Chalcogen Or Nitrogen Bonded Indirectly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/399)
  • Publication number: 20080200467
    Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.
    Type: Application
    Filed: November 2, 2007
    Publication date: August 21, 2008
    Inventors: Dinesh Patel, Richard D. Gless, Heather K. Webb Hsu, Sampath Kumar Anandan, Bhaskar R. Aavula
  • Publication number: 20080193428
    Abstract: The present invention relates to the use of benzoic acid and/or its sodium salt in combination with saccharide(s) as active components in the manufacture of a vaginal composition for modulating vaginal flora and vaginal acidity, thereby maintaining the pH value of vaginal secretion within a range from 3.5 to 4.5; and the present invention further relates to a vaginal composition and a method for modulating and maintaining normal vaginal flora and vaginal acidity.
    Type: Application
    Filed: April 27, 2006
    Publication date: August 14, 2008
    Applicants: Shenzhen Phlora Biotechnology Limited, HK Phlora Health Science & Technology Ltd.
    Inventors: Ruyun Zhou, Zhongming Zeng
  • Publication number: 20080182885
    Abstract: The present invention relates to the compounds of formula (I), their preparation and use as antifungal and/or antibacterial agents. where the values for R1, R2, R3, R4, R5 and A are as defined herein.
    Type: Application
    Filed: January 25, 2008
    Publication date: July 31, 2008
    Inventors: Marcel Borgers, Maarten van Geffen, Jannie Ausma
  • Publication number: 20080166310
    Abstract: A regime or regimen for promoting and/or inducing and/or stimulating the pigmentation of keratin materials and/or for preventing and/or limiting the depigmentation and/or bleaching and/or for preventing and/or limiting the canities thereof, more particularly of human keratin fibers such as the hair, beard hair, moustache hair, the eyelashes and the eyebrows, includes administering to an individual in need of such treatment at least one 2-oxyacetamide compound of formula (I), or a salt and/or solvate thereof:
    Type: Application
    Filed: December 10, 2007
    Publication date: July 10, 2008
    Applicant: L'OREAL
    Inventors: Roger Rozot, Philippe Breton, Michel Neuwels, Christophe Boulle
  • Publication number: 20080161376
    Abstract: The present invention relates to methods of treatment of vulvovaginitis caused by nonspecified Candida isolates using controlled release antimycotic delivery systems. The invention utilizes a minimal number of administrations to obtain cessation of the condition. The methods and systems are especially effective against any Candida species causing vaginal irritation, and thus reduce the need for identification of the isolate prior to treatment.
    Type: Application
    Filed: December 12, 2007
    Publication date: July 3, 2008
    Applicant: DRUGTECH CORPORATION
    Inventors: Daniel J. Thompson, Elio P. Mariani, R. Saul Levinson, Herbert G. Luther
  • Publication number: 20080153892
    Abstract: Compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia
    Type: Application
    Filed: March 12, 2008
    Publication date: June 26, 2008
    Applicant: Probiodrug AG
    Inventors: Stephan Schilling, Andre J. Niestroj, Ulrich Heiser, Mirko Buchholz, Hans-Ulrich Demuth
  • Publication number: 20080139455
    Abstract: Novel compounds, compositions comprising compounds, and methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, restenosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyltransferase activity.
    Type: Application
    Filed: October 12, 2007
    Publication date: June 12, 2008
    Applicant: Forbes Medi-Tech (Research), Inc.
    Inventor: John J. Nestor
  • Publication number: 20080139636
    Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).
    Type: Application
    Filed: June 20, 2007
    Publication date: June 12, 2008
    Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • Publication number: 20080140036
    Abstract: The present invention relates to a composition for use as an antimicrobial medicament comprising a biocidally active compound. The invention also relates to a medicament comprising at least one biocidally active compound and a fungal cell or fungal cell fragment wherein molecules of the at least one biocidally active compound are encapsulated or partially encapsulated by the fungal cell or fungal cell fragment.
    Type: Application
    Filed: January 18, 2005
    Publication date: June 12, 2008
    Inventors: Rachael Buck, Michael Edward Donald Crothers, Gordon Nelson
  • Publication number: 20080107727
    Abstract: A multiple-unit oral sustained release preparation is provided which allows controlled release of imidafenacin [4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide]. The preparation serves to ensure a prolonged effect of imidafenacin and prevent rapid elevation in the blood levels of imidafenacin. Specifically, granules or powders comprising imidafenacin dispersed in a water-insoluble polymer or a higher alcohol are used in the preparation. These preparations achieve sustained release of imidafenacin since the molecular network structure that the water-insoluble polymer or the higher alcohol forms during the preparation of the granules or powders serves to control the rate of diffusion of imidafenacin in water. Granules comprising a core granule having two layers of an inner imidafenacin coating and an outer water-insoluble polymer coating are used in the preparation. The water-insoluble polymer coating serves to control the rate of diffusion of imidafenacin in water and ensure sustained release of imidafenacin.
    Type: Application
    Filed: January 30, 2006
    Publication date: May 8, 2008
    Inventors: Katashi Nakashima, Yoshinobu Aoki, Kazuo Kazama, Toshihiro Ishizaki
  • Patent number: 7365070
    Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: April 29, 2008
    Assignee: Ore Pharmaceuticals Inc.
    Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
  • Patent number: 7361678
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: April 22, 2008
    Assignee: TransTech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • Patent number: 7358369
    Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: April 15, 2008
    Inventors: Ilse Zolle, Friedrich Hammerschmidt
  • Patent number: 7351825
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: April 1, 2008
    Assignee: Japan Tobacco Inc.
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Patent number: 7345077
    Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: March 18, 2008
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Todd Heidelbaugh, Daniel Gil, Michael Garst, Larry A. Wheeler, Phong X. Nguyen, Dario G. Gomez
  • Publication number: 20080057136
    Abstract: The invention relates to antimicrobial compositions that can be used for disinfecting and can be applied in various aspects of the national economy, medicine, and laboratories of all types. The antimicrobial compositions comprise a chelating metal complex compound with a monodentate bidentate or polydentate ligand that exhibits affinity to hydrogen ion, an ionogenic surfactant, and a solvent. The compositions of the invention display antiseptic properties. The antimicrobial compositions are active against Gram-positive and Gram-negative bacteria, fungi, viruses, and spores, and can be applied in a broad temperature interval. Methods of using the compositions of the present invention in the treatment and prevention of diseases caused by a variety of pathogens are further provided.
    Type: Application
    Filed: November 11, 2004
    Publication date: March 6, 2008
    Applicant: Veckis Industries Ltd.
    Inventors: Victor S. Polyakov, Valeriy V. Ermilov, Vladimir S. Kuzmin, Oleg I. Lukashov
  • Publication number: 20080058400
    Abstract: A skin external preparation includes at least arginine, aspartic acid, isoleucine, leucine, lysine, threonine, glycine, histidine, serine, valine, tyrosine, cysteine, phenylalanine, hydroxyproline and acylglutamine among amino acids, or salts thereof, and a skin external preparation includes: at least arginine, aspartic acid, isoleucine, leucine, lysine and threonine among amino acids, or salts thereof, and a hydrolyzed silk.
    Type: Application
    Filed: August 20, 2007
    Publication date: March 6, 2008
    Inventors: Chunying Yang, Mario Aoki, Takashi Usami
  • Patent number: 7326705
    Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl group, R1, R2, R3 and R4 are as defined herein, and where X is N, R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: February 5, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
  • Publication number: 20080020057
    Abstract: Personal care compositions comprise (a) from about 5 wt. % to about 50 wt. % of a detersive surfactant, (b) from about 0.05 wt. % to about 20 wt. % of wax particles having a melting point of at least about 100° C. and an average mean particle size as measured in said personal care composition of less than about 0.15 ?m; and (c) at least about 20 wt. % of a cosmetically acceptable medium; wherein the personal care composition is substantially clear.
    Type: Application
    Filed: July 18, 2006
    Publication date: January 24, 2008
    Inventors: Michael Frederick Niebauer, Brandon Scott Lane
  • Patent number: 7312199
    Abstract: A process is provided for making (?)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar elution solvent, optionally concentrating the eluate, optionally regenerating the resin by desorbing the remaining catechins, and optionally concentrating the desorbed catechins.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: December 25, 2007
    Assignee: DSM IP Assets B.V.
    Inventors: David Carl Burdick, Heinz Egger, Andrew George Gum, Ingo Koschinski, Elena Muelchi, Isabelle Prevot-Halter
  • Patent number: 7297794
    Abstract: Phenoxy amine compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: November 20, 2007
    Assignee: Emisphere Technologies, Inc.
    Inventors: David Gschneidner, Kelly Kraft, Chen Zhu, Yi Chen
  • Patent number: 7294644
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, m and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: November 13, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Mayweg, Hans Peter Marty, Werner Mueller, Robert Narquizian, Werner Neidhart, Philippe Pflieger, Stephan Roever
  • Patent number: 7282503
    Abstract: Disclosed are fungicidal mixtures containing a synergistically effective amount of A) a triazolopyrimidine of formula I, and B) imidazole derivatives of formula II, wherein X1 and X2 represent halogen and phenyl which can be substituted by halogen or alkyl, or X1 and X2 form a difluoromethylendioxyphenyl group along with the bridging C?C double bond, X3 represents cyano or halogen, and X4 represents dialkylamino or isoxazol-4yl that can carry two alkyl radicals. The invention also relates to methods for controlling destructive fungi by means of mixtures of compounds I and II, agents containing said mixtures, and the use of compounds I and II for producing such mixtures.
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: October 16, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Jordi Tormo i Blasco, Thomas Grote, Eberhard Ammermann, Reinhard Stierl, Siegfried Strathmann, Ulrich Schöfl
  • Patent number: 7279478
    Abstract: This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: September 3, 2003
    Date of Patent: October 9, 2007
    Assignee: Merck Frosst Canada & Co.
    Inventors: Michael Boyd, Marc Gagnon, Cheuk Lau, Christophe Mellon, John Scheigetz
  • Patent number: 7271271
    Abstract: Compounds are provided having the formula: wherein variables R0, R1, R2, R3, R4, Q, L and subscript n are as described herein. The subject compounds are useful for treatment of infammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: September 18, 2007
    Assignee: Amgen SF, LLC
    Inventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic
  • Patent number: 7250412
    Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: March 15, 2004
    Date of Patent: July 31, 2007
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
  • Patent number: 7250434
    Abstract: Certain imidazole compounds are CCK1 modulators useful in the treatment of CCK1 mediated diseases.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: July 31, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: J. Guy Breitenbucher, Michael D. Hack, Clark A. Sehon
  • Patent number: 7235690
    Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 26, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7232817
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: June 19, 2007
    Assignees: G.D. Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7229988
    Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: June 12, 2007
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Patent number: 7220770
    Abstract: A class of imidazolyl compounds is described for use in treating inflammation.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: May 22, 2007
    Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk, Renee M. Huff
  • Patent number: 7217718
    Abstract: Methods of inducing immune tolerance by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed: Additionally methods of suppressing an immune response by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed. Further disclosed are methods for treating autoimmune diseases by administering an immunosuppressive agent and a compound represented by Formula (I). The variables of Formula (I) are described herein.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: May 15, 2007
    Assignee: Genzyme Corporation
    Inventor: John M. Williams
  • Patent number: 7214698
    Abstract: The present invention relates to new beta-agonists of general formula 1: wherein the groups R1 to R12 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these compounds and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: May 8, 2007
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Thomas Trieselmann, Bradford S. Hamilton, Dirk Stenkamp, Stephan Georg Mueller
  • Patent number: 7205328
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: April 17, 2007
    Assignee: IRM LLC
    Inventors: Yun He, Tao Jiang, Kelli L. Kuhen, David Archer Ellis, Baogen Wu, Tom Yao-Hsiang Wu, Badry Bursulaya
  • Patent number: 7189859
    Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.
    Type: Grant
    Filed: August 6, 2003
    Date of Patent: March 13, 2007
    Inventors: Ilse Zolle, Friedrich Hammerschmidt
  • Patent number: 7176198
    Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which ?7 is known to be involved.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: February 13, 2007
    Assignee: Pfizer Inc.
    Inventors: David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Daniel Patrick Walker, Donn G. Wishka, Vincent E. Groppi, Jr.
  • Patent number: 7166590
    Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.
    Type: Grant
    Filed: May 28, 2002
    Date of Patent: January 23, 2007
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Masashi Kato
  • Patent number: 7157078
    Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.
    Type: Grant
    Filed: February 2, 2004
    Date of Patent: January 2, 2007
    Assignee: The University of Florida Research Foundation, Inc.
    Inventors: Philip Frederick Brode, III, Garry Steven Garren, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
  • Patent number: 7144909
    Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: December 5, 2006
    Assignee: Karo Bio AB
    Inventors: Johan Malm, Erik Flöistrup, Spiros Grivas, Yi-Lin Li
  • Patent number: 7132421
    Abstract: The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity
    Type: Grant
    Filed: June 15, 2004
    Date of Patent: November 7, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nader Fotouhi, Emily Aijun Liu, Binh Thanh Vu
  • Patent number: 7115632
    Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: October 3, 2006
    Assignee: G. D. Searle & Co.
    Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
  • Patent number: 7071358
    Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: July 4, 2006
    Assignee: Amgen Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Patent number: 7064124
    Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: June 20, 2006
    Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.
    Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
  • Patent number: 7053114
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: May 30, 2006
    Assignee: Sugen, Inc.
    Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
  • Patent number: 7048910
    Abstract: The invention relates to the use of one or more compounds selected from compounds of formulae Ia and Ib, the physiologically compatible salts of compounds of formula Ia and Ib and the stereoisomer forms of compounds of formula La and Ib, wherein R1, R2, R3, R4 and n have the meaning cited in claim 1.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: May 23, 2006
    Assignee: Merck Patent GmbH
    Inventors: Joachim Buenger, Hansjuergen Driller, Olaf den Hollander
  • Patent number: 7041303
    Abstract: A method of treating myocardial damage secondary to myocardial infarction using moxonidine or a physiologically compatible salt thereof. Pharmaceutical preparations containing moxonidine and its physiologically compatible acid addition salts are suitable for use in acute myocardial infarction and/or postmyocardial infarction management. In addition to a beneficial influence, promoting recovery and/or rehabilitation, on the myocardial status following myocardial infarction, moxonidine and its physiologically compatible acid addition salts, especially when used in the management of postmyocardial infarction patients in the chronic stage, also show a preventive effect against the progression of heart failure after myocardial infarction.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: May 9, 2006
    Assignee: Solvay Pharmaceuticals GmbH
    Inventor: Regina Geertruida Schoemaker
  • Patent number: 7029706
    Abstract: The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: April 18, 2006
    Inventor: Carlos Alberto Marrodan
  • Patent number: 7001918
    Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in the
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: February 21, 2006
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Patent number: RE38962
    Abstract: Compounds of formula (I), wherein X and Y are independently carbon or nitrogen but not both simultaneously carbon, R1 is a group (II) and R2 is a group (III), R5 being a carbonate, carbamate or phosphate residue, are useful as anti-gestative, immuno-suppressant and anti-tumor agents
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: January 31, 2006
    Assignee: Geange Ltd.
    Inventor: Carla Rossi
  • Patent number: RE39634
    Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.
    Type: Grant
    Filed: July 1, 2004
    Date of Patent: May 15, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, Kai Xie