Piperazine Ring Patents (Class 544/121)
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Patent number: 6699989Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds.Type: GrantFiled: August 28, 2000Date of Patent: March 2, 2004Inventor: B. Vithal Shetty
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Patent number: 6689779Abstract: The present invention relates to novel oxazolidinone derivatives, their pharmaceutically acceptable salts and a process for the preparation thereof. More particularly, the present invention relates to oxazolidinone derivatives having pyridine or pyrimidine moeity substituted by heterocycle and heteroaromaticcycle at 4-position of phenyl ring. The compounds of the present invention have wide antibacterial spectrum, superior antibacterial activity and low toxicity, such that the compound of this invention can be used as an antibacterial agent.Type: GrantFiled: November 27, 2002Date of Patent: February 10, 2004Assignee: Dong A Pharm. Co., Ltd.Inventors: Jae-Gul Lee, Won-Bin Leem, Jong-Hwan Cho, Sung-Hak Choi, Jong-Jin Lee, Sang-Kuk Park, Tae-Hoo Lee, Dong-Goo Kim, Hyun-Jung Sung
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Patent number: 6683181Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: November 5, 2002Date of Patent: January 27, 2004Assignee: Pharmacia and Upjohn ComapnyInventors: Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
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Patent number: 6677336Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: January 13, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
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Patent number: 6670363Abstract: The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared to known compounds such as fluconazole and itraconazole and the processes for the preparation thereof. This invention also relates to pharmaceutical compositions containing the compounds of the present invention and their use in treating and/or preventing fungal infections in mammals, preferably humans.Type: GrantFiled: May 22, 2000Date of Patent: December 30, 2003Assignee: Ranbaxy Laboratories LimitedInventors: Ashwani Kumar Verma, Sudershan K. Arora, Jasbir Singh Arora, Ashok Rattan
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Patent number: 6670364Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: January 29, 2002Date of Patent: December 30, 2003Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Publication number: 20030232814Abstract: Compounds of the general formula (I): 1Type: ApplicationFiled: May 16, 2003Publication date: December 18, 2003Inventors: Bjorn M. Nilsson, Erik Ringberg
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Patent number: 6660858Abstract: The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: wherein R1 to R4 and Z have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminobenzoxazole derivative compounds.Type: GrantFiled: March 28, 2001Date of Patent: December 9, 2003Assignee: Lion Bioscience AGInventors: Scott C. Sutton, Amy L. Hannah, Yuewu Chen, Shirong Zhu
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Patent number: 6653313Abstract: The present invention relates to compounds of the formula wherein each A is independently halo; Y is —(CH2)m—, —C(O)— or —S(O)—; R1 and R2 are independently C1-4 alkyl; R3 is substituted azacycloalkyl etc.; R4 is phenyl substituted at the 2-position with a substituent selected from substituted C1-7 alkyl, substituted C1-7 alkoxy, amine, etc; R5 is hydrogen or C1-4 alkyl; m is 0, 1 or 2; and n is 0, 1, 2, 3, 4 or 5. The present invention also relates to pharmaceutical compositions containing such compounds and to the use of such compounds in the treatment and prevention of inflammation, asthma, allergic rhinitis, pain and other disorders.Type: GrantFiled: July 11, 2001Date of Patent: November 25, 2003Assignee: Warner-Lambert Company LLCInventors: Mitsuhiro Kawamura, Makoto Kawai, Yuji Shishido, Tomoki Kato, Yasuhiro Katsu, Takafumi Ikeda, Noriaki Murase
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Patent number: 6649611Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disorders.Type: GrantFiled: March 29, 2001Date of Patent: November 18, 2003Assignee: Pfizer, Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Molly A. McGlynn, Christopher S. Poss
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Patent number: 6645904Abstract: The present invention relates to compounds of the formula in which one, two or three of the radicals R1, R2, R3 and R4 are where m and n are an integer from 1 to 10, R5, R6, R7 and R8 are, independently of one another, identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and the remaining radical(s) R1 to R4 are or —NR9R10, where R9 and R10 are identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and X− is an inorganic or organic anion or an equivalent of a multiply charged inorganic or organic anion. The invention further relates to mixtures of substances comprising compounds of the formula (1), to a process for preparing the compounds of the formula (1) and to the use thereof.Type: GrantFiled: April 30, 2002Date of Patent: November 11, 2003Assignee: Clariant GmbHInventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
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Patent number: 6642232Abstract: The present invention relates to certain 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives that inhibit kinases, in particular VEGFR and/or PDGFR kinases. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.Type: GrantFiled: October 10, 2002Date of Patent: November 4, 2003Assignee: Sugen, Inc.Inventors: Matthew Mattson, Tomas Vojkovsky, Congxin Liang, Peng Cho Tang, Huiping Guan
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 6620811Abstract: The present invention relates to compounds of the formula wherein R1, A and R are as described within. The compounds of the present invention have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have an affinity to the A2A-receptor and are therefore useful in the treatment of diseases related to this receptor.Type: GrantFiled: November 5, 2002Date of Patent: September 16, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20030153753Abstract: (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]-2-(3-hydroxy-4-methylbenzyl)piperazine dihydrochloride is obtained by debenzylating (2R)-4-benzyl-1-[3,5-bis(trifluoromethyl)-benzoyl]-2-(3-hydroxy-4-methylbenzyl)piperazine, then N-alkylating and converting to hydrochloride.Type: ApplicationFiled: December 13, 2002Publication date: August 14, 2003Inventors: Keiichi Koga, Ryoki Orii, Yosuke Fujii, Shunsuke Goto, Satoshi Hirabayashi
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Patent number: 6599902Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.Type: GrantFiled: May 30, 2002Date of Patent: July 29, 2003Assignee: Sugen, Inc.Inventors: Jingrong Cui, John Ramphal, Congxin Liang, Connie Li Sun, Chung Chen Wei, Peng Cho Tang
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Patent number: 6593327Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: December 14, 2001Date of Patent: July 15, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Clifford M. Bryant, James T. Palmer, Robert M. Rydzewski, Eduardo L. Setti, Zong-Qiang Tian, Shankar Venkatraman, Dan-Xiong Wang
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Publication number: 20030130275Abstract: The invention relates to novel sulphonamide compounds having 5-HT7 antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.Type: ApplicationFiled: November 27, 2002Publication date: July 10, 2003Applicant: SmithKline Beecham p.l.c.Inventor: Peter John Lovell
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Publication number: 20030125320Abstract: The present invention provides compounds of the formula: 1Type: ApplicationFiled: June 20, 2002Publication date: July 3, 2003Applicant: H. Lundbeck A/SInventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
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Patent number: 6583136Abstract: The present invention concerns compounds of formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or dioxolane ring substituted with aryl and azolmethyl; —A—B— represents an optionally substituted bivalent radical of formula —N═CH—, —CH═N—, —CH═CH—, —CH2—CH2; Alk represents C1-6alkanediyl; Y represents optionally substituted C1-6alkanediyl; R1 and R2 represent hydrogen, C1-6alkyl or arylC1-6alkyl; or R1 and R2 may be taken together to form an optionally substituted heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or phthalimid-1-yl; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; having broad-spectrum antifungal activity; their preparation, compositions containing them anType: GrantFiled: February 4, 2002Date of Patent: June 24, 2003Assignee: Janssen Pharmacuetica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx
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Patent number: 6579872Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: November 2, 2000Date of Patent: June 17, 2003Assignee: AstraZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6579982Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: August 9, 2000Date of Patent: June 17, 2003Assignee: Pfizer Inc.Inventor: Julian Blagg
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Patent number: 6573262Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.Type: GrantFiled: December 19, 2001Date of Patent: June 3, 2003Assignee: Bristol-Myers Sqibb CompanyInventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
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Patent number: 6562813Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: March 6, 2002Date of Patent: May 13, 2003Assignee: Pfizer Inc.Inventor: Harry Ralph Howard
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Patent number: 6555537Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.Type: GrantFiled: November 29, 2000Date of Patent: April 29, 2003Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 6548498Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives of the formula I as (R)-enantiomers, (S)-enantiomers, or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof. The present invention further relates to a process for the preparation of the compounds, to pharmaceutical compositions containing the compounds and to methods of treatment of 5-hydroxytryptamine-mediated disorders comprising administering the compounds.Type: GrantFiled: October 21, 1998Date of Patent: April 15, 2003Assignee: AstraZeneca ABInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Patent number: 6525049Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: February 25, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
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Patent number: 6525052Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Patent number: 6511980Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 10, 2001Date of Patent: January 28, 2003Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 6506750Abstract: N-(phenylacetyl)morpholine derivatives useful as NK1 receptor antagonists, a process for the preparation thereof, and pharmaceutical compositions containing them as active principle.Type: GrantFiled: September 24, 2001Date of Patent: January 14, 2003Assignee: Sanofi-SynthelaboInventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
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Patent number: 6498162Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: November 1, 2000Date of Patent: December 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Publication number: 20020177598Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: ApplicationFiled: November 29, 2000Publication date: November 28, 2002Applicant: Schering AktiengschellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 6476026Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: March 15, 2000Date of Patent: November 5, 2002Assignee: Axys Pharmaceuticals, Inc.Inventors: Clifford M. Bryant, James T. Palmer, Robert M. Rydzewski, Eduardo L. Setti, Zong-Qiang Tian, Shankar Venkatraman, Dan-Xiong Wang
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6472388Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: November 6, 2001Date of Patent: October 29, 2002Assignee: Pfizer IncInventor: Harry Ralph Howard
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Patent number: 6465643Abstract: The present invention relates to compounds of the formula in which one, two or three of the radicals R1, R2, R3 and R4 are where m and n are an integer from 1 to 10, R5, R6, R7 and R8 are, independently of one another, identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and the remaining radical(s) R1 to R4 are or —NR9R10, where R9 and R10 are identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and X− is an inorganic or organic anion or an equivalent of a multiply charged inorganic or organic anion. The invention further relates to mixtures of substances comprising compounds of the formula (1), to a process for preparing the compounds of the formula (1) and to the use thereof.Type: GrantFiled: July 17, 2000Date of Patent: October 15, 2002Assignee: Clariant GmbHInventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
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Patent number: 6465456Abstract: This invention describes isoxazolinone derivatives which possess antibacterial activity and are useful in the treatment of bacterial diseases. More particularly, new isoxazolinones are provided having the general formula I wherein R1, R2, R3, L and L1 are as described in the specification.Type: GrantFiled: June 28, 2001Date of Patent: October 15, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Dane M. Springer, Jason T. Goodrich, Zhaoxing Meng, Lawrence B. Snyder
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Patent number: 6462046Abstract: Compounds having the structure are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the piperazine derivatives of the invention make them particularly useful in the treatment of those conditions selected from the group consisting of diabetes, atherosclerosis, hyperglycemia, hyperlipidemia, obesity, syndrome X, insulin resistance, hypertension, heart failure and cardiovascular disease in mammals.Type: GrantFiled: December 11, 2000Date of Patent: October 8, 2002Assignee: Advanced SynTech, LLCInventors: Boliang Lou, Adnan M. M. Mjalli
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6455520Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: March 23, 2001Date of Patent: September 24, 2002Assignee: Astra Zeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6448244Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.Type: GrantFiled: November 9, 2000Date of Patent: September 10, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken
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Patent number: 6440974Abstract: Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.Type: GrantFiled: February 20, 2001Date of Patent: August 27, 2002Assignee: Schering CorporationInventors: Ronald J. Doll, Carmen Alvarez, Tarik Lalwani, Yi-Tsung Liu
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Patent number: 6432949Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q1 is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and Q2 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: February 2, 2001Date of Patent: August 13, 2002Assignee: AstraZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6423708Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.Type: GrantFiled: December 8, 2000Date of Patent: July 23, 2002Assignee: Pfizer INCInventors: Megan Ann Gibbs, Harry Ralph Howard, Jeffrey Scott Sprouse, Joel Barry Schachter, Phillip Branch Chappell
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Patent number: 6413987Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.Type: GrantFiled: June 6, 2000Date of Patent: July 2, 2002Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6407106Abstract: N-triazolylmethyl-piperazine compounds which exhibit neurokinin receptor antagonistic activity corresponding to the formula I: wherein R1, R2 and R3 have the meanings given in the specification; pharmaceutical compositions containing these compounds; a process for preparing these compounds, and intermediate products of this process.Type: GrantFiled: July 27, 2001Date of Patent: June 18, 2002Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Uwe Schoen, Holger Sann, Reinhard Brueckner, Christian Eeckhout
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Patent number: 6407103Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: December 6, 2000Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: David A. Nugiel, David J. Carini, Susan V. Di Meo, Eddy W. Yue
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Patent number: 6403593Abstract: The present invention relates to triazole compounds of the following formula: where R1, R2, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: January 13, 2000Date of Patent: June 11, 2002Assignee: Abbott LaboratoriesInventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
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Publication number: 20020065276Abstract: N-triazolylmethyl-piperazine compounds which exhibit neurokinin receptor antagonistic activity corresponding to the formula I: 1Type: ApplicationFiled: July 27, 2001Publication date: May 30, 2002Inventors: Daniel Jasserand, Uwe Schoen, Holger Sann, Reinhard Brueckner, Christian Eeckhout
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Patent number: RE37729Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler