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Compositions comprising zopiclone derivatives and methods of making and using the same

ActiveUS7189715B2Minimizing spread and worseningGood curative effectBiocideOrganic chemistryZopicloneMedicinal chemistry

The invention is directed to racemic and stereomerically pure compounds of Formula 3:and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.

Compositions comprising zopiclone derivatives and methods of making and using the same

Compositions comprising zopiclone derivatives and methods of making and using the same

Compositions comprising zopiclone derivatives and methods of making and using the same

Owner:WOODWARD SPECIALTY LLC

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

ActiveUS20140329884A1Good curative effectDelay moreBiocideOrganic chemistryMedicinePlasmid dna

The present invention provides novel 1,3,5-triazinane-2,4,6-trione derivatives, such as compounds of any one of Formulae (I) and (II), and salts thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, or plasmid DNA). The present invention also provides methods and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and / or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, and lung diseases.

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

Owner:MASSACHUSETTS INST OF TECH

19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof

ActiveUS9512165B2Eliminate potential for oxidationImprove bioavailabilityOrganic active ingredientsSenses disorderSubstance abuserWithdrawal syndrome

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I), and pharmaceutically acceptable salts thereof; wherein, R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof

19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof

19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

Neuroactive steroids and methods of use thereof

InactiveUS20160031930A1Maintain good propertiesGood metabolic stabilityOrganic active ingredientsSenses disorderNeuroactive steroidPharmacology

(3alpha,3beta)-disubstituted 17beta steroidal compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, are provided for the prevention and treatment of a variety of CNS-related conditions.

Owner:SAGE THERAPEUTICS

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.

Inhibitors of c-jun-n-terminal kinase (JNK)

Inhibitors of c-jun-n-terminal kinase (JNK)

Inhibitors of c-jun-n-terminal kinase (JNK)

Owner:DANA FARBER CANCER INST INC

19-NOR neuroactive steroids and methods of use thereof

ActiveUS9365611B2Eliminate potential for oxidationImprove bioavailabilityOrganic active ingredientsSenses disorderWithdrawal syndromeSubstance abuser

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, tinnitus, and status epilepticus.

19-NOR neuroactive steroids and methods of use thereof

19-NOR neuroactive steroids and methods of use thereof

19-NOR neuroactive steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

19-nor neuroactive steroids and methods of use thereof

ActiveUS20160083418A1Eliminate potential for oxidationInhibit metabolismOrganic active ingredientsSenses disorderSubstance abuserWithdrawal syndrome

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, tinnitus, and status epilepticus.

19-nor neuroactive steroids and methods of use thereof

19-nor neuroactive steroids and methods of use thereof

19-nor neuroactive steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

ActiveUS9725481B2Eliminate potential for oxidationImprove bioavailabilityOrganic active ingredientsNervous disorderSubstance abuserWithdrawal syndrome

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5-to6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

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.

Stabilized polypeptides as regulators of rab gtpase function

Stabilized polypeptides as regulators of rab gtpase function

Stabilized polypeptides as regulators of rab gtpase function

Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

19-nor neuroactive steroids and methods of use thereof

InactiveUS20160068563A1Eliminate potential for oxidationImprove bioavailabilityNervous disorderEstrane derivativesSubstance abuserWithdrawal syndrome

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, tinnitus, status epilepticus.

19-nor neuroactive steroids and methods of use thereof

19-nor neuroactive steroids and methods of use thereof

19-nor neuroactive steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

InactiveUS20160229887A1Useful in therapyReduces avoids symptom causeOrganic active ingredientsSenses disorderSedationNeuroactive steroid

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L 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.

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Owner:SAGE THERAPEUTICS

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.

Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof

Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof

Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC +1

Polyamine-fatty acid derived lipidoids and uses thereof

ActiveUS20160002178A1Increase exposureIncrease concentrationOrganic active ingredientsOrganic chemistryRespiratory diseaseFatty acid

The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R—C(═O)—O— moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and / or for treating and / or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders.

Polyamine-fatty acid derived lipidoids and uses thereof

Polyamine-fatty acid derived lipidoids and uses thereof

Polyamine-fatty acid derived lipidoids and uses thereof

Owner:MASSACHUSETTS INST OF TECH

Compositions and methods for treating CNS disorders

InactiveUS20170233433A1Reduces avoids symptom 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.

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Owner:SAGE THERAPEUTICS

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.

Inhibitors of c-Jun-<i>N</i>-terminal kinase (JNK)

Inhibitors of c-Jun-<i>N</i>-terminal kinase (JNK)

Inhibitors of c-Jun-<i>N</i>-terminal kinase (JNK)

Owner:DANA FARBER CANCER INST INC

Ras inhibitors and uses thereof

ActiveUS20160046661A1Stop growthStop the spreadBiocideSugar derivativesDiseasePancreas Cancers

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.

Ras inhibitors and uses thereof

Ras inhibitors and uses thereof

Ras inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC

Neuroactive steroids, compositions, and uses thereof

ActiveUS10246482B2Reduces avoids symptom causeGood curative effectKetal steroidsSubstance abuserWithdrawal syndrome

Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Owner:SAGE THERAPEUTICS

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

ActiveUS9315472B2Good curative effectDelay moreOrganic chemistryHeterocyclic compound active ingredientsDiseaseHepatic Diseases

The present invention provides novel 1,3,5-triazinane-2,4,6-trione derivatives, such as compounds of any one of Formulae (I) and (II), and salts thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, or plasmid DNA). The present invention also provides methods and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and / or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, and lung diseases.

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

1,3,5-triazinane-2,4,6-trione derivatives and uses thereof

Owner:MASSACHUSETTS INST OF TECH

Janus kinase inhibitors and uses thereof

ActiveUS20170044111A1Decrease kinase activityReduced activityOrganic chemistryKinase activityMedicine

The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and / or treating and / or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and / or viral infection). (I) (II)

Janus kinase inhibitors and uses thereof

Janus kinase inhibitors and uses thereof

Janus kinase inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC

Compositions and methods for treating CNS disorders

InactiveUS20190177358A1Reduces avoids symptom causeGood curative effectOrganic active ingredientsNervous disorderDiseaseSedation

Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b 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.

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Owner:SAGE THERAPEUTICS

Compositions and methods for treating CNS disorders

ActiveUS20170240589A1Reduces avoids symptom causeGood curative effectOrganic active ingredientsNervous disorderDiseaseSedation

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b 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.

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Compositions and methods for treating CNS disorders

Owner:SAGE THERAPEUTICS

Hydrophobically tagged janus kinase inhibitors and uses thereof

ActiveUS20170044112A1Improve biological activityReduces avoids symptom causeOrganic chemistryAutoimmune diseaseKinase inhibition

The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and / or treating and / or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and / or viral infection).

Hydrophobically tagged janus kinase inhibitors and uses thereof

Hydrophobically tagged janus kinase inhibitors and uses thereof

Hydrophobically tagged janus kinase inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC

Hydrophobically tagged janus kinase inhibitors and uses thereof

ActiveUS9862688B2Reduces avoids symptom causeGood curative effectOrganic chemistryAutoimmune diseaseKinase inhibition

The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and / or treating and / or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and / or viral infection).

Hydrophobically tagged janus kinase inhibitors and uses thereof

Hydrophobically tagged janus kinase inhibitors and uses thereof

Hydrophobically tagged janus kinase inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC

Neuroactive steroids and methods of use thereof

InactiveUS20170305960A1Excellent propertyGood metabolic stabilityOrganic active ingredientsSenses disorderNeuroactive steroidStereochemistry

Compounds are provided according to Formula (I):and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.

Neuroactive steroids and methods of use thereof

Neuroactive steroids and methods of use thereof

Neuroactive steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

19-nor c3, 3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof

ActiveUS20160083417A1Eliminate potential for oxidationInhibit metabolismOrganic active ingredientsNervous disorderDiseaseSubstance abuser

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

19-nor c3, 3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof

19-nor c3, 3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof

19-nor c3, 3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof

Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

InactiveUS20170348327A1Reduce depressionRelieve symptomsOrganic active ingredientsNervous disorderEssential tremorPregnanolone

Described herein are methods of treating tremor, e.g., essential tremor; depression, e.g., postpostum depression; and anxiety disorder, the method comprising administering to a human subject suffering from tremor, e.g., essential tremor; depression, e.g., postpostum depression, an anxiety disorder with a neuroactive steroid or a composition comprising a neuroactive steroid (e.g., pregnanolone, allopregnanolone, alphadalone, ganaxolone, or alphaxolone).

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Neuroactive steroids, compositions, and uses thereof

Owner:SAGE THERAPEUTICS

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.

Stabilized polypeptides as regulators of RAB GTPase function

Stabilized polypeptides as regulators of RAB GTPase function

Stabilized polypeptides as regulators of RAB GTPase function

Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

Janus kinase inhibitors and uses thereof

ActiveUS10017477B2Reduces avoids symptom causeGood curative effectOrganic chemistryKinase activityAutoimmune disease

The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and / or treating and / or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and / or viral infection). (I) (II)

Janus kinase inhibitors and uses thereof

Janus kinase inhibitors and uses thereof

Janus kinase inhibitors and uses thereof

Owner:DANA FARBER CANCER INST INC

Multi-tailed lipids and uses thereof

ActiveUS20160158363A1Good curative effectDelay moreOrganic chemistrySpecial deliveryLipid formationDisease

The present invention provides multi-tailed lipid compounds, and salts and stereoisomers thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, plasmid DNA, small molecule, protein, peptide). The present invention also provides methods, and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and / or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases (e.g., liver diseases), respiratory diseases (e.g., lung diseases), painful conditions, psychiatric disorders, metabolic disorders, and spleen diseases.

Multi-tailed lipids and uses thereof

Multi-tailed lipids and uses thereof

Multi-tailed lipids and uses thereof

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.

Brush-arm star polymer imaging agents and uses thereof

Brush-arm star polymer imaging agents and uses thereof

Brush-arm star polymer imaging agents and uses thereof

Owner:MASSACHUSETTS INST OF TECH +1

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