Ring Carbons Shared By Each Of The Three Cyclos (e.g., 1,8-naphthalimides, Etc.) Patents (Class 514/296)
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Patent number: 7148352Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: GrantFiled: August 16, 2002Date of Patent: December 12, 2006Assignee: Queen's University at KingstonInventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Patent number: 7135481Abstract: Methods of treating a solid tumor are disclosed comprising administering amonafide in combination with an antiproliferative agent.Type: GrantFiled: February 25, 2005Date of Patent: November 14, 2006Assignee: ChemGenex Pharmaceuticals, Inc.Inventor: Dennis M. Brown
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Patent number: 6989390Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X? or R1 is —(CH2)nN+HR3R4 X? or —(CH2)nNR3R4 when R2 is —N+HR6R7. R2 is —OR5, halogen, —NR6R7, —N+HR6R7 X?? sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X? is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).Type: GrantFiled: October 20, 2003Date of Patent: January 24, 2006Assignee: Xanthus Life Sciences, Inc.Inventors: Alfred M. Ajami, David O. Barlow
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Patent number: 6921771Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: February 19, 2002Date of Patent: July 26, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Patent number: 6903127Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: July 30, 2002Date of Patent: June 7, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Patent number: 6890945Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: July 30, 2002Date of Patent: May 10, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214825Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214824Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214823Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 14, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040214826Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pharmacia & Upjohn CompanyInventors: Robert M. McCall, Martin Durham Meglasson
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Patent number: 6809112Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually mating amount is from about 0.003 thru 0.2 mg/kg/dose.Type: GrantFiled: July 30, 2002Date of Patent: October 26, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20040176337Abstract: This invention relates to topical compositions of an antibacterial benzoquinolizine-2-carboxylic acid, incorporated either as the single therapeutic ingredient in hitherto undescribed pharmaceutical compositions, or as an ingredient in novel combination with at least one agent selected from a retinoid, an antifungal agent, another antibacterial compound and/or a steroid/non-steroid anti-inflammatory agent, to processes for preparation of the compositions, to use of the compositions in preparation of a medicament, and to a method of therapeutic or prophylactic use of such a composition for the treatment of dermal, ophthalmic, otic and nasal infections, with or without attendant inflammation.Type: ApplicationFiled: December 31, 2003Publication date: September 9, 2004Applicant: WOCKHARDT LIMITEDInventors: Dilip G. Saoji, Rajendra N. Nagori, Milind C. Shukla, Sachin Bhagwat, Shrikant V. Gupte, Mahesh V. Patel, Rasendrakumar Jha, Anil Kukreja, Noel J. De Souza
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Publication number: 20040132763Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): 1Type: ApplicationFiled: October 20, 2003Publication date: July 8, 2004Applicant: Xanthus Life Sciences, Inc.Inventors: Alfred M. Ajami, David O. Barlow
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Patent number: 6693198Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X− or R1 is —(CH2)nN+HR3R4 X− or —(CH2)nNR3R4 when R2 is —N+HR6R7. R2 is —OR5, halogen, —NR6R7, —N+HR6R7 X− sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X− is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).Type: GrantFiled: April 22, 2002Date of Patent: February 17, 2004Assignee: Xanthus Life Sciences, Inc.Inventors: Alfred M. Ajami, David O. Barlow
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Publication number: 20040029879Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: July 31, 2003Publication date: February 12, 2004Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Patent number: 6670369Abstract: The use of phanquinone for the manufacture of a pharmaceutical composition for the prevention or the treatment of Alzheimer's disease is disclosed. Also methods of treatment or prevention of Alzheimer's disease are disclosed.Type: GrantFiled: October 19, 2000Date of Patent: December 30, 2003Assignee: P.N. Gerolymatos S.A.Inventors: Michel Xilinas, Panayotis Nikolas Gerolymatos
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Publication number: 20030229026Abstract: The present invention provides selective kinase inhibitors of formula (I).Type: ApplicationFiled: December 2, 2002Publication date: December 11, 2003Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
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Publication number: 20030225119Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.Type: ApplicationFiled: May 28, 2002Publication date: December 4, 2003Applicant: WOCKHARDT LIMITEDInventors: Noel J. de Souza, Prasad K. Deshpande, Milind C. Shukla, Siddiqui M. Jaweed Mukarram, Dilip Ganesh Kulkarni, Ansari Azizur Rahman, Ravindra D. Yeole, Mahesh V. Patel, Shrikant V. Gupte
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Publication number: 20030212065Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).Type: ApplicationFiled: April 25, 2003Publication date: November 13, 2003Inventors: Sylvia McBrinn, Richard Wayne Anderson
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Publication number: 20030203932Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): 1Type: ApplicationFiled: April 22, 2002Publication date: October 30, 2003Applicant: Xanthus Life Sciences, Inc.Inventors: Alfred M. Ajami, David O. Barlow
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Publication number: 20030203923Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: ApplicationFiled: July 26, 2002Publication date: October 30, 2003Inventors: Gregory M. Ross, Egor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Patent number: 6630173Abstract: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a naphthalimide and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the naphthalimide comprises amonafide (5-amino-2-[2-(dimethylamine)ethyl]-1H-benz[de-]isoquinoline-1,3-(2H)-dione). Antiproliferative agents of the invention comprise alkylating agents, intercalating agents, metal coordination complexes, pyrimidine nucleosides, purine nucleosides, inhibitors of nucleic acid associated enzymes and proteins, and agents affecting structural proteins and cytoplasmic enzymes. The invention comprises the described methods as well as compositions comprising a naphthalimide and an antiproliferative agent.Type: GrantFiled: April 12, 2001Date of Patent: October 7, 2003Assignee: Chemgenex Therapeutics, Inc.Inventor: Dennis M. Brown
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Publication number: 20030181479Abstract: The present invention relates to novel substituted imidazoles, to the use of these compounds as medicaments, to pharmaceutical compositions comprising the compounds, and to a method of treatment employing these compounds and compositions. The present compounds show a high and selective binding affinity to the histamine H3 receptor indicating a histamine H3 receptor antagonistic or agonistic activity. As a result, the compounds are useful for the treatment of disorders related to the histamine H3 receptor. More particularly, the present compounds possess a histamine H3 receptor agonistic activity and are accordingly useful in the treatment of disorders in which a histamine H3 receptor activation is beneficial.Type: ApplicationFiled: November 8, 2002Publication date: September 25, 2003Applicant: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Rudolf Hurnaus, Dirk Stenkamp, Stephan Mueller, Bernd Krist
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Publication number: 20030144517Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.Type: ApplicationFiled: November 22, 2002Publication date: July 31, 2003Applicant: WOCKHARDT LIMITEDInventors: Noel J. De Souza, Shivkumar Agarwal, Mahesh V. Patel, Satish B. Bhawsar, Rupinder K. Beri, Ravindra D. Yeole, Nitin Shetty
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Publication number: 20030092676Abstract: 1Type: ApplicationFiled: May 21, 2002Publication date: May 15, 2003Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
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Patent number: 6492380Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: GrantFiled: December 8, 1999Date of Patent: December 10, 2002Assignee: Queen's University at KingstonInventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Publication number: 20020177559Abstract: Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: ApplicationFiled: July 31, 2001Publication date: November 28, 2002Applicant: WOCKHARDT LIMITEDInventors: Noel John de Souza, Mahesh Vithalbhai Patel, Shrikant V. Gupte, Dilip J. Upadhyay, Milind Chintaman Shukla, Nishith C. Chaturvedi, Satish B. Bhawsar, Sheela Chandresekharan Nair, Mohammed A. Jafri, Habil Fakhruddin Khorakiwala
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Publication number: 20020169182Abstract: A pharmaceutical composition comprising a compound of Formula I 1Type: ApplicationFiled: January 11, 2001Publication date: November 14, 2002Inventors: Ashok Tehim, Xiannong Chen
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Patent number: 6451808Abstract: Metformin is formulated as a pharmaceutical composition that also includes a 5-hydroxytryptamine-3 receptor antagonist to suppress the gastrointestinal side effects that are associated with metformin administration in many patients.Type: GrantFiled: October 17, 2000Date of Patent: September 17, 2002Assignee: DepoMed, Inc.Inventor: Verne E. Cowles
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Publication number: 20020107247Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: February 19, 2002Publication date: August 8, 2002Inventors: Robert B. McCall, Martin Durham Meglasson
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Publication number: 20020107257Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).Type: ApplicationFiled: October 29, 2001Publication date: August 8, 2002Inventors: Sylvia McBrinn, Richard Wayne Anderson
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Patent number: 6410505Abstract: A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a ring nitrogen atom and bears, at the 4 position, an amino nitrogen atom, carrying a hydrogen. The remaining unsatisfied valences, if present, of the ring nitrogen atoms or the amino nitrogen atoms, or all, are occupied by one or more alkyl substituents. Each of the 1,8-naphthalimide ring system is free of an azo substituent and is also free of a nucleofuge. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species can cause structural changes in lipid and any associated proteins and polypeptides, extra- or intra-cellular or transmembrane, leading to polymerization and crosslinking.Type: GrantFiled: June 28, 1999Date of Patent: June 25, 2002Assignee: Microbiomed Corp.Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
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Patent number: 6380193Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.Type: GrantFiled: September 1, 1998Date of Patent: April 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Publication number: 20010031722Abstract: A previously unknown histone acetylase inhibitor, 6-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-hexanoic acid hydroxyamide, termed “scriptaid,” can be used to enhance transcription. Scriptaid can be added to transactivation assays, or can be used, for example, to increase production of therapeutic polypeptides in vitro and in vivo.Type: ApplicationFiled: January 3, 2001Publication date: October 18, 2001Inventors: Scott E. Kern, Gloria Su
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Patent number: 6303569Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: August 21, 1998Date of Patent: October 16, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri
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Patent number: 6300331Abstract: The present invention relates to a naphthalimidobenzamide derivative represented by the following formula (1): (wherein, R1 represents a hydrogen atom, etc., Y represents a hydrogen atom or —CON(R4)—A2—X2, R2 and R4 are the same or different and each independently represents a hydrogen atom, etc., A1 and A2 are the same or different and each independently represents an alkylene group which may be interrupted at least once by —N(R3)— (R3 representing a hydrogen atom, etc.) and X1 and X2 are the same or different and each independently represents a (hetero)aryl group which may have a substituent, etc.) or salt thereof; and a pharmaceutical comprising it as an effective ingredient. The compound is useful as an antitumor agent and the like.Type: GrantFiled: March 3, 2000Date of Patent: October 9, 2001Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Kazuharu Noguchi, Motoji Wakida, Kenji Suzuki, Yuji Yamada, Tetsuji Asao
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Patent number: 6300340Abstract: A compound of formula (I) in which: m, and n, which may be identical or different, represent 0 or 1, X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino, Z represent a linear or branched C4 to C12 alkylene chain in which one or more —CH2— are optionally replaced by any one of the following atoms or groups: —NR—, —O—, —S—, —SO—, SO2—, or —CONH—, or by a substituted or unsubstituted heterocylcic, A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharamaceutically and acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.Type: GrantFiled: July 14, 2000Date of Patent: October 9, 2001Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stéphane Leonce
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Patent number: 6133259Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 9, 1998Date of Patent: October 17, 2000Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6066632Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: May 23, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
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Patent number: 5998405Abstract: The present invention discloses compounds of the formula, or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereofwhereinX and Y together forms .dbd.O, .dbd.S, .dbd.NOR.sup.2, .dbd.CR.sup.3 R.sup.4, .dbd.N--CN, .dbd.N--NR.sup.7 R.sup.8, --(CH.sub.2).sub.m --, or--W'--(CH.sub.2).sub.p --W"--, or one of X and Y is hydrogen and the other is --OR.sup.5, --SR.sup.5, or --NR.sup.5 R.sup.6Z is hydrogen, --COOR.sup.9 ;R.sup.3 and R.sup.4 are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, aryl, arylalkyl, or --(CH.sub.2).sub.q --COOR.sup.2 ;R.sup.2, R.sup.5 and R.sup.6 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, --CO-alkyl, or --SO.sub.2 -alkyl;R.sup.7 and R.sup.8 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl;R.sup.9 is alkyl, alkenyl or alkynyl;R.sup.Type: GrantFiled: June 4, 1998Date of Patent: December 7, 1999Assignee: NeuroSearch A/SInventors: J.o slashed.rgen Scheel-Kruger, Gunnar M. Olsen, Elsbet .O slashed.stergaard Nielsen, Bjarne Hugo Dahl, Leif Helth Jensen
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Patent number: 5990106Abstract: This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formulaA--Priesters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic acid residue, and A is a bicyclic amino group represented by the following formula and joined to the 7-position of the pyridonecarboxylic acid or a position equivalent to the 7-position thereof. ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group or an amino-protecting group; R.sub.3 and R.sub.4 may be the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, an oxo group, a lower alkoxy group or a lower alkyl group; and n is an integer of 0 or 1.The above-described pyridonecarboxylic acid derivatives, esters thereof and salts thereof are useful as antibacterial agents.Type: GrantFiled: August 4, 1997Date of Patent: November 23, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Masato Sakamoto, Katsumi Chiba, Yukio Tominaga, Akira Minami
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Patent number: 5948776Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15.ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.Type: GrantFiled: February 28, 1997Date of Patent: September 7, 1999Assignees: Zymogenetic, Inc., Osteoscreen, Inc.Inventors: Charles Petrie, Mark W. Orme, Nand Baindur, Kirk G. Robbins, Gregory R. Mundy
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Patent number: 5869479Abstract: Relief from the symptoms of rhinitis is obtained by treatment with: (a) an antihistaminic effective amount of a histamine H.sub.1 receptor antagonist; together with (b) a sufficient amount of a histamine H.sub.3 receptor antagonist to provide a nasal decongestant effect. The components may be administered together in a single dosage form, or separately in the same or different dosage forms to maintain therapeutic systemic levels of both components.Type: GrantFiled: August 14, 1997Date of Patent: February 9, 1999Assignee: Schering CorporationInventors: William Kreutner, John A. Hey
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Patent number: 5863912Abstract: Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity and amelioration of cyclophosphamide-associated toxicity is achieved by an initial intravenous infusion of DPPE over an approximately one hour period prior to cyclophosphamide treatment.Type: GrantFiled: September 5, 1996Date of Patent: January 26, 1999Assignee: Manitoba Cancer Treatment and Research FoundationInventor: Lorne J. Brandes
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Patent number: 5854277Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: December 29, 1998Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
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Patent number: 5854263Abstract: 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 29, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5854273Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.Type: GrantFiled: July 23, 1997Date of Patent: December 29, 1998Assignee: ADIR et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
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Patent number: 5840903Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;m is 1 or 2;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.Type: GrantFiled: July 27, 1992Date of Patent: November 24, 1998Assignee: G. D. Searle & Co.Inventors: Daniel Lee Flynn, Robert L. Shone
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Patent number: 5789418Abstract: Disclosed herein are compounds pharmaceutical compositions containing same of the formula1. A compound of the Formula ##STR1## wherein X, X', X" and X'", A, B, D, R, and R' are as identified in the specification and their preparation. Pharmaceutical compositions containing same can be used in the treatment of cancer.Type: GrantFiled: February 18, 1997Date of Patent: August 4, 1998Assignee: BASF AktiengesellschaftInventors: Gerhard Keilhauer, Cynthia Romerdahl, Miguel Fernandez Brana, Xiao-Dong Qian, Peter Bousquet, Jose Maria Castellano Berlanga, Marina Moran Moset, Maria Jesus Perez De Vega
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Patent number: RE39265Abstract: 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: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley