The Additional Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/61)
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Publication number: 20090023704Abstract: The present invention relates to novel xanthine compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: April 17, 2008Publication date: January 22, 2009Applicant: ASTRAZENECA ABInventors: Leifeng Cheng, Sara Holmqvist, Florian Raubacher, Peter Schell
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Patent number: 7465726Abstract: Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3?, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.Type: GrantFiled: August 1, 2005Date of Patent: December 16, 2008Assignee: OSI Pharmaceuticals, Inc.Inventors: Saleh Ahmed, Oscar Barba, Jason Bloxham, Graham Dawson, William Gattrell, John Kitchin, Neil Anthony Pegg, Imaad Saba, Shazia Sadiq, Colin Peter Sambrook Smith, Don Smyth, Amo G. Steinig, Robin Wilkes, Bijoy Panicker, Paula Tavares, Matthew Cox, An-Hu Li, Hanqing Dong, Lifu Ma, Kenneth (‘Ken’) Foreman, Qinghua (‘Felix’) Weng, Kathryn Stolz
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Publication number: 20080293697Abstract: This invention relates to compounds of formula (I).Type: ApplicationFiled: March 30, 2005Publication date: November 27, 2008Inventors: Andrew Simon Bell, David Graham Brown, David Nathan Abraham Fox, Ian Roger Marsh, Andrew Ian Morrell, Dafydd Rhys Owen, Michael John Palmer, Carol Ann Winslow, Hwang Fun Lu, Thomas Edward Rogers
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Publication number: 20080269131Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: November 9, 2006Publication date: October 30, 2008Inventors: Dirk A. Heerding, Tammy J. Clark, Jack Dale Leber, Igor Safonov
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Patent number: 7439238Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.Type: GrantFiled: January 9, 2006Date of Patent: October 21, 2008Assignee: The Hong Kong University of Science and TechnologyInventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
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Patent number: 7405295Abstract: Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I-a, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I-a effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction.Type: GrantFiled: June 4, 2004Date of Patent: July 29, 2008Assignee: CGI Pharmaceuticals, Inc.Inventors: Kevin S. Currie, Robert W. DeSimone, Scott A. Mitchell, Douglas A. Pippin, James W. Darrow, Xiaobing Qian, Mark Velleca, Dapeng Qian
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Publication number: 20080102405Abstract: A resist composition comprising as a quencher a nitrogen-containing organic compound bearing a nitrogen-containing heterocycle and having a molecular weight of at least 380 exhibits a high resolution and satisfactory mask coverage dependence and is useful in microfabrication using electron beam or deep-UV.Type: ApplicationFiled: October 24, 2007Publication date: May 1, 2008Inventors: Takeru Watanabe, Youichi Ohsawa, Masaki Ohashi, Wataru Kusaki, Tomohiro Kobayashi
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Patent number: 7361662Abstract: A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as kinase modulators.Type: GrantFiled: November 4, 2003Date of Patent: April 22, 2008Assignee: Les Laboratoires ServierInventors: Sylvain Rault, Jean-Charles Lancelot, Marina Kopp, Daniel-Henri Caignard, Bruno Pfeiffer, Pierre Renard
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Patent number: 7358244Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: May 27, 2004Date of Patent: April 15, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 7326702Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, V, W, X and Z are substituents. The present invention also relates to methods for using such compounds.Type: GrantFiled: March 28, 2006Date of Patent: February 5, 2008Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Michael Schwaebe, Adam Siddiqui-Jain, Terence Moran
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Patent number: 7326699Abstract: The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof-alone or in combination with one or more other pharmaceutically active compounds-for the treatment of a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.Type: GrantFiled: May 13, 2002Date of Patent: February 5, 2008Assignee: Novartis AGInventors: Hans-Georg Capraro, Pascal Furet, Carlos Garcia-Echeverria, Paul William Manley
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Patent number: 7312209Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.Type: GrantFiled: December 20, 2002Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 7268128Abstract: Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, these compounds are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.Type: GrantFiled: June 14, 2004Date of Patent: September 11, 2007Assignee: Ausbio Pharma Co., Ltd.Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Patent number: 7235538Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.Type: GrantFiled: July 17, 2003Date of Patent: June 26, 2007Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Lise Brown Christiansen, Jane Marie Lundbeck, Christian K. Sams, Marit Kristiansen
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Patent number: 7229990Abstract: A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1–4C)alkyl, (2–4C)alkenyl, (2–4C)alkynyl, (6–14C)aryl or (4–13C)heteroaryl; R3 is (1–8C)alkyl, (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1—X2 is C?C, C(O)—NH, NH—C(O), C(O)—O, O—C(O), C?N, N?C or S or O. The compounds of the invention can be used in fertility regulation therapies.Type: GrantFiled: September 17, 2001Date of Patent: June 12, 2007Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Johan Karstens
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Patent number: 7217702Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.Type: GrantFiled: April 4, 2005Date of Patent: May 15, 2007Assignee: Adenosine Therapeutics, LLCInventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7211545Abstract: The imidazo[1,2-a]pyrimidines given by the following formula [I]: [wherein R1 and R2 represent a C1–C6 alkyl group optionally substituted by one or more selected from the group consisting of C1–C4 alkoxy group, C2–C8 dialkylamino group, C1–C4 alkylthio group, C2–C5 alkoxycarbonyl group, cyano group and halogen atoms; or R1 and R2 represent a 3–8 membered heterocyclic group together with the nitrogen atom bonded with R1 and R2; R3 represents a halogen atom or C1–C4 alkyl group; and Ar represents a phenyl group optionally substituted by a halogen atom or atoms; and the like] have excellent activity for controlling plant diseases.Type: GrantFiled: August 29, 2002Date of Patent: May 1, 2007Assignee: Sumitomo Chemical Company, LimitedInventor: Hiroshi Ikegami
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Patent number: 7196078Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: October 6, 2005Date of Patent: March 27, 2007Assignee: Schering CorpoartionInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
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Patent number: 7157451Abstract: Novel heterocyclic dihydropyrimidine 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: GrantFiled: September 12, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
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Patent number: 7138398Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).Type: GrantFiled: September 12, 2003Date of Patent: November 21, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
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Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
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Patent number: 7071187Abstract: The present invention provides a novel naphthyridine derivative that is effective for relieving pain, less toxic, and also is effective for treating diabetic neuropathy, the derivative being represented by the general formula (1): wherein R1, R2, R3 and R4 are as described in the description.Type: GrantFiled: February 21, 2002Date of Patent: July 4, 2006Assignee: Otsuka Pharmaceutical Factory, Inc.Inventor: Tadao Shibutani
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Patent number: 7067515Abstract: The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: June 27, 2006Assignee: Pfizer Inc.Inventors: Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Vincent E. Groppi, Jr.
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Patent number: 7026317Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.Type: GrantFiled: November 21, 2001Date of Patent: April 11, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul J. Gilligan, Richard G. Wilde
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Patent number: 7015217Abstract: The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof. In formula I, A is selected from —COR5, —CO2H, —CO2R6, —C(O)NHOH, —C(O)NHOR5, —C(O)NHOR6, —NHRa, —N(OH)COR5, —N(OH)CHO, —SH, —CH2SH, —S(O)(?NH)Ra, —S(?NH)2Ra, —SC(O)Ra, —PO(OH)2, and —PO(OH)NHRa; B is a thiomorpholine ring; X is absent or is CR3R4; and Ua, Xa, Ya, Za, R1, R2, Rb, and q are defined in the present specification.Type: GrantFiled: October 7, 2002Date of Patent: March 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Chu-Biao Xue
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Patent number: 6987116Abstract: This invention provides compounds of Formula (1a)-(1f) wherein: X, R1, and R2 are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection and process for producing said compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 17, 2006Assignee: WyethInventors: Diane Harris Boschelli, Nan Zhang, Ana Carolina Barrios Sosa, Haris Durutlic, Biqi Wu
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Patent number: 6984640Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted deriviatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.Type: GrantFiled: July 14, 1999Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
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Patent number: 6960580Abstract: The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. More particularly, the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: GrantFiled: March 8, 2002Date of Patent: November 1, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Anjali Pandey
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Patent number: 6939007Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.Type: GrantFiled: October 28, 2003Date of Patent: September 6, 2005Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6924283Abstract: The invention provides a compound of formula I: wherein R1, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection, atherosclerosis or restenosis using such compounds or salts.Type: GrantFiled: August 29, 2002Date of Patent: August 2, 2005Assignee: PfizerInventor: Atli Thorarensen
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Patent number: 6908916Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: November 14, 2002Date of Patent: June 21, 2005Assignee: Bristol Myers Squibb CompanyInventors: Harold Mastalerz, Guifen Zhang, James G. Tarrant, Gregory D. Vite
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Patent number: 6900206Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. wherein: Z is Q is selected from the group consisting of: —W— is — represents a carbon-carbon bond or does not exist; and A is NR13R14.Type: GrantFiled: June 9, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Alicia Regueiro-Ren, Qiufen May Xue
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Patent number: 6864259Abstract: The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: May 29, 2002Date of Patent: March 8, 2005Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Kim Marie Hutchings, Dai Nguyen, Rajeshwar Singh, Howard Daniel Hollis Showalter
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Patent number: 6861422Abstract: The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: GrantFiled: February 26, 2003Date of Patent: March 1, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Matthias Hoffmann, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky
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Patent number: 6841558Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating, or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 9, 2001Date of Patent: January 11, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Jennifer J. Bennett
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Patent number: 6828315Abstract: The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives.Type: GrantFiled: October 25, 2001Date of Patent: December 7, 2004Assignee: Warner-Lambert LLCInventors: Bernard Gaudilliere, Remi Lavalette, Charles Andrianjara, Francine Breuzard
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Patent number: 6806268Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula IA and or IB:Type: GrantFiled: May 30, 2002Date of Patent: October 19, 2004Assignee: Alteon, Inc.Inventor: Martin Gall
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Patent number: 6787650Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.Type: GrantFiled: April 5, 2002Date of Patent: September 7, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
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Patent number: 6774233Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: August 10, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6767906Abstract: This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is &agr;) —S(═O)k—NR6R7, in which k is 1 or 2, wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen &agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or &agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, &bgr;) N-(aryl lower alkyl)carbamoyl, or &ggr;) a radical of the formula —NH—S(═O)i—R8, in which i is 1 or 2, R8 is an aliphatic, carbocyclic or heterocyclic radical; or &dgr;) a radical of the formula —NH—C(═O)—R9, and the other variable substituents are as defined herein.Type: GrantFiled: August 10, 2001Date of Patent: July 27, 2004Assignee: Novartis AGInventors: Patricia Imbach, Hans-Georg Capraro, Jürg Zimmermann, Giorgio Caravatti, Pascal Furet, Wolfgang Karl-Diether Brill
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Patent number: 6756371Abstract: The compounds of formula (I) in which R1, R2, A, B and Ar have the meanings as given in the description are novel effective PDe4 inhibitorsType: GrantFiled: April 12, 2002Date of Patent: June 29, 2004Assignee: Altana Pharma AGInventor: Geert Jan Sterk
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Patent number: 6747145Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.Type: GrantFiled: September 4, 2001Date of Patent: June 8, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6730681Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: May 4, 2004Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
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Patent number: 6730676Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: June 18, 2002Date of Patent: May 4, 2004Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Leslie Joseph Street
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Patent number: 6713473Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.Type: GrantFiled: February 19, 2002Date of Patent: March 30, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoyuki Nishikawa, Masaharu Sugai, Kozo Aoki, Makoto Suzuki, Akihiko Ikegawa, Kazunobu Takahashi, Fukuichi Ohsawa, Naomi Masuda, Nobukazu Kakui, Jiro Tanaka, Yuji Tabata, Kenji Asai
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Patent number: 6713474Abstract: Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant rejections and imflammatory disorders.Type: GrantFiled: March 29, 2000Date of Patent: March 30, 2004Assignee: Abbott GmbH & Co. KGInventors: Gavin C. Hirst, David Calderwood, Rainer Munschauer, Lee D. Arnold, David N. Johnston, Paul Rafferty
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Patent number: 6699859Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and a chloro at the 8-position are selective ligands for GABAZA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.Type: GrantFiled: June 26, 2000Date of Patent: March 2, 2004Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Andrew Mitchinson, Leslie Joseph Street
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Patent number: 6696439Abstract: The present invention relates to substituted furo[3,2-b]pyridine compounds of formula I: or a pharmaceutical acid addition salt thereof; where; R is E—D is C═CH or CH—CH2; R1 is hydrogen or C1-C4 alkyl; R2 is hydrogen, halo, hydroxy, —NR3R4, —SR3, —C(O)R3, —C(O)MR3R4, —NR3SO2R5, —NHC(Q)NR3R4, —NHC(O)OR3, or —NR3C(O)R5; R3, R4, and R5 are independently hydrogen, C1-C4 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, or —(CH2)naryl; or R3 and R4 combine, together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, piperazine, 4-substituted piperazine, morpholine, or thiomorpholine ring; n is 0, 1, 2, 3, 4, 5, or 6; and Q is O or S. The present invention further relates to pharmaceutical.Type: GrantFiled: August 1, 2001Date of Patent: February 24, 2004Assignee: Eli Lilly and CompanyInventors: Sandra Ann Filla, Brian Michael Mathes
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Patent number: RE39112Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH?CH— or —C?C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc.Type: GrantFiled: December 24, 1998Date of Patent: May 30, 2006Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Ohashi, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi