Additional Hetero Atom In The Polycyclo Ring System Patents (Class 514/215)
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Patent number: 7067510Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1–C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 11, 2003Date of Patent: June 27, 2006Assignee: Eli Lilly and CompanyInventor: Owen Brendan Wallace
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Patent number: 7056910Abstract: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 27, 2001Date of Patent: June 6, 2006Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Koshio, Akio Kakefuda, Ippei Sato, Ryutaro Wakayama, Masanao Sanagi
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Patent number: 7056909Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: July 20, 2001Date of Patent: June 6, 2006Assignee: Merck & Co., Inc.Inventor: Jiabing Wang
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Patent number: 7049310Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.Type: GrantFiled: April 3, 2002Date of Patent: May 23, 2006Assignee: Affinium Pharmaceuticals, Inc.Inventors: Walter J. Burgess, Dalia Jakas, William F. Huffman, William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas
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Patent number: 7037919Abstract: Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.Type: GrantFiled: October 6, 2000Date of Patent: May 2, 2006Assignee: Kaken Pharmaceutical Co. Ltd.Inventors: Keigo Hanada, Kazuyuki Furuya, Kiyoshi Inoguchi, Motonori Miyakawa, Naoya Nagata
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Patent number: 7030109Abstract: The present invention discloses radioligands of 9-arylsulfone of the formula (X) or a pharmaceutically acceptable salt or enantiomer thereof, which are useful in diagnosing depression, obesity and other CNS disorders.Type: GrantFiled: April 25, 2003Date of Patent: April 18, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Eric Jon Jacobsen, Kalpana M. Merchant
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Patent number: 7022694Abstract: The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, R6 and --- have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are useful as 5-HT ligands.Type: GrantFiled: July 11, 2002Date of Patent: April 4, 2006Assignee: Pharmacia & UpJohn CompanyInventors: Jian-Min Fu, Jeanette Kay Morris, Arthur Glenn Romero
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Patent number: 6987104Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6960577Abstract: Methods for treating a patient suffering from or susceptible to treatment resistant major depression comprising administering olanzapine and fluoxetine are disclosed.Type: GrantFiled: May 10, 2002Date of Patent: November 1, 2005Assignee: Eli Lilly and CompanyInventor: Gary Dennis Tollefson
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Patent number: 6953787Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: April 10, 2003Date of Patent: October 11, 2005Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Patent number: 6933304Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively antagonizing the ?V?3 and/or the ?V?5 integrin without significantly antagonizing the IIb/IIIa or ?V?6 integrin.Type: GrantFiled: June 15, 2001Date of Patent: August 23, 2005Assignee: Pharmacia CorporationInventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark Laurence Boys, Nizal Samuel Chandrakumar, Hung-Fun Lu
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Patent number: 6903090Abstract: Disclosed are compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.Type: GrantFiled: March 20, 2003Date of Patent: June 7, 2005Assignee: PfizerInventors: Kristine E. Frank, Brad A. Acker, Michael D. Ennis, Jed F. Fisher, Jian-min Fu, William W. McWhorter, Jr., Jeanette K. Morris, Donald Joseph Rogier, Eric Jon Jacobsen
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Patent number: 6897211Abstract: The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-?) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.Type: GrantFiled: November 18, 2002Date of Patent: May 24, 2005Assignee: Pliva-Istrazivacki Institut d.o.o.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Zeljko Zupanovic, Boska Hrvacic
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Patent number: 6875762Abstract: The present invention provides compounds of formula I: wherein R1, R2, X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I).Type: GrantFiled: December 23, 2003Date of Patent: April 5, 2005Assignee: PfizerInventors: Jackson B. Hester, Bruce N. Rogers, Eric Jon Jacobsen, Michael D. Ennis, Brad A. Acker, Susan L. Vander Velde, Kristine E. Frank
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Patent number: 6852741Abstract: The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by co-administration of metanicotine and at least one compound which exhibits antagonist activity, or both agonistic and antagonists activity, toward one or more nicotinic acetylcholine receptor subtypes. The subject invention, in another aspect, pertains to pharmaceutical compositions containing metanicotine and at least one compound which inhibits antagonistic activity, or both agonistic and antagonistic activity, toward one or more nicotinic acetylcholine receptor subtypes.Type: GrantFiled: December 31, 2001Date of Patent: February 8, 2005Assignee: University of FloridaInventor: Roger L. Papke
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Patent number: 6852730Abstract: Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided.Type: GrantFiled: February 7, 2003Date of Patent: February 8, 2005Assignee: Neurogen CorporationInventors: George Maynard, Jun Yuan, Stanislaw Rachwal
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Publication number: 20040248879Abstract: Pharmaceutically acceptable salts of compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.Type: ApplicationFiled: March 29, 2004Publication date: December 9, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: Stacie Canan-Koch, Jan-Jon Chu, Jia Liu, Jean Matthews
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Publication number: 20040248880Abstract: The present invention discloses radioligands of 9-arylsulfone of the formula (X) 1Type: ApplicationFiled: April 12, 2004Publication date: December 9, 2004Inventors: Eric Jon Jacobsen, Kalpana M. Merchant
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Patent number: 6828314Abstract: The invention provides compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.Type: GrantFiled: March 20, 2003Date of Patent: December 7, 2004Assignee: PfizerInventors: Kristine E. Frank, Brad A. Acker, Michael D. Ennis, Jed F. Fisher, Jian-min Fu, Eric Jon Jacobsen, William W. McWhorter, Jr., Jeanette K. Morris, Donald Joseph Rogier
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Publication number: 20040242623Abstract: The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof: 1Type: ApplicationFiled: July 29, 2004Publication date: December 2, 2004Inventors: Romano Difabio, Collin F. Regan, Yves St-Denis, Fabrizio Micheli, Michael K. Schwaebe
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Publication number: 20040229862Abstract: The invention relates to 2-imidazo-benzothiazoles of general formula 1Type: ApplicationFiled: May 11, 2004Publication date: November 18, 2004Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20040224939Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications including use as antibacterial agents.Type: ApplicationFiled: February 5, 2004Publication date: November 11, 2004Inventors: Louis S. Chupak, Frederick Earl Boyer, Susan Hagen, Takushi Kaneko, Manjinder Lall, Martin Pettersson, Joysula Venkata Nagendra Vara Prasad
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Publication number: 20040220178Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) 1Type: ApplicationFiled: February 26, 2004Publication date: November 4, 2004Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael G. Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
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Publication number: 20040209864Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) 1Type: ApplicationFiled: February 25, 2004Publication date: October 21, 2004Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
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Publication number: 20040204398Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: February 27, 2004Publication date: October 14, 2004Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Publication number: 20040198717Abstract: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.Type: ApplicationFiled: April 16, 2004Publication date: October 7, 2004Inventors: Paul J Coleman, Lou Anne Neilson
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Publication number: 20040192670Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as &agr;v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;15 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.Type: ApplicationFiled: March 11, 2003Publication date: September 30, 2004Inventors: John H Hutchinson, Aiwen Li
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Publication number: 20040180875Abstract: The present invention is directed to novel compounds represented by structural Formula (I): 1Type: ApplicationFiled: December 19, 2003Publication date: September 16, 2004Inventors: Taekyu Lee, Wenting Chen, Wei Deng, Albert J. Robichaud, Ruth R. Wexler
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Publication number: 20040176354Abstract: Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine.Type: ApplicationFiled: March 12, 2004Publication date: September 9, 2004Inventors: Rebecca Guggemos Bakker-Arkema, Milton Lethan Pressler
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Patent number: 6777406Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7, R8, R9, X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Publication number: 20040147505Abstract: The present invention relates to novel diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. A diazabicycloalkane derivative selected from those represented by Formula I, by Formula II, by Formula III, by Formula IV, and by Formula V.Type: ApplicationFiled: December 1, 2003Publication date: July 29, 2004Inventors: Dan Peters, Gunnar M Olsen, Elsebet Ostergaard Nielsen, Philip K Ahring, Tino Dyhring Jorgensen, Frank Abilgaard Slok
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Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: 6765004Abstract: The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions involving increased vascular resistance and cardiac insufficiency which include hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis or water retention in a subject in need thereof.Type: GrantFiled: June 12, 2000Date of Patent: July 20, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Michael N. Greco, Leonard R. Hecker, Bruce E. Maryanoff, Jay M. Matthews
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Publication number: 20040138202Abstract: The present invention provides compounds of formula I: 1Type: ApplicationFiled: December 23, 2003Publication date: July 15, 2004Applicant: Pharmacia and Upjohn CompanyInventors: Jackson B. Hester, Bruce N. Rogers, Eric Jon Jacobsen, Michael D. Ennis, Brad A. Acker, Susan L. Vander Velde, Kristine E. Frank
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Patent number: 6737419Abstract: Stable tablets comprising benazepril hydrochloride are prepared by employing zinc stearate as the lubricant.Type: GrantFiled: April 12, 2002Date of Patent: May 18, 2004Inventor: Bernard Charles Sherman
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Publication number: 20040092502Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1Type: ApplicationFiled: December 19, 2001Publication date: May 13, 2004Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Publication number: 20040092503Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.Type: ApplicationFiled: August 19, 2003Publication date: May 13, 2004Inventors: Thomas Arrhenius, Jie Fei Cheng, Mark E Wilson, Rossy Serafimov
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Patent number: 6730707Abstract: The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders.Type: GrantFiled: July 25, 2001Date of Patent: May 4, 2004Assignees: Inspire Pharmaceuticals, Inc., Universidad Complutense de MadridInventors: Jesus J. Pintor, Maria A. Peral, Ward M. Peterson, Robert Plourde, Jr., Edward G. Brown, Benjamin R. Yerxa
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Publication number: 20040077630Abstract: The present invention relates to compounds of formulas (IA) and (IB): 1Type: ApplicationFiled: September 15, 2003Publication date: April 22, 2004Inventor: Pier Giovanni Baraldi
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Patent number: 6720316Abstract: The present invention provides compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.Type: GrantFiled: August 2, 2002Date of Patent: April 13, 2004Assignee: Pharmacia & Upjohn CompanyInventor: William W. McWhorter, Jr.
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Patent number: 6713471Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: March 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
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Publication number: 20040058906Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: August 27, 2003Publication date: March 25, 2004Applicant: Schering CorporationInventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee, Thavalakulam K. Sasikumar
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Publication number: 20040048912Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: 1Type: ApplicationFiled: June 9, 2003Publication date: March 11, 2004Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
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Patent number: 6699989Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds.Type: GrantFiled: August 28, 2000Date of Patent: March 2, 2004Inventor: B. Vithal Shetty
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Publication number: 20040038963Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: ApplicationFiled: November 12, 2002Publication date: February 26, 2004Inventor: Jiabing Wang
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Publication number: 20040034012Abstract: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 27, 2003Publication date: February 19, 2004Inventors: Hiroyuki Koshio, Akio Kakefuda, Ippei Sato, Ryutaro Wakayama, Masanao Sanagi
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Publication number: 20040023947Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: ApplicationFiled: May 27, 2003Publication date: February 5, 2004Applicant: X-Ceptor Therapeutics Inc.Inventors: Richard Martin, Tie-Lin Wang, Brenton T. Flatt, Xiao-Hui Gu, Ronald Griffith
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Publication number: 20040019037Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: ApplicationFiled: July 10, 2003Publication date: January 29, 2004Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Publication number: 20040006066Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: 1Type: ApplicationFiled: December 3, 2002Publication date: January 8, 2004Inventors: David Garrett Loughhead, Counde O'Yang