Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
March 2, 2012
Publication date:
June 28, 2012
Applicant:
ChemoCentryx, Inc.
Inventors:
Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Type:
Application
Filed:
December 29, 2011
Publication date:
June 28, 2012
Inventors:
Francesco G. Salituro, Jeffrey Saunders
Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
Type:
Application
Filed:
September 28, 2011
Publication date:
May 31, 2012
Inventors:
Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
Type:
Application
Filed:
December 21, 2011
Publication date:
April 26, 2012
Inventors:
Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
Abstract: The present invention relates to crystalline form II-S, its preparation and its use to prepare other crystalline forms of posaconazole, in particular crystalline form IV of posaconazole.
Type:
Application
Filed:
July 9, 2010
Publication date:
April 26, 2012
Applicant:
SANDOZ AG
Inventors:
Josef Wieser, Arthur Pichler, Andreas Hotter, Ulrich Griesser, Christoph Langes
Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.
Type:
Application
Filed:
December 16, 2011
Publication date:
April 19, 2012
Inventors:
Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.
Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
Type:
Application
Filed:
December 23, 2009
Publication date:
March 15, 2012
Applicant:
BIAL - PORTELA & Cª, S.A.
Inventors:
Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
Type:
Application
Filed:
March 3, 2010
Publication date:
March 8, 2012
Inventors:
Kai Schiemann, Melanie Schultz, Wolfgang Staehle
Abstract: Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and/or inhibition of pain and other conditions mediated by the vanilloid receptor 1.
Type:
Application
Filed:
August 19, 2011
Publication date:
February 23, 2012
Applicant:
Gruenenthal GmbH
Inventors:
Robert FRANK, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry
Abstract: Novel triazole derivatives of the formula (I) in which R1-R6 and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
Type:
Grant
Filed:
April 20, 2007
Date of Patent:
February 21, 2012
Assignee:
Merck Patent GmbH
Inventors:
Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.
Type:
Application
Filed:
February 9, 2010
Publication date:
February 16, 2012
Applicant:
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Inventors:
Paul J. Hergenrother, Quinn Patrick Peterson, Danny Chung Hsu, Diana C. West, Timothy M. Fan, Chris J. Novotny
Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
Type:
Grant
Filed:
January 27, 2009
Date of Patent:
February 14, 2012
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Kristof Van Emelen, Hans Louis Jos De Winter, Alexy Borisovich Dyatkin, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.
Type:
Application
Filed:
December 17, 2008
Publication date:
January 19, 2012
Inventors:
Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Victoria D. Wong
Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.
Type:
Application
Filed:
March 3, 2010
Publication date:
January 19, 2012
Inventors:
Wolfgang Staehle, Kai Schiemann, Melanie Schultz
Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C?O)—N(R3)(R4), or —(C?O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.
Abstract: The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
Type:
Application
Filed:
June 2, 2011
Publication date:
December 22, 2011
Applicant:
ALBANY MOLECULAR RESEARCH, INC.
Inventors:
Christopher L. CIOFFI, Mark A. WOLF, Peter R. GUZZO, Shuang LIU, Kashinath SADALAPURE, Visweswaran PARTHASARATHY, Jun-Ho MAENG
Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).
Type:
Application
Filed:
October 27, 2010
Publication date:
December 15, 2011
Applicant:
Bayer CropScience AG
Inventors:
Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
Type:
Application
Filed:
May 5, 2011
Publication date:
November 10, 2011
Applicant:
Infinity Pharmaceuticals
Inventors:
Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.
Type:
Application
Filed:
July 14, 2011
Publication date:
November 3, 2011
Inventors:
William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).
Abstract: Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.
Type:
Application
Filed:
April 7, 2008
Publication date:
October 27, 2011
Applicant:
THE JOHNS HOPKINS UNIVERSITY
Inventors:
Jun O. Liu, Curtis R. Chong, Jing Xu, Jun Lu, Shridhar Bhat
Abstract: The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.
Type:
Grant
Filed:
January 11, 2008
Date of Patent:
October 11, 2011
Assignee:
Critical Outcome Technologies, Inc.
Inventors:
Wayne R. Danter, Martyn Brown, Franck LePifre
Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
Type:
Application
Filed:
August 10, 2009
Publication date:
September 15, 2011
Applicants:
Merck Sharp & Dohme Corp., Scynexis, Inc.
Inventors:
Mark L Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Ahmed Mamai
Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
March 5, 2004
Date of Patent:
September 13, 2011
Assignee:
Novartis AG
Inventors:
Graham Charles Bloomfield, Ian Bruce, Catherine Leblanc, Mrinalini Sachin Oza, Lewis Whithead, Bernard Cuenoud, Thomas Hugo Keller, Louise Kirman, Clive McCarthy, Gaynor Elizabeth Woodward
Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.
Type:
Grant
Filed:
June 5, 2008
Date of Patent:
August 30, 2011
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z 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:
Grant
Filed:
September 5, 2008
Date of Patent:
June 14, 2011
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
June 7, 2011
Assignee:
Nereus Pharmaceuticals, Inc.
Inventors:
Yoshio Hayashi, Michael A. Palladino, Jr., Jennifer Grodberg
Abstract: The present invention relates to a pharmaceutical composition comprising crystalline form Y of posaconazole. The pharmaceutical composition can be used to treat or prevent fungal infections.
Type:
Application
Filed:
May 28, 2009
Publication date:
May 5, 2011
Applicant:
SANDOZ AG
Inventors:
Josef Wieser, Arthur Pichler, Andreas Hotter, Ulrich Griesser, Christoph Langes, Christian Laschober
Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
Type:
Application
Filed:
June 14, 2010
Publication date:
May 5, 2011
Inventors:
Weiwen YING, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.
Type:
Grant
Filed:
January 5, 2007
Date of Patent:
May 3, 2011
Assignee:
AstraZeneca AB
Inventors:
Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
Abstract: The present invention relates to crystalline form IV of posaconazole and pharmaceutical compositions comprising the same. The pharmaceutical composition can be used to treat or prevent fungal infections.
Type:
Application
Filed:
June 25, 2009
Publication date:
March 17, 2011
Applicant:
Sandoz AG
Inventors:
Josef Wieser, Arthur Pichler, Andreas Hotter, Ulrich Griesser, Christoph Langes
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
July 8, 2010
Publication date:
December 30, 2010
Applicant:
Chemocentryx, Inc.
Inventors:
Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
Type:
Application
Filed:
August 25, 2010
Publication date:
December 16, 2010
Applicant:
SIEMENS MEDICAL SOLUTIONS USA, INC.
Inventors:
Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.
Type:
Application
Filed:
June 11, 2010
Publication date:
December 16, 2010
Inventors:
Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y? are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
Type:
Application
Filed:
May 11, 2010
Publication date:
December 16, 2010
Inventors:
Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Type:
Grant
Filed:
December 9, 2003
Date of Patent:
November 30, 2010
Assignee:
ChemoCentryx, Inc.
Inventors:
Andrew M. K. Pennell, James B. Aggen, J. J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Valeri V. Martichonok
Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
Type:
Application
Filed:
September 19, 2008
Publication date:
November 18, 2010
Applicant:
Amgen Inc.
Inventors:
Liping H. Pettus, Kelvin K.C. Sham, Andrew Tasker, Shimin Xu
Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.
Type:
Grant
Filed:
August 10, 2007
Date of Patent:
November 16, 2010
Assignee:
Palatin Technologies, Inc.
Inventors:
Kevin Burris, Yi-Qun Shi, Shubh D. Sharma, Yadi Reddy Bonuga, Papireddy Purma
Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to 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. The invention further relates to 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 atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
Type:
Grant
Filed:
December 22, 2008
Date of Patent:
October 19, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
Abstract: Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.
Abstract: The invention relates to novel 5-hydroxytryptamine (5-HT) receptor modulator compounds of formula (I); wherein A, B, R1-R5, T, W, X, Y, Z and m are defined herein, to pharmaceutical compositions comprising these compounds and to their use in the treatment of conditions associated with 5-HT action.
Type:
Application
Filed:
August 6, 2008
Publication date:
October 14, 2010
Inventors:
Jonathan Richard Heal, Joseph Michael Sheridan, William Dennys Ormrod Hamilton, Simon James Grimshaw, Sorin Vasile Filip