The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Publication number: 20090035267Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof, which can inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: July 31, 2007Publication date: February 5, 2009Inventors: Joel D. Moore, Datong Tang, Yat Sun Or, Zhe Wang
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Patent number: 7476673Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 7470687Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in Claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.Type: GrantFiled: May 8, 2006Date of Patent: December 30, 2008Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
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Patent number: 7470689Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: August 31, 2006Date of Patent: December 30, 2008Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Günter Müller, Cécile Combeau, Christine Delaisi, Anke Steinmetz, Ingrid Sassoon
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Publication number: 20080318923Abstract: It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.Type: ApplicationFiled: January 30, 2006Publication date: December 25, 2008Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Yoshinori Sekiguchi, Takeshi Kuwada, Masato Hayashi, Dai Nozawa, Yuri Amada, Tsuyoshi Shibata, Shuji Yamamoto, Hiroshi Ohta, Taketoshi Okubo, Takeshi Koami
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Publication number: 20080318899Abstract: The invention relates to novel chemical compounds and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: November 2, 2005Publication date: December 25, 2008Inventors: Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdelena Zasadzki
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Patent number: 7468368Abstract: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.Type: GrantFiled: June 5, 2003Date of Patent: December 23, 2008Assignee: Sanofi AventisInventors: Françoise Bono, Michaël Bosch, Victor Dos Santos, Jean-Marc Herbert, Dino Nisato, Bernard Tonnerre, Jean Wagnon
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Publication number: 20080311079Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Vertex Pharmaceuticals IncorporatedInventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
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Patent number: 7462617Abstract: The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: September 1, 2004Date of Patent: December 9, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Patent number: 7462613Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.Type: GrantFiled: November 19, 2003Date of Patent: December 9, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Swen Hölder, Thorsten Naumann, Karl Schönafinger, David William Will, Hans Matter, Günther Müller, Dominique Le Suisse, Bernard Baudoin, Thomas Rooney, Franck Halley, Gilles Tiraboschi, Cécile Combeau, Ingrid Sassoon, Anke Steinmetz
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Publication number: 20080287452Abstract: The present invention relates to heteroaryl/aryl pyrimidine analogs, methods of making aryl/heteroaryl pyrimidine analogs, compositions comprising a aryl/heteroaryl pyrimidine analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a heteroaryl/aryl pyrimidine analog.Type: ApplicationFiled: May 16, 2008Publication date: November 20, 2008Applicant: WyethInventors: Matthew Gregory BURSAVICH, Adam Matthew GILBERT, Diane Barbara HAUZE, Charles William MANN, Jeffrey Claude PELLETIER
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Publication number: 20080280916Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.Type: ApplicationFiled: February 25, 2008Publication date: November 13, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Andreas Bilich, Michael D. Winther, Yigal Paul Goldberg
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Publication number: 20080280889Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the invention.Type: ApplicationFiled: April 5, 2005Publication date: November 13, 2008Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D.P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Patent number: 7449465Abstract: This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.Type: GrantFiled: July 12, 2004Date of Patent: November 11, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Christopher John Love, Ludwig Paul Cooymans, Nele Vandermaesen, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Werner Constant Johan Embrechts
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Publication number: 20080269232Abstract: The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.Type: ApplicationFiled: November 14, 2005Publication date: October 30, 2008Inventors: Song Li, Chunlai Mi, Zhibing Zheng, Guoming Zhao, Xinbo Zhou, Zehui Gong
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Patent number: 7442699Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: August 24, 2005Date of Patent: October 28, 2008Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
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Publication number: 20080261987Abstract: 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: ApplicationFiled: July 21, 2006Publication date: October 23, 2008Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Publication number: 20080255133Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 18, 2008Publication date: October 16, 2008Applicant: ARDEA BIOSCIENCES, INC.Inventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
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Publication number: 20080221063Abstract: The invention relates to heterocyclic derivatives of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R1 is hydrogen or C1-3alkyl; R2 is selected from hydroxy, C1-5alkyl, carboxy, cyano, tetrazolyl, N—C1-5alkyltetrazolyl, oxazolyl, C1-5oxazolyl, isoxazolyl, C1-5 isoxazolyl, hydroxyC1-5alkyl, carboxy C1-5alkyl, C1-5alkoxyoxo C1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di(C1-5alkyl)carbamoyl, C1-5alkylcarbamoyl C1-4alkyl, hydroxy C1-5alkylcarbamoyl, C1-5alkoxy C1-5alkylcarbamoyl; —C1-5alkyl-Y1, —COOCHR17R18 and —CONR17R18; and R3 is hydrogen or halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals.Type: ApplicationFiled: July 5, 2006Publication date: September 11, 2008Applicant: ASTRAZENECA ABInventors: Christer Alstermark, Kjell Andersson, Ulf Fahlander, Kenneth Granberg
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Publication number: 20080214553Abstract: The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.Type: ApplicationFiled: March 10, 2006Publication date: September 4, 2008Inventors: Jeffrey Letourneau, Christopher Riviello, Koc-Kan Ho, Jui-Hsiang Chan, Michael Ohlmeyer, Patrick Jokiel, Irina Neagu, John Richard Morphy, Susan Elizabeth Napier
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Publication number: 20080214495Abstract: The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkyleType: ApplicationFiled: July 5, 2006Publication date: September 4, 2008Applicant: ASTRAZENECA ABInventors: Christer Alstermark, Kosrat Amin, Kjell Andersson, Yantao Chen, Ulf Fahlander, Kevin Michael Foote, Kenneth Granberg, Daniel Hovdal
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Patent number: 7419979Abstract: The invention relates to heterocyclic derivatives of formula (I), wherein R2 is amino, a group OR4 or a group —Y—R5 where R4 is hydrogen or C1-4alkyl, Y is C1-4alkylene, R5 is hydrogen, halo, hydroxy, C1-2alkoxy, C1-2alkoxyC1-2alkoxyC1-4, or a group NR7R8 where R7 and R8 are independently selected from hydrogen, C1-2alkyl, hydroxyC1-2alkyl or alkoxyC1-2alkyl, or R7 and R8 together with the nitrogen atom to which they are attached form a saturated 5-6-membered heterocyclic ring which optionally contains an additional heteroatom; n is one or two and each R1 is independently selected from halo, haloC1-2alkyl, hydroxy, oxo, amino, C1-2alkylamino or di-C1-2dialkylamino; or a pharmaceutically acceptable salt thereof. These compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals.Type: GrantFiled: January 5, 2005Date of Patent: September 2, 2008Assignee: AstraZeneca ABInventors: Emma Bratt, Yantao Chen, Kenneth Granberg, Ingemar Nilsson
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Publication number: 20080207629Abstract: The invention relates to novel liquid preparation comprising a substituted benzimidazol, preferably pimobendan as pharmaceutically active compound. In particular, the present invention relates to liquid preparation comprising an etherified cyclodextrin derivative, preferably in a concentration of about 20 to 70% (w/v) and said substituted benzimidazol, preferably in a concentration of about 0.005 to 0.15% (w/w).Type: ApplicationFiled: November 5, 2007Publication date: August 28, 2008Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Martin Folger, Stefan Lehner
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Publication number: 20080200431Abstract: The invention relates to compounds of formula (I), Chemical formula should be inserted here.Type: ApplicationFiled: July 5, 2006Publication date: August 21, 2008Applicant: ASTRAZENECA ABInventors: Christer Alstermark, Kosrat Amin, Kjell Andersson, Ulf Fahlander, Kenneth Granberg, Daniel Hovdal
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Publication number: 20080200472Abstract: A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.Type: ApplicationFiled: August 17, 2007Publication date: August 21, 2008Inventors: Donald J. Kyle, Qun Sun
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Publication number: 20080182851Abstract: The present invention provides Stearoyl CoA Desaturase (SCD) inhibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase 1 (SCD1) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase (SCD) inhibitors.Type: ApplicationFiled: November 19, 2007Publication date: July 31, 2008Applicant: Glenmark Pharmaceuticals S.A.Inventors: Abraham Thomas, V.S. Prasada Rao Lingam, Shantaram Kashinath Phatangare, Neelima Khairatkar-Joshi, Daisy Manish Shah, Deepak Vitthal Ukirde, Dattaguru Anandrao More
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Publication number: 20080176854Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: July 24, 2008Applicant: Laboratorios Del Dr. Esteve S.AInventors: Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
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Publication number: 20080176831Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N— or —S—; R1 may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: ApplicationFiled: May 17, 2005Publication date: July 24, 2008Applicant: BASF AktiengesellschaftInventors: Anja Schwogler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Muller, Thomas Grote, Wassilios Grammenos, Udo Hunger, Carsten Blettner, Peter Schafer, Oliver Wagner, Reinhard Stierl, Ulrich Schofl, Siegfried Strathmann, Maria Scherer
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Patent number: 7396831Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: July 8, 2008Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
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Publication number: 20080153836Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: April 10, 2006Publication date: June 26, 2008Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jorg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Publication number: 20080153835Abstract: A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cyanoiminopiperazine Compound are disclosed.Type: ApplicationFiled: September 4, 2007Publication date: June 26, 2008Inventors: Donald J. Kyle, Qun Sun, Laykea Tafesse, Chongwu Zhang, Xiaoming Zhou
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Publication number: 20080153834Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 11, 2007Publication date: June 26, 2008Inventors: Peter A. Blomgren, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Jeffrey E. Kropf, Kevin S. Currie
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Publication number: 20080146581Abstract: A pharmaceutical composition having improved solubility comprising a hydrophobic drug or pharmaceutically acceptable salt thereof and a compound having at least one carboxylic acid moiety, wherein the molar ratio of the compound having at least one carboxylic acid moiety to the hydrophobic drug or pharmaceutically acceptable salt thereof is from about 0.1:1 to about 25:1. The pharmaceutical composition exhibits rapid dissolution upon contact with physiological solvents, such as water, saliva or gastrointestinal fluids.Type: ApplicationFiled: February 15, 2008Publication date: June 19, 2008Applicant: Sandoz AGInventors: Gary Barbera, Chetan Chhabildas Doshi, Mahendra R. Patel, Pablo Davila, Satishkumar Ambalal Patel
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Publication number: 20080132509Abstract: Substituted biaryl analogues of Formula (I) are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localizations studies.Type: ApplicationFiled: December 13, 2005Publication date: June 5, 2008Applicant: Neurogen CorporationInventors: Charles A. Blum, Bertrand L. Chenard, Kevin J. Hodgetts, Xiaozhang Zheng
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Patent number: 7381725Abstract: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: August 4, 2003Date of Patent: June 3, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Stephen Robert Fletcher, Angus Murray MacLeod, Monique Bodil Van Niel, Kevin Wilson
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Patent number: 7381719Abstract: A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3?, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: September 17, 2003Date of Patent: June 3, 2008Assignee: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Marta Garcia De La Torre, Nuria Diaz Buezo, William Glen Holloway, James Edward Matt, Charles Howard Mitch, Concepcion Pedregal-Tercero, Dana Rae Smith, Russell Dean Stucky, Kumiko Takeuchi
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Publication number: 20080125434Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 20, 2005Publication date: May 29, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vandna Raina, Serguei Sviridov, Vishnumurthy Kodumuru, Nagasree Chakka, Shifeng Liu, Shaoyi Sun, Duanjie Hou
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Publication number: 20080119457Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein A, Q1, Q2, Q3, R31, and R41 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: May 22, 2008Inventors: Kenneth He Huang, John Mangette, Thomas Barta, Steven E. Hall, James Veal, Philip Hughes
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Patent number: 7368447Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: August 26, 2005Date of Patent: May 6, 2008Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Patent number: 7365073Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 23, 2004Date of Patent: April 29, 2008Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Farouz, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
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Patent number: 7365075Abstract: The present invention provides Aryl Sulfonamide Compounds having the formula: and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.Type: GrantFiled: December 20, 2004Date of Patent: April 29, 2008Assignee: Amgen Inc.Inventors: Michael R. DeGraffenreid, Xiao He, Jay P. Powers, Daqing Sun, Xuelei Yan
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Patent number: 7361657Abstract: This invention concerns the use of compounds of formula (I) wherein ?a1=a2?a3=a4—is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7354924Abstract: This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: October 20, 2004Date of Patent: April 8, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
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Publication number: 20080076774Abstract: The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.Type: ApplicationFiled: April 22, 2005Publication date: March 27, 2008Applicant: Exelixis, Inc.Inventors: Neel K. Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Lynne Canne Bannen, Diva Sze-Ming Chan, Baili Chen, Erick Wang Co, Simona Costanzo, Steven Charles Defina, Larisa Dubenko, Maurizio Franzini, Ping Huang, Vasu Jammalamadaka, Richard George Khoury, Moon Hwan Kim, Rhett Ronald Klein, Donna Tra Le, Morrison B. Mac, John M. Nuss, Jason Jevious Parks, Kenneth D. Rice, Tsze H. Tsang, Amy Lew Tsuhako, Yong Wang, Wei Xu
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Publication number: 20080070915Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compnounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.Type: ApplicationFiled: June 28, 2005Publication date: March 20, 2008Inventors: Jerome Emile Georges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Patent number: 7335658Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: July 29, 2004Date of Patent: February 26, 2008Assignee: Xenon Pharmaceuticals Inc.Inventors: Nagasree Chakka, Mikhail Chafeev, Sultan Chowdhury, Jian-Min Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Michael D Winther, Zaihui Zhang, Melwyn Abreo, Mark W Holladay, Wenbao Li, Sengen Sun, Chi Tu, Heinz W Gschwend
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Patent number: 7332493Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: March 14, 2005Date of Patent: February 19, 2008Assignee: OSI PharmaceuticalsInventors: John Charles Kath, Joel Morris, Samit Kumar Bhattacharya
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Patent number: 7320977Abstract: The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans and/or animals.Type: GrantFiled: April 8, 2003Date of Patent: January 22, 2008Assignee: Bayer Healthcare AGInventors: Rudolf Schohe-Loop, Elmar Burchardt, Christiane Faeste, Claudia Hirth-Dietrich, Jörg Keldenich, Andreas Knorr, Thomas Lampe, Paul Naab, Delf Schmidt, Gunter Schmidt