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公开(公告)号:US09737505B2
公开(公告)日:2017-08-22
申请号:US14925350
申请日:2015-10-28
Inventor: Alexis Denis , Olivier Mirguet , Jérôme Toum
IPC: A61K31/4025 , A61K39/395 , C07D405/14 , A61K45/06
CPC classification number: A61K31/4025 , A61K39/3955 , A61K45/06 , C07D405/14 , A61K2300/00
Abstract: The compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate) possesses physicochemical properties suitable for pharmaceutical development and is capable of generating (R)-1-[6-[(R)-2-carboxy-pyrrolidin-1-yl]-6-oxo-hexanoyl]pyrrolidine-2-carboxylic acid (CPHPC) in quantities capable of depleting serum amyloid P component (SAP) efficiently following oral administration, making it useful in the treatment of amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
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公开(公告)号:US10246447B2
公开(公告)日:2019-04-02
申请号:US15574947
申请日:2016-05-19
Inventor: Anne Marie Jeanne Bouillot , Alexis Denis , John Liddle , Olivier Mirguet , Ann Louise Walker
IPC: C07D413/12
Abstract: Compounds of formula (I) wherein: R1 is heteroaryl optionally substituted by methyl, ethyl, halo or ═O; and R2 is H, methyl or ethyl. and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel disease, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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公开(公告)号:US20180099955A1
公开(公告)日:2018-04-12
申请号:US15837297
申请日:2017-12-11
Inventor: Alexis Denis , Olivier Mirguet , Jérôme Toum
IPC: C07D405/14 , A61K39/395 , A61K9/00 , A61K31/4025 , A61K39/00
Abstract: The present invention relates to the compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
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公开(公告)号:US09701668B2
公开(公告)日:2017-07-11
申请号:US14787608
申请日:2015-04-27
Inventor: Alexis Denis , Olivier Mirguet , Jérôme Toum
IPC: C07D405/14 , A61K31/4025 , A61K9/00 , A61K39/395 , A61K39/00
CPC classification number: C07D405/14 , A61K9/0053 , A61K31/4025 , A61K39/3955 , A61K2039/505
Abstract: The present invention relates to the compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate) of formula (I), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
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公开(公告)号:US10328052B2
公开(公告)日:2019-06-25
申请号:US15771442
申请日:2016-10-25
Inventor: Alexis Denis , Olivier Mirguet , Jérôme Toum
IPC: C07D405/14 , A61K31/4025 , A61K39/395
Abstract: The present invention relates to the compound ((2R,2′R)-bis(((tetrahydro-2H-pyran-4-carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
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公开(公告)号:US20180170921A1
公开(公告)日:2018-06-21
申请号:US15900043
申请日:2018-02-20
Inventor: Anne Marie Jeanne BOUILLOT , Alexis Denis , John Liddle , Ann Louise Walker
IPC: C07D413/12
CPC classification number: C07D413/12
Abstract: The present invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, which are Kynurenine monooxygenase (KMO) inhibitors, which are useful in the treatment of various disorders, which may include, but are not limited to, for diseases such as, for example: acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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公开(公告)号:US09932328B2
公开(公告)日:2018-04-03
申请号:US15537805
申请日:2015-12-17
Inventor: Anne Marie Jeanne Bouillot , Alexis Denis , Ann Louise Walker , John Liddle
IPC: A61K31/416 , C07D413/12
CPC classification number: C07D413/12
Abstract: Compound of formula (I) wherein: R1 is heteroaryl either unsubstituted or substituted by methyl, ethyl, halo or ═O; and R2 is H, methyl or ethyl; and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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公开(公告)号:US10597385B2
公开(公告)日:2020-03-24
申请号:US15837297
申请日:2017-12-11
Inventor: Alexis Denis , Olivier Mirguet , Jérôme Toum
IPC: A61K31/4025 , C07D405/14 , A61K9/00 , A61K39/395 , A61K39/00
Abstract: The present invention relates to the compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
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公开(公告)号:US10273232B2
公开(公告)日:2019-04-30
申请号:US15900043
申请日:2018-02-20
Inventor: Anne Marie Jeanne Bouillot , Alexis Denis , John Liddle , Ann Louise Walker
IPC: C07D413/12
Abstract: The present invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, which are Kynurenine monooxygenase (KMO) inhibitors, which are useful in the treatment of various disorders, which may include, but are not limited to, for diseases such as, for example: acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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公开(公告)号:US20190100517A1
公开(公告)日:2019-04-04
申请号:US16207745
申请日:2018-12-03
Inventor: Anne Marie Jeanne Bouillot , Alexis Denis , John Liddle , Ann Louise Walker
IPC: C07D417/12
Abstract: Compounds of formula (I) wherein: R1 is heteroaryl optionally substituted by methyl, ethyl, halo or ═O; and R2 is H, methyl or ethyl. and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel disease, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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