Patents Assigned to Merrell Pharmaceuticals Inc.
  • Piperidinyl thiacyclic derivatives
    Patent number: 5650416
    Abstract: Piperidinyl thiacyclic derivatives of the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the specification, are useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 22, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
  • Substituted pyrrolidin-3-yl-alkyl-piperidines
    Patent number: 5648366
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 15, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Tieu-Binh Le, Elizabeth M. Kudlacz, George D. Maynard
  • Diarylalkyl piperidines useful as multi-drug resistant tumor agents
    Patent number: 5648365
    Abstract: Diarylalkyl piperidines of formula (1) ##STR1## reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: July 15, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Sai P. Sunkara, Jules Freedman
  • Method of treating cancer by conjunctive therapy with N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine and a cytotoxic agent
    Patent number: 5646124
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: July 8, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Nellikunja J. Prakash, Terry L. Bowlin
  • Process for piperidine derivatives
    Patent number: 5644061
    Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: July 1, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Chi-Hsin Richard King, Michele A. Kaminski
  • Process for making (2S,5S)-5-fluoromethylornithine
    Patent number: 5637768
    Abstract: The present invention is directed to a process for making (2S,5S)-5-fluoromethylornithine through the reaction of wet penicillin acylase with (2R,5R) and (2S,5S)-6-fluoromethyl-3-(phenylactyl)-amino-2-piperidone and the addition of an acid to the resulting product.
    Type: Grant
    Filed: July 18, 1995
    Date of Patent: June 10, 1997
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Karin Jund, Jean-Bernard Ducep
  • Mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and ACE
    Patent number: 5635502
    Abstract: The present invention relates to certain novel mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and of ACE.These mercaptoacetylamide bicyclic lactam derivatives can be described by the following formula: ##STR1## wherein R is hydrogen, a C.sub.1 -C.sub.4 alkyl, an Ar--Y--group, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3 or diphenylmethyl;R.sub.1 is hydrogen, acetyl, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3, benzoyl or a group of the formula ##STR2## R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, --CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y--group;A is --CH.sub.2 --, --O--, or --S--;B is --S--or --O--; andpharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 3, 1995
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Gary A. Flynn
  • Method of treating cancer by conjunctive therapy with N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine and a cytotoxic agent
    Patent number: 5635218
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Nellikunja J. Prakash, Terry L. Bowlin
  • Substituted pyrrolidin-3-yl-alkyl-piperidines
    Patent number: 5635510
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, George D. Maynard
  • Method of effecting immunosuppression by administering carbocyclic adenosine analogs
    Patent number: 5631258
    Abstract: 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: Grant
    Filed: April 26, 1995
    Date of Patent: May 20, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser
  • Process for piperidine derivatives
    Patent number: 5631375
    Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators, these piperidine derivatives can be described by the following formulas: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen; orR.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;R.sub.3 is --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched;each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts, hydrates and individual optical isomers thereof.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: May 20, 1997
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Chi-Hsin R. King, Michele A. Kaminski, Teng-Man Chen
  • Piperidinyl thiacyclic derivatives
    Patent number: 5631268
    Abstract: Piperidinyl thiacyclic derivatives of the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the specification, are useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: May 20, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John M. Kane, George D. Maynard, Hsien C. Cheng, Mark W. Dudley
  • 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE
    Patent number: 5629309
    Abstract: The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.
    Type: Grant
    Filed: December 14, 1995
    Date of Patent: May 13, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
  • Hypotriglyceridemic aminoacetylmercapto derivatives
    Patent number: 5624921
    Abstract: The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholesterolemia.
    Type: Grant
    Filed: August 9, 1995
    Date of Patent: April 29, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, John F. French, Richard C. Dage
  • Synthetic peptide lung surfactants having covalently bonded antioxidants
    Patent number: 5623052
    Abstract: Synthetic pulmonary surfactants having antioxidant properties consisting of a complex of a polypeptide of 3-4 amino acid residues, with an antioxidant moiety, and a lipid consisting of one or more of the lipids associated with natural pulmonary surfactant were prepared. These surfactants are useful in the treatment of respiratory distress syndrome.
    Type: Grant
    Filed: July 14, 1995
    Date of Patent: April 22, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Larry R. McLean, J. Vincent Edwards
  • Process for piperidine derivatives
    Patent number: 5618940
    Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: April 8, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Chi-Hsin R. King, Michele A. Kaminski
  • Treatment of obsessive-compulsive disorders with 5-HT.sub.2 antagonists
    Patent number: 5618824
    Abstract: The present invention is directed to 5-HT.sub.2 antagonists and their use as agents in the treatment of obsessive-compulsive disorders (OCD). The invention is particularly directed to the compound (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol which is a member of a class of 5-HT.sub.2 antagonists known as N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5-HT.sub.2 receptor site.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: April 8, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Christopher J. Schmidt, John H. Kehne, Robert A. Padich
  • 2-'-ethenylidene cytidine, uridine and guanosine derivatives
    Patent number: 5616702
    Abstract: This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: April 1, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Michael L. Edwards, Donald P. Matthews, James R. McCarthy
  • Method of controlling tumor growth rate
    Patent number: 5614557
    Abstract: .alpha.-Fluoromethyl- or .alpha.-difluoromethylornithine, and certain derivatives thereof, can be used alone or in combination with cytotoxic agents for the treatment of neoplastic diseases.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: March 25, 1997
    Assignee: Marion Merrell et Compagnie C/O Merrell Pharmaceuticals Inc.
    Inventors: Philippe Bey, Michel Jung
  • Inhibition of metastasis in patients having cancer with pyridyloxazole-2-ones
    Patent number: 5610171
    Abstract: This invention is directed to pyridinyloxazole-2-ones which are useful in inhibiting metastasis in patients having cancer. The pyridinyloxazole-2-ones act to inhibit protein kinase C and thereby modulate metastasis in patients having cancer.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: March 11, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Alan J. Bitonti