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52 results about "Monoacylglycerol lipase" patented technology

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Monoacylglycerol lipase, also known as MAG lipase, MAGL, MGL or MGLL is a protein that, in humans, is encoded by the MGLL gene. MAGL is a 33-kDa, membrane-associated member of the serine hydrolase superfamily and contains the classical GXSXG consensus sequence common to most serine hydrolases. The catalytic triad has been identified as Ser122, His269, and Asp239.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100331300A1Antibacterial agentsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Methods and compositions related to targeting monoacylglycerol lipase

InactiveUS20110275650A1Strong inhibitory activityHigh selectivityBiocideSenses disorder2-ArachidonoylglycerolEndogenous cannabinoid

This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.

Methods and compositions related to targeting monoacylglycerol lipase

Methods and compositions related to targeting monoacylglycerol lipase

Methods and compositions related to targeting monoacylglycerol lipase

Owner:THE SCRIPPS RES INST

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100324011A1Antibacterial agentsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

ActiveUS8415341B2BiocideOrganic active ingredientsDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, r, R2 and Z are defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

InactiveUS20120077797A1BiocideOrganic active ingredientsDiseaseEnantiomer

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows:wherein Y, Z, and n are defined herein; andwherein Yb and Zb are as defined herein.

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

ActiveUS20160318864A1Superior MAGL inhibitory actionNervous disorderOrganic chemistryHuntingtons choreaDepressant

The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative diseases (e.g., Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis and the like), anxiety disorder, pain (e.g., inflammatory pain, carcinomatous pain, nervous pain and the like), epilepsy and the like. The present invention relates to a compound represented by the formula (I):wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

Owner:TAKEDA PHARMACEUTICALS CO LTD

Methods and compositions related to targeting monoacylglycerol lipase

InactiveUS8772318B2BiocideSenses disorderPharmaceutical medicineCell biology

This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.

Methods and compositions related to targeting monoacylglycerol lipase

Methods and compositions related to targeting monoacylglycerol lipase

Methods and compositions related to targeting monoacylglycerol lipase

Owner:THE SCRIPPS RES INST

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100324014A1Antibacterial agentsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

ActiveUS20100324015A1BiocideOrganic active ingredientsMedicinal chemistryDisease cause

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, r, R2 and Z are defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

InactiveUS20120058986A1BiocideOrganic active ingredientsDiseaseMedicinal chemistry

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Q and Z are defined herein.

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100331299A1Antibacterial agentsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

ActiveUS8513423B2Organic active ingredientsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows:wherein Y, Z, and R are defined herein.

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100324013A1Antibacterial agentsOrganic active ingredientsDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Azetidinyl diamides as monoacylglycerol lipase inhibitors

ActiveUS20100324012A1Antibacterial agentsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, Z, R1, and s are defined herein.

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Azetidinyl diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

InactiveCN103080103AOrganic active ingredientsNervous disorderDiseaseEnantiomer

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (la) and Formula (lb) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

ActiveUS20130102584A1Organic active ingredientsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows:wherein Y, Z, and R are defined herein.

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

ActiveUS20100324016A1Organic active ingredientsBiocideDiseaseMonoacylglycerol lipase

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows:wherein R1, W andare defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors

InactiveUS20110166138A1Compound screeningBiocideCannabinoid receptorFatty acid

Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.

Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors

Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors

Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors

Owner:NORTHEASTERN UNIV

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

ActiveUS8435977B2Organic active ingredientsBiocideDiseaseMonoacylglycerol lipase

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows:wherein R1, W andare defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

ActiveUS20130196969A1Organic active ingredientsBiocideDiseaseLipase inhibitors

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Q and Z are defined herein.

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

ActiveUS20130196968A1BiocideOrganic active ingredientsDiseaseLipase inhibitors

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows:wherein Q and Z are defined herein.

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof

ActiveUS10570146B2Slow degradationReduce inactivationOrganic active ingredientsOrganic chemistryCarbamateDepressant

Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH / MAGL. More particularly, compounds of formula IIhave utility in a variety of therapeutic uses such as treatment of pain, inflammation, neuropathy, or appetite disorder.

Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof

Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof

Urea/carbamates FAAH MAGL or dual FAAH/MAGL inhibitors and uses thereof

Owner:NORTHEASTERN UNIV

Piperidin-4-yl-zetidine diamides as monoacylglycerol lipase inhibitors

InactiveCN103260703AOrganic active ingredientsNervous disorderDiseaseEnantiomer

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: Formula (I), wherein Y, Z, and R are defined herein.

Piperidin-4-yl-zetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-zetidine diamides as monoacylglycerol lipase inhibitors

Piperidin-4-yl-zetidine diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

ActiveUS9624170B2Superior MAGL inhibitory actionNervous disorderOrganic chemistryHuntingtons choreaDepressant

The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative diseases (e.g., Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis and the like), anxiety disorder, pain (e.g., inflammatory pain, carcinomatous pain, nervous pain and the like), epilepsy and the like. The present invention relates to a compound represented by the formula (I):wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (MAGL) inhibitors

Owner:TAKEDA PHARMA CO LTD

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

ActiveUS20130184251A1Organic active ingredientsBiocideDiseaseGlycerol

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows:wherein Y, r, R2 and Z are defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Urea/carbamates faah magl or dual faah/magl inhibitors and uses thereof

ActiveUS20170247387A1Slow degradationReduce inactivationOrganic chemistryAmidohydrolaseMonoacylglycerol lipase

Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH / MAGL.

Urea/carbamates faah magl or dual faah/magl inhibitors and uses thereof

Urea/carbamates faah magl or dual faah/magl inhibitors and uses thereof

Urea/carbamates faah magl or dual faah/magl inhibitors and uses thereof

Owner:NORTHEASTERN UNIV

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitor

InactiveCN102548983AOrganic active ingredientsNervous disorderDiseaseMedicinal chemistry

Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I), wherein Y, r, R2 and Z are defined herein.

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitor

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitor

Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitor

Owner:JANSSEN PHARMA NV

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

InactiveUS8637498B2BiocideNervous disorderDiseaseEnantiomer

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows:wherein Y, Z, and n are defined herein; andwherein Yb and Zb are as defined herein.

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors

ActiveUS8575363B2BiocideNervous disorderDiseaseEnantiomer

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows:wherein Y, Z, and R1, and R2 are defined herein.

Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors

Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors

Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors

Owner:JANSSEN PHARMA NV

Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors

InactiveUS9271962B2Compound screeningBiocideFatty acidAmidohydrolase

Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.

Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors

Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors

Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors

Owner:NORTHEASTERN UNIV

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