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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

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Owner:SAGE THERAPEUTICS

Methods and compositions for reducing body fat and adipocytes

ActiveUS8426471B1Improve propertiesEnhance pharmaceuticallyCosmetic preparationsBiocideReducing bodiesProdrug

Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I):or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, and R4 are as defined herein.

Methods and compositions for reducing body fat and adipocytes

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Owner:TOPOKINE 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

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

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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.

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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

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Owner:SAGE THERAPEUTICS

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.

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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

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Owner:SAGE THERAPEUTICS

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

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Owner:SAGE THERAPEUTICS

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.

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Owner:SAGE THERAPEUTICS

Methods and compositions for reducing body fat and adipocytes

ActiveUS20130178525A1Improve propertiesEnhance pharmaceuticallyBiocideCosmetic preparationsReducing bodiesProdrug

Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and / or (V):or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7′, Z, Y, n, y, and x, are as defined herein.

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Owner:TOPOKINE THERAPEUTICS

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

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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.

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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.

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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

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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).

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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

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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.

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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).

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Owner:SAGE THERAPEUTICS

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)

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Owner:DANA FARBER CANCER INST INC

19-nor neuroactive steroids and methods of use thereof

ActiveUS20170233432A1Eliminate potential for oxidationImprove bioavailabilityNervous disorderEstrane derivativesWithdrawal 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, status epilepticus.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

ActiveUS20180037602A1Optimal chemical reactivity and biological activityReduces avoids symptom causeOrganic active ingredientsNervous disorderGABA ModulatorsSedation

Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

ActiveUS10329320B2Reduces avoids symptom causeGood curative effectOrganic active ingredientsNervous disorderSedationNeuroactive steroid

Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such for inducing sedation and / or anesthesia.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

ActiveUS20180215779A1Reduces avoids symptom causeGood curative effectOrganic active ingredientsNervous disorderSedationNeuroactive steroid

Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1a and R1b 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.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

ActiveUS20170247406A1Reduces 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.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

PendingUS20180179247A1Eliminate potential for oxidationInhibit metabolismOrganic active ingredientsNervous disorderWithdrawal syndromeSubstance abuse disorder

Provided herein are 19-nor C3, 3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined herein, and A is a heteroaryl ring system comprising 3 or 4 nitrogens 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.

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Owner:SAGE THERAPEUTICS

Neuroactive steroids, compositions, and uses thereof

InactiveUS20160152658A1Convenient treatmentGood curative effectOrganic active ingredientsNervous disorderSedationNeuroactive steroid

Described herein are neuroactive steroids of the Formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof; wherein R1a and R1b 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.

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Owner:SAGE THERAPEUTICS

(hetero)arylamide compound for inhibiting protein kinase activity

ActiveUS20190382374A1Superior kinase inhibitory activityEliminate side effectsCompounds screening/testingOrganic chemistryStereoisomerismInhibitory effect

Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition comprising the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase for preparing a plurality of drugs comprising an anti-tumour drug.