Patents Represented by Attorney, Agent or Law Firm William Lee
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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: 6355801Abstract: A process is provided for producing a compound having the formula: by: (a) reacting a compound having the formula with a compound having the formula in the presence of an organic base selected from the group consisting of: triethylamine; N,N-diisopropylethylamine; 1,8-diazabicyclo[5.4.0]undec-7-ene(1,5-5); 1,5-diazabicyclo[4.3.0]non-5-ene; or 1,4-diazabicyclo[2.2.2]octane to form a compound having the formula (b) reducing the compound of formula (4.0) to form the compound of formula (1.0), wherein X is Cl, Br, I or F.Type: GrantFiled: November 6, 2000Date of Patent: March 12, 2002Assignee: Schering CorporationInventors: Brigitte Giesinger, Ingrid Mergelsberg
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Patent number: 6346524Abstract: A method for treating a patient afflicted with cancer is provided, in which temozolomide is administered to the patient for at least two cycles of a cyclical dosing schedule, wherein each cycle has a dosing period of 5 to 25 days, in which temozolomide is administered daily, at a dose of 40 to 150 mg/m2/day, followed by a rest period of 5 to 14 days in which temozolomide is not administered. Also provided is a medical kit for administering temozolomide, having printed instructions for administering temozolomide according to the cyclical dosing schedule set forth above, and a supply of temozolomide in dosage units for at least one cycle, wherein each dosage unit contains 5 to 250 mg of temozolomide and a pharmaceutically acceptable carrier.Type: GrantFiled: March 27, 2000Date of Patent: February 12, 2002Assignee: Schering CorporationInventor: Mohamed H. Ragab
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Patent number: 6316483Abstract: Aqueous nasal spray compositions comprising a medicament and an aqueous carrier comprising water soluble polymers selected from the group consisting of polyvinylpyrrolidone and mixtures thereof.Type: GrantFiled: November 5, 1999Date of Patent: November 13, 2001Assignee: Schering CorporationInventors: Joseph A. Haslwanter, William F. Rencher
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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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Patent number: 6265614Abstract: Intermediates having the formula wherein BI is —CH2OH or —CH2ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; TI is —OH or QI is phenyl, naphthyl ohr heteroaryl having 1-3 substituents; Ra and Rc are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl cycloalkyl, aryl, or —OH; or Ra and Rc together with the C—N—C chain to which they are bound, form a 5-7 membered ring; Rb and Rd are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl, or —OH; and D is a directing group capable of directing lithiation alpha to a nitrogen atom of a nitrogen compound having D as a substituent bound to the nitrogen atom when the nitrogen compound is reacted with s-butyl lithium, are disclosedType: GrantFiled: October 13, 2000Date of Patent: July 24, 2001Assignee: Schering CorporationInventors: Anantha R. Sudhakar, Suhan Tang
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Patent number: 6228985Abstract: The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara tType: GrantFiled: May 21, 1998Date of Patent: May 8, 2001Assignee: Schering CorporationInventors: Christine H. Blood, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 6204282Abstract: The present invention provides compounds having the formula wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y1 each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, —CF3, and —C(O)OH; R1, R2, R3 and R4 are as defined herein; R5, R6, R7, R8, R9, R10, R11 and R12 are independently selected from H or C1-C3 alkyl; and wherein are positioned meta or para relative to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.Type: GrantFiled: November 29, 1999Date of Patent: March 20, 2001Assignee: Schering CorporationInventors: Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 5520764Abstract: A laminate comprises a first substrate including a first layer of a blend of a polyolefin and an antifogging agent, and a bonding layer of polyolefin, preferably an ethylene unsaturated ester copolymer or low density polyethylene; a second substrate bonded to the bonding layer of the first substrate and comprising polyester or nylon; and a conventional adhesive between the first and second substrates; the bonding layer pre-treated by corona discharge before wind-up, and again treated by corona discharge before lamination. The laminates of the present invention exhibit much improved bond strength compared with conventional laminates.Type: GrantFiled: April 7, 1995Date of Patent: May 28, 1996Assignee: W.R. Grace & Co.-Conn.Inventors: Gloria G. Toney, Robert A. Young, David V. Babb
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Patent number: 5486387Abstract: An impact resistant film suitable for medical solution pouches and the packaging of parenteral materials generally includes an interior layer of an ethylene vinyl acetate copolymer and outer layers of a propylene homopolymer or copolymer blended with a styrene ethylene butylene styrene copolymer. In some cases, a flexible copolyester may be substituted for one of the outer blend materials. Sacrificial layers may be optionally be included on one or both outer surfaces of the film to improve processing.Type: GrantFiled: August 27, 1993Date of Patent: January 23, 1996Assignee: W. R. Grace & Co.-Conn.Inventor: Walter B. Mueller