The Hetero Ring Contains Four Members Including Nitrogen And Carbon Patents (Class 548/950)
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Publication number: 20090247503Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicants: Versitech Limited, Morningside Ventures LimitedInventors: Dan Yang, Chengyong Li, Shiwu Chen
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Patent number: 7579340Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.Type: GrantFiled: August 22, 2007Date of Patent: August 25, 2009Assignee: Pfizer IncInventors: Ronald Biediger, Jie Chen, Daxin Gao, Robert Market, Chengde Wu
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Publication number: 20090209512Abstract: Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof: wherein R1 and R2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.Type: ApplicationFiled: February 13, 2009Publication date: August 20, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Noboru IWAKAMI, Shigeki MARUBUCHI, Tomohiro OKUDA
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Patent number: 7572792Abstract: The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.Type: GrantFiled: April 25, 2005Date of Patent: August 11, 2009Assignees: Merck & Co., Inc., Merck Sharp & Dohme LimitedInventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
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Publication number: 20090186834Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: ApplicationFiled: March 24, 2006Publication date: July 23, 2009Applicant: MICROBIA, INC.Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
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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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Patent number: 7521552Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.Type: GrantFiled: December 8, 2004Date of Patent: April 21, 2009Assignee: WyethInventors: Yanzhong Wu, Arkadiy Rubezhov, Jean Schmid, Jay Thomas Afragola
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Publication number: 20090093453Abstract: Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof: wherein R1 and R2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.Type: ApplicationFiled: April 24, 2007Publication date: April 9, 2009Applicant: Toyama Chemical Co., LtdInventors: Noboru Iwakami, Shigeki Marubuchi, Tomohiro Okuda
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Publication number: 20090087379Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.Type: ApplicationFiled: April 20, 2007Publication date: April 2, 2009Inventors: Erik Arstad, Matthias Eberhard Glaser
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Patent number: 7504522Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH—O—] group.Type: GrantFiled: April 29, 2004Date of Patent: March 17, 2009Assignee: Vernalis Research LimitedInventors: James Edward Paul Davidson, Claire Elizabeth Dawson, Kerry Harrison, Howard Langham Mansell, Robert Mark Pratt, Sukhjit Sohal, Victoria Jane Ruston
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Publication number: 20090069576Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.Type: ApplicationFiled: March 27, 2006Publication date: March 12, 2009Applicant: TOYAMA CHEMICAL CO., LTDInventors: Akihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Publication number: 20090069284Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: ApplicationFiled: October 21, 2008Publication date: March 12, 2009Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20090048224Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: September 5, 2008Publication date: February 19, 2009Applicants: Amgen, Inc., Array BioPharma, Inc.Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090036422Abstract: The present invention relates to compounds of formula wherein Ar, R1, R2, R3, R4, R5, n, o, and p are as defined herein or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds of formula I can be used for the treatment of sleep disorders, such as sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: ApplicationFiled: July 24, 2008Publication date: February 5, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090029962Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: July 21, 2008Publication date: January 29, 2009Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7479504Abstract: The present invention encompasses compounds of Formula 1: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.Type: GrantFiled: January 15, 2003Date of Patent: January 20, 2009Assignee: Merck & Co., Inc.Inventors: Robert L. Bugianesi, George A. Doherty, Amy Gentry, Jeffrey J. Hale, Christopher L. Lynch, Sander G. Mills, William E. Neway, III
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Publication number: 20090018114Abstract: The present application relates to cannabinoid receptor ligands containing compounds of formula (I) wherein A, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: July 8, 2008Publication date: January 15, 2009Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson
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Patent number: 7473779Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.Type: GrantFiled: September 12, 2003Date of Patent: January 6, 2009Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
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Publication number: 20080305082Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.Type: ApplicationFiled: September 14, 2005Publication date: December 11, 2008Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
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Patent number: 7462629Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: GrantFiled: May 19, 2004Date of Patent: December 9, 2008Assignee: IRM LLCInventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Yi Fan, Wenqi Gao
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Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
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Publication number: 20080293685Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.Type: ApplicationFiled: May 22, 2008Publication date: November 27, 2008Applicant: Chevron U.S.A. Inc.Inventors: Deyuan Kong, Frederick W. Lam, Steven F. Sciamanna, Earl Shelton, Shenggao Liu, Robert M. Carlson
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Patent number: 7456164Abstract: The invention relates to 3- or 4-monosubstituted phenol and thiophenol derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol and thiophenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: May 9, 2005Date of Patent: November 25, 2008Assignee: Pfizer, IncInventors: Patrick Bernardelli, Andrew Michael Cronin, Alexis Denis, Stephen Martin Denton, Henry Jacobelli, Mark Ian Kemp, Edwige Lorthiois, Fiona Rousseau, Delphine Serradeil-Civit, Fabrice Vergne
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Publication number: 20080234247Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Applicant: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7423061Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: GrantFiled: August 12, 2004Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Stephanie Springer, Mei Su, Dingwei Yu
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Patent number: 7419986Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: September 2, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080207588Abstract: The present invention is concerned with certain novel derivatives of Formula I, wherein R, R1 to R10 are as described in the specification, and at least one CR5R6, or CR7R8, or CR9R10 is a an optionally substituted azetidine ring or an optionally substituted oxetan ring, which may be useful in the manufacture of pharmaceutical compositions for treating disorders mediated by lipoxygenases. They may also be useful in the manufacture of pharmaceutical formulations for the treatment of lipoxygenase mediated disorders.Type: ApplicationFiled: December 9, 2005Publication date: August 28, 2008Inventors: Daniel T. W. Chu, Donald R James, Bing Wang
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Patent number: 7402670Abstract: Chiral synthesis from an achiral starting material by chiral diamine-mediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.Type: GrantFiled: September 28, 2005Date of Patent: July 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Xiaohu Deng, Neelakandha Mani
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Patent number: 7393858Abstract: The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: March 4, 2004Date of Patent: July 1, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Olivier Dirat, Jason Matthew Elliott, Ian Thomas Huscroft, Richard Alexander Jelley, Janusz Jozef Kulagowski, Piotr Antoni Raubo, Duncan Edward Shaw, Francine Sternfeld, Christopher John Swain
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Publication number: 20080113957Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is —C(R3R4)—; Y is —N(R5)—; Z is (—C(?N—R5?)—; and R1, R2, R3, and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.Type: ApplicationFiled: June 12, 2006Publication date: May 15, 2008Inventors: Brian McKittrick, Zhaoning Zhu, Andrew Stamford
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Patent number: 7361670Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.Type: GrantFiled: December 28, 2004Date of Patent: April 22, 2008Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
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Publication number: 20080064677Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: July 24, 2006Publication date: March 13, 2008Inventors: Ashis K. Saha, Nili Schutz, Anurag Sharadendu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa Rao Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
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Patent number: 7335681Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: September 15, 2006Date of Patent: February 26, 2008Assignee: The Regents of the University of MichiganInventor: James A. Shayman
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Patent number: 7335666Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: February 26, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080045690Abstract: A description is given of azetidine derivatives and methods for producing them, and of their use as a latent curing component for resins having functional groups which are reactive toward amino groups. The particular advantages of the curing component proposed in accordance with the invention, such as effective producibility, high environmental friendliness, and excellent storage stability of the resin/curing agent mixtures, make these azetidine derivatives outstandingly suitable for one-component, moisture-hardening polymer compositions, which are of special interest in particular for the production of (floor) coatings, sealants, and adhesives.Type: ApplicationFiled: December 2, 2004Publication date: February 21, 2008Inventors: Stefan Ingrisch, Alois Maier, Thomas Pfeuffer, Norbert Steidl, Andrea Gantner, Herbert Winkelmann
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Patent number: 7326796Abstract: The present invention provides novel fluorine-containing copolymers which comprise at least one fluorinated olefin, at least one polycyclic ethylenically unsaturated monomer with a fused 4-membered heterocyclic ring and, optionally, other components. The copolymers are useful for photoimaging compositions and, in particular, photoresist compositions (positive-working and/or negative-working) for imaging in the production of semiconductor devices. The copolymers are especially useful in photoresist compositions having high UV transparency (particularly at short wavelengths, e.g., 157 nm) which are useful as base resins in resists and potentially in many other applications.Type: GrantFiled: August 8, 2003Date of Patent: February 5, 2008Assignee: E.I. du Pont de Nemours and CompanyInventors: Andrew E. Feiring, Frank L. Schadt, III, Viacheslav Alexandrovich Petrov, Bruce Edmund Smart, William Brown Farnham
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Patent number: 7288538Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.Type: GrantFiled: August 23, 2004Date of Patent: October 30, 2007Assignee: Encysive Pharmaceuticals, Inc.Inventors: Chengde Wu, Daxin Gao, Ronald Biediger, Jie Chen, Robert V. Market
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Patent number: 7285565Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: January 14, 2005Date of Patent: October 23, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20070232581Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: March 29, 2007Publication date: October 4, 2007Inventors: Yong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu
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Patent number: 7271130Abstract: Fungicidal compounds of the general formula (1) wherein X, Y, Z, R1, R2, R3, R4 and R5 have the definitions given in claim 1Type: GrantFiled: November 10, 2003Date of Patent: September 18, 2007Assignee: Syngenta LimitedInventors: Roger Salmon, David William Langton
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Patent number: 7256186Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: September 15, 2004Date of Patent: August 14, 2007Assignee: Schering CorporationInventors: Dimitri A. Pissarntiski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7253185Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: April 29, 2005Date of Patent: August 7, 2007Assignees: The Regents of the University of Michigan, Genzyme CorporationInventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Patent number: 7253204Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 25, 2005Date of Patent: August 7, 2007Assignee: MethylGene Inc.Inventors: Daniel Delorme, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain, Zhihong Zhou, Isabelle Paquin, Frederic Gaudette, Ljubomir Isakovic
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Publication number: 20070173487Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: July 24, 2006Publication date: July 26, 2007Inventors: Ashis K. Saha, Nili Schutz, Anurag Sharadendu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa Rao Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
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Patent number: 7241757Abstract: There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 2, 2004Date of Patent: July 10, 2007Assignee: AstraZeneca ABInventors: Tord Inghardt, Olle Karlsson, Marcel Linschoten, Jan-Erik Nyström
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Patent number: 7235544Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: June 17, 2004Date of Patent: June 26, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, John David Harling, Wendy Rebecca Irving, Savvas Kleanthous, Nigel Stephen Watson, Robert John Young
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Patent number: 7229803Abstract: The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing cyclic secondary amines suitable for ultimately synthesizing piperidine-2-carboxylic acid and proline derivatives, useful, for example as thrombin inhibitors.Type: GrantFiled: April 8, 2002Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Thomas Friedrich, Norbert Zimmermann, Rainer Stürmer
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Patent number: 7208602Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: February 5, 2003Date of Patent: April 24, 2007Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs