Patents Represented by Attorney, Agent or Law Firm T. Helen Payne
-
Patent number: 5830863Abstract: Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.Type: GrantFiled: December 13, 1996Date of Patent: November 3, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Stephen H. Buck, Scott L. Harbeson, John L. Krstenansky, Chester F. Hassman, III, James R. McCarthy
-
Patent number: 5817661Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 Y.sub.7, Y.sub.9 are each nitrogen and Y.sub.8 is a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5817672Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5817874Abstract: The present invention is a process of converting a hydroxy aromatic into a 2-hydroxy-N-arylacetamide, comprising:(1) treating a reaction mixture comprising a salt of a hydroxy aromatic with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture.Type: GrantFiled: March 18, 1997Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Norton P. Peet, John J. Weidner
-
Patent number: 5817660Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5807742Abstract: A method for producing high level expression of neuropeptide receptors and stable cell lines useful therein. This method involves culturing a cell line containing amplified copies of a cDNA sequence encoding a neuropeptide receptor containing an expression control sequence taken from the .beta.-actin transcriptional control element.Type: GrantFiled: August 1, 1996Date of Patent: September 15, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Josephine Yuen-Wai Lai, Alden Keith Henderson, Stephen Henderson Buck, William R. Roeske, Henry J. Yamamura, Shigetada Nakanishi
-
Patent number: 5789540Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.Type: GrantFiled: March 28, 1995Date of Patent: August 4, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: John L. Krstenansky, Simon J. T. Mao
-
Patent number: 5739354Abstract: The present invention relates to a novel process for preparing preparing N-methyl-D-phenylalanyl-N-?1-?3-?(aminoiminomethyl)amino!propyl!-3,3-diflu oro-2-oxohexyl!-L-prolinamide or a pharmaceutically acceptable salt thereof and to a key intermediate by directly guanylating Dakin-West intermediates.Type: GrantFiled: January 23, 1997Date of Patent: April 14, 1998Assignee: Hoechst Marion Roussel, Inc.Inventor: Duane E. Rudisill
-
Patent number: 5731286Abstract: Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.Type: GrantFiled: March 5, 1997Date of Patent: March 24, 1998Assignee: Merrell Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Stephen H. Buck
-
Patent number: 5723466Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group,R is a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: March 3, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5719193Abstract: This invention relates to a method of potentiating cell-mediated immunity which comprises administering to a patient a cell-mediated immunity potentiating amount of a compound of the formula:RHN--Z--NH--(CH.sub.2).sub.m --NH--Z--NHRor a pharmaceutically acceptable salt thereof, wherein m is an integer 3 to 12, Z is a saturated C.sub.2 -C.sub.6 alkylene moiety of straight or branched chain configuration, each R group is independently H, a C.sub.1 -C.sub.6 saturated or unsaturated hydrocarbyl, or --(CH.sub.2).sub.x --(Ar)--X wherein X is H, C.sub.1 -C.sub.6 alkoxy, halogen, C.sub.1 -C.sub.4 alkyl, or --S(O).sub.x R.sub.1, x is an integer 0, 1 or 2, and R.sub.1 is C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: April 14, 1995Date of Patent: February 17, 1998Assignee: Merrell Pharmaceuticals, Inc.Inventors: Terry L. Bowlin, Nellikunja J. Prakash
-
Patent number: 5696248Abstract: Novel oligonucleotide analogs of the formulae I and II ##STR1## in which A, B, D, R.sup.1, R.sup.2, T, U, V, W, X, Y, Z, a, b, m, m', n and n' have the meanings stated in the description, with valuable physical, biological and pharmacological properties, and a process for the preparation thereof are described. Application thereof relates to the use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex forming oligonucleotides), as probes for detecting nucleic acids and as aids in molecular biology.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Carolin Carolus
-
Patent number: 5677291Abstract: A method of lowering plasma cholesterol level in a patient with hypercholesterolemia, by administration of a compound of formula (1) ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group; andR.sub.5 is a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar)wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or napthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, chloro, fluoro or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: January 2, 1996Date of Patent: October 14, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Simon J. T. Mao, Mark T. Yates, Roger A. Parker
-
Patent number: 5654287Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: August 5, 1997Assignee: Merrell Phamaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
-
Patent number: 5646124Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: July 8, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
-
Patent number: 5635218Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: June 3, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
-
Patent number: 5631258Abstract: This invention relates to methods of effecting immunosuppression and inhibiting tumor necrosis factor .alpha. in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of a compound of the formula ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3 is N, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof. Also presented are pharmaceutical compositions comprising compounds of the same formula.Type: GrantFiled: April 26, 1995Date of Patent: May 20, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser
-
Patent number: 5624930Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: March 22, 1995Date of Patent: April 29, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5605903Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is inthe CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: March 22, 1995Date of Patent: February 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5561136Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: May 9, 1995Date of Patent: October 1, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin