The Aryl Ring Or Aryl Ring System And Amino Nitrogen Are Bonded Directly To The Same Acylic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 514/655)
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Publication number: 20090197970Abstract: The present invention relates to the polymorph form II of Cinacalcet hydrochloride, methods for the preparation of pure form II of Cinacalcet hydrochloride, and pharmaceutical compositions comprising the new polymorphic form in an pharmaceutically effective amount The present invention also provides novel solvates of Cinacalcet hydrochloride, methods for the preparation of these solvates, the use of these novel solvates for the preparation of pure Cinacalcet hydrochloride, the use of these novel solvates for the preparation of polymorphic form II of Cinacalcet hydrochloride and pharmaceutical compositions comprising the acetic acid solvate of Cinacalcet hydrochloride.Type: ApplicationFiled: June 25, 2007Publication date: August 6, 2009Inventors: Johannes Ludescher, Ulrich Griesser, Doris Braun, Josef Wieser
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Publication number: 20090192173Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.Type: ApplicationFiled: October 22, 2008Publication date: July 30, 2009Inventors: Marina Nikolaevna PROTOPOPOVA, Leo Einck, Boris Nikonenko, Ping Chen
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Publication number: 20090143374Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, use in the reduction of A? peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase.Type: ApplicationFiled: December 8, 2008Publication date: June 4, 2009Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Publication number: 20090137653Abstract: This invention is directed to substituted benzylamines which are useful as inhibitors of the CYP2A6 enzyme. Pharmaceutical compositions comprising the compounds and methods of using the compounds to treat nicotine dependence are also disclosed.Type: ApplicationFiled: April 6, 2006Publication date: May 28, 2009Applicant: INFLAYZME PHARMACEUTICALS LTD.Inventors: Omar Ghosheh, Jeffery R. Raymond
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Publication number: 20090099266Abstract: Antifungal nail coat compositions containing an allylamine, an N,N-di(C1-C8) alkylamino substituted, (C4-C18) alkyl (C2-C18) carboxylic ester or a pharmaceutically acceptable acid addition salt thereof, a hydrophilic polymer, and a pharmaceutically acceptable, volatile organic carrier are disclosed. The composition provides a substantially water-soluble, fungicidal coating upon contact with a fungally susceptible or infected nail.Type: ApplicationFiled: December 9, 2008Publication date: April 16, 2009Inventors: Stanley W. Kepka, Y. Joseph Mo, Hang-Yong Wang, Mingqi Lu, William R. Pfister
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Publication number: 20090099202Abstract: External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.Type: ApplicationFiled: December 18, 2008Publication date: April 16, 2009Inventors: Toshihiro Shirouzu, Youichi Kawamura, Hiroki Kawatsura, Mitsuhiko Tokunaga
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Publication number: 20090093521Abstract: Synthesis of 2,5-bis-diamine-[1,4]benzoquinonic derivatives having the general formula (I), products and intermediates of said synthesis; the synthesis involves the use of p-benzoquinones having the general formula (IX) and diamines having the general formula (XI).Type: ApplicationFiled: June 13, 2005Publication date: April 9, 2009Inventors: Maria Laura Bolognesi, Rita Banzi, Anna Minarini, Carlo Melchiorre
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Publication number: 20090082469Abstract: The present application describes deuterium-enriched terbinafine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090075960Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicants: THE HOSPITAL FOR SICK CHILDREN, McMASTER UNIVERSITYInventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
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Publication number: 20090069441Abstract: Disclosed herein are motuporamine mimic agents and methods of making and using same. Particularly exemplified are motuporamine mimic agents comprising cytotoxic activity and/or anti-metaplastic activity.Type: ApplicationFiled: February 26, 2008Publication date: March 12, 2009Inventor: Otto Phanstiel
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Patent number: 7488759Abstract: The invention concerns salts of the compound of formula I with malic acid, their preparation, corresponding pharmaceutical compositions and their use as antimycotics.Type: GrantFiled: November 29, 2006Date of Patent: February 10, 2009Assignee: Novartis AGInventors: Danielle Giron, Jean-Louis Reber, Stefan Hirsch
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Publication number: 20080319087Abstract: The invention is directed to the use of ambroxol or pharmaceutically acceptable salts thereof for preparing a medical composition for treating or preventing infections caused by human rhinovirus. Surprisingly it was found that Ambroxol is capable to suppress the replication of human rhinovirus. Therefore, the ambroxol-containing medical composition is suitable to treat or prevent against all symptoms of a rhinovirus infection and provides a direct antivirale effect.Type: ApplicationFiled: August 3, 2006Publication date: December 25, 2008Inventors: Anke Esperester, Liane Paul
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Publication number: 20080317690Abstract: The invention provides a biological dressing for treatment of a dermatological disease comprised of one or more resins or other film-forming agents, a topically acceptable volatile solvent, and a pharmacologically active agent. The combined one or more resins are present in a suitable amount such that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin, nail or mucosal membrane to which the composition is applied, and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition.Type: ApplicationFiled: November 7, 2006Publication date: December 25, 2008Inventor: Alex Battaglia
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Publication number: 20080299165Abstract: A flowable composition suitable for use as a controlled release implant, the composition comprising a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid; a biocompatible polar aprotic solvent selected from the group consisting of an amide, an ester, a carbonate, a ketone, an ether, and a sulfonyl; wherein the biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid, and antifungal active.Type: ApplicationFiled: February 17, 2006Publication date: December 4, 2008Inventors: Jing-song Tao, Ronald Erwin Boch, Alain H. Curaudeau, Peter Lutwyche, Agnes How-Ching Chan
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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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Patent number: 7456222Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: July 1, 2005Date of Patent: November 25, 2008Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human ServicesInventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
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Publication number: 20080280815Abstract: The present invention relates to a method for lowering serum lipids, eg. triglycerides and/or cholesterol in a subject comprising administering a GLP-1 agonist to said subject.Type: ApplicationFiled: August 22, 2007Publication date: November 13, 2008Applicant: Novo Nordisk A/SInventors: Liselotte Bjerre Knudsen, Johan Selmer, Jeppe Sturise, Philip Just Larsen
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Publication number: 20080268067Abstract: This invention relates to methods of inhibiting a Cav3 calcium channel in a cell using a C2-C10 alkyl alcohol, or mixtures thereof. This invention further relates to methods of treating a thalamocortical dysrhythmia disorder in a mammal and for treating a neurological disorder in a mammal associated with the thalamocortical dysrhythmia using a C2-C10 alkyl alcohol, a lipophilic molecule with a partition coefficient substantially similar to that of a C2-C10 alkyl alcohol, or mixtures thereof, or a pharmaceutical composition comprising the same.Type: ApplicationFiled: March 10, 2008Publication date: October 30, 2008Inventors: Rodolfo R. Llinas, Mutsuyuki Sugimori, Francisco Urbano
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Publication number: 20080261986Abstract: Pharmaceutical formulations suitable for iontophoresis thereof that provide enhanced iontophoretic delivery of an anti-fungal drug to at least one body surface are described. Also described are pharmaceutical formulations suitable for iontophoresis comprising terbinafine and methods for administering terbinafine to a body surface via iontophoresis. In one embodiment, the body surface includes a nail plate and/or the skin.Type: ApplicationFiled: March 27, 2008Publication date: October 23, 2008Inventors: Phillip M. Friden, Hyun Kim, Bireswar Chakraborty
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Publication number: 20080262096Abstract: Novel squaric acid compounds of the formula (I), in which R, R1, R1?, R2 and X have the meanings indicated in Claim (1), are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: December 9, 2005Publication date: October 23, 2008Inventors: Werner Mederski, Rolf Gericke, Dieter Dorsch, Markus Klein, Norbert Beier, Florian Lang
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Publication number: 20080255093Abstract: The present invention is drawn to combinations of pharmaceutical agents having similar chemical and/or pharmacological properties, wherein the combinations maximize the therapeutic effect of the drug while minimizing their adverse effects. The methods and compositions of the invention are particularly useful in the treatment of obesity and related conditions which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) or bupropion in combination with an anti-epileptic agent (e.g., topiramate, zonisamide), CB1 antagonists (e.g., rimonabant), or a 5HT2C-selective serotonin receptor agonist, (e.g., lorcaserin) for the treatment of obesity and related conditions. The invention also features kits for use in the practice of these novel therapies.Type: ApplicationFiled: April 29, 2008Publication date: October 16, 2008Inventors: Peter Y. Tam, Leland F. Wilson
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Publication number: 20080234206Abstract: The invention relates to compositions of amino acid and peptide conjugates comprising phentermine. Phentermine is covalently attached to at least one amino acid via its amine group to the N-terminus, the C-terminus, a side chain of the peptide carrier. Also discussed are methods for treating obesity.Type: ApplicationFiled: September 13, 2006Publication date: September 25, 2008Applicant: SHIRE LLCInventor: Travis Mickle
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Publication number: 20080221101Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: October 25, 2007Publication date: September 11, 2008Applicant: Amgen Inc.Inventors: Thomas S. Coulter, Adam James Davenport, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael Gerard Kelly, Steve Fong Poon, Andrew Tasker, Ning Xi, Qing Ping Zeng
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Publication number: 20080220103Abstract: Provided is a method of treating a fungal infection on an animal epidermis, nail or hair, or in an orifice of an animal. The method comprises contacting the fungus infection with a composition comprising an antifungal botanical.Type: ApplicationFiled: March 13, 2008Publication date: September 11, 2008Inventors: Jay Birnbaum, Thomas Blake, Mahmoud Ghannoum, Steven Vallespir
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Publication number: 20080221176Abstract: This invention relates to compounds that are modulators of the liver X receptors (LXRs), and also to the methods for the making and use of such compounds.Type: ApplicationFiled: August 23, 2006Publication date: September 11, 2008Inventors: John Loren Collins, Eugene Lee Stewart, William Zuercher, Esther Chao, Robert Wiethe, Justin Caravella
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Publication number: 20080207537Abstract: Application of a reducing agent followed by an oxidising agent to a nail substantially increases the permeability thereof, thereby enabling the passage of drugs across the nail.Type: ApplicationFiled: June 6, 2006Publication date: August 28, 2008Applicant: MedPharm LimitedInventors: Robert Turner, Marc Barry Brown, Stuart Allen Jones
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Publication number: 20080200535Abstract: There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.Type: ApplicationFiled: August 24, 2007Publication date: August 21, 2008Applicant: Asahi Kasei Pharma CorporationInventors: Yutaka Ohmori, Masakazu Komatsu
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Publication number: 20080193508Abstract: A topical composition for treating nail fungal infections that utilizes an acidic antifungal agent with a molecular weight no greater than 170 Daltons in a formulation having a pH less than or equal to the pKa of the acidic antifungal agent plus one. Possible antifungal agents include omadine, octanoic acid, sorbic acid, hexanoic acid, and benzoic acid. The antifungal agent can be combined with a delivery system such as a lacquer, a gel, a patch, or a hydrating system. A second therapeutic agent such as a 5-fluorocystine or terbinafine can be included.Type: ApplicationFiled: February 8, 2008Publication date: August 14, 2008Applicant: DermWoRX, Inc.Inventors: David M. Cohen, Eugene R. Cooper
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Publication number: 20080188568Abstract: The invention is an increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages. The allylamine active ingredient is prepared in an acidic environment; the acidic environment altering the physiochemical properties of the active ingredient resulting in the active ingredient having a positive charge. The positive charge and enhancers used in the formula allow for increased penetration of the active ingredient through skin and skin appendages. The positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle.Type: ApplicationFiled: February 5, 2008Publication date: August 7, 2008Inventors: Pichit Suvanprakorn, Panida Vayumhasuwan, Nardo Zaias
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Publication number: 20080167312Abstract: Disclosed herein are substituted allylamines having structural Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.Type: ApplicationFiled: December 10, 2007Publication date: July 10, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080146620Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.Type: ApplicationFiled: November 13, 2007Publication date: June 19, 2008Applicant: Japan Tobacco Inc.Inventors: Kimiya Maeda, Hironobu Nagamori, Hiroshi Nakamura, Hisashi Shinkai, Yasunori Suzuki, Daisuke Takahashi, Toshio Taniguchi
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Publication number: 20080139665Abstract: The invention relates to the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to assay systems allowing to test LSD1 inhibitors for their ability to inhibit LSD1 function.Type: ApplicationFiled: February 16, 2006Publication date: June 12, 2008Inventors: Roland Schuele, Eric Metzger
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Publication number: 20080132442Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include greater than 30% by weight of the active agent, and may be formulated as solutions, solids, semisolids, microparticles, or crystals. Methods related to the implantation and use of the biodegradable drug delivery systems for treating nail unit conditions are also described.Type: ApplicationFiled: February 11, 2008Publication date: June 5, 2008Inventors: Frank M. Kochinke, Corinne Bright
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7119122Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: October 2, 2002Date of Patent: October 10, 2006Assignee: Astrazeneca ABInventors: Stephen Connolly, Glen Ernst
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Patent number: 7022882Abstract: Neuroprotectant agents are provided which do not contain peptides and axe protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitatoxic cell death.Type: GrantFiled: October 5, 2001Date of Patent: April 4, 2006Assignee: The Regents of the University of CaliforniaInventors: Kwok-Keung Tai, Sylvie E. Blondelle, Richard A. Houghten, Mauricio Montal
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Patent number: 6939895Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.Type: GrantFiled: December 19, 2002Date of Patent: September 6, 2005Assignee: NPS Pharmaceuticals, Inc.Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
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Patent number: 6924313Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.Type: GrantFiled: December 23, 2002Date of Patent: August 2, 2005Assignee: Pfizer Inc.Inventors: James A. Sikorski, Richard C. Durley, Melvin L. Rueppel, Deborah A. Mischke, Barry L. Parnas
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Patent number: 6919317Abstract: Synergistic combinations of a squalene epoxidase inhibitor such as terbinafine and a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro, 33-desoxyascomycin are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin plays a role, such as atopic dermatitis and seborrhoeic dermatitis, and in situations of fungal resistance.Type: GrantFiled: February 16, 2001Date of Patent: July 19, 2005Assignee: Novartis AGInventors: Neil Stewart Ryder, Friedrich Karl Mayer
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Patent number: 6890958Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.Type: GrantFiled: September 18, 2002Date of Patent: May 10, 2005Assignee: G.D. Searle, LLCInventors: James A. Sikorski, Kevin C. Glenn
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Patent number: 6881748Abstract: A bioreductive conjugate comprises a bioreductive moiety with at least one therapeutic agent linked thereto and physiologically acceptable derivatives thereof. The bioreductive moiety incorporates an aromatic ring substituted with a nitro group and the conjugate is such that bioreduction of the nitro group causes release of the therapeutic agent by a through bond elimination and the residue of the bioreductive moiety to undergo an intramolecular cyclization reaction in which the nitrogen of the original nitro group provides an atom of the thus formed ring.Type: GrantFiled: August 19, 1999Date of Patent: April 19, 2005Assignee: The Victoria University of ManchesterInventors: Sally Freeman, Mohammed Jaffor, Ian Stratford
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Patent number: 6855711Abstract: Use of a compound of formula (I), wherein R1 is H or hydrocarbyl; R2 is a hydrophobic radical; R3 is 3-(C2-C6)acyl-4-hydroxyphenyl, 3-hydroxyimino (C2-C6)-alkyl-4-hydroxyphenyl, or COOZ, wherein Z is H, (C1-C6) alkyl, aryl, aryl or ar(C1-C6) alkyl; and n is 1-20; and of a compound of formula (II), wherein R4 is (C1-C6) alkyl, cyano (C1-C6) alkyl, (C1-C6) alkoxy (C1-C6) alkyl or —CH2NR7R8, wherein R7 and R8, the same or different, is each H or (C1-C6) alkyl, or together with the N atom form a saturated or unsaturated 5-7 membered ring optionally containing a further heteroatom selected from N, O or S, the further N atom being optionally substituted, and either R5 is H and R6 is (C2-C6) acyl or hydroxyimino (C2-C6) alkyl, or R5 and R6 together with the phenyl ring form a quinoline, a 1,2,3,4-tetrahydroquinoline or a perhydroquinoline ring, for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease or stroke.Type: GrantFiled: June 7, 2000Date of Patent: February 15, 2005Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.Inventors: Rivka Warshawsky, Moussa B. H. Youdim, Dorit Ben-Shachar, Abraham Warshawsky
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Patent number: 6787570Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.Type: GrantFiled: December 16, 2002Date of Patent: September 7, 2004Assignee: Pfizer, Inc.Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
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Patent number: 6765023Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: July 20, 2004Assignee: Pfizer, Inc.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6750255Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.Type: GrantFiled: January 17, 2002Date of Patent: June 15, 2004Assignees: NPS Pharmaceuticals, Inc., Kirin Beer KabushikiInventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
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Patent number: 6723752Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1 )-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6710089Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: March 23, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6710088Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.Type: GrantFiled: January 29, 2002Date of Patent: March 23, 2004Assignee: NPS Pharmaceuticals, Inc.Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
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Patent number: RE39530Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.Type: GrantFiled: September 11, 2003Date of Patent: March 27, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann