Katholieke Universiteit LeuvenInventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
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Patent number: 8318676Abstract: The invention relates to the use of creatine, creatinine and/or derivatives thereof and/or their salts in an agent for hardening, strengthening, restructuring or increasing the shine, volume or combability of keratin fibers, particularly of human hair.Type: GrantFiled: August 16, 2007Date of Patent: November 27, 2012Assignee: Wella AGInventors: Rudolf Bimczok, Thomas Kripp, Beate Grasser, Christian Springob
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20120165380Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, acute, neuropathic and chronic.Type: ApplicationFiled: October 17, 2011Publication date: June 28, 2012Applicant: ALLERGAN, INC.Inventors: Daniel W. Gil, John E. Donello, Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha
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Publication number: 20120035235Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.Type: ApplicationFiled: October 17, 2011Publication date: February 9, 2012Applicant: ALLERGAN, INC.Inventors: Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha, Daniel W. Gil, John E. Donello
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Patent number: 8071636Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.Type: GrantFiled: June 5, 2009Date of Patent: December 6, 2011Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha, Daniel W. Gil, John E. Donello
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Patent number: 8063231Abstract: Described herein are novel N-(2 and/or 3-substituted benzyl)-4,5-dihydro-1H-imidazol-2-amine derivatives processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals modulators of subtype ?2B and/or ?2C adrenergic receptors.Type: GrantFiled: June 5, 2009Date of Patent: November 22, 2011Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha
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Publication number: 20110218208Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20110214810Abstract: A composition that includes aldimines of Formula (I). The composition can be a two-component polyurethane composition. The composition can have a long open time, but build up an early strength quickly, and in the cured state can have high tensile strength and a high modulus of elasticity. The composition can be odorless or at least low-odor before, during and after curing.Type: ApplicationFiled: May 16, 2011Publication date: September 8, 2011Applicant: SIKA TECHNOLOGY AGInventors: Urs BURCKHARDT, Ursula Stadelmann
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Patent number: 8013004Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: December 4, 2009Date of Patent: September 6, 2011Assignee: Bristol-Myers Squibb CompanyInventors: T. G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
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Publication number: 20110207788Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: ApplicationFiled: August 21, 2006Publication date: August 25, 2011Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Wolfgang Wernet, Alfred Hahn
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Publication number: 20110178143Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 14, 2008Publication date: July 21, 2011Applicant: ALLERGAN, INC.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Dario G. Gomez, Santosh N. Sinha, Smit S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil
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Patent number: 7981437Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.Type: GrantFiled: November 15, 2006Date of Patent: July 19, 2011Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20110160265Abstract: Disclosed herein is a method of treating motor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity.Type: ApplicationFiled: October 14, 2008Publication date: June 30, 2011Inventors: Lauren M.B. Luhrs, Daniel W. Gil, John E. Donello
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Patent number: 7968707Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 27, 2007Date of Patent: June 28, 2011Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 7968576Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: September 8, 2008Date of Patent: June 28, 2011Inventors: Roger A. Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen J. O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Publication number: 20110150819Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: ApplicationFiled: February 2, 2011Publication date: June 23, 2011Inventors: Christian Melander, John Cavanagh, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards
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Patent number: 7964736Abstract: Cyclocreatine phosphate can be prepared in large quantities from inexpensive starting materials to afford a stable product.Type: GrantFiled: December 29, 2005Date of Patent: June 21, 2011Assignee: Nour Heart, Inc.Inventors: Ahmed Farghaly, Elgebaly A. Salwa
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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: 7871960Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.Type: GrantFiled: May 18, 2006Date of Patent: January 18, 2011Assignee: BASF SEInventors: Markus Kordes, Norbert Götz, Michael Rack, Christopher Koradin, Livio Tedeschi, Deborah L. Culbertson
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Patent number: 7858653Abstract: The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine.Type: GrantFiled: December 5, 2007Date of Patent: December 28, 2010Assignee: Hoffman-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7838681Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.Type: GrantFiled: April 30, 2004Date of Patent: November 23, 2010Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris SudInventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
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Publication number: 20100221182Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: ApplicationFiled: December 21, 2007Publication date: September 2, 2010Inventors: Ajay Purohit, Thomas D, Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
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Publication number: 20100137385Abstract: Certain substituted amino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, R4, A, B and Q are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: February 2, 2007Publication date: June 3, 2010Applicant: Bayer CropScience AGInventors: John A. Dixon, Benjamin J. Dugan, Zeinab M. Elshenawy, Edward J. Barron, Stephen F. Donovan, Manorama M. Patel, George Theodoridis, Roland Andree, Hans-Georg Schwarz, Eva-Maria Franken, Olga Malsam, Christian Arnold
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Publication number: 20100130432Abstract: This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.Type: ApplicationFiled: December 15, 2006Publication date: May 27, 2010Inventors: Justin O. Brower, Thomas A. Dix
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Publication number: 20100130742Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.Type: ApplicationFiled: January 26, 2010Publication date: May 27, 2010Inventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20100087655Abstract: A method for producing N-(2-amino-1,2-dicyanovinyl)imidates represented by the following formula (1-III) under low temperature conditions within a short period of time in high yield is provided. In addition, a method for producing N-(2-amino-1,2-dicyanovinyl)formamidine represented by the following formula (2-II) which is suitably applicable to a cyclization reaction for producing AICN, AICA or the like and which enhances yield of the cyclization reaction is provided. In addition, a method for producing aminoimidazole derivatives represented by the following formula (3-V) in high yield by using diaminomaleonitrile as a starting material is provided.Type: ApplicationFiled: April 17, 2008Publication date: April 8, 2010Applicant: Nippon Soda Co., LtdInventors: Mitsuru Takase, Fuminori Komatsu
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Publication number: 20100010217Abstract: The present invention generally relates to methods for the preparation of compounds that contain imidazole moieties. In some embodiments, the methods include the reaction of a diamine with a dichloroimmonium compound to produce the imidazole moiety. In some embodiments, the methods are employed to prepare compounds having the Formulas II, II or III below: I II III wherein the constituent variables are as described herein.Type: ApplicationFiled: March 23, 2007Publication date: January 14, 2010Inventors: Nicholas M. Valiante, James Sutton, Jiong Lan
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Patent number: 7642280Abstract: The present invention provides compounds with activity as inhibitors of acyl glucosaminylinositol amidases with amidase activity against S-conjugate amides, particularly mycothiol-derived S-conjugate amides. Certain of the invention compounds are naturally occurring compounds obtained from marine sponges and other organisms. The invention further provides methods for using the compounds to inhibit virulence and reduce antibiotic resistance of mycothiol-producing bacteria.Type: GrantFiled: April 8, 2002Date of Patent: January 5, 2010Assignees: The Regents of the University of California, National Institutes of HealthInventors: Robert C. Fahey, Gerald L. Newton, Carole A. Bewley, Gillian Nicholas
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Publication number: 20090306398Abstract: Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an ?-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.Type: ApplicationFiled: June 5, 2009Publication date: December 10, 2009Applicant: ALLERGAN, INC.Inventors: Wenkui K. Fang, Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Michael E. Garst, Santosh C. Sinha
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Patent number: 7531577Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.Type: GrantFiled: June 20, 2007Date of Patent: May 12, 2009Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20090018150Abstract: Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.Type: ApplicationFiled: July 23, 2004Publication date: January 15, 2009Applicant: ASTERAND UK LIMITEDInventors: Richard Anthony Borman, Robert Alexander Coleman, Kenneth Lyle Clark, Alexander William Oxford, George Hynd, Janet Ann Archer, Amanda Aley, Neil Victor Harris
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Publication number: 20090018180Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: June 25, 2008Publication date: January 15, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20080293751Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: ApplicationFiled: November 15, 2007Publication date: November 27, 2008Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20080293569Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.Type: ApplicationFiled: November 15, 2006Publication date: November 27, 2008Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20080280869Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: October 13, 2005Publication date: November 13, 2008Inventors: Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Jeffrey A. Campbell, Hongyu Ren, Guangming Chen
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Patent number: 7442717Abstract: Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them.Type: GrantFiled: February 3, 2004Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Armin Hofmeister, Klaus Wirth, Hans-Willi Jansen
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Patent number: 7439395Abstract: The present invention relates to a two-step process for the preparation of guanidinium salts of the formula (1), where the substituents R have a meaning indicated in Claim, and A? is a sulfonate, alkyl- or arylsulfate, hydrogensulfate, imide, methanide, carboxylate, phosphate, phosphinate, phosphonate, borate, thiocyanate, perchlorate, fluorosilicate or nitrate, and to intermediate compounds from this process.Type: GrantFiled: January 17, 2005Date of Patent: October 21, 2008Assignee: Merck Patent GmbHInventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, German Bissky, Helge Willner
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Patent number: 7427618Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 30, 2004Date of Patent: September 23, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz, Christoph van Amsterdam
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Publication number: 20080200335Abstract: The present invention relates to 1-(imidazolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and their agriculturally acceptable salts, wherein A is a radical of the formula A1 or A2. The invention relates also to agricultural compositions and to seed comprising at least one compound I and/or a salt thereof, as well as a method of combating animal pests, a method for protecting crops from attack or infestation by animal pests and a method for protecting non-living materials from attack or infestation by animal pests, a method for the protection of seeds from animal pests and of the seedlings' roots and shoots from animal pests by applying a pesticidally effective amount of at least one 1-(imidazolin-2-yl)amino-1,2-diphenylethane compound I and/or a salt thereof.Type: ApplicationFiled: May 18, 2006Publication date: August 21, 2008Inventors: Markus Kordes, Norbert Gotz, Michael Rack, Christopher Koradin, Livio Tedeschi, Deborah L. Culbertson