Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/223)
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Publication number: 20090124610Abstract: Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof, wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R1a is an optionally substituted aryl or heteroaryl group; R1b is hydrogen or a group R1a; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BG1) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N?C(RZ), (RZ)C?N, (RZ)N—C(O), (RZ)2C—C(O), N?N and (RZ)C?C(R6); J4-J3 is a group N?C(RZ) or a group (RZ)N—CO; and RZ is hydrogen or a substituent.Type: ApplicationFiled: April 25, 2007Publication date: May 14, 2009Inventors: Gordon Saxty, Marinus Leendert Verdonk, John Caldwell, Ian Collins, Kwai-Ming Cheung, Tatiana Faria Da Fonseca McHardy
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Patent number: 7528156Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 22, 2004Date of Patent: May 5, 2009Assignee: AstraZeneca ABInventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
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Publication number: 20090105249Abstract: The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds 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: October 14, 2005Publication date: April 23, 2009Applicant: Euro-Celtique S.A.Inventors: Elfrida R. Benjamin, Zhengming Chen, Deyou Sha, Laykea Tafesse, Samuel F. Victory, John W.F. Whitehead, Xiaoming Zhou
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Publication number: 20090076026Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: November 5, 2008Publication date: March 19, 2009Inventors: Yu-Hua JI, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
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Publication number: 20090048227Abstract: Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Pasun K. Chakravarty, Pengcheng Patrick Shao, Feng Ye
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Publication number: 20090042851Abstract: 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: ApplicationFiled: July 21, 2008Publication date: February 12, 2009Applicant: SANOFI-AVENTISInventors: Pierre DESPEYROUX, Evelyne Fontaine, Gilles Courtemanche, Pierrick Rochard, Claudine Serradeil-Le Gal
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Patent number: 7488741Abstract: 4-Aminopiperidine derivatives, pharmaceutical compositions containing the same, and methods for their preparation are provided herein for the treatment of disorders of the central and/or peripheral nervous systems. In particular, the potent antidepressant activity shown by the disclosed 4-aminopiperidine derivatives are particularly useful for the prevention and/or the treatment of depression, severe depression with anxiety, anxiety disorders and affective disorders.Type: GrantFiled: September 30, 2003Date of Patent: February 10, 2009Assignee: UCB Pharma, S.A.Inventors: Yves Lamberty, Christophe Genicot
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Publication number: 20090023733Abstract: The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] 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) mediated disease state.Type: ApplicationFiled: March 6, 2007Publication date: January 22, 2009Inventors: Peter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
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Publication number: 20090023777Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.Type: ApplicationFiled: March 6, 2008Publication date: January 22, 2009Inventors: Mathai Mammen, Richard Wilson, Sarah Dunham, Adam Hughes, Craig Husfeld, Yu-Hua Ji, Li Li, Trevor Mischki, Ioanna Stergiades, David Oare
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Publication number: 20090023710Abstract: There is provided a compound having Formula (I) wherein each of R1, R2, R3, R4, R5, R6 and R7 are independently selected from (a) H, (b) R17, —OC(R17)3, —OCH(R17)2, —OCH2R17, —C(R17)3, —CH(R17)2, or —CH2R17 wherein R17 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(R11)C(O)R13; 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, alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; each of rings A and B are selected from five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a furtType: ApplicationFiled: January 2, 2008Publication date: January 22, 2009Inventors: Nigel Vicker, Joanna Mary Day, Helen Victoria Bailey, Wesley Heaton, Ana Maria Ramos Gonzalez, Christopher Mark Sharland, Michael John Reed, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 7473692Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).Type: GrantFiled: September 25, 2002Date of Patent: January 6, 2009Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: János Galambos, Katalin Nógrádi, Éva Ágainé Csongor, György Miklós Keserü, István Vágó, György Domány, Béla Kiss, István Gyertyán, István Laszlovszky, Judit Laszy
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Publication number: 20080275087Abstract: 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: ApplicationFiled: June 24, 2008Publication date: November 6, 2008Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx
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Publication number: 20080269190Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides 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: April 23, 2008Publication date: October 30, 2008Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
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Publication number: 20080262226Abstract: A method is provided for making compounds comprising a beta-adrenergic inhibiting moiety and a linking moiety, the method comprising: a) reacting a compound of formula (A): (R1—(CH—O—CH2)) with at least one of NH3, NH4, NH4ClNH3 and R12?NH2 thereby forming a compound of formula (B): (R1—CH(OH)—CH2—NHR12?); and b) reacting a compound of formula (B) with a compound of formula (C): (R3?O), thereby forming a compound of formula (D): (R1—COH—CH2—N(R3)(R12?)), wherein R1 comprises the beta-adrenergic inhibiting moiety or comprises the beta-adrenergic inhibiting moiety when bonded to —COH—CH2—N(R12?)— of formula (D); R3 comprises the linking moiety and is bonded to the =0 of formula (C) via a carbon atom; and R12? is selected from hydrogen and a protecting group.Type: ApplicationFiled: November 7, 2007Publication date: October 23, 2008Applicant: ARTESIAN THERAPEUTICS, INC.Inventor: Gang Chen
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Publication number: 20080255345Abstract: The invention relates to iRNA agents that preferably include a modification that targets CC chemokine receptor 5 (CCR5). The invention also relates to methods of making and using such modified iRNA agents.Type: ApplicationFiled: November 21, 2007Publication date: October 16, 2008Inventors: Muthiah Manoharan, Kallanthottahil G. Rajeev
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Publication number: 20080227784Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R5 represents a halogen atom, cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R6 represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR7, —O—CH2— or —N(R8)—CH2—, R7 represents hydrogen atom or a C1-4 alkyl group, or R7 may combine with a substituent of R6 to represent a single bond, methylene group or ethylene group, R8 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation ofType: ApplicationFiled: June 19, 2007Publication date: September 18, 2008Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN. INC.Inventors: Ryukou TOKUYAMA, Toshifumi WAKAMATSU, Tatsurou ICHIGE, Susumu MUTO, Akiko ITAI
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Publication number: 20080194826Abstract: A compound represented the general formula (V): wherein X is CH or N; and Ya is a group of the general formula selected from:Type: ApplicationFiled: March 20, 2008Publication date: August 14, 2008Inventors: Ryuuta Fukutomi, Hitoshi Inoue, Koji Kawamura, Takuya Kishimoto, Masashi Suzuki, Rie Shibayama, Kazuko Kojima, Kouichirou Hagihara
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Publication number: 20080176902Abstract: The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methyl-propyl)oxy]-4-hydroxyphenyl}acetamide hemi-fumarate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy.Type: ApplicationFiled: July 31, 2006Publication date: July 24, 2008Applicant: ASTRAZENECA ABInventors: Julien Giovannini, Bo-Goran Josefsson
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Patent number: 7381735Abstract: The subject invention concerns analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.Type: GrantFiled: October 24, 2005Date of Patent: June 3, 2008Assignee: Aryx TherapeuticsInventor: Pascal Druzgala
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Publication number: 20080119516Abstract: It was an object of the present invention to provide novel compounds 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 syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.Type: ApplicationFiled: July 29, 2004Publication date: May 22, 2008Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Antoni Torrens Jover, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
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Patent number: 7368443Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.Type: GrantFiled: March 31, 2004Date of Patent: May 6, 2008Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Publication number: 20080096922Abstract: A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3?m+n?8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: —SO2—, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.Type: ApplicationFiled: April 4, 2005Publication date: April 24, 2008Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hitoshi Ban, Shigehiro Asano
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Publication number: 20080081824Abstract: The present application describes modulators of CCR3 of formula (I): or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, Q1, R1, R2, R3, R4, R5, R6, R7, T1, T2, W1, W2, W3 and Z1 are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.Type: ApplicationFiled: September 29, 2006Publication date: April 3, 2008Inventors: Changsheng Zheng, Dean A. Wacker
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Publication number: 20080045544Abstract: 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: August 6, 2007Publication date: February 21, 2008Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Patent number: 7317103Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.Type: GrantFiled: January 13, 2004Date of Patent: January 8, 2008Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Miles P. Smith
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Patent number: 7301023Abstract: A method for resolving enantiomers of a compound containing the structure of the forula: wherein R4 or R5 may contan one or more asymmetric centers, by mixing a racemic mixture of enantiomers of a compound, containing the structure of said formula; in a solvent, with a resolving compound having a defined sterospecificity, to form a solution and with said resolving agent being capable of binding with at least one but not all of said enantiomers to form a precipitate, containing said at least one of said enantiomers in sterospecific form and collecting either the precipitate and purifying it or collecting the solution with contained other of said enantiomers and recrystallizing the enantiomer contained in said solution.Type: GrantFiled: May 23, 2002Date of Patent: November 27, 2007Assignee: Pfizer Inc.Inventors: Mark E. Flanagan, Michael J. Munchhof
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Patent number: 7262211Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: GrantFiled: December 4, 2002Date of Patent: August 28, 2007Assignee: Dendreon CorporationInventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
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Publication number: 20070149544Abstract: 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: ApplicationFiled: August 3, 2006Publication date: June 28, 2007Applicant: DECODE CHEMISTRY, INC.Inventors: Vincent SANDANAYAKA, Jasbir SINGH, Li-Ming ZHOU, Mark E. GURNEY
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Patent number: 7208604Abstract: Synthetic pathways are disclosed for synthesizing derivatives or analogs of fentanyl. Specifically set out are pathways for synthesizing alfentanil, sufentanil and remifentanil. The disclosed methods require fewer steps and produce a greater yield of product than methods reported in the prior art.Type: GrantFiled: February 24, 2006Date of Patent: April 24, 2007Assignee: Mallinckrodt Inc.Inventors: Jacob Mathew, J. Kendall Killgore
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Patent number: 7192963Abstract: A compound of the formula wherein R1, R2 and R3 are as defined above, useful as inhibitors of protein kinases, such as the enzyme Janus Kinase 3.Type: GrantFiled: April 21, 2005Date of Patent: March 20, 2007Assignee: Pfizer IncInventors: Todd A. Blumenkopf, Mark E. Flanagan, Michael J. Munchhof
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Patent number: 7183277Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: March 31, 2003Date of Patent: February 27, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
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Patent number: 7176316Abstract: The present invention relates to compounds of the general formula wherein X and Y are each independently selected from —CH2— or —O—, with the proviso that X and Y are not simultaneously —O—; A is —S(O)2— or —C(O)—; and R1, R2, R3, and R4 are as defined in the specification. The compounds are GlyT-1 inhibitors and are useful for the treatment of psychoses, pain, dysfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: February 13, 2004Date of Patent: February 13, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Simona Maria Ceccarelli, Emmanuel Pinard, Henri Stadler
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Patent number: 7176210Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described hereinType: GrantFiled: January 21, 2004Date of Patent: February 13, 2007Assignee: Pfizer Inc.Inventor: David A. Griffith
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Patent number: 7169928Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.Type: GrantFiled: June 1, 2004Date of Patent: January 30, 2007Assignee: Societe Civile BioprojectInventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Charon Robin Ganellin, Fabien Leurquin, Sigurd Elz
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Patent number: 7135483Abstract: Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent.Type: GrantFiled: November 29, 2001Date of Patent: November 14, 2006Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: 7084140Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: September 5, 2002Date of Patent: August 1, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Patent number: 7064137Abstract: Compounds of general formula (I): R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.Type: GrantFiled: May 16, 2002Date of Patent: June 20, 2006Assignee: Astrazeneca ABInventors: William Brown, Andrew Griffin, Christopher Walpole
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Patent number: 7022716Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: December 27, 2002Date of Patent: April 4, 2006Assignee: WyethInventors: Baihua Hu, Fuk-Wah Sum, Michael Sotirios Malamas
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Patent number: 6995268Abstract: 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: June 14, 2001Date of Patent: February 7, 2006Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 6974825Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: July 29, 2003Date of Patent: December 13, 2005Assignee: AstraZeneca Canada Inc.Inventors: Benjamin Pelcman, Edward Roberts
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Patent number: 6943177Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.Type: GrantFiled: August 30, 2002Date of Patent: September 13, 2005Assignee: University of Kentucky Research FoundationInventors: Linda P. Dwoskin, Peter A. Crooks, Marlon D. Jones
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Patent number: 6911544Abstract: The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine and (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.Type: GrantFiled: October 9, 2003Date of Patent: June 28, 2005Assignees: Pfizer Inc., DSM Pharmaceuticals, Inc.Inventors: Robert Seemayer, Thomas C. Nugent, Jack Liang
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Patent number: 6911458Abstract: The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: June 14, 2001Date of Patent: June 28, 2005Assignee: Astra ZenecaInventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
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Patent number: 6903085Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditionsType: GrantFiled: August 18, 2000Date of Patent: June 7, 2005Assignee: AstraZeneca, ABInventors: Stephen Thom, Andrew Baxter, Nicholas Kindor, Thomas McInally, Brian Springthorpe, Matthew Perry, David Harden, Richard Evans, David Marriott
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Patent number: 6900228Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: GrantFiled: March 9, 1999Date of Patent: May 31, 2005Assignee: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6900329Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Patent number: 6897306Abstract: Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.Type: GrantFiled: July 16, 2002Date of Patent: May 24, 2005Assignee: Pfizer Products, Inc.Inventors: Simon Bailey, Stephane Billotte, Paul Vincent Fish, Kim James, Nicholas Murray Thomson, Andrew Michael Derrick