Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/183)
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Patent number: 5744473Abstract: 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: GrantFiled: September 16, 1996Date of Patent: April 28, 1998Assignee: Euro-Celtique, S.A.Inventors: Mark Chasin, Peter Hofer, David Cavalla
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Patent number: 5739340Abstract: 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: GrantFiled: April 2, 1997Date of Patent: April 14, 1998Assignee: Elf SanofiInventors: Jean Gubin, Michel Renard
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Patent number: 5714479Abstract: 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: GrantFiled: February 20, 1996Date of Patent: February 3, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
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Patent number: 5695684Abstract: 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: GrantFiled: March 27, 1995Date of Patent: December 9, 1997Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
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Patent number: 5677311Abstract: 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: GrantFiled: February 1, 1996Date of Patent: October 14, 1997Assignee: Eisai Co., Ltd.Inventors: Shuhei Miyazawa, Yorihisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
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Patent number: 5670526Abstract: 1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.Type: GrantFiled: December 21, 1995Date of Patent: September 23, 1997Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Dharmpal S. Dodd, Takao Nishi
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Patent number: 5665745Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
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Patent number: 5663449Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 2, 1997Assignee: Hoechst Marion Roussel, Inc.Inventor: Joseph T. Strupczewski
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Patent number: 5658911Abstract: 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: GrantFiled: September 20, 1994Date of Patent: August 19, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
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Patent number: 5654314Abstract: 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: GrantFiled: March 28, 1995Date of Patent: August 5, 1997Assignee: Boehringer Ingelheim KGInventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
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Patent number: 5654319Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5650413Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 22, 1997Assignee: Glycodesign Inc.Inventors: Jeremy Carver, Rajan Shah
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Patent number: 5639745Abstract: 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: GrantFiled: May 25, 1995Date of Patent: June 17, 1997Assignee: SanofiInventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina Morgan Ross, Stanley J. Schmidt
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Patent number: 5639764Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 17, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5637710Abstract: 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: GrantFiled: December 22, 1995Date of Patent: June 10, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
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Patent number: 5633261Abstract: Immunostimulting swainsonine derivatives and methods for their synthesis are provided.Type: GrantFiled: June 1, 1995Date of Patent: May 27, 1997Assignee: Toronto Research Chemicals, Inc.Inventor: David Dime
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Patent number: 5629326Abstract: 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: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: 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
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Patent number: 5627281Abstract: 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: GrantFiled: July 3, 1996Date of Patent: May 6, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: Nick Nikolaides, John F. Gerster
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Patent number: 5624927Abstract: 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: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5621106Abstract: Immunostimulating derivatives of swainsonine and methods for their syntheses are disclosed.Type: GrantFiled: June 1, 1995Date of Patent: April 15, 1997Assignee: Toronto Research Chemicals, Inc.Inventor: David Dime
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Patent number: 5618826Abstract: 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: GrantFiled: May 30, 1995Date of Patent: April 8, 1997Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
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Patent number: 5616705Abstract: 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: GrantFiled: April 19, 1996Date of Patent: April 1, 1997Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
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Patent number: 5614543Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
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Patent number: 5612342Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
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Patent number: 5612343Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5607945Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 4, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5605908Abstract: 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: GrantFiled: October 24, 1994Date of Patent: February 25, 1997Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 5605913Abstract: 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: GrantFiled: June 6, 1995Date of Patent: February 25, 1997Assignee: Hoechst Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Yulin Chiang, Edward J. Glamkowski, Kenneth J. Bordeau, Grover C. Helsley
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Patent number: 5602159Abstract: 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: GrantFiled: June 6, 1995Date of Patent: February 11, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5602158Abstract: 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: GrantFiled: June 6, 1995Date of Patent: February 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5599821Abstract: 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: GrantFiled: June 6, 1995Date of Patent: February 4, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5597842Abstract: 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: GrantFiled: June 6, 1995Date of Patent: January 28, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5593995Abstract: 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: GrantFiled: June 6, 1995Date of Patent: January 14, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5591745Abstract: 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: GrantFiled: June 6, 1995Date of Patent: January 7, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5589494Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 31, 1996Assignee: 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
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Patent number: 5580890Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5580887Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: 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
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Patent number: 5580886Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5580891Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
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1-[(2-pyrimidinyloxy)alkyl]-3-(heteroaryl)pyrrolidines and related compounds and therapeutic utility
Patent number: 5580875Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Joseph T. Strupczewski -
Patent number: 5580879Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: 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
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Patent number: 5574032Abstract: 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: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: 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
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Patent number: 5571814Abstract: 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: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: 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
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Patent number: 5571803Abstract: 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: GrantFiled: December 22, 1995Date of Patent: November 5, 1996Assignee: 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
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Patent number: 5563148Abstract: 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: GrantFiled: April 25, 1995Date of Patent: October 8, 1996Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
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Patent number: 5561128Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 1, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5559117Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
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Patent number: 5559116Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5556909Abstract: 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: GrantFiled: December 2, 1994Date of Patent: September 17, 1996Assignee: Sanofi Winthrop Inc.Inventor: Ranjit C. Desai
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Patent number: 5552398Abstract: 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: GrantFiled: November 14, 1994Date of Patent: September 3, 1996Assignee: SmithKline Beecham p.l.c.Inventors: Francis D. King, Laramie M. Gaster, Paul A. Wyman