One Of The Cyclos Has At Least Seven Members Patents (Class 546/93)
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Patent number: 7037919Abstract: Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.Type: GrantFiled: October 6, 2000Date of Patent: May 2, 2006Assignee: Kaken Pharmaceutical Co. Ltd.Inventors: Keigo Hanada, Kazuyuki Furuya, Kiyoshi Inoguchi, Motonori Miyakawa, Naoya Nagata
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Patent number: 6962924Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising: a) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of from about 55° C. to 70° C., and stirring for 30 to 45 minutes after mixing, and thereafter filtering the solid thereby prepared in hot condition; to yield the polymorphic form 2 having a DSC of 232° C.±2° C.; or b) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of form about 15° C. room temperature (25° C.) and stirring at this temperature for 30 to 45 minutes, then filtering at room temperature; to yield the polymorphic form 1 having a DSC of 224° C.±2° C.Type: GrantFiled: July 17, 2003Date of Patent: November 8, 2005Assignee: Sandoz AGInventors: Anup Kumar Ray, Hiren Patel, Mahendra R Patel
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Patent number: 6894059Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obsructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: GrantFiled: March 23, 2000Date of Patent: May 17, 2005Assignee: UCB S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmund Differding, James Ellis, Marie-Agnes Lassoie, Michelle Young, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Patent number: 6881842Abstract: A process for easily and industrially advantageously producing both a tricyclic fused heterocyclic derivative having acetylcholinesterase inhibitory activity and an intermediate for the derivative. The process for producing the target compounds comprises the following reaction.Type: GrantFiled: September 20, 2001Date of Patent: April 19, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadao Kawarasaki, Hideo Hashimoto, Kiminori Tomimatsu
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Patent number: 6875867Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.Type: GrantFiled: May 30, 2002Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Paul R. Brodfuehrer, Thomas R. Sattelberg, Joydeep Kant, Xinhua Qian
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Publication number: 20040266810Abstract: The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): 1Type: ApplicationFiled: June 23, 2004Publication date: December 30, 2004Applicant: Schering CorporationInventors: Swapan K. Chowdhury, Anima Ghosal, Robert M. Iannucci, Wenqing Feng, Tze-Ming Chan, Shmuel Zbaida, Kevin B. Alton, Ronald J. Doll, Keith P. Minor
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Publication number: 20040242619Abstract: Provided are processes for preparation of polymorphic forms of desloratadine.Type: ApplicationFiled: March 12, 2004Publication date: December 2, 2004Inventors: Zoltan G. Toth, Viktor Gyollai, Adrienne Kovacsne-Mezei, Csaba Szabo, Judith Aronhime, Claude Singer
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Patent number: 6812345Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.Type: GrantFiled: June 24, 2003Date of Patent: November 2, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
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Patent number: 6800636Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 20, 2001Date of Patent: October 5, 2004Assignee: Schering CorporationInventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Publication number: 20040157872Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: February 9, 2004Publication date: August 12, 2004Inventors: Alan B. Cooper, Ronald J. Doll, Anil K. Saksena, Viyyoor M. Girijavallabhan
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Publication number: 20040138226Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17&bgr;-hydroxysteroid dehydrogenase, 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 type 3 17&bgr;-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.Type: ApplicationFiled: December 15, 2003Publication date: July 15, 2004Applicant: SCHERING CORPORATIONInventors: Timothy J. Guzi, Yi-Tsung Liu, Ronald J. Doll, Anil Saksena, Viyyoor M. Girijavallabhan, Jonathan A. Pachter
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Publication number: 20040132744Abstract: Nitric acid salts with medicines active in the respiratory system pathology treatment.Type: ApplicationFiled: December 17, 2003Publication date: July 8, 2004Applicant: Nicox S.A.Inventor: Piero Del Soldato
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Publication number: 20040122232Abstract: An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula I 1Type: ApplicationFiled: October 1, 2003Publication date: June 24, 2004Applicant: SCHERING CORPORATIONInventors: Frank X. Chen, Yee-Shing Wong, Jeffrey M. Eckert, Feng Liang, Nanfei Zou, Agnes S. Kim-Meade, Marc Poirier, Tiruvettipuram K. Thiruvengadam, George G. Wu
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Publication number: 20040122018Abstract: Disclosed are novel tricyclic compounds represented by the formula (1.Type: ApplicationFiled: December 19, 2002Publication date: June 24, 2004Applicant: Schering CorporationInventors: Hugh Y. Zhu, F. George Njoroge, Alan B. Cooper, Timothy Guzi, Dinanath F. Rane, Keith P. Minor, Ronald J. Doll, Viyyoor M. Girijavallabhan, Bama Santhanam, Patrick A. Pinto, Bancha Vibulbhan, Kartik M. Keertikar, Carmen S. Alvarez, John J. Baldwin, Ge Li, Chia-Yu Huang, Ray A. James, W. Robert Bishop, James J-S Wang, Jagdish A. Desai
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Patent number: 6750347Abstract: A process is provided for preparing a compound having the formula wherein R is H or Cl.Type: GrantFiled: June 18, 2002Date of Patent: June 15, 2004Assignee: Schering-CorporationInventors: Marc Poirier, Yee-Shing Wong, George G. Wu
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Patent number: 6740661Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 20, 2001Date of Patent: May 25, 2004Assignee: Schering CorporationInventors: Arthur G. Taveras, Ronald J. Doll, Alan B. Cooper, Johan A. Ferreira, Timothy Guzi, Alan K. Mallams, Dinanath F. Rane, Viyyoor M. Girijavallabhan, Adriano Afonso, Cynthia J. Aki, Jianping Chao, Carmen Alvarez, Joseph M. Kelly, Tarik Lalwani, Jagdish A. Desai, James J-S Wang, Jay Weinstein
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Publication number: 20040058949Abstract: This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine.Type: ApplicationFiled: July 17, 2003Publication date: March 25, 2004Inventors: Anup Kumar Ray, Hiren Patel, Mahendra R. Patel
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Patent number: 6706892Abstract: Methods of and compositions for pulmonary delivery of therapeutic agents which are capable of forming covalent bonds with a site of interest or which have formed a covalent bond with a pulmonary solution protein are disclosed. Therapeutic agents useful in the invention include wound healing agents, antibiotics, anti-inflammatories, anti-oxidants, anti-proliferatives, immunosupressants, anti-infective and anti-cancer agents.Type: GrantFiled: September 6, 2000Date of Patent: March 16, 2004Assignee: Conjuchem, Inc.Inventors: Alan M. Ezrin, Angelica Fleser, Martin Robitaille, Peter G. Milner, Dominique P. Bridon
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Publication number: 20040048875Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: ApplicationFiled: August 8, 2003Publication date: March 11, 2004Applicant: UCB S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Michelle Young, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Patent number: 6699872Abstract: Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.Type: GrantFiled: November 1, 2001Date of Patent: March 2, 2004Assignee: Schering CorporationInventors: Stacy W. Remiszewski, Alan K. Mallams
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Patent number: 6689789Abstract: Novel compounds of the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO−; R1 and R3 are the same or different and each represents halo; R2 and R4 are the same or different and each is selected from H and halo, provided that at least one of R2 and R4 is H; T is a substituent selected from SO2R or Z is O or S; n is zero or an integer from 1 to 6; R is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, heterocycloalkyl, or N(R5)2; R5 is H, alkyl, aryl, heteroaryl or cycloalkyl. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.Type: GrantFiled: September 4, 2002Date of Patent: February 10, 2004Assignee: Schering CorporationInventors: Alan B. Cooper, Ronald J. Doll, Anil K. Saksena, Viyyoor M. Girijavallabhan
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Patent number: 6673781Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.Type: GrantFiled: February 1, 2002Date of Patent: January 6, 2004Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
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Publication number: 20030229099Abstract: Disclosed are novel tricyclic compounds represented by the formula (1.Type: ApplicationFiled: February 27, 2002Publication date: December 11, 2003Inventors: Hugh Y. Zhu, F. George Njoroge, Alan B. Cooper, Timothy Guzi, Dinanath F. Rane, Keith P. Minor, Ronald J. Doll, Viyyoor M. Girijavallabhan, Bama Santhanam, Patrick A. Pinto, Bancha Vibulbhan, Kartik M. Keertikar, Carmen S. Alvarez, John J. Baldwin, Ge Li, Chia-Yu Huang, Ray A. James, W. Robert Bishop, James J-S Wang, Jagdish A. Desai
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Publication number: 20030220347Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.Type: ApplicationFiled: September 12, 2002Publication date: November 27, 2003Applicant: UCB S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Michelle Young, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Patent number: 6642222Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.Type: GrantFiled: May 3, 2000Date of Patent: November 4, 2003Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Patent number: 6627636Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.Type: GrantFiled: December 4, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 6620821Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and pharmaceutically acceptable salts thereof, n is 0 or 1; x is 0, 1, 2, 3 or 4; y is 0, 1, 2, 3 or 4, provided that at least one of x and y is other than 0; and optionally one or more carbons of (CH2)x and/or (CH2)y together with additional carbons form a 3 to 7 membered spirocyclic ring; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; R3 is H or lower alkyl; R4 and R7 are as defined herein.Type: GrantFiled: December 4, 2001Date of Patent: September 16, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 6608202Abstract: In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen, and intermediates therefor from easily available starting materials by a simple route.Type: GrantFiled: August 20, 2002Date of Patent: August 19, 2003Assignee: Schering CorporationInventors: Henry J. Doran, Pat M. O'Neill, Robert P. Williams
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Publication number: 20030144314Abstract: In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen, 1Type: ApplicationFiled: August 20, 2002Publication date: July 31, 2003Applicant: Schering CorporationInventors: Henry J. Doran, Pat M. O'Neill, Robert P. Williams
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Patent number: 6579883Abstract: The invention relates to compounds of formula (I), to a method for producing them and to their use in medicaments as NOS inhibitors.Type: GrantFiled: May 10, 2001Date of Patent: June 17, 2003Assignee: Schering AktiengesellschaftInventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Hölscher, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Macdougall McDonald
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Patent number: 6576639Abstract: Novel compounds, such as: are disclosed. Also disclosed are methods for inhibiting the abnormal growth of cells, for inhibiting farnesyl protein transferase and for treating cancers using the novel compounds.Type: GrantFiled: March 8, 2000Date of Patent: June 10, 2003Assignee: Schering CorporationInventors: Ronald J. Doll, Joseph M. Kelly, Alan K. Mallams, F. George Njoroge, Stacy W. Remiszewski, Arthur G. Taveras
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Publication number: 20030092726Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: September 4, 2002Publication date: May 15, 2003Inventors: Alan B. Cooper, Ronald J. Doll, Anil K. Saksena, Viyyoor M. Girijavallabhan
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Publication number: 20030055035Abstract: 1Type: ApplicationFiled: May 3, 2000Publication date: March 20, 2003Inventors: Willilam A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Publication number: 20030050319Abstract: A process is provided for preparing a compound having the formula 1Type: ApplicationFiled: June 18, 2002Publication date: March 13, 2003Inventors: Marc Poirier, Yee-Shing Wong, George G. Wu
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Patent number: 6528523Abstract: The present invention describes compounds useful for the inhibition of Farnesyl Protein Transferase. This invention also discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with FPT.Type: GrantFiled: November 27, 2001Date of Patent: March 4, 2003Assignee: Schering CorporationInventors: F. George Njoroge, Bancha Vibulbhan, Viyyoor M. Girijavallabhan, Xiongwei Shi
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Patent number: 6528522Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.Type: GrantFiled: September 18, 2001Date of Patent: March 4, 2003Assignee: Schering CorporationInventors: Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Jr., Adriano Afonso
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Publication number: 20030040520Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: December 20, 2001Publication date: February 27, 2003Inventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Publication number: 20030028026Abstract: The present invention relates to nitric acid salts with medicines active in the respiratory system pathology treatment.Type: ApplicationFiled: May 22, 2002Publication date: February 6, 2003Applicant: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6514520Abstract: An antihistaminic syrup is stabilized against degradation of the active ingredient, by the addition of and about 0.05 to about 5 mg/mL of an aminopolycarboxylic acid such as a salt of ethylenediaminetetraacetic acid.Type: GrantFiled: July 5, 2001Date of Patent: February 4, 2003Assignee: Schering CorporationInventors: Farah J. Munayyer, Frank Guazzo, Elliot I. Stupak, Imtiaz A. Chaudry, Joel A. Sequeira
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Patent number: 6509346Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.Type: GrantFiled: July 28, 1999Date of Patent: January 21, 2003Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C. B. Harriman
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Patent number: 6506767Abstract: Crystalline polymorphs of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cycloheptic[1,2-b]pyridine represented by the formula pharmaceutical compositions containing such polymorphs, and methods of using such polymorphs to treat allergic reactions in mammals such as man are disclosed.Type: GrantFiled: July 1, 1998Date of Patent: January 14, 2003Assignee: Schering CorporationInventors: Doris P. Schumacher, Junning Lee, Lawrence R. Rogers, Charles G. Eckhart, Naneshwar S. Sawant, Michael B. Mitchell
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Patent number: 6506756Abstract: The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.Type: GrantFiled: September 18, 2001Date of Patent: January 14, 2003Assignee: Schering CorporationInventors: Neng-Yang Shih, Daniel M. Solomon, John J. Piwinski, Andrew T. Lupo, Jr., Michael J. Green
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Publication number: 20020198216Abstract: The present invention discloses novel tricyclic compounds represented by the formula (1.Type: ApplicationFiled: August 28, 2001Publication date: December 26, 2002Inventors: F. George Njoroge, Bancha Vibulbhan, Alan B. Cooper, Timothy Guzi, Dinanath F. Rane, Keith P. Minor, Ronald J. Doll, Viyyoor M. Girijavallabhan, Bama Santhanam, Patrick A. Pinto, Hugh Y. Zhu, Kartik M. Keertikar, Carmen S. Alvarez, John J. Baldwin, Ge Li, Chia-Yu Huang, Ray A. James, W. Robert Bishop, James J-S Wang, Jagdish A. Desai
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Patent number: 6495689Abstract: Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy.Type: GrantFiled: June 21, 2001Date of Patent: December 17, 2002Assignee: Schering CorporationInventors: Charles F. Bernard, Michael Casey, Frank Xing Chen, Denise C. Grogan, Marc Poirier, Robert P. Williams, Yee-Shing Wong, George G. Wu
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Patent number: 6495690Abstract: This invention relates to process for producing annulated pyridine bases by reacting cyclic ketones with aliphatic aldehyde in presence of ammonia in gaseous phase in the presence of a catalyst. This process provides an eco-friendly, more economical and highly selective heterogeneous method.Type: GrantFiled: March 27, 2001Date of Patent: December 17, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Shivanand Janardan Kulkarni, Kondapuram Vijaya Raghavan, Radha Rani Vippagunta, Srinivas Nagabandi
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Patent number: 6492381Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 Also disclosed are novel compounds of the formulas: and Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.Type: GrantFiled: May 16, 2000Date of Patent: December 10, 2002Assignee: Schering Corp.Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
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Patent number: 6492519Abstract: A process is provided for preparing a compound having the formula comprising: (a) reacting a compound having the formula with an isocyanate having the formula R1NCO to produce a compound having the formula (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula in the presence of a strong base to produce a compound having the formula and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnRA, and Al(RA)2; RA is alkyl; X is halo; R1 is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group.Type: GrantFiled: April 17, 2001Date of Patent: December 10, 2002Assignee: Schering CorporationInventors: Marc Poirier, Yee-Shing Wong, George G. Wu
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Publication number: 20020160997Abstract: The present invention is a chemical compound of formula (I) 1Type: ApplicationFiled: December 14, 2001Publication date: October 31, 2002Inventors: Jonathan Mark Bentley, Michael John Bickerdike, Paul Hebeisen, Guy Anthony Kennett, Sean Lightowler, Patrizio Mattei, Jacques Mizrahi, Timothy James Morley, Jean-Marc Plancher, Hans Richter, Stephan Roever, Sven Taylor, Steven Paul Vickers
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Patent number: 6472530Abstract: This invention provides novel dithiepino[6,5-b]pyridines of the following formulae: These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.Type: GrantFiled: September 1, 2000Date of Patent: October 29, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John H. Dodd, Kenneth C. Rupert, James L. Bullington, Daniel A. Hall
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Patent number: RE38460Abstract: The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is or R″ and Y together form ═CH; R is (C1-C5) alkyl, wherein n is 0 or 1, X is H, (C1-C5) alkyl; (C1-C5) alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis-(C1-C5) alkyl; —(CH2)m COOZ, wherein m=0-5, Z is H or (C1-C5) alkyl; —CH═CH—G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl substituted by (C1-C5) alkyl at the nitrogen atom; R′ is H, (C1-C5) alkyl, pyridoyl, benzoyl substituted by (C1-C5) alkyloxy; R″ is H or (C1-C5) alkyl; processes for their use as acetylcholinesterase inhibitor.Type: GrantFiled: March 6, 2001Date of Patent: March 9, 2004Assignee: Shanghai Institute of Materia Medica Chinese Academy of SciencesInventors: Dayuan Zhu, Xican Tang