Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos (e.g., 3-azabicyclo-(3.2.2)nonanes, Etc.) Patents (Class 540/582)
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Publication number: 20150148328Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.Type: ApplicationFiled: June 21, 2013Publication date: May 28, 2015Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
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Publication number: 20140343042Abstract: The invention relates to the design and synthesis of novel anabaseine-based compounds, which are useful in treating or preventing a wide variety of conditions, including nervous system diseases or disorders, such as, schizophrenia, Alzheimer's disease, Parkinson's disease, drug dependence, and substance addiction, and compositions, kits, and methods thereof. The invention also provides novel anabaseine-based compounds, compositions, kits, and methods thereof for treating or preventing non-nerve system diseases or disorders (such as, inflammation and cancer) in a subject identified in need thereof. Certain enantiomeric compounds of the invention exhibited enhanced selectivity toward ?7 nAChRs relative to alpha4beta2 nAChRs. Other enantiomeric compounds of the invention exhibited enhanced selectivity for alpha4beta2 nAChRs relative to ?7 nAChRs.Type: ApplicationFiled: December 11, 2012Publication date: November 20, 2014Inventors: William R. Kem, Ferenc Soti, Hong Xing
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Patent number: 8841289Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: October 11, 2010Date of Patent: September 23, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
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Publication number: 20130184240Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.Type: ApplicationFiled: September 8, 2011Publication date: July 18, 2013Applicant: Shionogi & Co., Ltd.Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
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Patent number: 8399681Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: August 3, 2012Date of Patent: March 19, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
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Publication number: 20120329772Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: ApplicationFiled: July 9, 2012Publication date: December 27, 2012Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
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Patent number: 8263781Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: December 16, 2010Date of Patent: September 11, 2012Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20120208796Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.Type: ApplicationFiled: October 11, 2010Publication date: August 16, 2012Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
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Publication number: 20120156219Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20120071463Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: November 29, 2011Publication date: March 22, 2012Inventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Patent number: 8119659Abstract: The present invention relates to (2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.Type: GrantFiled: May 26, 2011Date of Patent: February 21, 2012Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, John Genus, Jacob Mathew
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Publication number: 20110257389Abstract: Cyclic amine compounds represented by formula (1) or salts thereof or N-oxides thereof, wherein Cy1 represents an unsubstituted or substituted aromatic ring; X represents oxygen, sulfur, unsubstituted or substituted nitrogen, sulfinyl, or sulfonyl; R1a and R2a, R1a and R4a, R2a and R3a, or R3a and R4a form saturated rings together; R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, and R5 which do not form the saturated rings are each independently hydrogen, hydroxyl, halogen, unsubstituted or substituted amino, nitro, or an organic group; Cy2 represents an unsubstituted or substituted aromatic ring with a proviso that Cy2 is an unsubstituted or substituted heteroaromatic ring when R1a and R2a form a saturated ring together and Cy1 is an unsubstituted or substituted phenyl, and Cy2 is a substituted pyridin-2-yl having one or more cyano as a substituent when Cy1 is an unsubstituted or substituted phenyl and Cy2 is a pyridin-2-yl.Type: ApplicationFiled: June 21, 2011Publication date: October 20, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Isami HAMAMOTO, Jun Takahashi, Makio Yano, Masahiro Kawaguchi, Daisuke Hanai, Takao Iwasa
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Publication number: 20110160185Abstract: Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: March 31, 2008Publication date: June 30, 2011Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marc Vendrell Escobar
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Publication number: 20110059937Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Inventor: Jakob Busch-Petersen
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Publication number: 20100324024Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: February 3, 2009Publication date: December 23, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Publication number: 20100249097Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.Type: ApplicationFiled: February 12, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Torsten HAACK, Petra LENNIG
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Publication number: 20100249099Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: Pathway Therapeutics LimitedInventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20100113420Abstract: Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: March 31, 2008Publication date: May 6, 2010Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marc Vendrell Escobar
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20090258858Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.Type: ApplicationFiled: October 28, 2005Publication date: October 15, 2009Inventors: Jakob Busch-Petersen, Jeffrey Charles Boehm, Huijie Li, John J. Taggart, Hong Xing Yan
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Publication number: 20090203668Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof wherein W, L, R3, R3a, R3b and R4 are defined herein.Type: ApplicationFiled: April 16, 2009Publication date: August 13, 2009Inventors: James J. Li, Lawrence G. Hamann, Haixia Wang, Zheming Ruan, Christopher B. Cooper, Jun Li, Jeffrey A. Robi
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Patent number: 7572817Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: June 10, 2003Date of Patent: August 11, 2009Assignee: AstraZeneca ABInventor: Magnus Polla
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Publication number: 20090163469Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: December 18, 2008Publication date: June 25, 2009Inventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Vito Guagnano, Patricia Imbach
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Patent number: 7247728Abstract: This application relates to bicyclic N-aryl amides of the formula R1 is a 1-aza-bicyclo[3.2.1]octyl group, a 1-aza-bicyclo[2.2.2]oct-3-yl; R2 is an optionally sustituted 8- to 10- membered heteroaryl, naphthyl, or azulenyl group; and R3 is H or (C1C6)alkyl; or a salt, solvate, or solvate of a salt of these compounds. A process for preparing these compounds, medicaments containing them, and methods for using them in treatment are also disclosed and claimed.Type: GrantFiled: December 6, 2002Date of Patent: July 24, 2007Assignee: Bayer Healthcare AGInventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Timo Flessner, Martin Hendrix, Marja van Kampen, Christoph Methfessel
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Patent number: 7196108Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: GrantFiled: March 6, 2003Date of Patent: March 27, 2007Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Patent number: 7176198Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat a disease or condition in which ?7 is known to be involved.Type: GrantFiled: July 25, 2003Date of Patent: February 13, 2007Assignee: Pfizer Inc.Inventors: David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Daniel Patrick Walker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Patent number: 7001900Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1–2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 21, 2006Assignee: Pfizer Inc.Inventors: Eric Jon Jacobsen, Jason K. Myers, Daniel Patrick Walker, Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Brad A. Acker, Vincent E. Groppi, Jr.
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6911543Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 1, 2002Date of Patent: June 28, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Steven Charles Reitz
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6849620Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 17, 2002Date of Patent: February 1, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
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Patent number: 6812234Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: April 29, 2003Date of Patent: November 2, 2004Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
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Publication number: 20040147505Abstract: The present invention relates to novel diazabicycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. A diazabicycloalkane derivative selected from those represented by Formula I, by Formula II, by Formula III, by Formula IV, and by Formula V.Type: ApplicationFiled: December 1, 2003Publication date: July 29, 2004Inventors: Dan Peters, Gunnar M Olsen, Elsebet Ostergaard Nielsen, Philip K Ahring, Tino Dyhring Jorgensen, Frank Abilgaard Slok
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Patent number: 6552015Abstract: The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, Y, U, W, k, A, E, V, R4 and R5 are as defined herein, pharmaceutical compositions thereof, and methods of use thereof in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of compounds of formula (I) and intermediates useful therefor.Type: GrantFiled: August 1, 2001Date of Patent: April 22, 2003Assignee: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randall James Gallaschun
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Patent number: 6531468Abstract: The present invention provides diazabicyclooctane derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein the group represents R1 and R2 are selected independently from H, (C1-C6)alkyl, (C1-C6)fluoroalkyl, halogen (e.g., F.Type: GrantFiled: August 1, 2001Date of Patent: March 11, 2003Assignee: Pfizer IncInventors: Anton Franz Joseph Fliri, Randall James Gallaschun
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Publication number: 20020160998Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacylic compounds. The present invention relates in particular to five-membered heteroaromatic olefinic azacyclic compounds and five-membered heteroaromatic acetylenic azacylic compounds, including isoxazolyl olefinic cycloalkylamines and isoxazolyl acetylenic cycloalkylamines.Type: ApplicationFiled: April 30, 2001Publication date: October 31, 2002Inventor: Thomas Jeffrey Clark
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Patent number: 6465491Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: April 4, 2001Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 6353099Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: August 17, 2000Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann, Theodore M. Kamenecka
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Patent number: 6235747Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: March 13, 1997Date of Patent: May 22, 2001Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 5977129Abstract: The present invention relates to compounds of formula I: whereinone or both G is an azacyclic ring of formula II: ##STR1## and Z is oxygen or sulfur and the remaining variables are as defined in the specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: May 3, 1995Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5952324Abstract: Phenyloxazolidinone compound of formula (I)or a pharmaceutically acceptable salt thereof characterized by a bicyclic thiazine or oxazine substituent. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: GrantFiled: May 14, 1997Date of Patent: September 14, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Richard C. Thomas, Gary L. Cleek, Lisa M. Thomasco, Robert C. Gadwood
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Patent number: 5912343Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.Type: GrantFiled: December 31, 1996Date of Patent: June 15, 1999Assignee: Bridgestone CorporationInventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
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Patent number: 5852189Abstract: Relatively pure tertiaryaminoalkyllithium initiators suitable for anionic polymerization reactions are prepared at low temperatures in an organic ether by reacting an equivalent excess of lithium metal with a tertiaryaminoalkylhalide. The lithium initiators are very stable at moderate temperatures when the ether is replaced by an aliphatic, a cycloaliphatic, or an aromatic solvent. Yields of the initiator in excess of 98% are readily achieved.Type: GrantFiled: December 31, 1996Date of Patent: December 22, 1998Assignee: Bridgestone CorporationInventors: William L. Hergenrother, Michael L. Kerns, David F. Lawson
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Patent number: 5847125Abstract: Compounds of formula (II) wherein Ar is naphthyl, naphthylmethyl, 1,2,3,4-tetrahydronaphthyl, phenethyl, styryl, indanyl or a substituted derivative of any of the foregoing, or 3,4-dichlorophenyl, R.sub.1 is H, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkenyl, cycloalkyl, --(CH.sub.2).sub.q aryl, --(CH.sub.2).sub.q (substituted aryl), --(CH.sub.2).sub.q heterocyclic or --(CH.sub.2).sub.q (substituted heterocyclic), wherein q is 0 to 4, R.sub.2 is H, methyl or ethyl, R.sub.3 is C.sub.1 to C.sub.3 alkylene or is absent, T is carboxyl, --CONR.sub.4 R.sub.5 (wherein R.sub.4 and R.sub.5 are independently H or C.sub.1 to C.sub.4 alkyl), --COOR.sub.13 (wherein R.sub.13 is C.sub.1 to C.sub.4 alkyl, benzyl or substituted benzyl) or tetrazolyl, X is --C(O)-- or --CH.sub.2 --, and Y is --NR.sub.6 R.sub.7 or --O--R.sub.6 (wherein R.sub.6 and R.sub.7 are independently H, C.sub.1 to C.sub.15 hydrocarbyl or halo-substituted C.sub.1 to C.sub.Type: GrantFiled: July 7, 1994Date of Patent: December 8, 1998Assignee: James Black Foundation LimitedInventor: Iain Mair McDonald
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Patent number: 5744607Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.Type: GrantFiled: October 18, 1996Date of Patent: April 28, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
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Patent number: 5707985Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Tanabe Seiyaku Co. Ltd.Inventors: Thomas Charles McKenzie, Gilbert M. Rishton, Nancy K. Harn, Wolfgang Scholz, James Hu
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Patent number: RE39558Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: December 23, 2004Date of Patent: April 10, 2007Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati