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56results about How to "Reduces and avoids symptom and cause" patented technology
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Inhibitors of c-jun-n-terminal kinase (JNK)
ActiveUS20140309249A1Reduce tumor burdenStop growthOrganic active ingredientsBiocideKinase activityNeuro-degenerative disease
The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.
Owner:DANA FARBER CANCER INST INC
Drug delivery polymer and uses thereof
ActiveUS9381253B2Stop growthStop the spreadOrganic active ingredientsPlatinum organic compoundsPancreas CancersProstate cancer
Owner:MASSACHUSETTS INST OF TECH
Stabilized polypeptides as regulators of rab gtpase function
ActiveUS20140235549A1Stop growthStop the spreadPeptide-nucleic acidsPeptide/protein ingredientsRing-closing metathesisPharmaceutical drug
The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Host targeted inhibitors of dengue virus and other viruses
ActiveUS20150166532A1Delay or minimize one or more symptoms associatedReduces and avoids symptom and causeBiocideOrganic chemistryHerpes simplex diseaseDisease injury
Novel antiviral compounds of Formulae (I)-(III) are provided: (I) (II) (III) The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENY)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).
Owner:DANA FARBER CANCER INST INC +1
Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof
ActiveUS20150246913A1Amplify tyrosine kinase signalingDownstream signaling can be enhancedBiocideOrganic chemistryDiseaseTec kinase
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and / or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
Owner:DANA FARBER CANCER INST INC +1
Inhibitors of c-Jun-N-terminal kinase (JNK)
ActiveUS9382239B2Stop growthStop the spreadOrganic active ingredientsNervous disorderKinase activityNeuro-degenerative disease
The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.
Owner:DANA FARBER CANCER INST INC
Ras inhibitors and uses thereof
Described herein are compounds of Formulae (I)-(II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., lung cancer, large bowel cancer, pancreas cancer, biliary tract cancer, or endometrial cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject.
Owner:DANA FARBER CANCER INST INC
Drug delivery polymer and uses thereof
ActiveUS20140308234A1Reduce tumor burdenStop growthOrganic active ingredientsSugar derivativesProstate cancerEsophagus Cancers
Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as cisplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH
Drug delivery polymer and uses thereof
ActiveUS20160296631A1Stop growthStop the spreadOrganic active ingredientsPlatinum organic compoundsPancreas CancersProstate cancer
Owner:MASSACHUSETTS INST OF TECH
Host targeted inhibitors of dengue virus and other viruses
ActiveUS9879003B2Delay or minimize one or more symptoms associatedReduces and avoids symptom and causeOrganic chemistryHerpes simplex diseaseJunin virus
Novel antiviral compounds of Formulae (I)-(III) are provided: (I) (II) (III) The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENY)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).
Owner:DANA FARBER CANCER INST INC +1
Drug delivery polymers and uses thereof
ActiveUS20170348431A1Reduce molecular weightReduces and avoids symptom and causePowder deliveryOrganic active ingredientsPancreas CancersProstate cancer
Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as oxaliplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, colorectal cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH
Stabilized polypeptides as regulators of RAB GTPase function
ActiveUS9487562B2Stop growthStop the spreadPeptide-nucleic acidsPeptide/protein ingredientsRing-closing metathesisPharmaceutical drug
The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Drug delivery polymers and uses thereof
ActiveUS10105449B2Reduces and avoids symptom and causeGood curative effectHeavy metal active ingredientsPowder deliveryPancreas CancersProstate cancer
Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as oxaliplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, colorectal cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH
Brush-arm star polymer imaging agents and uses thereof
ActiveUS20190038782A1Improve the level ofHigh relaxivitiesPowder deliveryNanomedicineSolubilityNitrate
Disclosed are methods, compositions, reagents, systems, and kits to prepare nitroxide-functionalized brush-arm star polymer organic radical contrast agent (BASP-ORCA) as well as compositions and uses thereof. Various embodiments show that BASP-ORCA display unprecedented per-nitroxide and per-molecule transverse relaxivities for organic radical contrast agents, exceptional stability, high water solubility, low in vitro and in vivo toxicity, and long blood compartment half-life. These materials have the potential to be adopted for tumor imaging using clinical high-field 1H MRI techniques.
Owner:MASSACHUSETTS INST OF TECH +1
Core-to-surface polymerization for the synthesis of star polymers and uses thereof
ActiveUS20190030067A1Reduce concentrationReduces and avoids symptom and causeOrganic active ingredientsIn vivoMetal
Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
Owner:MASSACHUSETTS INST OF TECH
Indazole derivatives and uses thereof
ActiveUS9738610B2Facilitate investigation of the various mechanisms employedCombat increasingly prevalent drug-resistanceOrganic active ingredientsAntimycoticsProtozoaCandida famata
Owner:WHITEHEAD INST FOR BIOMEDICAL RES +1
N-arylated analogues and uses thereof
ActiveUS20190373890A1Enhance therapeutic efficacyImproves overall therapyBiocideOrganic chemistryCystic fibrosis lungsPolymicrobial Infections
The present invention provides novel compounds of Formula (I′) and (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for killing a microorganism (e.g., bacteria, fungi, viruses, protozoa, or multicellular parasites), the prevention and / or treatment of infectious diseases (e.g., infections by microorganisms, bacterial infection, cystic fibrosis infection, foreign body infection, urinary tract infection (UTI), or infections leading to biofilms), controlling and / or eradicating biofilms (e.g., bacterial biofilms), preventing biofilm formation, sterilizing a surface, and / or eradicating persister cells (e.g., in a subject in need thereof or in a subject involving a biofilm).
Owner:UNIV OF FLORIDA RES FOUNDATION INC
Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof
InactiveUS20190112305A1Enhanced signalEnhance signaling downstreamOrganic chemistryAntineoplastic agentsDiseaseTec kinase
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and / or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
Owner:BETH ISRAEL DEACONESS MEDICAL CENT INC +1
Diphosphate mimetics and uses thereof
ActiveUS20140163079A1Convenient treatmentReduces and avoids symptomBiocideNervous disorderKinase activityAGT II
The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and / or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and / or kinase-associated conditions.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Compounds for treating infectious diseases
ActiveUS9505735B2Improve propertiesEnhance pharmaceuticallyAntimycoticsOrganic chemistryIsrapafantMedicinal chemistry
The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwt1 activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwt1 activity.
Owner:WHITEHEAD INST FOR BIOMEDICAL RES +1
Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
ActiveUS20200361906A1Convenient treatmentReduces and avoids symptomOrganic chemistryAntineoplastic agentsAutoimmune conditionStage melanoma
The present invention provides novel compounds of Formulae (I′) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and / or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK12), and therefore, induce cellular apoptosis and / or inhibit transcription in the subject.
Owner:DANA FARBER CANCER INST INC
Thiohydantoin derivatives and uses thereof
ActiveUS9944607B2Increase virulenceReliable discriminationBiocideOrganic active ingredientsProtozoaProtozoal Infection
Owner:THE BROAD INST INC +2
Enterobactin conjugates and uses thereof
ActiveUS20150105337A1Convenient treatmentReduces and avoids symptomBiocideSaccharide with carbocyclic radicalsBowels diseasesFibrosis
The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and / or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and / or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.
Owner:MASSACHUSETTS INST OF TECH
Phenylsulfonamido-benzofuran derivatives and uses thereof in the treatment of proliferative diseases
ActiveUS20180237406A1Stop growthStop the spreadOrganic active ingredientsOrganic chemistryFuranDisease
Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and / or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and / or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.
Owner:MEMORIAL SLOAN KETTERING CANCER CENT
N-arylated analogues and uses thereof
ActiveUS11419335B2Reduces and avoids symptom and causeGood curative effectBiocideOrganic active ingredientsProtozoaInfectious Disorder
The present invention provides novel compounds of Formula (I′) and (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for killing a microorganism (e.g., bacteria, fungi, viruses, protozoa, or multicellular parasites), the prevention and / or treatment of infectious diseases (e.g., infections by microorganisms, bacterial infection, cystic fibrosis infection, foreign body infection, urinary tract infection (UTI), or infections leading to biofilms), controlling and / or eradicating biofilms (e.g., bacterial biofilms), preventing biofilm formation, sterilizing a surface, and / or eradicating persister cells (e.g., in a subject in need thereof or in a subject involving a biofilm).
Owner:UNIV OF FLORIDA RES FOUNDATION INC
Compositions and methods for treating CNS disorders
ActiveUS20200024301A1Reduces and avoids symptom and causeGood curative effectOrganic active ingredientsNervous disorderDiseaseSedation
Described herein are neuroactive steroids of the Formula (I); or a pharmaceutically acceptable salt thereof, wherein, R1, R2a, R2b, R3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.
Owner:SAGE THERAPEUTICS
Inhibitors of cyclin-dependent kinase 12 (CDK12) and uses thereof
ActiveUS20210317105A9Reduces and avoids symptom and causeGood curative effectOrganic chemistryAntineoplastic agentsAutoimmune conditionStage melanoma
The present invention provides novel compounds of Formulae (I′) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and / or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK12), and therefore, induce cellular apoptosis and / or inhibit transcription in the subject.
Owner:DANA FARBER CANCER INST INC
Therapeutic Compounds and Uses Thereof
Owner:KALA PHARMA
Methods for treating polycystic kidney disease and polycystic liver disease
ActiveUS20150105361A1Reduces and avoids symptom and causeGood curative effectOrganic active ingredientsDigestive systemPhysiologyCyst
The present invention provides compounds of Formula (I) or (II), which are thought to be able to inhibit mTOR (mammalian target of rapamycin) signaling pathway, induce UPR (unfolded protein response), and / or perturb mitochondrial function of a cyst cell (e.g., a cyst cell causing polycystic kidney disease (PKD, e.g., autosomal dominant PKD (ADPKD) or autosomal recessive PKD (ARPKD)) or polycystic liver disease (PLD, e.g., autosomal dominant PLD (ADPLD) or autosomal recessive PLD (ARPLD)). The invention also provides pharmaceutical compositions, kits, and methods involving the compounds described herein for use in treating PKD or PLD, inhibiting the growth of a cyst cell, and / or killing a cyst cell.
Owner:YALE UNIV +1
Benzimidazole derivatives and uses thereof
ActiveUS9790188B2Reduces and avoids symptom and causeGood curative effectOrganic active ingredientsNervous disorderBenzimidazole derivativeCell Aggregations
Owner:WHITEHEAD INST FOR BIOMEDICAL RES +1
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