Patents Represented by Attorney, Agent or Law Firm Tatsuya Ikeda
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Patent number: 6358491Abstract: The invention provides novel peptide-based pharmacophores and compounds which bind somatostatin receptors with high affinity and which exhibit improved pharmacokinetic properties over known somatostatin analogs. The pharmacophores and compounds of the invention may be used in labeled or unlabeled form for diagnosing and/or treating somatostatin responsive diseases. The invention also provides radiopharmaceuticals and kits comprising these compounds, as well as methods for diagnosing and/or treating somatostatin receptor mediated diseases.Type: GrantFiled: September 16, 1999Date of Patent: March 19, 2002Assignee: Berlex Laboratories, Inc.Inventors: John Lister-James, Richard T. Dean, Daniel A. Pearson, David M. Wilson
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Patent number: 6248304Abstract: This invention provides scintigraphic imaging agents and reagents for preparing said agents, methods for radiolabeling said reagents and kits containing non-radioactive reagents and other components for the convenient preparation of the scintigraphic imaging agents. More specifically, the invention provides scintigraphic imaging agents that are radiolabeled compounds which bind with high affinity to GPIIb/IIIa receptors on activated platelets and using such radiolabeled compounds derivatives to image sites in a mammalian body.Type: GrantFiled: September 27, 1996Date of Patent: June 19, 2001Assignee: Berlex Laboratories, Inc.Inventors: John Lister-James, Richard T. Dean
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Patent number: 5846992Abstract: Herein is described an ocular composition comprising an ocular decongestant such as phenylephrine and certain labdane derivatives which are intraocular pressure lowering agents. The composition not only markedly reduces the ocular reddening otherwise produced by such labdane compounds, but also unexpectedly prolongs and frequently potentiates their intraocular pressure lowering effect. Both of these effects are very beneficial to the use of such labdanes for the treatment of glaucoma.Also described herein is an ocular composition comprising para-aminoclonidine (an .alpha..sub.2 -adrenoreceptor agonist) and certain labdane derivatives mentioned above. The composition reduces the ocular reddening and lacrimation, and also potentiates the intraocular pressure lowering effect.Type: GrantFiled: March 6, 1997Date of Patent: December 8, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Paul Gary Conway, Grover Cleveland Helsley, Joachim Eggert Roehr
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Patent number: 5478753Abstract: There is described a positive calibrator/control composition for use in assays for the detection of antibodies to infectious disease agents. The composition includes a composite antibody of a nonspecific IgM immunoglobulin moiety covalently linked to a specific, non-IgM antibody moiety. Also described is an assay method which utilizes the positive calibrator or control composition.Type: GrantFiled: June 29, 1993Date of Patent: December 26, 1995Assignee: PB Diagnostic Systems, Inc.Inventors: T. Philip Wong, Russell A. Hammond
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Patent number: 5405856Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl;m is 1 or 2;eachR.sub.4 is independently hydrogen or loweralkyl; andY is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: April 2, 1993Date of Patent: April 11, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
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Patent number: 5401749Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R.sub.2 and R.sub.3 are independently H or CH.sub.3 ; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6 where R.sub.4 is hydrogen or loweralkyl, and R.sub.5 and R.sub.6 are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR.sub.7 R.sub.8 or CR.sub.7 R.sub.8 --CR.sub.9 R.sub.10 ; and L and Q are independently CR'.sub.7 R'.sub.8, CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10, CR'.sub.7 .dbd.CR'.sub.9 or CR'.sub.7 R'.sub.8 --CR'.sub.9 R'.sub.10 --CR.sub.11 R.sub.12, where each of R.sub.7 through R.sub.12 and R'.sub.7 through R'.sub.Type: GrantFiled: July 8, 1988Date of Patent: March 28, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5391553Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.Type: GrantFiled: September 14, 1988Date of Patent: February 21, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Grover C. Helsley, Kevin J. Kapples
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Patent number: 5389629Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: January 10, 1991Date of Patent: February 14, 1995Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Richard C. Effland
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Patent number: 5356910Abstract: There is disclosed a method of alleviating obsessive compulsive disorders which comprises administration of an effective amount of a compound of the formula. ##STR1## where m is 1 or 2;R is H, halogen, loweralkyl, loweralkoxy, arylloweralkoxy, hydroxy, nitro, amino, loweralkylamino or diloweralkylamino;R.sub.1 is H or loweralkyl;R.sub.2 is H or loweralkyl; andR.sub.3 is H, halogen or loweralkyl.Type: GrantFiled: July 19, 1993Date of Patent: October 18, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Sathapana Kongsamut, Craig P. Smith, Ann T. Woods
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Patent number: 5350762Abstract: There are disclosed various compounds of the formula below, ##STR1## where the various parameters R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, m and n are as defined in the specification, which show activities as a monoamine oxidase inhibitor demonstrating a utility for the treatment of depression, and activities as a cholinesterase inhibitor demonstrating a utility for the treatment of various memory dysfunctions such as Alzheimer's disease.Type: GrantFiled: March 8, 1993Date of Patent: September 27, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Lawrence L. Martin, Larry Davis
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Patent number: 5328920Abstract: There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorder.Type: GrantFiled: October 21, 1992Date of Patent: July 12, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Lawrence L. Martin, Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5300498Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters n, R.sub.1, R.sub.2 and X are as defined in the specification which are selective inhibitors of the reuptake of the serotonin and as such are useful for the treatment of depression and obsessive compulsive disorder.Type: GrantFiled: June 4, 1993Date of Patent: April 5, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventor: Gregory M. Shutske
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Patent number: 5298626Abstract: There are disclosed various compounds of the formula below, ##STR1## wherein n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.Type: GrantFiled: November 13, 1992Date of Patent: March 29, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
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Patent number: 5240927Abstract: There are disclosed various compounds of the formula depicted below, ##STR1## where the parameters m, n, p, q, X and R are as defined in the specification, as being useful as antipsychotic agents.Type: GrantFiled: May 19, 1992Date of Patent: August 31, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Nicholas J. Hrib, John G. Jurcak
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Patent number: 5234941Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: August 5, 1992Date of Patent: August 10, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Denise M. Flanagan, Lawrence L. Martin
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Patent number: 5232927Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl;each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or aryllowralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl,--SH, loweralkylthio,--NHCOR.sub.4 or--NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl;with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.Type: GrantFiled: April 18, 1991Date of Patent: August 3, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 5231093Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: August 5, 1992Date of Patent: July 27, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Denise M. Flanagan, Lawrence L. Martin
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Patent number: 5221682Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dematoses.Type: GrantFiled: May 3, 1991Date of Patent: June 22, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
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Patent number: 5214059Abstract: There are described compounds of the formula ##STR1## where A is CH or N;X is hydrogen, loweralkyl, halogen, trifluromethyl, loweralkoxy, arylloweralkoxy, hydroxy or phenylamino;Y is hydrogen, loweralkyl, halogen, loweralkoxy, arylloweralkoxy or hydroxy;R.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl or aryloxycarbonyl;R.sub.3 is hydrogen, alkyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ;which compounds are useful as topical antiinflammatory agents for the treatment of skin disorders.Type: GrantFiled: August 10, 1992Date of Patent: May 25, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
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Patent number: D373782Type: GrantFiled: May 2, 1994Date of Patent: September 17, 1996Assignee: International Polarizer, Inc.Inventor: Robert Shelton