Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/223)
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Patent number: 8211916Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: January 22, 2008Date of Patent: July 3, 2012Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20120165533Abstract: Provided are an optically active diazabicyclooctane derivative defined by formula (F) below, which is useful as a pharmaceutical intermediate for ?-lactamase inhibitor, and a process for preparing the same. In formula (F) above, R1 represents CO2R, CO2M, or CONH2, wherein R represents a methyl group, a tert-butyl group, an allyl group, a benzyl group, or a 2,5-dioxopyrrolidin-1-yl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.Type: ApplicationFiled: June 30, 2011Publication date: June 28, 2012Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao ABE, Masayuki Okue, Yoshiaki Sakamaki
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Patent number: 8207373Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.Type: GrantFiled: May 18, 2007Date of Patent: June 26, 2012Assignee: Anaconda PharmaInventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Publication number: 20120129816Abstract: The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.Type: ApplicationFiled: March 3, 2009Publication date: May 24, 2012Applicant: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti
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Publication number: 20110312965Abstract: The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.Type: ApplicationFiled: December 21, 2009Publication date: December 22, 2011Inventors: Walter Cabri, Giuseppe Giannini, Gianfranco Battistuzzi, Domenico Alloatti, Claudio Pisano, Sabrina Dallavalle, Tiziana Brunetti
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Publication number: 20110294851Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: August 5, 2011Publication date: December 1, 2011Applicant: THERAVANCE, INC.Inventors: YuHua JI, Craig HUSFELD, Rick LEE, YongQi MU
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Publication number: 20110237592Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: October 29, 2009Publication date: September 29, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ingo Hartung, Marion Hitchcock, Knut Eis, Florian Puhler
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Publication number: 20110230487Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 17, 2011Publication date: September 22, 2011Inventors: Tai Wei LY, Garrett Thomas Potter, Jared Andrew Forrester
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Publication number: 20110218160Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20110207777Abstract: Compounds of formula (I), salts and solvates are provided, Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: August 25, 2011Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20110190300Abstract: The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is ?O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0-2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: May 30, 2008Publication date: August 4, 2011Inventors: Akira Matsumura, Hidenori Mikamiyama, Jiangchao Yao
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Publication number: 20110172270Abstract: 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1 that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: ApplicationFiled: January 6, 2011Publication date: July 14, 2011Applicant: LABORATORIOS DEL DR. ESTEVE S.AInventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Patent number: 7968534Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.Type: GrantFiled: July 21, 2008Date of Patent: June 28, 2011Assignee: Sanofi-AventisInventors: Pierre Despeyroux, Evelyne Fontaine, Gilles Courtemanche, Pierrick Rochard, Claudine Serradeil-Le Gal
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Publication number: 20110136843Abstract: The present invention relates to a combination of (a) a chemokine receptor 1 (CCR1) antagonist and (b) a muscarinic antagonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treatment of airway diseases, such as chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases.Type: ApplicationFiled: February 21, 2008Publication date: June 9, 2011Inventors: Tomas Eriksson, Johan Hansson, Marguerite Mensonides-Harsema, John Mo
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Publication number: 20110117591Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.Type: ApplicationFiled: October 20, 2010Publication date: May 19, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
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Patent number: 7923564Abstract: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.Type: GrantFiled: June 7, 2010Date of Patent: April 12, 2011Assignee: ACADIA Pharmaceuticals, Inc.Inventors: Mikkel Boas Thygesen, Nathalie Schlienger, Bo-Ragnar Tolf, Carl-Magnus A. Andersson, Fritz Blatter, Jörg Berghausen
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Publication number: 20110077247Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: DAC S.r.I.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20110028515Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.Type: ApplicationFiled: July 23, 2010Publication date: February 3, 2011Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Patent number: 7879879Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: June 7, 2006Date of Patent: February 1, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham, Adam Hughes, Craig Husfeld, Eric Stangeland, Yan Chen
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Publication number: 20110021565Abstract: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5? or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 4, 2010Publication date: January 27, 2011Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
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Publication number: 20110003855Abstract: Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: The Regents of the University of CaliforniaInventors: Thomas C. Hermann, Maia Carnevali
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Publication number: 20100311794Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventor: Chandrasekar Venkataramani
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Publication number: 20100311792Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 26, 2008Publication date: December 9, 2010Inventors: Bin Shao, Jiangchao Yao
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Publication number: 20100291026Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 20, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 7829582Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 27, 2007Date of Patent: November 9, 2010Assignee: Eli Lilly and CompanyInventors: Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Publication number: 20100280071Abstract: Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: November 4, 2010Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20100273782Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Baaum
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Patent number: 7803795Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: September 28, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Laurence Anne Mevellec, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Patent number: 7790899Abstract: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.Type: GrantFiled: May 15, 2007Date of Patent: September 7, 2010Assignee: ACADIA Pharmaceuticals, Inc.Inventors: Bo-Ragnar Tolf, Nathalie Schlienger, Mikkel Boas Thygesen
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Publication number: 20100222350Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Patent number: 7786308Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: March 28, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ioana Drutu, Miguel Garcia-Guzman Blanco, Lewis R. Makings, Gabriel Raffai, Valentin Boris Zunic
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Publication number: 20100210630Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: April 30, 2010Publication date: August 19, 2010Inventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Publication number: 20100190829Abstract: Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: June 20, 2008Publication date: July 29, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao
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Patent number: 7750012Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2006Date of Patent: July 6, 2010Assignee: deCODE genetics ehfInventors: Vincent Sandanayaka, Jasbir Singh, Li-Ming Zhou, Mark E. Gurney
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Publication number: 20100152098Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: November 5, 2009Publication date: June 17, 2010Applicant: Mpex Pharmaceuticals, Inc.Inventors: Tomasz Glinka, Olga Rodny, Keith A. Bostian, David M. Wallace, Robert I. Higuchi, Chun Chow, Chi Ching Mak, Gavin Hirst, Brian Eastman
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Patent number: 7732615Abstract: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2 -methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.Type: GrantFiled: September 26, 2005Date of Patent: June 8, 2010Assignee: ACADIA Pharmaceuticals Inc.Inventors: Mikkel Boas Thygesen, Nathalie Schlienger, Bo-Ragnar Tolf, Carl-Magnus A. Andersson, Fritz Blatter, Jörg Berghausen
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Publication number: 20100087485Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or ?-cell protection.Type: ApplicationFiled: December 9, 2009Publication date: April 8, 2010Inventors: Markus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Michael Loeffler, Thomas Luebbers, Fabienne Ricklin
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Publication number: 20100081692Abstract: The invention provides 1-benzyl-4-piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma. The compounds are inhibitors of the CCR1 receptor.Type: ApplicationFiled: October 31, 2006Publication date: April 1, 2010Applicant: ASTRAZENECA ABInventors: Martin Hemmerling, Nafizal Hossain, Svetlana Ivanova, Tesfaledet Mussie, Igor Shamovsky, Asa Sjoholm Timen
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Patent number: 7683079Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or ?-cell protection.Type: GrantFiled: December 14, 2005Date of Patent: March 23, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Michael Loeffler, Thomas Luebbers, Fabienne Ricklin
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Publication number: 20100022595Abstract: The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 13, 2007Publication date: January 28, 2010Applicant: Purdue Pharma L.P.Inventors: Zhengming Chen, Khondaker Islam, Donald J. Kyle, Deyou Sha, Bin Shao, Jiangchao Yao, Xiaoming Zhou
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Publication number: 20090306136Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 13, 2007Publication date: December 10, 2009Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
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Patent number: 7626032Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: April 24, 2008Date of Patent: December 1, 2009Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Patent number: 7595331Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: December 8, 2004Date of Patent: September 29, 2009Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20090170870Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: December 12, 2008Publication date: July 2, 2009Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu, Cameron Smith
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Patent number: 7550485Abstract: The present invention is directed to substituted N-heterocycle derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: June 23, 2009Assignee: WyethInventors: Paige Erin Mahaney, Lori Krim Gavrin, Douglas John Jenkins
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Patent number: 7538124Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: June 24, 2008Date of Patent: May 26, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
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Publication number: 20090131453Abstract: The invention relates to compounds of formula (I): processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.Type: ApplicationFiled: June 14, 2007Publication date: May 21, 2009Inventors: Jonathan Thomas Seal, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
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Patent number: 7534892Abstract: The present invention provides a compound of the formula (I): (wherein, R1 is ethyl optionally substituted by halogen or amino optionally substituted by lower alkyl, R2 and R3 are each independently hydrogen or lower alkyl, X is cycloalkylene, lower alkylene or piperidinediyl, Z is optionally substituted phenyl or optionally substituted heterocyclyl) prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: June 23, 2005Date of Patent: May 19, 2009Assignee: Shionogi & Co., Ltd.Inventor: Takuji Nakatani
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Publication number: 20090124663Abstract: This invention relates to novel N-phenyl-piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: June 7, 2006Publication date: May 14, 2009Applicant: NeuroSearch A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Ostergaard Nielsen, David Tristam Brown