One Of The Cyclos Has At Least Seven Members Patents (Class 546/93)
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Publication number: 20020151714Abstract: The invention concerns a process for preparing 1,4-disubstituted piperidine compounds of formula (I), in which Y =-(CH2) n , n being 0. 1. 2 or 3; oxygen; sulphur; vinyl, -CH 2 -0-; -0-CH 2; -CH 2 -S- or -S-CH 2 , and R and Z mean substituents known per se. Compounds in which Z means -CH 2 -CH 2 - are produced in that the correspondingly substituted 5,6-dihydro- 11 H -benzo[5,6]-cyclohepta-[1,2-b] pyridin-11-one compound is reacted with the corresponding 1-substituted 4-piperidone in a single process step by means of reductive dimerization in the presence of a finely dispersed metal of the IVth and/or Vth and/or VIth subgroup of the periodic table of elements or a low-valent oxidation stage of a corresponding metal compound of this type, the finely dispersed metal or the low-valent oxidation stage being produced in situ by means of a reducing agent and in the presence of an inert solvent. Preferably 4-(5.Type: ApplicationFiled: January 31, 2000Publication date: October 17, 2002Inventors: MAX REY, STEFAN GLADOW
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Patent number: 6451801Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines 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 preferable 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: GrantFiled: March 24, 2000Date of Patent: September 17, 2002Assignee: UCB, S.A.Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
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Publication number: 20020119973Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: July 28, 1999Publication date: August 29, 2002Inventors: JAY R. LULY, YOSHISUKE NAKASATO, ETSUO OHSHIMA, HIROKI SONE, OSAMU KOTERA, GERALDINE C.B. HARRIMAN
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Publication number: 20020119981Abstract: 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: ApplicationFiled: November 1, 2001Publication date: August 29, 2002Inventors: Stacy W. Remiszewski, Alan K. Mallams
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Patent number: 6440989Abstract: Novel phenyl-substituted tricyclic 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: February 13, 2001Date of Patent: August 27, 2002Assignee: Schering CorporationInventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
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Publication number: 20020115679Abstract: 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: ApplicationFiled: November 27, 2001Publication date: August 22, 2002Inventors: F. George Njoroge, Bancha Vibulbhan, Viyyoor M. Girijavallabhan, Xiongwei Shi
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Publication number: 20020103207Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: December 20, 2001Publication date: August 1, 2002Inventors: 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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Patent number: 6426352Abstract: Novel tricyclic sulfonamide 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 sulfonamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.Type: GrantFiled: August 13, 1999Date of Patent: July 30, 2002Assignee: Schering CorporationInventors: F. George Njoroge, Bancha Vibulbhan, Arthur G. Taveras, Ronald J. Doll, Viyyoor M. Girijavallabhan
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Publication number: 20020086859Abstract: 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: ApplicationFiled: September 18, 2001Publication date: July 4, 2002Inventors: Neng-Yang Shih, Daniel M. Solomon, John J. Piwinski, Andrew T. Lupo, Michael J. Green
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Patent number: 6413984Abstract: The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being substituted by one or two R5 groups; R1 represents a hydrogen atom, a C1-C6 alkyl, a C2-C6 alkenyl, a C1-C2 perfluoroalkyl or a C1-C6 fluoroalkyl group; R2, R3 or R4, independently of one another, represent a hydrogen atom, a C1-C6 alkyl, group or a C2-C6 alkenyl group, or R1 and R2 can together form a C1-C6 alkylene chain, or a C3-C6 alkenylene chain; R5 represents a C1-C6 alkyl group, and R6 represents a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, C3-C6 cycloalkyl, C3-C6 cycloalkenyl or a benzyl.Type: GrantFiled: August 1, 2001Date of Patent: July 2, 2002Assignee: Sanofi-SynthelaboInventors: Christophe Philippo, Alain Braun, Philippe R. Bovy
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Publication number: 20020082272Abstract: 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: ApplicationFiled: September 18, 2001Publication date: June 27, 2002Inventors: Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Adriano Afonso
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Patent number: 6410541Abstract: 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 R represents a cycloalkyl or a heterocycloalkyl ring that is substitued. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.Type: GrantFiled: January 24, 2001Date of Patent: June 25, 2002Assignee: Schering CorporationInventors: Stacy W. Remiszewski, Ronald J. Doll, Carmen Alvarez, Tarik Lalwani
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Publication number: 20020077331Abstract: Disclosed is a process for preparing a compound having the formula: 1Type: ApplicationFiled: June 21, 2001Publication date: June 20, 2002Inventors: 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: 6399615Abstract: Novel compounds of the formula: wherein 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 wherein R5 is H (C1-C6)alkyl or a bond; b and c are independently 0 to 3 and Y is a three, four, five or six membered cycloalkyl ring, pyridyl, pyrazinyl or phenyl are disclosed. Pharmaceutical Compositions containing such compounds, methods of inhibiting farnesyl protein transferase and methods for treating tumor cells using such compounds or compositions are also disclosed.Type: GrantFiled: August 7, 2000Date of Patent: June 4, 2002Assignee: Schering CorporationInventors: Timothy J. Guzi, Dinanath F. Rane
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Publication number: 20020061901Abstract: 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 1Type: ApplicationFiled: December 4, 2001Publication date: May 23, 2002Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
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Patent number: 6391887Abstract: The invention relates to compounds of formula (I), as defined herein. The invention also relates to the use of the inventive compounds for treatment of a disease caused by the effects of nitrogen monoxide in pathological conditions.Type: GrantFiled: August 14, 2000Date of Patent: May 21, 2002Assignee: Schering AktiengesellschaftInventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Holscher, Detlev Sulzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
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Patent number: 6387905Abstract: Novel compounds of the formula: are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: wherein R1, R3 and R4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.Type: GrantFiled: March 1, 2001Date of Patent: May 14, 2002Assignee: Schering CorporationInventors: F George Njoroge, Arthur G. Taveras, Ronald J. Doll, Tarik Lalwani, Carmen Alvarez, Stacy W. Remiszewski
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Patent number: 6372909Abstract: 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, by (A) reacting a compound having the formula wherein RA, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula: wherein RA, RB, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl.Type: GrantFiled: November 18, 1999Date of Patent: April 16, 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: 6372747Abstract: 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 16, 1999Date of Patent: April 16, 2002Assignee: Schering CorporationInventors: Arthur G. Taveras, Ronald J. Doll, Alan B. Cooper, Johan A. Ferreira, Timothy Guzi, Dinanath F. Rane, Viyyoor M. Girijavallabhan, Cynthia J. Aki, Jianping Chao, Carmen Alvarez, Joseph M. Kelly, Tarik Lalwani, Jagdish A. Desai, James J-S Wang
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Patent number: 6365588Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of the formulas 5.0, 5.1 and 5.2, wherein R is —C(R20)(R21)(R46), and 5.3, 5.3A and 5.3B, wherein R is —N(R25)(R48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.Type: GrantFiled: July 9, 1999Date of Patent: April 2, 2002Assignee: Schering CorporationInventors: Robert W. 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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Publication number: 20020035261Abstract: A process is provided for preparing a compound having the formula 1Type: ApplicationFiled: April 17, 2001Publication date: March 21, 2002Inventors: Marc Poirier, Yee-Shing Wong, George G. Wu
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Patent number: 6358968Abstract: 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: January 14, 2000Date of Patent: March 19, 2002Assignee: Schering CorporationInventors: Stacy W. Remiszewski, Alan K. Mallams
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Publication number: 20020028826Abstract: 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 1Type: ApplicationFiled: June 6, 2001Publication date: March 7, 2002Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
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Publication number: 20020019400Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: March 1, 2001Publication date: February 14, 2002Inventors: FGeorge Njoroje, Arthur G. Taveras, Ronald J. Doll, Tarik Lalwani, Carmen Alvarez, Stacy W. Remiszewski
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Patent number: 6335347Abstract: A polymorph form 2 of ethyl 4(8-chloro-5,6,-dihydro-11H- benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidene carboxylate (hereinafter “loratadine”) represented by the formula Pharmaceutical composition containing the polymorph form 2, and methods of using the polymorph form 2 to treat allergic reactions in mammals such as man are disclosed.Type: GrantFiled: October 8, 1998Date of Patent: January 1, 2002Assignee: Schering CorporationInventors: Dinesh Gala, Donald J. DiBenedetto
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Patent number: 6329385Abstract: 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 the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1999Date of Patent: December 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Publication number: 20010039283Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: April 4, 2001Publication date: November 8, 2001Inventors: Alan B. Cooper, Ronald J. Doll, Anil K. Saksena, Viyyoor M. Girijavallabhan
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Patent number: 6307048Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.Type: GrantFiled: November 18, 1999Date of Patent: October 23, 2001Assignee: Schering CorporationInventors: Shen-Chun Kuo, Charles F. Bernard, Frank Xing Chen, Donald Hou, Agnes S. Kim-Meade, George G. Wu
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Patent number: 6300338Abstract: 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: 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: July 7, 1999Date of Patent: October 9, 2001Assignee: Schering CorporationInventors: 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: 6288233Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.Type: GrantFiled: September 21, 2000Date of Patent: September 11, 2001Assignee: Schering CorporationInventors: Shen-Chun Kuo, Frank Xing Chen
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Publication number: 20010016585Abstract: Novel phenyl-substituted tricyclic 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: ApplicationFiled: February 13, 2001Publication date: August 23, 2001Inventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
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Publication number: 20010014681Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: February 20, 2001Publication date: August 16, 2001Inventors: Ronald J. Doll, Carmen Alvarez, Tarik Lalwani, Yi-Tsung Liu
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Patent number: 6271378Abstract: Disclosed is a process for preparing a compound having the formula: wherein R1 is selected from the group consisting of: alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, and cycloalkylalkyl, R1 being optionally substituted by substituents selected from halo, —OH, alkyl, alkoxy, or —CF3, said process comprising the following steps: (a) reacting a ketone having the formula with a carbanion having the formula wherein R1 is as defined above, and R2 and R3 are independently selected from the group consisting of —ORA and —RA, wherein RA is alkyl, phenyl, substituted phenyl, cycloalkyl, substituted cycloalkyl, cycloalkylalkyl, or substituted cycloalkylalkyl; (b) treating the reaction mixture from step (a) with a protonating agent; and (c) thermally decomposing the product of 16, to form the compound of formula (I). The compounds made by this process have antihistaminic activity, e.g., loratadine.Type: GrantFiled: December 16, 1999Date of Patent: August 7, 2001Assignee: Schering CorporationInventors: Henry J. Doran, Pat M. O'Neill
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Publication number: 20010007870Abstract: Novel compounds of the formula: 1Type: ApplicationFiled: January 24, 2001Publication date: July 12, 2001Inventors: Stacy W. Remiszewski, Ronald J. Doll, Carmen Alvarez, Tarik Lalwani
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Patent number: 6248750Abstract: There are disclosed compounds having the formula wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, —SH, loweralkylthio, —NHCOR2 or —NR3R4 where R2 is hydrogen or loweralkyl, and R3 and R4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.Type: GrantFiled: March 24, 2000Date of Patent: June 19, 2001Assignee: Hoechst Roussel PharmaceuticalsInventors: Gregory Michael Shutske, Kevin James Kapples
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Patent number: 6242458Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of the formulas 5.1 and 5.2 are disclosed.Type: GrantFiled: September 21, 1999Date of Patent: June 5, 2001Assignee: Schering CorporationInventors: 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: 6239140Abstract: 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: June 15, 1998Date of Patent: May 29, 2001Assignee: Schering CorporationInventors: Alan B. Cooper, Ronald J. Doll, Anil K. Saksena, Viyyoor M. Girijavallabhan
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Patent number: 6228865Abstract: 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: November 23, 1999Date of Patent: May 8, 2001Assignee: Schering CorporationInventors: Ronald J. Doll, Carmen Alvarez, Tarik Lalwani, Yi-Tsung Liu
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Patent number: 6228856Abstract: Novel compounds of the formula: are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: wherein R1, R3 and R4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.Type: GrantFiled: October 14, 1999Date of Patent: May 8, 2001Assignee: Schering CorporationInventors: F George Njoroge, Arthur G. Taveras, Ronald J. Doll, Tarik Lalwani, Carmen Alvarez, Stacy W. Remiszewski
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Patent number: 6218401Abstract: Novel phenyl-substituted tricyclic 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: August 13, 1999Date of Patent: April 17, 2001Assignee: Schering CorporationInventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
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Patent number: 6211193Abstract: 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 R represents a cycloalkyl or a heterocycloalkyl ring that is substitued. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.Type: GrantFiled: June 15, 1998Date of Patent: April 3, 2001Assignee: Schering CorporationInventors: Stacy W. Remiszewski, Ronald J. Doll, Carmen Alvarez, Tarik Lalwani
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Patent number: 6191140Abstract: 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: October 20, 1999Date of Patent: February 20, 2001Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Patent number: 6159986Abstract: Therapies and compounds for the inhibition of memory loss. In one embodiment, a combination of Huperzine A and hypericin is employed.Type: GrantFiled: November 2, 1999Date of Patent: December 12, 2000Inventor: David A. Altman
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Patent number: 6159984Abstract: Novel compounds of the formula: ##STR1## wherein a represents N or NO, R.sup.1 and R.sup.3 are halo, R.sup.2 and R.sup.4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents ##STR2## wherein R.sub.5 is H (C.sub.1 -C.sub.6)alkyl or a bond; b and c are independently 0 to 3 and Y is a three, four, five or six membered cycloalkyl ring, pyridyl, pyrazinyl or phenyl are disclosed. Pharmaceutical Compositions containing such compounds, methods of inhibiting farnesyl protein transferase and methods for treating tumor cells using such compounds or compositions are also disclosed.Type: GrantFiled: June 15, 1998Date of Patent: December 12, 2000Assignee: Schering CorporationInventors: Timothy J. Guzi, Dinanath F. Rane
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Patent number: 6150355Abstract: A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.Type: GrantFiled: March 13, 1998Date of Patent: November 21, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
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Patent number: 6143758Abstract: Novel compounds, such as: ##STR1## 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: November 12, 1998Date of Patent: November 7, 2000Assignee: Schering CorporationInventors: Ronald J. Doll, Joseph M. Kelly, Alan K. Mallams, F. George Njoroge, Stacy W. Remiszewski, Arthur G. Taveras
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Patent number: 6130228Abstract: Compounds of Formula (I), methods for their preparation, pharmaceutical formulations and use thereof.Type: GrantFiled: August 25, 1998Date of Patent: October 10, 2000Assignee: University of StrathclydeInventors: George Rennet Proctor, Alan Lang Harvey, Maureen Theresa McKenna, Steven John Mullins
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Patent number: 6084100Abstract: The process consists of the reductive coupling between the compounds: 8-chloro-5,6-dihydrobenzo[5,6]cyclohepta[1,2-b]pyridin-11-one (formula VII) ##STR1## and ethyl 4-oxopiperidine-1-carboxylate (formula IV) ##STR2## through the action of low-valent titanium species.Type: GrantFiled: April 13, 1998Date of Patent: July 4, 2000Assignee: Medichem, S.A.Inventors: Alberto Stampa, Pelayo Camps, Gloria Rodriguez, Jordi Bosch, Maria del Carmen Onrubia
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Patent number: 6075144Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.Type: GrantFiled: June 13, 1994Date of Patent: June 13, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory Michael Shutske, Kevin James Kapples
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Patent number: 6075025Abstract: 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 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## 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: March 11, 1998Date of Patent: June 13, 2000Assignee: Schering CorporationInventors: 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