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Preparation of C-Pyrazine-Methylamines

Application Number: 20120041202
Publication Date: 2012-02-16
Inventors: Rechka, Josef A.; Mao, Yunyu; Mulvihill, Kristen Michelle; Tavares-Greco, Paula A.

A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.

METHOD FOR PRODUCING FLUORINE-CONTAINING POLYETHER CARBOXYLIC ACID AMIDE

Application Number: 20120041201
Publication Date: 2012-02-16
Inventors: Kokin, Keisuke; Abe, Hideki; Takahashi, Yusuke; Murata, Seiichiro

A fluorine-containing polyether carboxylic acid amide represented by the general formula: C_nF_2n+1O(C₃F₆O)_mRfCONHAr, wherein Rf is a fluorocarbon group having 1 to 2 carbon atoms, Ar is a nitrogen-containing heterocyclic group, n is an integer of 1 to 3, and m is an integer of 10 to 30, is produced by reacting a fluorine-containing polyether carboxylic acid fluoride represented by the general formula: ...

PROCESS FOR THE PREPARATION OF BOSENTAN

Application Number: 20120041200
Publication Date: 2012-02-16
Inventors: Biffi, Giancarlo; Feliciani, Lazzaro; Viscardi, Enrico

The invention concerns a new process for the preparation of bosentan or bosentan monohydrate by reaction of compound of Formula II with ethylene glycol in the presence of potassium bases and the potassium salt of bosentan.

Process for the Preparation of Doxazosin and Salts Thereof

Application Number: 20120041199
Publication Date: 2012-02-16
Inventors: Kankan, Rajendra Narayanrao; Rao, Dharmaraj Ramachandra; Birari, Dilip Ramdas

The present invention relates to a process for the preparation of doxazosin or salts ...

Process for Preparing 5,7 Diaminopyrazolo [1,5-a] Pyrimidine Compounds

Application Number: 20120041198
Publication Date: 2012-02-16
Inventors: Liotta, Dennis C.; Jogalekar, Ashutosh S.; Snyder, James P.; Barrett, Anthony G.M.; Fuchter, Matthew John; Cook, Matthew J.; Kroll, Sebastian H.B.

Processes for the preparation of certain 5,7-diaminopyrazolo[1,5-α]pyrimidine compounds comprising the reaction of a primary or secondary amine and a protected 5-halo-7-aminopyrazolo[1,5-α]pyrimidine compound in solvent system comprising water and one or more organic solvents, optionally in the presence of an exogenous ...

Pyrido[3,2-h]quinazolines and/or 5,6-dihydro Derivatives Thereof, a Method for the Production Thereof and Doped Organic Semiconductor Material Containing These

Application Number: 20120041197
Publication Date: 2012-02-16
Inventors: Kussler, Manfred; Lux, Andrea; Salbeck, Josef

The present invention relates to pyrido[3,2-h]quinazolines and/or 5,6-dihydro derivatives thereof, methods for their production and doped organic semiconductor material which use such ...

Proteasome Inhibitors and Methods of Using the Same

Application Number: 20120041196
Publication Date: 2012-02-16
Inventors: De Munari, Sergio; D'Arasmo, Germano; Menta, Ernesto; Bernardini, Raffaella; Bernareggi, Alberto; Chatterjee, Sankar; Oliva, Ambrogio; Iqbal, Mohamed; Ferretti, Edmondo; Cassará, Paolo G.; Messina McLaughlin, Patricia A.

The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome ...

Heterocyclic compounds

Application Number: 20120041195
Publication Date: 2012-02-16
Inventors: Leriche, Caroline; Middlemiss, David; Auclair, Eric; Le Roux, Jacques

The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted triazolopyridine compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder. In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular ...

NITROGEN AND SULFUR-CONTAINING HETROCYCLE DERIVATIVES

Application Number: 20120041194
Publication Date: 2012-02-16
Inventor: Armilli, Murty N.

The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds ...

SUBSTITUTED INTERNAL VINYL-BORONIC ACIDS AND BORONIC ACID DERIVATIVES

Application Number: 20120041193
Publication Date: 2012-02-16
Inventors: Mokri, Homayoun H.; Cefalo, Dustin R.; Math, Shivanand K.; LaMunyon, James B.; Testa, Charles A.

Disclosed herein are vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives useful as synthetic intermediates for the preparation of therapeutic agents. Also disclosed are methods of synthesis of vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid ...

SUBSTITUTED SPIROCYCLIC AMINES USEFUL AS ANTIDIABETIC COMPOUNDS

Application Number: 20120041012
Publication Date: 2012-02-16
Inventors: Duffy, Joseph L.; Aster, Susan D.; Ye, Feng; Liang, Gui-Bai; Shao, Patrick

Substituted spirocyclic amines of structural formula I are selective antagonists of the somatostatin sub-type receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

SUBSTITUTED BENZOFUSED DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS

Application Number: 20120041011
Publication Date: 2012-02-16
Inventors: GHARAT, Laxmikant Atmaram; JOSHI, Uday Mukund; KHAIRATKAR-JOSHI, Neelima; KADAM, Suresh Mahadev

The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing ...

PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL

Application Number: 20120041009
Publication Date: 2012-02-16
Inventor: Mizuno, Hajime

A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.

CDK INHIBITOR SALTS

Application Number: 20120041007
Publication Date: 2012-02-16
Inventors: Fornaretto, Maria Gioia; Zampieri, Massimo; Airoldi, Annalisa; Brasca, Maria Gabriella

The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described ...

FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPAI MODULATORS

Application Number: 20120041004
Publication Date: 2012-02-16
Inventors: Thomas, Abraham; Chaudhari, Sachin Sundarlal; Mukhopadhyay, Indranil; Khairatkar-Joshi, Neelima; Kadam, Ashok Bhausaheb; Dhone, Sachin Vasantrao; Kumar, Sukeerthi; Patil, Nisha Parag; Deshmukh, Vishal Govindrao; Chikhale, Rajendra Prakash

The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical ...

INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME

Application Number: 20120041003
Publication Date: 2012-02-16
Inventors: Kym, Philip R.; Xin, Zhili; Souers, Andrew J.; Liu, Gang

The present invention relates to compounds of formula (I):

wherein R¹, R², and R³, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also ...

SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINES AS METABOTROPIC GLUTAMATE ANTAGONISTS

Application Number: 20120041002
Publication Date: 2012-02-16
Inventors: Gatti McArthur, Silvia; Goetschi, Erwin; Woltering, Thomas Johannes; Wichmann, Juergen

The present invention relates to compounds of formula (I)

wherein A, E G, J, L, M, R¹, R², and R³are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS ...

CARBONYLAMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE

Application Number: 20120041001
Publication Date: 2012-02-16
Inventors: Van Brandt, Sven Franciscus Anna; Backx, Leo Jacobus Jozef; Van Emelen, Kristof; Verdonck, Marc Gustaaf Celine

This invention comprises the novel compounds of formula (I)

wherein n, m, t, R¹, R², R³, R⁴, R⁵, L, Q, X, Y and

have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a ...

IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY

Application Number: 20120041000
Publication Date: 2012-02-16
Inventors: Berdini, Valerio; Murray, Christopher William; Freyne, Eddy Jean Edgard; Bonnet, Pascal Ghislain André; Ligny, Yannick Aimé Eddy; Saxty, Gordon; Papanikos, Alexandra; Wroblowski, Berthold

The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. ...

P38 KINASE INHIBITING AGENTS

Application Number: 20120040999
Publication Date: 2012-02-16
Inventors: Yang, Ginger Xu-Qiang; Sahoo, Soumya P.; Koyama, Hiroo; Miller, Daniel J.

Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and ...

2-ALKYL PIPERIDINE MGLUR5 RECEPTOR MODULATORS

Application Number: 20120040998
Publication Date: 2012-02-16
Inventors: Zhang, Xu-Fang; Roecker, Anthony J.; Mercer, Swati P.; Williams, Theresa

The present invention is directed to 2-alkylpiperidines which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 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 ...

VINYL-ARYL DERIVATIVES FOR INFLAMMATION AND IMMUNE-RELATED USES

Application Number: 20120040997
Publication Date: 2012-02-16
Inventor: Chen, Shoujun

The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune ...

3-BENZOFURANYL-INDOL-2-ONE DERIVATIVES SUBSTITUTED AT THE 3 POSITION, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF

Application Number: 20120040996
Publication Date: 2012-02-16
Inventors: Baroni, Marco; Puleo, Letizia

The invention relates to 3-benzofuranyl-indol-2-one derivatives substituted at the 3 position and of the formula (I) where R1, R2, R3, R4, R5 and n are such as defined in claim 1, to a method for preparing same, and to the therapeutic use of said compounds.

DESIGN, SYNTHESIS AND EVALUATION OF PROCASPASE ACTIVATING COMPOUNDS AS PERSONALIZED ANTI-CANCER DRUGS

Application Number: 20120040995
Publication Date: 2012-02-16
Inventors: Hergenrother, Paul J.; Peterson, Quinn Patrick; Hsu, Danny Chung; West, Diana C.; Fan, Timothy M.; Novotny, Chris J.

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 ...

NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM

Application Number: 20120040993
Publication Date: 2012-02-16
Inventors: Fridkin, Mati; Youdim, Moussa B. H.; Zheng, Hailin

Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and ...

OLIGOOXOPIPERAZINES AND METHODS OF MAKING AND USING THEM

Application Number: 20120040992
Publication Date: 2012-02-16
Inventors: Arora, Paramjit S.; Tosovska, Petra; Guarracino, Danielle; Bullock, Brooke

The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also ...

3-AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS

Application Number: 20120040991
Publication Date: 2012-02-16
Inventors: Di Fabio, Romano; Gianotti, Massimo; Pavone, Francesca; Amantini, David; Ferroni, Francesco

Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.

INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES

Application Number: 20120040990
Publication Date: 2012-02-16
Inventors: Schnider, Patrick; Grundschober, Christophe; Ratni, Hasane; Rogers-Evans, Mark; Bissantz, Caterina

The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I:

wherein the residues R¹to R³are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for ...

2-HYDROXYETHYL-1H-QUINOLIN-2-ONE DERIVATIVES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY

Application Number: 20120040989
Publication Date: 2012-02-16
Inventors: Hubschwerlen, Christian; Zumbrunn Acklin, Cornelia; Rueedi, Georg; Surivet, Jean-Philippe

The invention relates to antibacterial compounds of formula I

- wherein
- R¹represents alkoxy;
- each of U and V represents CH and W represents CH or N, or
- U represents N, V ...

DERIVATIVES OF 6,7-DIHYDRO-3H-OXAZOLO[3,4-a]PYRAZINE-5,8-DIONE

Application Number: 20120040988
Publication Date: 2012-02-16
Inventors: SACURAI, Sérgio Luiz; Zaim, Márcio Henrique; Touzarim, Carlos Eduardo da Costa; Keppler, Artur Franz; De Nucci, Gilberto

The present invention describes a series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, the derivative (R)-3-(1,3-benzodioxol-5-yl)-1-(1H-indol-3-yl)-7-methyl-6,7-dihydro[1,3]oxazolo[3,4-a]pyrazine-5,8-dione, its enantiomer ...

DERIVATIVES OF 6-(6-NH-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS

Application Number: 20120040987
Publication Date: 2012-02-16
Inventors: Ugolini, Antonio; Nemecek, Conception; Wentzler, Sylvie; Bacque, Eric

The invention relates to novel products of the formula (I) where: (II) is a single or double bond; Rb is a hydrogen or fluorine atom; Ra is a NH-Rc radical in which Rc is an optionally substituted heterocycloalkyl, aryl, heteroaryl or -alkylcycloalkyl radical; X is S, SO, or SO2; A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl; alkoxy; O-phenyl; —O— (CH2)n-phenyl with n=1 to 4; or NR1R2 with R1 being H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 form a cycle ...

OMEGA CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS

Application Number: 20120040986
Publication Date: 2012-02-16
Inventors: WOOD, Jill E.; RIEDL, Bernd; DUMAS, Jacques; KHIRE, Uday; LOWINGER, Timothy B.; SCOTT, William J.; SMITH, Roger A.; MONAHAN, Mary-Katherine; NATERO, Reina; RENICK, Joel; SIBLEY, Robert N.

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such ...

TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY

Application Number: 20120040985
Publication Date: 2012-02-16
Inventors: Flatt, Brenton T.; Morrissey, Michael; Boren, Brant Clayton; Gu, Xiao-Hui; Martin, Richard; Wang, Tie-Lin; Mohan, Raju; Bollu, Venkataiah; Julien, Jackaline Dalgard; Haq, Nadia; Hudson, Sarah; Pratt, Benjamin

The present invention comprises TGR5 agonists of structural formula I,

wherein X, R¹, R², and R⁵are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating ...

THIADIAZOLE AND OXADIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

Application Number: 20120040984
Publication Date: 2012-02-16
Inventors: Nicolai, Eric; Fett, Eykmar; Mougenot, Patrick; Namane, Claudie; Philippo, Christophe

The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.

Phthalazine Compounds as P38 Map Kinase Modulators and Methods of Use Thereof

Application Number: 20120040983
Publication Date: 2012-02-16
Inventors: Herberich, Bradley J.; Falsey, James R.; Tasker, Andrew; Rzasa, Robert M.; Zhang, Dawei

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A⁴, L, R¹, R², R³, R⁵and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 ...

Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions

Application Number: 20120040982
Publication Date: 2012-02-16
Inventors: LOTZ, Ralf; HIMMELSBACH, Frank; MARK, Michael; ECKHARDT, Matthias; LANGKOPF, Elke; MAIER, Roland

The present invention relates to substituted xanthines of general formula

wherein R¹to R⁴are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV ...

THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS

Application Number: 20120040981
Publication Date: 2012-02-16
Inventors: Oguro, Yuya; Kurasawa, Osamu

The present invention relates to a compound represented by the formula (I):

wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of ...

QUINAZOLINONE COMPOUNDS

Application Number: 20120040980
Publication Date: 2012-02-16
Inventors: Huggins, Penelope Jane; Parsons, Jack Gordon

The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).

IMIDAZO[1,2-B]PYRIDAZINES, PROCESSES, USES, INTERMEDIATES AND COMPOSITIONS

Application Number: 20120040979
Publication Date: 2012-02-16
Inventors: FALCÓ, José Luís; Palomer, Albert; Guglietta, Antonio

The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof.

Compounds of formula (I) are useful for treating or preventing diseases associated with GABA_Areceptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.

Heterocyclic Fused Cinnoline M1 Receptor Positive Allosteric Modulators

Application Number: 20120040978
Publication Date: 2012-02-16
Inventors: Kuduk, Scott D.; Beshore, Douglas C.

The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in 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.

INHIBITORS OF HCV NS5A

Application Number: 20120040977
Publication Date: 2012-02-16
Inventors: Li, Leping; Zhong, Min

Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis ...

BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF

Application Number: 20120040975
Publication Date: 2012-02-16
Inventors: Hao, Jinsong; Shah, Unmesh; Liu, Hong; Biswas, Dipshikha; Chackalamannil, Samuel; Neelamkavil, Santhosh Francis; Boyle, Craig D.; Neustadt, Bernard R.; Xia, Yan; Lankin, Claire M.; Stamford, Andrew; Harris, Joel M.

The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a ...

MIF MODULATORS

Application Number: 20120040974
Publication Date: 2012-02-16
Inventors: Jorgensen, William L.; Bucala, Richard J.

The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF ...

DERIVATIVES OF [1,3]OXAZIN-2-ONE USEFUL FOR THE TREATMENT OF METABOLIC DISEASES SUCH AS LIPID DISORDERS

Application Number: 20120040973
Publication Date: 2012-02-16
Inventors: Ye, Yuanjie; Tice, Colin M.; Singh, Suresh B.; Leftheris, Katerina; Claremon, David A.; Zhuang, Linghang

This invention relates to novel compounds of an 11 β-HSD1 inhibitor disclosed herein, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11/3-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of ...

DUAL MODULATORS OF 5HT2A AND D3 RECEPTORS

Application Number: 20120040972
Publication Date: 2012-02-16
Inventors: Gobbi, Luca; Roche, Olivier; Jaeschke, Georg; Rodriguez Sarmiento, Rosa Maria; Steward, Lucinda

The present invention relates to compounds of the formula (I)

wherein R¹, R², X and n are as defined in the specification as dual modulators of the serotonin 5-HT_2aand dopamine D₃receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, ...

N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR

Application Number: 20120040969
Publication Date: 2012-02-16
Inventors: Haupt, Andreas; Unger, Liliane; Drescher, Karla; Lao, Yanbin; Pohlki, Frauke; Relo, Ana-Lucia; Vogg, Barbara; Backfisch, Gisela; Wicke, Karsten; Bespalov, Anton; Delzer, Juergen; Zhang, Min

The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT_{6 ...}

DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND

Application Number: 20120040968
Publication Date: 2012-02-16
Inventors: Iwai, Yoshinori; Kamikawa, Akio; Tomiyama, Hiroshi; Kurosawa, Kazuo; Iikubo, Kazuhiko; Kondoh, Yutaka; Matsuya, Takahiro; Shimada, Itsuro

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.

As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention ...

Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine Compounds and Their Use

Application Number: 20120040967
Publication Date: 2012-02-16
Inventors: Cherry, Michael; Collins, Ian; Reader, John Charles; Matthews, Thomas Peter; Cheung, Kwai Ming; Proisy, Nicolas; Klair, Sukhbinder Singh; Scanlon, Jane Elizabeth; Williams, David Hugh; Piton, Nelly; Addison, Glynn Jonathan

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in ...

ANTI-VIRAL COMPOUNDS, TREATMENT, AND ASSAY

Application Number: 20120040966
Publication Date: 2012-02-16
Inventors: Maddry, Joseph A.; Severson, Bill; Jonsson, Colleen B.; Noah, James W.; Noah, Diana L.; Chen, Xi

The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end ...

N-SUBSTITUTED PIPERIDINES AND THEIR USE AS PHARMACEUTICALS

Application Number: 20120040964
Publication Date: 2012-02-16
Inventors: Li, Yanlong; Zhang, Colin; Metcalf, Brian W.; Zhuo, Jincong; Xu, Meizhong; Yao, Wenqing

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone ...