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公开(公告)号：US20240300969A1
公开(公告)日：2024-09-12
申请号：US18409959
申请日：2024-01-11
发明人： Scott Duncan , Tarek A. Zeidan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号： C07D491/113 , A61K31/4015 , C07C229/12 , C07C229/18 , C07C317/18 , C07C317/28 , C07D207/12 , C07D207/40 , C07D207/408 , C07D211/92 , C07D295/088
CPC分类号： C07D491/113 , A61K31/4015 , C07C229/12 , C07C229/18 , C07C317/18 , C07C317/28 , C07D207/12 , C07D207/40 , C07D207/408 , C07D211/92 , C07D295/088
摘要： The present invention provides compounds of formula (I),
wherein:
R1 is unsubstituted C1-C6 alkyl;
La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and
R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl;
or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.-
2.发明公开公开(公告)号：US20240245676A1
公开(公告)日：2024-07-25
申请号：US18543767
申请日：2023-12-18
IPC分类号： A61K31/496 , A61K31/00 , C07D401/12
CPC分类号： A61K31/496 , A61K31/00 , C07D401/12
摘要： Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
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公开(公告)号：US20240091237A1
公开(公告)日：2024-03-21
申请号：US18510590
申请日：2023-11-15
IPC分类号： A61K31/5513 , A61K9/20 , A61K9/24 , A61K31/485
CPC分类号： A61K31/5513 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/2095 , A61K31/485
摘要： Described herein, in part, are tablets, such as immediate release multi-layer or bilayer tablets for orally delivering olanzapine and samidorphan, methods of using said tablets in the treatment of disorders described herein, and kits comprising said tablets.
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公开(公告)号：US11905298B2
公开(公告)日：2024-02-20
申请号：US17547118
申请日：2021-12-09
发明人： Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号： C07C229/12 , C07D491/113 , A61K31/4015 , C07D207/40 , C07D207/12 , C07D207/408 , C07D211/92 , C07D295/088 , C07C229/18 , C07C317/18 , C07C317/28
CPC分类号： C07D491/113 , A61K31/4015 , C07C229/12 , C07C229/18 , C07C317/18 , C07C317/28 , C07D207/12 , C07D207/40 , C07D207/408 , C07D211/92 , C07D295/088
摘要： The present invention provides compounds of formula (I), wherein:
R1 is unsubstituted C1-C6 alkyl;
La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and
R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10aryl;
or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.-
公开(公告)号：US11883394B2
公开(公告)日：2024-01-30
申请号：US17211352
申请日：2021-03-24
IPC分类号： A61K31/496 , C07D401/12 , A61K31/00
CPC分类号： A61K31/496 , A61K31/00 , C07D401/12
摘要： Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
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公开(公告)号：US20230158017A1
公开(公告)日：2023-05-25
申请号：US18056975
申请日：2022-11-18
IPC分类号： A61K31/485 , C07D211/62 , C07D217/04 , C07D221/22 , C07D221/28 , C07D223/04 , C07D401/12 , C07D405/12 , C07D489/00 , C07D489/09
CPC分类号： A61K31/485 , C07D211/62 , C07D217/04 , C07D221/22 , C07D221/28 , C07D223/04 , C07D401/12 , C07D405/12 , C07D489/00 , C07D489/09
摘要： The present application relates methods for treating a depressive symptom comprising administering an effective amount of a μ opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.
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公开(公告)号：US20230150941A1
公开(公告)日：2023-05-18
申请号：US18051216
申请日：2022-10-31
IPC分类号： C07D215/227 , A61K31/497 , C07D263/58 , C07D401/12 , C07D417/12 , C07D471/04 , C07F9/6558 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/14 , A61K31/496 , C07D215/22
CPC分类号： C07D215/227 , A61K31/497 , C07D263/58 , C07D401/12 , C07D417/12 , C07D471/04 , C07F9/65583 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/14 , C07F9/6558 , A61K31/496 , C07D215/22 , C07D241/04
摘要： Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
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公开(公告)号：US20220401426A1
公开(公告)日：2022-12-22
申请号：US17808234
申请日：2022-06-22
发明人： Sean Cunningham , Seamus Mulligan , Michael Myers
摘要： A pharmaceutical composition which comprises therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hour or more and the use of the composition to treat various neurological diseases.
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公开(公告)号：US11518745B2
公开(公告)日：2022-12-06
申请号：US17020499
申请日：2020-09-14
IPC分类号： C07D215/227 , A61K31/497 , C07D263/58 , C07D401/12 , C07D417/12 , C07D471/04 , C07F9/6558 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/14 , A61K31/496 , C07D215/22 , C07D241/04
摘要： Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
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公开(公告)号：US20220280502A1
公开(公告)日：2022-09-08
申请号：US17505896
申请日：2021-10-20
发明人： Daniel R. Deaver , Mark Todtenkopf
IPC分类号： A61K31/485 , A61K31/439 , A61K31/496 , A61K31/519 , A61K31/5513 , A61K31/554 , C07D221/28 , C07D405/06 , A61K9/20 , A61K31/551
摘要： The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
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