Abstract: 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:
Grant
Filed:
June 7, 1995
Date of Patent:
October 6, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
Abstract: 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.
Abstract: 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:
Grant
Filed:
June 7, 1995
Date of Patent:
October 6, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Abstract: The present invention relates to a novel process for preparing cis-4-O-protected-substituted-2-cyclopentenol derivatives comprising, a) dissolving a 4-O-protected-2-cyclopentenone in a suitable organic solvent; and b) treating the solution with a suitable Lewis acid and a suitable reducing agent at a temperature of from about -100.degree. C. to about 20.degree. C. The cis-4-O-protected-substituted-2-cyclopentenol derivatives are useful intermediates in the preparation of various cyclopentanyl and cyclopentenyl purine analogs which are useful as immunosuppressants and in the preparation of various prostaglandins.
Type:
Grant
Filed:
June 17, 1997
Date of Patent:
September 15, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Timothy T. Curran, David A. Hay, Jonathan C. Evans
Abstract: This invention relates to compounds of the formula ##STR1## wherein X is halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, amino or trifluoromethyl; andY is --CN or --NR.sup.1 R.sup.2 ;wherel is an integer of 0, 1 or 2;m is an integer of 0, 1 or 2;n is an integer of 2, 3 or 4, except when Y is CN, in which case n can also be 1;R.sup.1 is hydrogen, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkylcarbonyl;R.sup.2 is hydrogen, (C.sub.1 -C.sub.10)alkylcarbonyl, (C.sub.3 -C.sub.12)cycloalkylcarbonyl, hydroxy-(C.sub.1 -C.sub.6)alkylcarbonyl, phenylcarbonyl, thienylcarbonyl or benzothienylcarbonyl;orR.sub.1 and R.sup.2 together with nitrogen atom to which they are attached form the ring ##STR2## where A is C.dbd.O or CH.sub.2 ;andB is C.dbd.O, CHOH, CH.sub.2 or CH.sub.2 CH.sub.2 ; andZ is halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, amino or trifluoromethyl p is 0 or 1; and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and their use for the treatment of psychoses.
Type:
Grant
Filed:
June 6, 1997
Date of Patent:
September 1, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Nicholas Joseph Hrib, John Gerard Jurcak, Abdul E. Mutlib
Abstract: A compound selected from the following formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, m and n are as defined in the specification having antipsychotic activity.
Type:
Grant
Filed:
October 9, 1996
Date of Patent:
September 1, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Nicholas Joseph Hrib, John Gerard Jurcak
Abstract: Peptides that bind to the interleukin-1 type I receptor (IL-1RtI) can be used to assay the amount of IL-1R, or an IL-1R agonist or antagonist, in a sample and comprise a sequence of amino acids selected from the group consisting of (1) WXXXGZ.sub.1 W where Z.sub.1 is L, I, A, or Q; (2) XXQZ.sub.5 YZ.sub.6 XX where Z.sub.5 is P or Aze where Aze is azetidine; and Z.sub.6 is S, A, V, or L; and (3) Z.sub.23 NZ.sub.24 SZ.sub.25 Z.sub.26 Z.sub.27 Z.sub.28 Z.sub.29 Z.sub.30 L where Z.sub.23 is D or Y; Z.sub.24 is D or S; Z.sub.25 is S or W; Z.sub.26 is S or Y; Z.sub.27 is D or V; Z.sub.28 is S or W; Z.sub.29 is F or L; and Z.sub.30 is D or L; and where each amino acid is indicated by standard one letter abbreviation; and each X can be selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids. Also provided are peptides which bind to the IL-1RtI, which are 11 to 40 amino acids in length, which comprise the core sequence of amino acids:Z.sub.31 XWZ.sub.32 Z.sub.33 Z.sub.34 Z.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
July 28, 1998
Assignees:
Affymax Technologies N.V., Hoechst Marion Roussel, Inc.
Inventors:
Ronald W. Barrett, Stephen D. Yanofsky, David Baldwin, Jeff W. Jacobs, Phillipe R. Bovy, Ellen M. Leahy, Richard S. Pottorf
Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined within, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
July 7, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
Abstract: This invention relates to a method of treating a patient in need of relief from convulsions which comprises administering to such a patient a convulsion-alleviating amount of a compound of the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, m and n are as defined within.
Type:
Grant
Filed:
July 8, 1996
Date of Patent:
July 7, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Francis Parker Huger, Craig Paul Smith, Sathapana Kongsamut, Lei Tang
Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
Type:
Grant
Filed:
October 25, 1994
Date of Patent:
July 7, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
Type:
Grant
Filed:
July 29, 1997
Date of Patent:
June 23, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
Abstract: The present invention is related to a novel process for preparing N-acetyl-(L)-4-cyanophenylalanine by resolving the racemic compound N-acetyl-(D,L)-4-cyanophenylalanine ethyl ester, and a novel process to prepare a stereoisomer of Ac-(L)-pAph-Chg-PalMe(3)-NH.sub.2 by using the intermediate N-acetyl-(L)-4-cyanophenylalanine.
Abstract: The present invention relates to a novel process for the preparation of 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones from 1-halo-3-trialkylsilanyl-benzenes. 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones are useful for the treatment of Alzheimer's disease and senile dementia. In addition, the present invention relates to a novel process for purifying 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones utilizing a novel extraction method.
Type:
Grant
Filed:
June 18, 1996
Date of Patent:
June 2, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Roberto Gandolfi, deceased, Dennis K. Klipa, Neal J. Fetner
Abstract: Novel spiro?cyclopent?b!indole-piperidines!, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro?cyclopent?b!indole-piperidines! and intermediates, or compositions thereof are disclosed.
Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.
Abstract: The present invention relates to certain mercaptoacetylamide disulfide derivatives of Formula (I) ##STR1## useful as inhibitors of enkephalinase and ACE.
Type:
Grant
Filed:
November 4, 1996
Date of Patent:
May 12, 1998
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Gary A. Flynn, Douglas W. Beight, Shujaath Mehdi, Alan M. Warshawsky, John F. French, John H. Kehne
Abstract: This application relates to a retractable batch reactor sampler that is temporarily attached to a reactor, for use in sampling small volumes of a reaction mixture within a reactor on single or multiple occasions, and then detached from the reactor, all without affecting an inert gas blanket already existing within the reactor.
Abstract: 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.
Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
Type:
Grant
Filed:
November 1, 1996
Date of Patent:
April 14, 1998
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Thomas T. Ortyl, Paul F. Skultety, Kristen C. Mitchell, Deepak S. Phadke, Faraneh Attarchi, Marquerite L. Pierce, Aaron W. Schoeneman, Joseph M. Schnitz