Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 540/599)
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Publication number: 20100273779Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: June 15, 2010Publication date: October 28, 2010Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Patent number: 7803795Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: September 28, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Laurence Anne Mevellec, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Patent number: 7790710Abstract: 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: GrantFiled: March 29, 2006Date of Patent: September 7, 2010Assignee: NYCOMED GmbHInventors: Thomas Fuchss, Andreas Strub, Wolf-Rüdiger Ulrich, Christian Hesslinger, Martin Lehner, Raimund Külzer, Rainer Boer, Manfrid Eltze
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Patent number: 7745427Abstract: The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: October 18, 2005Date of Patent: June 29, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Diem N. Nguyen, Christopher S. Burgey, James Z. Deng
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Patent number: 7732438Abstract: Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: June 8, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Anthony W. Shaw, Craig M. Potteiger
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Publication number: 20100137268Abstract: The present invention relates to new phthalazinone modulators of H1 receptor activity and/or modulators of LTC4 production, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 3, 2009Publication date: June 3, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100137285Abstract: 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: ApplicationFiled: November 30, 2009Publication date: June 3, 2010Applicant: ANGION BIOMEDICA CORP.Inventors: David E. Zembower, Jasbir Singh, Rama K. Mishra
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Patent number: 7709468Abstract: The present invention is directed to novel imidazopyrazine and imidazopyrimidine compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: September 1, 2006Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Kristine E. Frank, Patrick Betschmann, Gavin C. Hirst, Eric C. Brieinlinger, Michael J. Morytko, Richard W. Dixon
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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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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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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: 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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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: 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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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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Publication number: 20080312219Abstract: The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R? and R? each independently is a linear, branched or cyclic hydrocarbon group, or R? and R? together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP? is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.Type: ApplicationFiled: May 12, 2008Publication date: December 18, 2008Applicant: PHOTOPHARMICA LIMITEDInventors: Stanley Beames Brown, Cassandra Claire O'Grady, John Griffiths, Kirste Joanne Mellish, Richard George Tunstall, David John Howard Roberts, David Ian Vernon
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Patent number: 7459554Abstract: 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: GrantFiled: October 14, 2004Date of Patent: December 2, 2008Assignee: OSI Pharmaceuticals, Inc.Inventors: Han-Qing Dong, Kenneth Foreman, Mark Joseph Mulvihill, Anthony Innocenzo Nigro, Arno G. Steinig, Douglas Werner, Robin Wilkes
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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: 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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Publication number: 20080200454Abstract: Carbon-linked tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.Type: ApplicationFiled: February 14, 2008Publication date: August 21, 2008Inventors: Michael K. Ameriks, Frank U. Axe, James P. Edwards, Cheryl A. Grice, Hui Cai, Elizabeth Ann Gleason, Steven P. Meduna, Kevin L. Tays, John J. M. Wiener, Alvah T. Wickboldt
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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: 7393845Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 5, 2007Date of Patent: July 1, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
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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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Patent number: 7345038Abstract: An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound of formula I, pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as schizophrenia and depression, wherein formula I is or a pharmaceutically acceptable salt or thereof, wherein Z is wherein Y is methylene; X is oxygen; n is 0; R1 and R2 are each hydrogen or halogen; and R3 and R4 together with the nitrogen atom to which they are attached form i) a saturated non-aromatic 3 to 7 membered monocyclic ring, said ring i) being unsubstituted or substituted or substituted with one or more (C1–C4)alkyl, (C1–C4)alkoxy(C1–C4)alkyl, or hydroxy groups.Type: GrantFiled: March 12, 2004Date of Patent: March 18, 2008Assignee: Pfizer, IncInventors: Gene Michael Bright, Michael A. Brodney, Bishop Wlodecki
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Patent number: 7304051Abstract: Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases.Type: GrantFiled: August 4, 2004Date of Patent: December 4, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Brett D. Allison, Michael D. Hack, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen
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Patent number: 7304052Abstract: The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R2 being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl suType: GrantFiled: December 14, 2000Date of Patent: December 4, 2007Assignee: Janssen Pharmaceuitca N.V.Inventors: Frans Eduard Janssens, Jérôme Emile Georges Guillemont, François Maria Sommen
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Patent number: 7288651Abstract: Certain methods are disclosed that are useful in the preparation of CCK2 active amidophenyl-sulfonylamino-quinoxaline compounds of the formula: wherein R1, R2, Ra and Rb are defined.Type: GrantFiled: August 4, 2004Date of Patent: October 30, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani, Chennagiri R. Pandit
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Patent number: 7265103Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutiType: GrantFiled: March 27, 2003Date of Patent: September 4, 2007Assignee: Janssen Pharmaceutica NV.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Margaretha Henrica Maria Bakker, Ana Isabel De Lucas Olivares
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Patent number: 7265125Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: April 7, 2005Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7223750Abstract: Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl, (C1–C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1–C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. Therapeutic application.Type: GrantFiled: January 3, 2003Date of Patent: May 29, 2007Assignee: Sanofi-AventisInventors: Frédéric Galli, Odile LeClerc, Alistair Lochead, Alain Nedelec
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Patent number: 7196087Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—, A is —NR3— or —O—, R2 is optionally substituted aryl or optionally substituted heteroaryl, n is 1 or 2, m is 1 when Y is C and m is 2 when Y is S, and p, q, r, R1, R3, R4, R5, R6, R7, R8, R9, R10, Ra and Rb are as defined herein. The compounds are useful in the treatment of 5-HT6 and 5-HT2A mediated diseases.Type: GrantFiled: January 14, 2005Date of Patent: March 27, 2007Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
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Patent number: 7186710Abstract: The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors.Type: GrantFiled: April 23, 2002Date of Patent: March 6, 2007Assignee: Altana Pharma AGInventor: Geert Jan Sterk
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Patent number: 7176214Abstract: The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: GrantFiled: May 18, 2004Date of Patent: February 13, 2007Assignee: Bristol-Myers Squibb CompanyInventors: William J. Pitts, Makonen Belema, Patrice Gill, James Kempson, Yuping Qiu, Claude A. Quesnelle, Steven H. Spergel, Fred Christopher Zusi
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Patent number: 7173033Abstract: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.Type: GrantFiled: July 28, 2005Date of Patent: February 6, 2007Assignee: Astellas Pharma Inc.Inventors: Susumu Igarashi, Ryo Naito, Yoshinori Okamoto, Noriyuki Kawano, Issei Tsukamoto, Ippei Sato, Makoto Takeuchi, Hiroyuki Kanoh, Masato Kobori
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Patent number: 7141562Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.Type: GrantFiled: November 6, 2003Date of Patent: November 28, 2006Assignee: Roche Palo Alto LLCInventors: Hans Maag, Meng Sui, Shu-Hai Zhao
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Patent number: 7071184Abstract: 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: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 6974808Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.Type: GrantFiled: November 27, 2001Date of Patent: December 13, 2005Assignee: Bristol-Myers Squibb CompanyInventor: James R. McCarthy
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Patent number: 6964957Abstract: Pyrazole compounds represented by the formula: are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in treating ERAB, HADH2 or amyloid-? mediated diseases and conditions.Type: GrantFiled: August 17, 2001Date of Patent: November 15, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Melwyn A. Abreo, Jerry J. Meng, Charles S. Agree
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Patent number: 6962926Abstract: Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of MCP-1 function, and are useful in the prevention and treatment of chronic or acute inflammatory or autoimmune diseases, such as multiple sclerosis, and in the prevention and treatment of allergic hypersensitivity disorders.Type: GrantFiled: August 8, 2003Date of Patent: November 8, 2005Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Wenli Ma, Yukiharu Matsumoto, Kunihisa Baba, Hideaki Inagaki, Katsumasa Tanaka, Yoshiro Ishiwata, Shoji Yokochi, Masayuki Okamoto, Takashi Nakamura, Atsushi Miyachi, Mitsuaki Takeuchi, Kouji Matsushima
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Patent number: 6951851Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: October 4, 2005Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6951849Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: GrantFiled: April 3, 2003Date of Patent: October 4, 2005Assignee: ACADIA Pharmaceuticals Inc.Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
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Patent number: 6949540Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: September 27, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6936603Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: August 30, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6900226Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: August 27, 2001Date of Patent: May 31, 2005Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger