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Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Применить Всего найдено 11. Отображено 11.
06-07-2017 дата публикации

PRIMARY AMINES AND DERIVITVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20170189381A1
Принадлежит:

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 152.-. (canceled)53. A method for modulating an activity of a 5-HTserotonin receptor by contacting the receptor with N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , comprising administering to an individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.54. A method for treating a 5-HTassociated disorder in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.55. The method according to claim 54 , wherein said 5-HTassociated disorder is a sleep disorder.56. The method according to claim 54 , wherein said 5-HTassociated disorder is progressive multifocal leukoencephalopathy.57. The method according to claim 54 , wherein said 5-HTassociated disorder is hypertension.58. The method according to claim 54 , wherein said 5-HTassociated disorder is pain.59. The method according to claim 54 , wherein said 5-HTassociated disorder is claudication.60. The method according to claim 54 , wherein said 5-HTassociated disorder is peripheral artery disease.61. The method according to claim 54 , wherein said 5-HTassociated disorder is vasoconstriction.62. The method according to claim 54 , wherein said 5-HTassociated disorder is vasospasm.63. The method according to claim 54 , wherein said 5-HTassociated disorder is thrombosis.64. (canceled)65. The method of claim 54 , wherein the individual has coronary artery disease claim 54 , myocardial infarction claim 54 , transient ischemic attack claim 54 , angina claim 54 , ...

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22-11-2012 дата публикации

ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20120295938A1
Принадлежит:

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together. 3. The compound according to claim 1 , wherein V is O.4. The compound according to claim 1 , wherein W is —CHCH— optionally substituted with 1 to 2 substituents selected independently from the group consisting of Calkyl and oxo.5. The compound according to claim 1 , wherein W is —CHCH—CHC(CH)or —CHC(═O)—.6. The compound according to claim 1 , wherein Z is absent.7. The compound according to claim 1 , wherein Z is —CH— or —CHCH—.8. The compound according to claim 1 , wherein Ris Calkyl.9. The compound according to claim 1 , wherein Ris —CH.10. The compound according to claim 1 , wherein Ris H.11. The compound according to claim 1 , wherein Ris H claim 1 , Cl claim 1 , or Br.12. The compound according to claim 1 , wherein Q is —NRR.13. The compound according to claim 12 , wherein Ris H.14. The compound according to claim 12 , wherein Ris Cacyl claim 12 , or carbo-C-alkoxy each optionally substituted with 1 claim 12 , ...

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07-03-2019 дата публикации

PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20190070149A1
Принадлежит:

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 3. The process according to claim 1 , wherein X is O and V is O.4. The process according to claim 1 , wherein W is —CHCH— optionally substituted with 1 to 2 substituents selected independently from the group consisting of Calkyl claim 1 , Ccycloalkyl claim 1 , Chaloalkyl claim 1 , oxo and imino claim 1 , wherein said Calkyl is optionally substituted with Calkylsulfonyl.5. The process according to claim 1 , wherein W is —CHCH—.6. The process according to claim 1 , wherein Z is absent.7. The process according to claim 1 , wherein Z is —CH— or —CHCH— each optionally substituted with 1 or 2 substituents selected independently from the group consisting of Calkoxy and oxo.8. The process according to claim 1 , wherein Ris Calkyl.9. The process according to claim 1 , wherein Ris —CH.10. The process according to claim 1 , wherein Ris H.11. The process according to claim 1 , wherein Ris H claim 1 , Cl claim 1 , or Br.12. The process according to claim 1 , wherein Rand Rare both H.13. The process according to claim 1 , wherein Ris H claim 1 , and Ris{'sub': '1-12', 'Cacyl.'}14. The process according to claim 1 , wherein Ris H claim 1 , and Ris{'sub': '1-6', 'carbo-C-alkoxy.'}15. The process according to claim 1 , wherein Ris H claim 1 , and Ris —C(═O)OCRROC(═O)R claim 1 , wherein R claim 1 , Rand Rare each independently selected from H or CH.16. The process according to claim 1 , wherein R claim 1 , R claim 1 , and Rare each H.17. The process according to claim 1 , wherein Ris aryl optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 substituents selected independently from the group consisting of Cacyl claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Calkylcarboxamide claim 1 , Cdialkylamino claim 1 , cyano claim 1 , Ccycloalkyloxy claim 1 , halogen claim 1 , Chaloalkoxy claim 1 , Chaloalkyl claim 1 , ...

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12-06-2014 дата публикации

ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT 2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20140163032A1
Принадлежит: ARENA PHARMACEUTICALS, INC.

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 3. The compound according to or , wherein V is O.4. The compound according to any one of to , wherein W is —CHCH— optionally substituted with 1 to 2 substituents selected independently from the group consisting of Calkyl and oxo.5. The compound according to any one of to , wherein W is —CHCH— , —CHC(CH)— , or —CHC(═O)—.6. The compound according to any one of to , wherein Z is absent.7. The compound according to any one of to , wherein Z is —CH— or —CHCH—.8. The compound according to any one of to , wherein Ris Calkyl.9. The compound according to any one of to , wherein Ris —CH.10. The compound according to any one of to , wherein Ris H.11. The compound according to any one of to , wherein Ris H , Cl , or Br.12. The compound according to any one of to , wherein Q is —NRR.13. The compound according to claim 12 , wherein Ris H claim 12 ,14. The compound according to claim 12 , wherein Ris Cacyl claim 12 , or carbo-C-alkoxy each optionally substituted with 1 claim 12 , 2 claim 12 , 3 claim 12 , 4 claim 12 , or 5 substituents selected independently from the group consisting of Cacyloxy claim 12 , Calkylcarboxamide claim 12 , amino claim 12 , Calkylamino claim 12 , Cdialkylamino claim 12 , Calkylimino claim 12 , Calkylsulfinyl claim 12 , Calkylsulfonyl claim 12 , Calkylthio claim 12 , halogen claim 12 , nitro claim 12 , and phenyl.15. The compound according to any one of to claim 12 , wherein Ris Calkyl claim 12 , Ccycloalkyl claim 12 , Chaloalkyl claim 12 , heterocyclyl claim 12 , or heteroaryl claim 12 , and each is optionally substituted with 1 claim 12 , 2 claim 12 , 3 claim 12 , 4 claim 12 , or 5 substituents selected independently from the group consisting of Calkoxy claim 12 , Calkyl claim 12 , Calkylsulfonyl claim 12 , amino claim 12 , carbo-C-alkoxy claim 12 , carboxamide claim 12 , cyano claim 12 , ...

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21-08-2014 дата публикации

PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20140235622A1
Принадлежит: ARENA PHARMACEUTICALS, INC.

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 3. The method according to claim 1 , wherein X is O and V is O.4. The method according to claim 1 , wherein W is —CHCH— optionally substituted with 1 to 2 substituents selected independently from the group consisting of Calkyl claim 1 , Ccycloalkyl claim 1 , Chaloalkyl claim 1 , oxo and imino claim 1 , wherein said Calkyl is optionally substituted with Calkylsulfonyl.5. The method according to claim 1 , wherein W is —CHCH—.6. The method according to claim 1 , wherein Z is absent.7. The method according to claim 1 , wherein Z is —CH— or —CHCH— each optionally substituted with 1 or 2 substituents selected independently from the group consisting of Calkoxy and oxo.8. The method according to claim 1 , wherein Ris Calkyl.9. The method according to wherein Ris —CH.10. The method according to claim 1 , wherein Ris H.11. The method according to claim 1 , wherein Ris H claim 1 , Cl claim 1 , or Br.12. The method according to claim 1 , wherein Rand Rare both H.13. The method according to claim 1 , wherein Ris H claim 1 , and Ris Cacyl.14. The method according to claim 1 , wherein Ris H claim 1 , and Ris carbo-C-alkoxy.15. The method according to claim 1 , wherein Ris H claim 1 , and Ris —CO(═O)CRROC(═O)R claim 1 , wherein R claim 1 , Rand Rare each independently selected from H or CH.16. The method according to claim 1 , wherein R claim 1 , R claim 1 , and Rare each H.17. The method according to claim 1 , wherein Ris aryl optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 substituents selected independently from the group consisting of Cacyl claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Calkylcarboxamide claim 1 , Cdialkylamino claim 1 , cyano claim 1 , Ccycloalkyloxy claim 1 , halogen claim 1 , Chaloalkoxy claim 1 , Chaloalkyl claim 1 , and heteroaryl claim 1 , wherein said Calkyl is optionally ...

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25-06-2015 дата публикации

ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT 2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20150174102A1
Принадлежит:

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 146-. (canceled)47. A method for modulating the activity of a 5-HTserotonin receptor by contacting the receptor with N-[4-[2-(2-hydroxy-ethylamino)-ethoxy]-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof , comprising administering to an individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-[2-(2-hydroxy-ethylamino)-ethoxy]-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.48. A method for treating a 5-HTserotonin associated disorder in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-[2-(2-hydroxy-ethylamino)-ethoxy]-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.49. The method according to claim 48 , wherein said 5-HTmediated disorder is sleep disorder.50. The method according to claim 48 , wherein said 5-HTmediated disorder is progressive multifocal leukoencephalopathy.51. The method according to claim 48 , wherein said 5-HTmediated disorder is hypertension.52. The method according to claim 48 , wherein said 5-HTmediated disorder is pain.53. The method according to claim 48 , wherein said 5-HTmediated disorder is claudication.54. The method according to claim 48 , wherein said 5-HTmediated disorder is peripheral artery disease.55. The method according to claim 48 , wherein said 5-HTmediated disorder is vasoconstriction.56. The method according to claim 48 , wherein said 5-HTmediated disorder is vasospasm.57. The method according to claim 48 , wherein said 5-HTmediated disorder is thrombosis.58. A method for reducing platelet aggregation in an individual comprising administering to the individual ...

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24-09-2015 дата публикации

PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Номер: US20150265576A1
Принадлежит:

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. 152.-. (canceled)53. A method for modulating an activity of a 5-HTserotonin receptor by contacting the receptor with N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , comprising administering to an individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.54. A method for treating a 5-HTassociated disorder in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3-(2-methyl-2H-pyrazol-3-yl)-phenyl]-3-methoxy-benzamide , or a pharmaceutically acceptable salt thereof.55. The method according to claim 54 , wherein said 5-HTmediated disorder is a sleep disorder.56. The method according to claim 54 , wherein said 5-HTmediated disorder is progressive multifocal leukoencephalopathy.57. The method according to claim 54 , wherein said 5-HTmediated disorder is hypertension.58. The method according to claim 54 , wherein said 5-HTmediated disorder is pain.59. The method according to claim 54 , wherein said 5-HTmediated disorder is claudication.60. The method according to claim 54 , wherein said 5-HTmediated disorder is peripheral artery disease.61. The method according to claim 54 , wherein said 5-HTmediated disorder is vasoconstriction.62. The method according to claim 54 , wherein said 5-HTmediated disorder is vasospasm.63. The method according to claim 54 , wherein said 5-HTmediated disorder is thrombosis.64. A method for reducing platelet aggregation in an individual comprising administering to the individual in need thereof a therapeutically effective amount of an isolated compound that is N-[4-(2-amino-ethoxy)-3 ...

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06-08-2020 дата публикации

Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto

Номер: US20200247755A1
Принадлежит: Arena Pharmaceuticals Inc

The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

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13-01-2015 дата публикации

Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Номер: USRE45336E1
Принадлежит: Arena Pharmaceuticals Inc

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

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05-06-2018 дата публикации

Primary amines and derivitves thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Номер: US09987252B2
Принадлежит: Arena Pharmaceuticals Inc

The present invention pertains to certain compounds of Formula (Ia), and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infraction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

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03-05-2016 дата публикации

Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Номер: US09328107B2
Принадлежит: Arena Pharmaceuticals Inc

The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

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