Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To A Piperidine Ring Patents (Class 546/189)
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Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
Patent number: 7595312Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: October 16, 2003Date of Patent: September 29, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Eckhart Bauer, Marcus Schindler, Kirsten Arndt, Henri Doods -
Publication number: 20090203736Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: ApplicationFiled: February 5, 2009Publication date: August 13, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090203710Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseaseType: ApplicationFiled: March 6, 2009Publication date: August 13, 2009Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
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Publication number: 20090186874Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof. The compound of the present invention has a superior tachykinin receptor antagonistic action, particularly an SP receptor antagonistic action, and is useful as a pharmaceutical agent, for example, a tachykinin receptor antagonist, an agent for the prophylaxis or treatment of an abnormality of lower urinary tract functions, a digestive organ disease or a central nerve disease, and the like.Type: ApplicationFiled: January 13, 2005Publication date: July 23, 2009Inventors: Yoshinori Ikeura, Junya Shirai
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Publication number: 20090118267Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: February 13, 2006Publication date: May 7, 2009Inventors: Dirk Finsinger, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Kai Schiemann, Wolfgang Staehle, Christiane Amendt, Nina Heiss, Frank Zenke
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Patent number: 7507825Abstract: The invention relates to the method of manufacturing of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin by condensation of 7-ethyl-10-hydroxycamptothecin with 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride in a polar aprotic solvent in the presence of 4-dimethylaminopyridine.Type: GrantFiled: August 24, 2004Date of Patent: March 24, 2009Assignee: Pliva-Lachema A.S.Inventor: Petr Dobrovolny
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Patent number: 7482363Abstract: The present invention provides a compound of formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: GrantFiled: March 17, 2003Date of Patent: January 27, 2009Assignee: AstraZeneca ABInventors: Hitesh Sanganee, Brian Springthorpe
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Patent number: 7476681Abstract: In its many embodiments, the present invention provides a novel class of compounds as illustrated below, wherein the various moieties are described herein, as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, pharmaceutical compositions containing one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.Type: GrantFiled: February 24, 2006Date of Patent: January 13, 2009Assignee: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi
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Publication number: 20090005355Abstract: The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino group, R2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or —N(R3)—, R3 is hydrogen atom or an optionally substituted alkyl group, R4a and R4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or may be bonded to each other at the both ends to form an alkylene group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.Type: ApplicationFiled: July 1, 2005Publication date: January 1, 2009Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Tsutomu Miyake, Takeshi Yamanaka, Hidetoshi Asai, Yoshihiro Terakawa
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Publication number: 20080312280Abstract: The present invention relates to a compound of formula (I), or a salt thereof wherein the naphthalene ring is substituted in the 2, 3, 4, 5, 6, 7 or 8 position by R1, and R1 represents —CH2CH2COOH or —CH?C(CH3)COOH, and to processes for their preparation, to compositions containing them and to their use in the treatment of various inflammatory and/or allergic diseases, such as diseases such as allergic rhinitis.Type: ApplicationFiled: December 19, 2006Publication date: December 18, 2008Inventors: Simon Teanby Hodgson, Panayiotis Alexandrou Procopiou, Maria Victoria Vinader Brugarolas
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Publication number: 20080262037Abstract: The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: ApplicationFiled: April 5, 2005Publication date: October 23, 2008Applicant: ASTRAZENECA ABInventors: Tobias Mochel, Matthew Perry, Brian Springthorpe
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Publication number: 20080200460Abstract: Compounds of formula (I): wherein: when X is NR5, Y is absent or is CH2; when X is CH2, Y is absent, CH2, NR6, O, S, S(O) or S(O)2; Z is a 5- or 6-membered heterocyclyl ring; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: December 15, 2005Publication date: August 21, 2008Inventors: Dearg Brown, John Oldfield, Howard Tucker
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Patent number: 7410995Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.Type: GrantFiled: August 14, 1998Date of Patent: August 12, 2008Assignee: GPI Nil Holdings Inc.Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
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Publication number: 20080161571Abstract: The present invention is related to a process for the preparation of [1,4?]bipiperidinyl-1?-carbonyl chloride or its hydrochloride using methylene chloride as a solvent in the reaction of 4-piperidinopiperidine with phosgene and the removing the reaction solvent by using an additional distillation solvent to raise the distillation temperature.Type: ApplicationFiled: February 6, 2006Publication date: July 3, 2008Inventor: Ilpo Laitinen
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Patent number: 7361755Abstract: This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical.Type: GrantFiled: December 12, 2002Date of Patent: April 22, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Stephen Daniel Pastor, Sai Ping Shum
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Patent number: 7358251Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 29, 2005Date of Patent: April 15, 2008Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7354919Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: July 24, 2003Date of Patent: April 8, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao
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Patent number: 7351721Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: May 6, 2003Date of Patent: April 1, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7348324Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Type: GrantFiled: October 18, 2002Date of Patent: March 25, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
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Patent number: 7338976Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides.Type: GrantFiled: August 14, 1998Date of Patent: March 4, 2008Assignee: GPI NIL Holdings, Inc.Inventors: Douglas T. Ross, Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7297734Abstract: The present invention describes a process for preparing a synergistic stabilizer mixture comprising the components of the general formulae (I), (II) and (III) in accordance with claim 1, characterized by the reaction of compounds of the formula (V) with an epihalohydrin of the formula (VI) in the presence of a phase transfer catalyst and from 4 to 20 times the molar amount of an alkali metal hydroxide, relative to compound (V), at from 20 to 220° C. Removal of the excess epihalohydrin and phase separation are followed by polymerization at from 100 to 240° C.Type: GrantFiled: February 4, 2003Date of Patent: November 20, 2007Assignee: Clariant Produkte (Deutschland) GmbHInventor: Mathias Mehrer
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Patent number: 7265150Abstract: This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal.Type: GrantFiled: August 14, 1998Date of Patent: September 4, 2007Assignee: GPI NIL Holdings Inc.Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7238811Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: GrantFiled: May 13, 2003Date of Patent: July 3, 2007Assignee: AstraZeneca ABInventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
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Patent number: 7186827Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:Type: GrantFiled: October 27, 2004Date of Patent: March 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Carl Alan Busacca, Nizar Haddad, Suresh R. Kapadia, Lana Smith Keenan, Jon Charles Lorenz, Chris Hugh Senanayake, Xudong Wei
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Patent number: 7169797Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.Type: GrantFiled: February 4, 2004Date of Patent: January 30, 2007Assignee: Abbott LaboratoriesInventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
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Patent number: 7157585Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: May 11, 2005Date of Patent: January 2, 2007Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 7064211Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1–R7, X1, X2, R, Q, and n are as defined herein.Type: GrantFiled: September 22, 2003Date of Patent: June 20, 2006Assignee: Eisai Co., Ltd.Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Patent number: 7060701Abstract: Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl-SO2—, cycloalkyl-SO2—, fluoroalkyl-SO2—, R9-aryl-SO2—, R9-heteroaryl-SO2—, N(R22)(R23)—SO2—, alkyl-C(O)—, cycloalkyl-C(O)—, fluoroalkyl-C(O)—, R9-aryl-C(O)—, NH-alkyl-C(O)— or R9-aryl-NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are ?O, ?NOR10, ?N—NR11R12 or ?CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9–R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graType: GrantFiled: February 17, 2005Date of Patent: June 13, 2006Assignee: Schering CorporationInventor: Michael W. Miller
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Patent number: 7049440Abstract: An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula I is disclosed.Type: GrantFiled: October 1, 2003Date of Patent: May 23, 2006Assignee: Schering CorporationInventors: Frank X. Chen, Yee-Shing Wong, Jeffrey M. Eckert, Feng Liang, Nanfei Zou, Agnes S. Kim-Meade, Marc Poirier, Tiruvettipuram K. Thiruvengadam, George G. Wu
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Patent number: 7041679Abstract: The invention relates to crystalline forms of (R)-(+)-N-[[3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl]-4-phenylpiperidin-4-yl]-N-methylacetamide and to processes for preparing them.Type: GrantFiled: August 28, 2003Date of Patent: May 9, 2006Assignee: sanofi-aventisInventors: Alain Alcade, Gilles Anne-Archard, Patrick Gros-Claude, Olivier Monnier, Jérome Roche
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Patent number: 6995151Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.Type: GrantFiled: February 13, 2002Date of Patent: February 7, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Richard Dennis Dyer, Adam Richard Johnson, William Chester Patt
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Patent number: 6969713Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapyType: GrantFiled: December 18, 2000Date of Patent: November 29, 2005Assignee: AstraZeneca ABInventors: Premji Meghani, Colin Bennion
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Patent number: 6900326Abstract: A method of producing an N-alkoxycarbonylpiperidine derivative, comprising reacting an N-aralkylpiperidine derivative represented by the following general formula (1): wherein R1 represents an aralkyl group which may have a substituent, with a mesyl halide in the presence of a base, thereby obtaining a mesylated product represented by the following general formula (2): wherein R1 represents an aralkyl group which may have a substituent and Ms represents a mesyl group, and reacting the mesylated product with a dicarbonate represented by the following general formula (3): wherein R4 represents an alkyl group, in the presence of hydrogen and a catalyst containing palladium, thereby obtaining an N-alkoxycarbonylpiperidine derivative represented by the following general formula (4): wherein R4 represents an alkyl group and Ms represents a mesyl group.Type: GrantFiled: September 17, 2003Date of Patent: May 31, 2005Assignee: Yuki Gosei Kogyo Co., Ltd.Inventor: Kiyono Nakagawa
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Patent number: 6864266Abstract: This invention relates to the (R)-isomers of compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.Type: GrantFiled: July 1, 2003Date of Patent: March 8, 2005Assignee: Syntex (U.S.A.) LLCInventors: Christine E. Brotherton-Pleiss, Ann Marie Madera, Robert James Weikert
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Patent number: 6841668Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.Type: GrantFiled: April 4, 2003Date of Patent: January 11, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Deborah Judd, Sai P. Shum, Stephen D. Pastor
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Patent number: 6833457Abstract: According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.Type: GrantFiled: July 17, 2003Date of Patent: December 21, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Shokyo Miki, Mitsuhiro Takeda, Koji Nakamoto
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Patent number: 6831089Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.Type: GrantFiled: October 8, 2002Date of Patent: December 14, 2004Assignee: Schering CorporationInventors: Yuguang Wang, Samuel Chackalamannil
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Patent number: 6809093Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.Type: GrantFiled: December 19, 2000Date of Patent: October 26, 2004Assignee: H. Lee Moffitt Cancer & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 6806278Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.Type: GrantFiled: June 27, 2003Date of Patent: October 19, 2004Assignee: Syntex (U.S.A.) LLCInventors: Ann Marie Madera, Robert James Weikert
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Patent number: 6784182Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: February 4, 2002Date of Patent: August 31, 2004Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6777428Abstract: The present invention relates to a compound of formula I and a process for making: or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.Type: GrantFiled: December 4, 2001Date of Patent: August 17, 2004Assignee: Eli Lilly and CompanyInventors: Joseph Herman Krushinski, Jr., Vincent Mancuso, Freddy Andre Napora, John Mehnert Schaus
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Publication number: 20040157854Abstract: Compounds of the formula 1Type: ApplicationFiled: February 6, 2004Publication date: August 12, 2004Inventor: Michael W. Miller
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Patent number: 6770659Abstract: Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of racemic or enantiomerically enriched benzoyl piperidine compounds to treat central nervous system diseases and methods of treating central nervous system diseases in a mammal, in particular psychoses and cognition disorders.Type: GrantFiled: August 26, 2002Date of Patent: August 3, 2004Assignee: SK CorporationInventors: Yong-Moon Choi, Yong-Kil Kim, Jin-Uk Yoo, Eun-Ah Paek, Chun-Eung Park, Sung-Yong Seo, Coo-Min Chung, Joon Heo
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Publication number: 20040132736Abstract: There are disclosed compounds of the formula (I): 1Type: ApplicationFiled: September 5, 2002Publication date: July 8, 2004Applicant: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Alan K. Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
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Publication number: 20040127503Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17&bgr;-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17&bgr;-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 14, 2003Publication date: July 1, 2004Applicant: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi
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Patent number: 6750228Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: May 12, 2000Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E Barta, Daniel P Becker, Louis J Bedell, Terri L Boehm, Jeffrey N Carroll, Gary A DeCrescenzo, Yvette M Fobian, John N Freskos, Daniel P Getman, Joseph J McDonald, Madeleine H Li, Susan L Hockerman, Susan C Howard, Steve A Kolodziej, Deborah A Mischke, Joseph G Rico, Nathan W Stehle, Michael B Tollefson, William F Vernier, Clara I Villamil
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Publication number: 20040102627Abstract: This invention relates to 3-amino piperadine derivatives, their intermediates and methods of manufacture.Type: ApplicationFiled: November 20, 2003Publication date: May 27, 2004Applicant: Pfizer Inc.Inventor: David H.B. Ripin
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Publication number: 20040097546Abstract: Certain novel 4-substituted N-acylated piperidine 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: August 19, 2003Publication date: May 20, 2004Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Publication number: 20040092501Abstract: Certain novel 4-substituted N-acylated piperidine 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: August 19, 2003Publication date: May 13, 2004Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner