Piperazine derivatives and methods of use

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

CGRP peptide antagonists and conjugates

Disclosed is a composition of matter that involves a CGRP peptide antagonist. A pharmaceutical composition is disclosed that comprises the composition of matter and a pharmaceutically acceptable carrier, which can be configured for administration to a patient. Also disclosed is a method of producing the composition of matter. Methods of treating, preventing or mitigating migraine, are also disclosed.

Nitrogen-containing heterocyclyl ketones and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Nitrogen-Containing heterocyclyl ketones and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Antagonists of the bradykinin B1 receptor

The present invention relates to certain biologically active peptides and conjugated peptides which can be used as therapeutics or prophylactics against diseases or conditions linked to B1 as the causative agent. In a preferred embodiment of the invention biologically active PEG-conjugated peptides are provided. In one aspect of the present invention, pharmacologically active PEG-conjugated peptides of the present invention are useful to treat inflammation or pain.

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R¹, b, R³, d, R⁴, R⁵, R⁶ and R⁷ are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.

Cyclic amine derivatives and methods of use

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R3, d, R4, R5, R6 and R7 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.

Novel B1 bradykinin receptor antagonists

The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Triazoles and methods of use

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R¹, b, R⁴, R⁵, R⁶, R⁷ and R⁸ are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R4, R5, R6, R7 and R8 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Method of conjugating aminothiol containing molecules to vehicles

The present invention relates to a novel chemical process that provides novel vehicle derivatives that are exceptional 1,2- or 1,3-aminothiol specific reagents for conjugation to unprotected targeted compounds (e.g., polypeptides, peptides, or organic compounds) having or modified to have a 1,2- or 1,3 aminothiol group. The invention further relates to the methods of using novel water-soluble polymer derivatives and conjugates thereof.

Compounds and methods of use

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Triazoles and methods of use

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structuraldiagram,[Chemical formula should be inserted here. Please see paper copy]wherein A, R 1 , b, R 3 , d, R 4 , R 5 , R 6 and R 7 are any of a number of groups as defined in thespecification, and pharmaceutical compositions and methods of treatment utilizing suchcompounds.

Substituted amide derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Use of alcohol co-solvents to improve pegylation reaction yields

Disclosed is a method of of producing a composition of matter. The method involves obtaining a pharmacologically active peptide; and conjugating the peptide to a pharmaceutically acceptable polyethylene glycol (PEG) by reacting the peptide with a PEG-aldehyde compound at a free amine moiety on the peptide in a buffer solution comprising an alcohol co-solvent.

Fused heterocyclic derivatives useful as inhibitors of the hepatocyte growth factor receptor

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Substituted amide derivatives as protein kinase inhibitors

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Bicyclic compounds having bradykinin receptors affinity and pharmaceutical compositions thereof

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Cyclic amine derivatives and their use in the treatment of inflammation-related disorders mediated by bradykinin

Compounds of formula (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation mediated by Bradykinin. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes wherein q, t, R, Ra, Rb, Rc and R2 are as defined herein.

Pi3 kinase modulators and methods of use

The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Bicyclic compounds having bradykinin receptors affinity and pharmaceutical compositions thereof

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors

Selected compounds defined by Formula I, II, III, IV or V are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases.

Substituted amide derivatives as protein kinase inhibitors

Substituted amide derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Pl3 kinase modulators and methods of use

The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A, A, A, A, X, R and R are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Cgrp peptide antagonists and conjugates

Disclosed is a composition of matter that involves a CGRP peptide antagonist. A pharmaceutical composition is disclosed that comprises the composition of matter and a pharmaceutically acceptable carrier, which can be configured for administration to a patient. Also disclosed is a method of producing the composition of matter. Methods of treating, preventing or mitigating migraine, are also disclosed.

Novel B1 bradykinin receptor antagonists

Substituted amide derivatives as protein kinase inhibitors

Antagonists of the bradykinin B1 receptor

The present invention relates to composition of matter involving bradykinin B1 receptor antagonist peptides conjugated to a univalent vehicle, including peptides conjugated to univalent PEG. These compositions can be used as therapeutics or prophylactics against diseases or conditions, such as inflammation or pain, linked to the bradykinin B1 receptor.

PIPERAZINE DERIVATIVES AND METHOD OF USE

Fused heterocyclic derivatives and methods of use as c-Met inhibitors

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Novel b1 bradykinin receptor antagonists

The invention encompasses novel compounds of a formula I and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.

1,2,3,4-tetrahydropyrazin-2-yl acetamides and their use as bradykinin antagonists for the treatment of inflammation related disorders

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structuraldiagram,[Chemical formula should be inserted here. Please see paper copy]wherein A, R 1 , b, R 3 , d, R 4 , R 5 , R 6 and R 7 are any of a number of groups as defined in thespecification, and pharmaceutical compositions and methods of treatment utilizing suchcompounds.

Fused heterocyclic derivatives and methods of use

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Substituted amide derivatives as protein kinase inhibitors

Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Substituted Amide Derivatives as Protein Kinase Suspensions

Επιλεγμένες ενώσεις είναι αποτελεσματικές για την πρόληψη και τη θεραπεία ασθενειών, όπως ασθενειών που προκαλούνται μέσω HGF. Η εφεύρεση περιλαμβάνει νέες ενώσεις, ανάλογες ενώσεις, προφάρμακα και φαρμακευτικώς αποδεκτά άλατα αυτών, φαρμακευτικές συνθέσεις και μεθόδους για την πρόληψη και τη θεραπεία ασθενειών κι άλλων παθήσεων ή καταστάσεων που ενέχουν καρκίνο κλπ. Η παρούσα εφεύρεση επίσης σχετίζεται με μεθόδους παρασκευής τέτοιων ενώσεων όπως επίσης και με ενδιάμεσες ενώσεις χρήσιμες σε τέτοιες μεθόδους. Selected compounds are effective for the prevention and treatment of diseases, such as HGF-induced diseases. The invention includes novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for the prevention and treatment of diseases and other diseases or conditions involving cancer etc. The present invention also relates to methods of preparing such compounds as well. with intermediates useful in such methods.

FUSIONED HETEROCICLIC DERIVATIVES AND METHODS OF USE

Los compuestos seleccionados resultan eficaces para la profilaxis y el tratamiento de enfermedades, tales como las enfermedades mediadas por el factor HGF. La invencion incluye novedos compuestos, analogos, profarmacos y sus sales farmaceuticamente aceptables, composiciones farmaceuticas y metodos destinados a la profilaxis y el tratamiento de enfermedades y demas dolencias o estados que se relacionan con el cancer y otroas patalogias similares.

Bicyclic pyridazine compounds as Pim inhibitors

The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Piperazinderivate und anwendungsverfahren

Bicyclic Pyridazine Compounds as PIM Inhibitors

The invention relates to bicyclic compounds of formulas I and I′, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Antagonisten für calciumkanäle vom n-typ zur behandlung von schmerzen

N-type calcium channel antagonists for the treatment of pain

Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R?1, b, R4, R5, R6, R7 and R8¿ are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.