Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.05)
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Patent number: 7709466Abstract: The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3? (glycogen synthase kinase-3?) which are useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovary syndrome and syndrome X or immunodeficiency.Type: GrantFiled: October 24, 2006Date of Patent: May 4, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Guenter Mueller, Martin Bossart
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Patent number: 7709467Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 15, 2008Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20100105660Abstract: A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.Type: ApplicationFiled: May 5, 2008Publication date: April 29, 2010Inventors: Robin Alec Fairhurst, Rebecca Fraser, Paul Oakley, Stephen Paul Collingwood, Nichola Smith, Emily Stanley, Maria Ines Rodriguez Perez
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Publication number: 20100104665Abstract: Apparatus and methods deliver treatment agents simultaneously with capnic gases. The capnic gases can enhance the effectiveness of the treatment agent for treating rhinitis, lower the dosage of drug or concentration of agent necessary to achieve a therapeutic result, or both. Exemplary capnic gases include carbon dioxide, nitric oxide, nitrous oxide, and dilute acid gases.Type: ApplicationFiled: December 30, 2009Publication date: April 29, 2010Applicant: CAPNIA, INC.Inventors: Julia S. Rasor, Ned S. Rasor, Gerard F. Pereira
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Publication number: 20100075953Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.Type: ApplicationFiled: September 18, 2009Publication date: March 25, 2010Applicant: Glaxo Group LimitedInventors: Rachael Ancliff, Colin David Eldred, Ashley Paul Hancock, Thomas Daniel Heightman, Heather Hobbs, Simon Teanby Hodgson, David Matthew Wilson
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Publication number: 20100057047Abstract: A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.Type: ApplicationFiled: February 14, 2007Publication date: March 4, 2010Applicant: OptiNose ASInventors: Per Gisle Djupesland, Colin David Sheldrake, Roderick Peter Hafner
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Patent number: 7662811Abstract: 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: GrantFiled: July 15, 2005Date of Patent: February 16, 2010Assignee: Amgen Inc.Inventors: Benny C. Askew, Jr., Toshihiro Aya, Kaustav Biswas, Guolin Cai, Jian J. Chen, Nianhe Han, Qingyian Liu, Thomas Nguyen, Nobuko Nishimura, Rana Nomak, Tanya Peterkin, Wenyuan Qian, Kevin Yang, Chester Chenguang Yuan, Jiawang Zhu, Derin C. D'Amico, Jason B. Human, Qi Huang
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Publication number: 20100029619Abstract: The present invention provides a compound represented by the formula (I): wherein ring A is a ring which is optionally further substituted; R1 is a hydrogen atom or a substituent; R2 is a hydrogen atom or a substituent; R3 is a hydrogen atom or a substituent; R4 is a hydrogen atom or a substituent; R5 is a hydrogen atom or a substituent; R6 is a hydrogen atom or a substituent; X is ?N— or ?C(Z)- (Z is a hydrogen atom or a substituent); when X is ?C(Z)-, Z and R6 are optionally bonded to each other to form, together with the carbon atom bonded thereto, an optionally substituted ring, provided that when X is ?CH—, then R6 is not optionally substituted 2-piperidinyl, excluding N-imidazo[1,2-a]pyridin-2-yl-4-methyl-benzamide, N-imidazo[1,2-a]pyridin-2-yl-benzamide and N-(7-methylimidazo[1,2-a]pyridin-2-yl)-benzamide, or a salt thereof, and a pharmaceutical agent containing same.Type: ApplicationFiled: August 3, 2007Publication date: February 4, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTEDInventors: Osamu Uchikawa, Nozomu Sakai, Yoshito Terao, Hideo Suzuki
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Publication number: 20100016279Abstract: The invention concerns bicyclic compounds of Formula I wherein the integers X1, X2, X3, Ring A, R4, R5 and m are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of androgen-receptor associated conditions.Type: ApplicationFiled: December 18, 2008Publication date: January 21, 2010Applicant: AstraZeneca ABInventors: Robert Hugh Bradbury, Alfred Arthur Rabow, Neil James Hales
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Publication number: 20100016289Abstract: The present invention provides compounds of general formula I: (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: January 21, 2010Inventors: Kevin Sprott, Prakash Raman, Shomir Ghosh, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Patent number: 7648978Abstract: The present invention provides compounds having formula (I) or (II): and pharmaceutically acceptable derivatives thereof, wherein m, p, R1, R2, R3 and R4 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of diseases, disorders or conditions associated with HGF/SF or other cytokine activity.Type: GrantFiled: September 28, 2005Date of Patent: January 19, 2010Assignee: Angion Biomedica Corp.Inventors: David E. Zembower, Jasbir Singh, Rama K. Mishra
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Patent number: 7642252Abstract: The invention relates to compositions and methods useful in treating or preventing angiogenic disease. The invention provides for compositions comprising cephalotaxine alkaloids as antiangiogenic agents for treatment of a host with an angiogenic disease or for prophylactic treatment of a host to inhibit the onset or progression of an angiogenic disease.Type: GrantFiled: July 22, 2003Date of Patent: January 5, 2010Assignee: Chemgenex Pharmaceuticals, Inc.Inventor: Dennis M. Brown
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Publication number: 20090312307Abstract: Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 11, 2009Publication date: December 17, 2009Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Publication number: 20090304826Abstract: The invention provides a method and composition for treating dermatoses by topical application of a composition containing an antihistamine, an NSAID and optionally a botanical medicinal compound. The compositions are useful for skin conditions such as inflammatory skin conditions, including eczema, atopic dermatitis, non-allergic dermatitis, psoriasis and rosacea, or any inflammation of the skin.Type: ApplicationFiled: June 1, 2009Publication date: December 10, 2009Applicant: Fairfield Clinical Trials, LLCInventor: Edward M. Lane
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Publication number: 20090258862Abstract: Compounds of the formula (I): as well as pharmaceutically acceptable salts and solvates are disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: August 25, 2006Publication date: October 15, 2009Inventors: Steven L. Colletti, Hong Shen, James R. Tata, Michael J. Szymonifka
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Publication number: 20090253682Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: ApplicationFiled: April 16, 2009Publication date: October 8, 2009Inventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
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Publication number: 20090220583Abstract: There is provided homogeneous pharmaceutical compositions for the treatment of inflammatory disorders comprising an antiinflammatory and/or antihistaminic active ingredient, a polar lipid liposome and a pharmaceutically-acceptable aqueous carrier.Type: ApplicationFiled: June 8, 2006Publication date: September 3, 2009Inventors: Lena Pereswetoff-Morath, Anders Carlsson
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Publication number: 20090215750Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 20, 2009Publication date: August 27, 2009Inventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Publication number: 20090203672Abstract: Substituted sulfonamide compounds corresponding to the formula I? wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these substituted sulfonamide compounds for the treatment and/or inhibition of pain or other conditions.Type: ApplicationFiled: January 16, 2009Publication date: August 13, 2009Applicant: GRUENENTHAL GmbHInventors: Beatrix Merla, Stefan Oberboersch, Ruth Jostock, Michael Engels, Stefan Schunk, Melanie Reich, Sabine Hees
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Publication number: 20090192136Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: ApplicationFiled: July 22, 2008Publication date: July 30, 2009Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Patent number: 7563784Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: April 25, 2006Date of Patent: July 21, 2009Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20090181940Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.Type: ApplicationFiled: July 18, 2008Publication date: July 16, 2009Inventors: Patricia Anne Beck, Cara Cesario, Matthew Cox, Han-Qing Dong, Kenneth Foreman, Mark Joseph Mulvihill, Anthony Innocenzo Nigro, Lydia Saroglou, Arno G. Steinig, Yingchuan Sun, Qinghua Weng, Douglas Werner, Wilkes Robin, Williams Jonathan
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Publication number: 20090181950Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.Type: ApplicationFiled: May 17, 2007Publication date: July 16, 2009Applicant: GLAXO GROUP LIMITEDInventors: Rachael Ann Ancliff, Ashley Paul Hancock, Michael Joachim Kranz, Nigel James Parr
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Publication number: 20090131399Abstract: The compounds of formula (I) in which R1, R11 and A have the meanings as given in the description are novel effective iNOS inhibitors.Type: ApplicationFiled: March 29, 2006Publication date: May 21, 2009Applicant: NYCOMED GMBHInventors: Thomas Fuchss, Andreas Strub, Wolf-Rudiger Ulrich, Christian Hesslinger, Martin Lehner, Raimund Kulzer, Rainer Boer, Manfrid Eltze
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Publication number: 20090105225Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.Type: ApplicationFiled: April 18, 2007Publication date: April 23, 2009Applicant: GLAXO GROUP LIMITEDInventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Leanda Jane Kindon, Panayiotis Alexandrou Procopiou
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Patent number: 7514424Abstract: The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK˜antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS.Type: GrantFiled: December 17, 2003Date of Patent: April 7, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20090069297Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: April 3, 2008Publication date: March 12, 2009Applicant: Amgen Inc.Inventors: Victor Cee, Holly Deak, Bingfan Du, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Mathew Martin, Isaac Marx, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
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Patent number: 7494990Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: February 1, 2005Date of Patent: February 24, 2009Assignee: NYCOMED GmbHInventors: Wiro M. P. B. Menge, Geert Jan Sterk
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Publication number: 20090005363Abstract: The present invention relates to novel nicotinic acid derivatives, of formula (I) wherein the substituents are defined in the specification, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: ApplicationFiled: December 18, 2006Publication date: January 1, 2009Inventors: Ralf Glatthar, David Orain, Carsten Spanka
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Publication number: 20090005362Abstract: Compositions comprise: (a) a material selected from the group consisting of antihistamines, stabilizers, salts thereof, and combinations thereof; and (b) a vasoconstrictor, decongestant, or a salt thereof, provided when the material consists of an antihistamine or a salt thereof, at least one antihistamine other than ketotifen and salts thereof is present. In certain embodiments, the compositions have a pH maintainable at about 5 or less during storage. The compositions can be used to treat, alleviate or ameliorate ocular allergic conditions.Type: ApplicationFiled: June 26, 2007Publication date: January 1, 2009Inventors: Toan P. Vo, Erning Xia
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Publication number: 20080306047Abstract: The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R1 denotes amino, alkylamino, dialkylamino, amidino, alkylamidino, N-hydroxyamidino, or N-alkoxyamidino, Y denotes sulfonyl or carbonyl and R2 and R4 independently represent various organic residues, in the treatment or prevention of cardiac arrhythmia and/or in treatment or prevention of diseases in association with ischemic heart conditions.Type: ApplicationFiled: November 16, 2006Publication date: December 11, 2008Inventors: Manica Cerne, Uros Urleb, Metka V. Budihna, Gorazd Drevensek, Luka Peternel
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Publication number: 20080287419Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20080275027Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.Type: ApplicationFiled: July 17, 2006Publication date: November 6, 2008Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
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Publication number: 20080261947Abstract: Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). Because of inhibiting poly(ADP-ribose)polymerase, the compounds represented by formula (I) are useful as preventives and/or remedies for various ischemic diseases (in brain, cord, heart, digestive tract, skeletal muscle, retina, etc.), inflammatory diseases (inflammatory bowel disease, multiple cerebrosclerosis, arthritis, etc.), neurodegenerative diseases (extrapyramidal disorder, Alzheimer's disease, muscular dystrophy, lumbar spinal canal stenosis, etc.), diabetes, shock, head trauma, renal failure, hyperalgesia, etc. Moreover, these compounds are useful as agents against retroviruses (HIV etc.), sensitizers in treating cancer and immunosuppressants.Type: ApplicationFiled: June 11, 2008Publication date: October 23, 2008Inventors: Takuya Seko, Jun Takeuchi, Shinya Takahashi, Yoshihisa Kamanaka, Wataru Kamoshima
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Patent number: 7432255Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases which are associated with the modulation of histamine 3 (H3) receptors.Type: GrantFiled: April 26, 2007Date of Patent: October 7, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Patent number: 7427612Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: September 2, 2004Date of Patent: September 23, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Patent number: 7423030Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).Type: GrantFiled: October 11, 2006Date of Patent: September 9, 2008Assignee: Sanofi-AventisInventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
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Patent number: 7414047Abstract: Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 21, 2003Date of Patent: August 19, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Richard L. Apodaca, Jill A. Jablonowski, Kiev S. Ly, Chandravadan R. Shah, Devin M. Swanson, Wei Xiao
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Patent number: 7405209Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 14, 2005Date of Patent: July 29, 2008Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Robert Wells Marquis, Jr., Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Patent number: 7390799Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20080119457Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein A, Q1, Q2, Q3, R31, and R41 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: May 22, 2008Inventors: Kenneth He Huang, John Mangette, Thomas Barta, Steven E. Hall, James Veal, Philip Hughes
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Patent number: 7368445Abstract: The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.Type: GrantFiled: February 16, 2005Date of Patent: May 6, 2008Assignee: Eli Lilly and CompanyInventors: Hong-Yu Li, William Thomas McMillen, Yan Wang
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Patent number: 7365063Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CRaRb)r—, A is —NR3, m is 2, n is 1, q is 2, R2 is optioinally substituted aryl or optionally substituted heteroaryl, and p, R1, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of central nervous system diseases.Type: GrantFiled: February 7, 2007Date of Patent: April 29, 2008Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
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Patent number: 7351708Abstract: The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: December 6, 2006Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Olivier Roche
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Patent number: 7348323Abstract: The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: December 6, 2006Date of Patent: March 25, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Olivier Roche
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Publication number: 20080014274Abstract: An oral, liquid pharmaceutical composition is provided. The composition comprises phenylephrine and substantially aldehyde-free polyethylene glycol. The composition has phenylephrine stability compatible with the stability required for commercial preparations. Optionally, the composition may comprise one or more additional active agents.Type: ApplicationFiled: July 14, 2006Publication date: January 17, 2008Applicant: WyethInventors: William Bubnis, Stephanie Shield, Gayle P. Hoskovec
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Patent number: 7319097Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: August 30, 2005Date of Patent: January 15, 2008Assignee: Biovitrum ABInventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
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Publication number: 20070297990Abstract: The invention provides self-preserving compositions and methods for their production.Type: ApplicationFiled: June 27, 2006Publication date: December 27, 2007Inventors: Mandar V. Shah, Uday Doshi, Ken T. Holeva
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Patent number: 7307079Abstract: The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient. The invention relates to compounds of the general formula (1) wherein Y represents a group of the general formula (A), (B) or (C) and all other symbols have the meanings as given in the description.Type: GrantFiled: May 30, 2003Date of Patent: December 11, 2007Assignees: Solvay Pharmaceuticals, B.V., Arqule, Inc.Inventors: Jacobus A.J. Den Hartog, Jan H. Reinders, Guustaaf J.M. Van Scharrenburg, Maria L. Pras-Raves, Gary R. Gustafson