Chalcogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/238.8)
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Publication number: 20120015942Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20110281850Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: July 7, 2011Publication date: November 17, 2011Applicant: MANNKIND CORPORATIONInventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Aminothiolester compounds, pharmaceutical and cosmetic compositions containing same and uses thereof
Patent number: 8026231Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: March 28, 2006Date of Patent: September 27, 2011Assignee: CNRSInventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore -
Publication number: 20110195929Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.Type: ApplicationFiled: August 4, 2009Publication date: August 11, 2011Applicant: SUMMIT CORPORATION PLCInventors: Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
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Patent number: 7985776Abstract: A method of delivering a curcuminoid to a patient, which includes iontophoretically delivering a charged curcuminoid across the skin of an Alzheimer's Disease patient.Type: GrantFiled: June 27, 2008Date of Patent: July 26, 2011Assignee: Codman & Shurtleff, Inc.Inventors: Sean Lilienfeld, Thomas M. Di Mauro
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Publication number: 20110152267Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-increasing retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) compounds selected from the groups consisting of (i) a non-18 carbon chain length L-threo-sphinganine(s) or pharmaceuticeutically acceptable salt thereof, (ii) glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor(s), and (iii) sphingomyelin or dihydrosphingomyelin synthase inhibitor(s). Preferred L-threo-sphinganines are of carbon chain length 17 carbons, 19 carbons and 20 carbons. A preferred glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingomyelin or dihydrosphingomyelin synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol.Type: ApplicationFiled: November 12, 2010Publication date: June 23, 2011Inventors: Barry James Maurer, Charles Patrick Reynolds
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Patent number: 7964598Abstract: The present invention provides compounds that inhibit apoE4 domain interaction; and compositions, including pharmaceutical compositions, comprising the compounds. The present invention provides methods of treating apoE4-related disorders. The methods generally involve administering to an individual in need thereof a therapeutically effective amount of an apoE4 domain interaction inhibitor.Type: GrantFiled: October 4, 2005Date of Patent: June 21, 2011Assignee: The J. David Gladstone InstitutesInventors: Robert W. Mahley, Karl H. Weisgraber, Yadong Huang
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Publication number: 20110144111Abstract: Disclosed herein is a method for treating diseases associated with beta amyloid accumulation, including administering to a patient a therapeutically effective amount of morpholine or piperazine based compounds including a sulfuric or carboxylic acid structure represented by the following chemical formula 1 or a pharmaceutically acceptable salt thereof: (wherein Z, R1 and R2 are as defined in the specification).Type: ApplicationFiled: December 6, 2010Publication date: June 16, 2011Inventors: Dong Jin KIM, YoungSoo KIM, Hye Yun KIM
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Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Publication number: 20110071125Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 24, 2011Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
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Publication number: 20110046139Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.Type: ApplicationFiled: April 27, 2009Publication date: February 24, 2011Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
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Patent number: 7872007Abstract: It is disclosed a process for the preparation of 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone (BTG-1675A) comprising the steps of: i) reacting N-hydroxymorpholine with cycloesanone in the presence of an oxidation agent thus obtaining an isoxazolidine of Formula IV; and ii) converting the isoxazolidine of Formula IV into 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone. Advantageously, the oxidation agent of the step i) is selected from the group consisting of metal oxides, esters and amides of the azodicarboxylic acid and the step ii) of conversion is carried out by basic catalysis followed by trituration in an aromatic hydrocarbon, preferably toluene. The process disclosed allows to obtain BTG-1675A according to the invention in an amount of hundreds of grams and on an industrial scale. The invention further concerns a new process for preparing hydroxylamines, particularly N-hydroxymorpholine, which is used in the process for preparing BTG-1675A.Type: GrantFiled: February 12, 2007Date of Patent: January 18, 2011Assignee: Abiogen Pharma S.p.A.Inventor: Elio Napolitano
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Publication number: 20110002875Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.Type: ApplicationFiled: June 8, 2010Publication date: January 6, 2011Applicant: Bellus Health (International) LimitedInventors: Robert Kisilevsky, Walter Szarek, Donald Weaver
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Patent number: 7858610Abstract: (1) A preventive and/or a remedy for lower urinary tract diseases such as inflammation in the lower urinary tract, cystitis (interstitial cystitis, etc.) and urethritis; (2) an agent for improving bladder compliance and/or bladder capacity; and (3) an agent for protecting bladder mucosa and/or bladder epithelial cells and/or promoting the regeneration thereof; each containing an EP4 agonist. An EP4 agonist is useful in ameliorating symptoms of lower urinary tract diseases such as (1) frequent urination, (2) urgency of urination, (3) pain in the reproductive organs and/or lower urinary tract (for example, bladder pain, urinary tract pain, vulvar pain, vaginal pain, scrotal pain, perineal pain, pelvic pain, etc.) and/or (4) discomfort in the reproductive organs and/or lower urinary tract. Among all, a selective EP4 agonist is useful as a preventive and/or remedy for lower urinary tract diseases having no side effect.Type: GrantFiled: August 9, 2005Date of Patent: December 28, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiroki Okada, Takayuki Maruyama
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Publication number: 20100310599Abstract: The present invention is embodied by a composition capable inducing weight loss in a patient in need thereof.Type: ApplicationFiled: June 15, 2010Publication date: December 9, 2010Inventors: W. Blair GEHO, John R. LAU
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Publication number: 20100294686Abstract: An L2/L1 microemulsion composition comprising water, a compound of formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, and a salt of a compound of formula (I).Type: ApplicationFiled: December 19, 2007Publication date: November 25, 2010Applicant: SINCLAIR PHARMACEUTICALS LIMITEDInventor: Thomas Arnebrant
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Publication number: 20100298329Abstract: The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers.Type: ApplicationFiled: September 19, 2008Publication date: November 25, 2010Applicant: Massachusette Institute of TechnologyInventors: Alice T. Shaw, Tyler E. Jacks, Nicola Tolliday
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Publication number: 20100273785Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists of Formula I or II, and pharmaceutical compositions thereof: wherein X, Y, Z, and R1-R5 are as defined herein. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Inventors: Tai Wei Ly, Garrett Thomas Potter
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Publication number: 20100273782Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Baaum
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Publication number: 20100256150Abstract: A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: formula (II), (III) and (IV); or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: (V) and (VI); wherein R1 and R2 together represent an oxo group, or R1 and R2 each represent hydrogen, methoxy or ethoxy, or R1 and R2 together with the interjacent carbon atom represent a 1,3-dioxolane or 1,3-dioxane ring, attached via the 2 position and optionally bearing one or more methyl or ethyl groups; or a salt thereof, is suitable for the treatment of anxiety and depression.Type: ApplicationFiled: June 15, 2010Publication date: October 7, 2010Applicant: BTG International LimitedInventors: Phillip Parsons, Silvia Trasciatti, Sergio Rosini, Michael Annis
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Publication number: 20100249045Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.Type: ApplicationFiled: April 26, 2008Publication date: September 30, 2010Applicant: THERAQUEST BIOSCIENCES, INC.Inventor: Najib Babul
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Publication number: 20100215704Abstract: Morpholino compounds of Formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or pharmaceutically acceptable salts thereof, have been found to be surprisingly effective at promoting the healing of a wound.Type: ApplicationFiled: July 22, 2008Publication date: August 26, 2010Applicant: SINCLAIR PHARMACEUTICALS LIMITEDInventor: Olof Torgny Sjodin
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Publication number: 20100204234Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.Type: ApplicationFiled: March 27, 2008Publication date: August 12, 2010Inventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
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Patent number: 7737140Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: April 21, 2009Date of Patent: June 15, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20100137250Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: November 9, 2009Publication date: June 3, 2010Inventors: Fariborz Firooznia, Paul Gillespie, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jenny Tan, Kshitij Chhabilbhai Thakkar
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Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism
Publication number: 20100137194Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.Type: ApplicationFiled: November 23, 2009Publication date: June 3, 2010Applicants: EASTERN MICHIGAN UNIVERSITYInventors: Daniel A. Lawrence, Cory Emal, Jacqueline Cale, Enming J. Su, Mark Warnock, Shih-Hon Li, Jeanne A. Cupp -
Patent number: 7713967Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 1, 2009Date of Patent: May 11, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7713968Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: April 22, 2009Date of Patent: May 11, 2010Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100113450Abstract: The present invention provides an agent for preventing and alleviating wrinkles which has excellent effects of preventing and alleviating wrinkles formed by decreased barrier function of the skin owing to aging or photo aging, that is graphic wrinkles or linear wrinkles. The agent for preventing and alleviating wrinkles consisting of one or more compounds selected from the group consisting of gamma-aminobutyric acid derivatives represented by the following formula (1) or N,N,N-trimethyl gamma-aminobutyric acid represented by the following formula (3) and salts thereof: wherein R1 and R2 independently represent any of a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a benzyloxycarbonyl group, a cyclohexyl group, a cyclohexanemethyl group, a cyclohexanecarbonyl group, a guanidino group formed with nitrogen atom in the formula (1), an ureido group formed with nitrogen atom in the formula (1), and a group represented by following formula (2).Type: ApplicationFiled: March 14, 2008Publication date: May 6, 2010Applicant: SHISEIDO COMPANY LTD.Inventors: Makoto TSUNENAGA, Mikiko KAMINUMA, Masaru SUETSUGU, Chika KATAGIRI
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Publication number: 20100035881Abstract: The invention provides a novel wrinkle-improving agent that has an effect of improving wrinkles, that does not entail problems of safety or pain even when applied to the skin, and that contains a very safe substance as an active component. A discovery was made that N-benzoyl-?-alanine, other specific ?-alanine derivatives, and salts thereof have a wrinkle-improving effect, whereby a wrinkle-improving agent containing as an active component one, two, or more types of compounds selected from the group composed of these specific ?-alanine derivatives and the salts thereof was developed.Type: ApplicationFiled: September 15, 2006Publication date: February 11, 2010Applicant: SHISEIDO COMPANY, LTD.Inventors: Mikiko Kaminuma, Masaru Suetsugu, Makoto Tsunenaga, Kiyotaka Hasegawa, Shinji Inomata
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Patent number: 7655653Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.Type: GrantFiled: October 25, 2007Date of Patent: February 2, 2010Assignee: N.V. OrganonInventor: Hubert Jan Jozef Loozens
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Publication number: 20090325963Abstract: A method of delivering a curcuminoid to a patient, which includes iontophoretically delivering a charged curcuminoid across the skin of an Alzheimer's Disease patient.Type: ApplicationFiled: June 27, 2008Publication date: December 31, 2009Inventors: Sean Lilienfeld, Thomas M. Di Mauro
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Publication number: 20090270396Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: April 21, 2009Publication date: October 29, 2009Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20090238773Abstract: Use of a morpholino compound having the general formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention or treatment of halitosis.Type: ApplicationFiled: January 5, 2007Publication date: September 24, 2009Inventor: Rolf Valter Attstrom
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Publication number: 20090186829Abstract: Biomacromolecules such as proteins are inactivated by hydrophobic ANSA derivatives of the formula: wherein R1 and R2 are hydrophobic or affinity groups and R3 is selected from the group consisting of aminoacyl groups and peptidyl groups upon nitrosation. ANSA derivatives can be designed to selectively kill tumor cells and various pathogens, including bacteria, viruses, and fungi.Type: ApplicationFiled: March 26, 2009Publication date: July 23, 2009Applicant: New York UniversityInventors: Evgeny NUDLER, Audrei NEDOSPASOV
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Patent number: 7560459Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: November 2, 2005Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
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Publication number: 20090163487Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: ApplicationFiled: September 26, 2008Publication date: June 25, 2009Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20090149445Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.Type: ApplicationFiled: July 15, 2008Publication date: June 11, 2009Inventors: Michael Joseph Coghlan, Jonathan Edward Green, Timothy Alan Grese, Prabhakar Kondaji Jadhav, Donald Paul Matthews, Mitchell Irvin Steinberg, Kevin Robert Fales, Michael Gregory Bell
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Patent number: 7544676Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.Type: GrantFiled: November 9, 2006Date of Patent: June 9, 2009Assignee: Adolor CorporationInventors: Roland E. Dolle, Karin Worm
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Publication number: 20090105218Abstract: Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH?CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are notType: ApplicationFiled: May 30, 2005Publication date: April 23, 2009Applicant: 7TM PHARMA A/SInventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg
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Publication number: 20090082353Abstract: The present invention provides new method of treatment of epilepsy with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.Type: ApplicationFiled: March 30, 2006Publication date: March 26, 2009Inventors: Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Publication number: 20090082328Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 26, 2009Inventors: Yingfu Li, Joachim Rudolph, Jacques P. Dumas, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther
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Patent number: 7482343Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: November 15, 2006Date of Patent: January 27, 2009Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Han-Jie Zhou, David J. Morgans, Jr., Gustave Bergnes, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Nicholas D. Adams
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Publication number: 20090023731Abstract: Disclosed are urea and thiourea 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, and diabetic-related diseases.Type: ApplicationFiled: March 21, 2008Publication date: January 22, 2009Inventors: Richard D. Gless, JR., Sampath Kumar Anandan
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Publication number: 20090023735Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is selected from a group consisting of dialkylamino, NO2, CN, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, oxazol-2-yl, oxazolylaminocarbonyl, aryl, aroyl, aryl-CH(OH)—, arylaminocarbonyl, furanyl, where the aryl, aroyl and furanyl moieties may be substituted, guanidinyl-(CH2)z—N(R?)—, Het-(CH2)z—N(R?)—, Het-CO—N(R?)—, Het-CH(OH)— and Het-CO—, where Het is an optionally substituted 4-6-membered heterocyclic ring containing one or more heteroatoms sleeted from N, S and O, R? is hydrogen or alkyl, and z is an integer 1 to 5; RA is a group of formula (A), (B), (C) or (D) as defined in the claims; and RB is hydrogen, alkyl, alkanoyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminoalkyl, mono- or dialkylaminoalkyl or Het-alkyl, where Het is as defined above.Type: ApplicationFiled: September 15, 2006Publication date: January 22, 2009Inventors: Jyrki Heino, Mark Johnson, Jarmo Kapyla, Anne Marjamaki, Tommi Nyronen, Marika Ojala, Olli Pentikainen, Marjo Pihlavisto, Liisa Nissinen
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Publication number: 20090017102Abstract: The present invention is directed to novel codrugs comprising bupropion or hydroxybupropion and an opioid antagonist or an opioid agonist joined together by chemical bonding. The codrugs provide a significant increase in the transdermal flux across human skin, as compared to the basic opioid antagonist or opioid agonist.Type: ApplicationFiled: October 18, 2007Publication date: January 15, 2009Applicant: University of Kentucky Research FoundationInventors: Audra L. Stinchcomb, Peter A. Crooks, Mohamed O. Hamad, Paul K. Kiptoo
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Publication number: 20090018103Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: October 7, 2005Publication date: January 15, 2009Applicant: VITAE PHARMACEUTICAL, INCInventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillar, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Publication number: 20080317806Abstract: A compound of Formula (A), wherein R1 is C1-C5 alkyl, C3-C6 branched alkyl, C4-C7 cycloalkyl, C8-C12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R2 is H or R1; and X is halo, carbonyl carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.Type: ApplicationFiled: April 11, 2006Publication date: December 25, 2008Applicant: Murdoch UniversityInventors: Wayne Morris Best, Colette Gloria Sims, Richard Christopher Andrew Thompson, Simon Andrew Reid, Anthony Armson, James Alexander Reynoldson
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Publication number: 20080317883Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.Type: ApplicationFiled: October 22, 2007Publication date: December 25, 2008Inventors: Yong Moon Choi, Robert Gordon, Magali Haas, Ewa Malatynska