Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/183)
  • Patent number: 5744473
    Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. Also provided is a process of making compounds of Formula I. Compounds of the present invention are represented by Formula I: ##STR1## its pharmaceutically acceptable salts, hydrochloride salts, or prodrug forms thereof, wherein:X.sub.1a, X.sub.1b are independently selected from --NH and --N-lower alkyl;X.sub.2a, X.sub.2b are optionally present and are independently selected from S(O)n, O, CH.sub.2, and NH;P.sub.1a, P.sub.1b, P.sub.2a, P.sub.2b, P.sub.4a, and P.sub.4b are independently selected from N, or CH;R.sub.1a, R.sub.1b, R.sub.2a, R.sub.2b, R.sub.3a and R.sub.3b are independently selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 branched alkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: September 16, 1996
    Date of Patent: April 28, 1998
    Assignee: Euro-Celtique, S.A.
    Inventors: Mark Chasin, Peter Hofer, David Cavalla
  • Patent number: 5739340
    Abstract: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group,each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.
    Type: Grant
    Filed: April 2, 1997
    Date of Patent: April 14, 1998
    Assignee: Elf Sanofi
    Inventors: Jean Gubin, Michel Renard
  • Patent number: 5714479
    Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: February 3, 1998
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
  • Patent number: 5695684
    Abstract: A mesomorphic compound represented by a formula (I) containing a quinoline-2,6-diyl skeleton is suitable as a component for a liquid crystal composition providing improved response characteristics and a high contrast. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of electrode plates. The liquid crystal device may preferably be used as a display panel constituting a liquid crystal apparatus providing good display characteristics.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: December 9, 1997
    Assignee: Canon Kabushiki Kaisha
    Inventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
  • Patent number: 5677311
    Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: October 14, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Shuhei Miyazawa, Yorihisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
  • Patent number: 5670526
    Abstract: 1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: September 23, 1997
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Dharmpal S. Dodd, Takao Nishi
  • Patent number: 5665745
    Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 9, 1997
    Assignee: Eli Lilly and Company
    Inventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
  • Patent number: 5663449
    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: June 6, 1995
    Date of Patent: September 2, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 5658911
    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. 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: September 20, 1994
    Date of Patent: August 19, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
  • Patent number: 5654314
    Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: August 5, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
  • Patent number: 5654319
    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: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5650413
    Abstract: The invention relates to novel mannosidase inhibitors, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 22, 1997
    Assignee: Glycodesign Inc.
    Inventors: Jeremy Carver, Rajan Shah
  • Patent number: 5639745
    Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: June 17, 1997
    Assignee: Sanofi
    Inventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina Morgan Ross, Stanley J. Schmidt
  • Patent number: 5639764
    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: June 6, 1995
    Date of Patent: June 17, 1997
    Assignee: Hoechst-Marion-Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5637710
    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: December 22, 1995
    Date of Patent: June 10, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5633261
    Abstract: Immunostimulting swainsonine derivatives and methods for their synthesis are provided.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: May 27, 1997
    Assignee: Toronto Research Chemicals, Inc.
    Inventor: David Dime
  • Patent number: 5629326
    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: June 6, 1995
    Date of Patent: May 13, 1997
    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
  • Patent number: 5627281
    Abstract: 6,7-propylene-, butylene-, or pentylene-bridged imidazopyridin-4-amines and their intermediate compounds are described. Also disclosed are pharmaceutical compositions containing such compounds and methods of inducing interferon (.alpha.) biosynthesis and treating vital infections involving the use of such compounds.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: May 6, 1997
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Nick Nikolaides, John F. Gerster
  • Patent number: 5624927
    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: June 6, 1995
    Date of Patent: April 29, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5621106
    Abstract: Immunostimulating derivatives of swainsonine and methods for their syntheses are disclosed.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 15, 1997
    Assignee: Toronto Research Chemicals, Inc.
    Inventor: David Dime
  • Patent number: 5618826
    Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification; and acid addition and quaternary ammonium salts of formula (I) compounds are described. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: April 8, 1997
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 5616705
    Abstract: Compounds of the formula I ##STR1## where the substituents have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.
    Type: Grant
    Filed: April 19, 1996
    Date of Patent: April 1, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
  • Patent number: 5614543
    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: June 6, 1995
    Date of Patent: March 25, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
  • Patent number: 5612342
    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: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 5612343
    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: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5607945
    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: June 6, 1995
    Date of Patent: March 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5605908
    Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: October 24, 1994
    Date of Patent: February 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: Leander Merritt, John S. Ward
  • Patent number: 5605913
    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: June 6, 1995
    Date of Patent: February 25, 1997
    Assignee: Hoechst Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Yulin Chiang, Edward J. Glamkowski, Kenneth J. Bordeau, Grover C. Helsley
  • Patent number: 5602159
    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: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5602158
    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: June 6, 1995
    Date of Patent: February 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5599821
    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: June 6, 1995
    Date of Patent: February 4, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5597842
    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: June 6, 1995
    Date of Patent: January 28, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5593995
    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: June 6, 1995
    Date of Patent: January 14, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5591745
    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: June 6, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5589494
    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: June 6, 1995
    Date of Patent: December 31, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5580890
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5580887
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5580886
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5580891
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
  • Patent number: 5580875
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 5580879
    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: June 6, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5574032
    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: June 6, 1995
    Date of Patent: November 12, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571814
    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: June 6, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5571803
    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: December 22, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5563148
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: October 8, 1996
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 5561128
    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: June 6, 1995
    Date of Patent: October 1, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5559117
    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: June 6, 1995
    Date of Patent: September 24, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
  • Patent number: 5559116
    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: June 6, 1995
    Date of Patent: September 24, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5556909
    Abstract: Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: September 17, 1996
    Assignee: Sanofi Winthrop Inc.
    Inventor: Ranjit C. Desai
  • Patent number: 5552398
    Abstract: Compounds of formula (I), ##STR1## wherein L is N or CR.sub.c, wherein R.sub.c is hydrogen, alkoxy, halo, alkyl or cyano; Q is NR.sub.1, CH.sub.2, O, or S; R.sub.a is hydrogen, halo, alkyl, amino, nitro or alkoxy; R.sub.b is hydrogen, halo, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, aralkyl, alkanoyl, or alkanoylalkyl; R.sub.2 is alkoxy; R.sub.3 is hydrogen, chloro or fluoro; R.sub.4 is hydrogen, alkyl, amino optionally substituted by alkyl, halo, hydroxy or alkoxy; R.sub.5 is hydrogen, halo, alkyl, alkoxy, nitro, amino or alkylthio; R.sub.6 is hydrogen, halo, alkyl, alkoxy or amino; n is 0, 1, 2, 3, or 4; p and m are independently 0, 1 or 2; and R.sub.q is hydrogen or C.sub.1-6 are 5-HT.sub.4 receptor antagonists.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: September 3, 1996
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis D. King, Laramie M. Gaster, Paul A. Wyman