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488 results about "Macrocycle Compounds" patented technology
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Macrocyclic compound. An organic compound containing a large ring, that is, a closed chain of 12 or more carbon atoms; examples include crown ethers, cryptands, spherands, carcerands, cyclodextrins, cyclophanes, and calixarenes. Also known as macrocycle.
Macrocyclic compounds as inhibitors of viral replication
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
Owner:F HOFFMANN LA ROCHE & CO AG
Macrocycles useful in the treatment of Alzheimer's disease
Owner:PHARMACIA & UPJOHN CO
Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties
The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
Owner:SCHERING CORP
Macrocyclic compounds as inhibitors of viral replication
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
Owner:F HOFFMANN LA ROCHE & CO AG
Macrocyclic compounds as Trk kinase inhibitors
Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Owner:ARRAY BIOPHARMA INC
Biologically active peptidomimetic macrocycles
InactiveUS20090326192A1Strong penetrating powerImprove biological activityCompound screeningApoptosis detectionBioactive peptideMacrocycle Compounds
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Peptidomimetic macrocycles with improved properties
ActiveUS20100298201A1Prolong half-life in vivoHalogenated hydrocarbon active ingredientsNervous disorderBioactive peptideBiological organism
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Biologically Active Peptidomimetic Macrocycles
InactiveUS20110144303A1Strong penetrating powerImprove biological activityPeptide/protein ingredientsPeptide preparation methodsBioactive peptideBiological activity
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Therapeutic peptidomimetic macrocycles
InactiveUS20090275519A1Less treatmentReduce activated hPBL proliferationMetabolism disorderPeptidesMedicineBioactive peptide
The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
Owner:AILERON THERAPEUTICS INC
Macrocyclic hepatitis C serine protease inhibitors
The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.
Owner:ABBVIE INC +1
Process for preparing macrocyclic compounds
Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
Owner:BOEHRINGER INGELHEIM INT GMBH
Macrocyclic compounds useful as pharmaceuticals
The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein.
Owner:EISAI CO LTD
Methods for preparing purified polypeptide compositions
ActiveUS20100210515A1Useful in therapySenses disorderNervous disorderMedicinePolypeptide composition
The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Macrocyclic ghrelin receptor modulators and methods of using the same
ActiveUS20080194672A1Reduced and dysfunctional gastrointestinal motilityInhibit gastrointestinal motilityAntibacterial agentsOrganic active ingredientsSomatotropic hormonePharmaceutical Substances
The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC
Long-lived homogenous amide containing macrocyclic compounds
InactiveUS6054580ALower discharge levelHigh protection levelGroup 8/9/10/18 element organic compoundsOrganic-compounds/hydrides/coordination-complexes catalystsArylCompound a
A robust compound is provided having the formula: wherein Y1, Y2, Y3 and Y4 are oxidation resistant groups which are the same or different and which form 5- or 6-membered rings with a metal, M, when bound to D. D is a metal complexing donor atom, O or N. Each X is a position for addition of a substituent and, when D is N, each position is (i) not occupied such that a double bond is formed between D and an atom adjacent to D, or (ii) is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, alkoxy, phenoxy, halogen, halogenated alkyl, halogenated aryl, halogenated alkenyl, halogenated alkynyl, perhaloalkyl, perhaloaryl, a substituted or unsubstituted cycloalkyl ring, a substituted or unsubstituted cycloalkenyl ring, a substituted or unsubstituted saturated heterocyclic ring, a substituted or unsubstituted unsaturated heterocyclic ring, and at least one X is hydrogen, and when D is O, the position is not occupied.
Owner:CARNEGIE MELLON UNIV
Peptidomimetic macrocycles
InactiveUS20110223149A1Improved protease stabilityImprove stabilityNervous disorderPeptide/protein ingredientsProteinase activityBioactive peptide
The present invention provides biologically active peptidomimetic macrocycles with improved properties, such as protease resistance, relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Macrocyclic compounds as trk kinase inhibitors
Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Owner:ARRAY BIOPHARMA
Macrocyclic modulators of the ghrelin receptor
ActiveUS20060025566A1Promote gastrointestinal motilityModulating activity of receptorDigestive systemCyclic peptide ingredientsInflammationCentral nervous system
Owner:OCERA THERAPEUTICS INC
Macrocyclic compounds as inhibitors of viral replication
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
Owner:INTERMUNE INC
Biologically active peptidomimetic macrocycles
InactiveUS20130023646A1Improve biological activityReduced activityCompound screeningApoptosis detectionBioactive peptideMacrocycle Compounds
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
Labeling targeting agents with gallium-68 and gallium-67
InactiveUS7011816B2Safe and fastAccurate detectionOrganic active ingredientsRadioactive preparation carriersElutionPositron emission tomographic
A method and compositions are described for labeling a targeting agent with Ga-68, in which eluate from an acid-eluted Ge-68 / Ga-68 generator is combined with a macrocycle-containing targetable agent. The labeling method and compositions disclosed ensure that a simple elution of gallium-68, taken directly from a generator, can be used without further manipulation to quantitatively label a macrocycle-containing targetable agent. The Ga-68 labeled targeting agent so produced is useful with specific targeting agents, and is most especially useful in a pretargeting method for positron emission tomographic detection.
Owner:IMMUNOMEDICS INC
Macrocyclic modulators of the ghrelin receptor
ActiveUS7476653B2Promote gastrointestinal motilityModulating activity of receptorDigestive systemPeptide preparation methodsGrowth hormone-releasing peptideInflammation
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and / or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
Owner:OCERA THERAPEUTICS INC
Methods, compositions, and apparatuses for forming macrocyclic compounds
ActiveUS20070217965A1Improve production efficiencyHigh yieldHydrocarbon by dehydrogenationCyclic peptide ingredientsOligomerFiltration
This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and / or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation. More preferably, the macrocyclic compound spontaneous precipitates from the reaction medium and therefore can be easily recovered by simple filtration.
Owner:JOHNSON THOMAS E +1
Macrocyclic antagonists of the motilin receptor
The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates:wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
Owner:OCERA THERAPEUTICS INC
Biologically active peptidomimetic macrocycles
InactiveUS20140323701A1Improve biological activityReduced activityCompound screeningApoptosis detectionBioactive peptideMacrocycle Compounds
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Owner:AILERON THERAPEUTICS INC
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