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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 23. Отображено 23.
20-06-2017 дата публикации

Compositions and methods for modulating farnesoid X receptors

Номер: US0009682939B2

The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

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28-02-2019 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

Номер: US20190062283A1
Принадлежит:

The present invention relates to compounds of Formula I, 1. A method for preparing 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate , comprising contacting 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid in a solvent with meglumine in water solution under suitable conditions , thereby providing 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate.2. The method of claim 1 , comprising adding said meglumine in water solution to a suspension of said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid in acetone.3. The method of claim 1 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate has a dehydration point at about 71° C. by differential scanning calorimetry.4. The method of claim 1 , further comprising heating said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate at a temperature ranging from 60-90° C. under suitable conditions claim 1 , thereby providing a 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine salt.5. The method of claim 4 , comprising heating said 4-((N-benzyl-8-chloro-1-methyl-1 claim 4 ,4-dihydrochromeno[4 claim 4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate at about 80° C.6. The method of claim 5 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim 5 ,4-dihydrochromeno[4 claim 5 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine salt has a melting point of about 167.5° C. by differential scanning calorimetry.7. The method of claim 5 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim 5 ...

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12-03-2020 дата публикации

ANTIVIRAL PYRIDOPYRAZINEDIONE COMPOUNDS

Номер: US20200079772A1
Принадлежит:

The invention provides compounds of Formula (I) 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Cy is selected from phenyl claim 1 , pyridin-3-yl claim 1 , and cyclohexyl claim 1 , each of which is optionally substituted with 1 to 3 groups selected from halo claim 1 , CF claim 1 , and CN.5. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , halo claim 1 , methyl claim 1 , or halomethyl.7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris absent claim 1 , or Rrepresents one or two methyl groups.8. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CH— or —(CH)—.9. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is cyclopropyl substituted with a group selected from Calkyl claim 1 , oxo claim 1 , halo claim 1 , Calkoxy claim 1 , OH claim 1 , —SOR claim 1 , —SONR′R′ claim 1 , —SOR claim 1 , —S(═O)(═NR′)R claim 1 , —NR′SONR′R′ claim 1 , —NR′SOR claim 1 , —NR′R′ claim 1 , —OR claim 1 , —NR′COOR claim 1 , —C(O)NR′R′ claim 1 , and COOR′.11. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Cy is phenyl claim 1 , and is optionally substituted with 1 or 2 groups selected from halo claim 1 , CN claim 1 , OH claim 1 , Calkyl claim 1 , and Calkoxy.15. The compound according to claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , wherein Zand Zare not both H.16. The compound according to claim 14 , or a ...

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19-08-2021 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

Номер: US20210253534A1
Принадлежит:

The present invention relates to compounds of Formula I, 1. A crystalline form of 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid , produced by contacting 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid in a solvent with meglumine in water solution under suitable conditions.2. The crystalline form of claim 1 , produced by adding said meglumine in water solution to a suspension of said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid in acetone.3. The crystalline form of claim 1 , having a dehydration point at about 71° C. as determined by differential scanning calorimetry.4. The crystalline form of claim 1 , wherein said crystalline form is 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate.5. The crystalline form of claim 4 , produced by further heating said 4-((N-benzyl-8-chloro-1-methyl-1 claim 4 ,4-dihydrochromeno[4 claim 4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate at a temperature ranging from 60-90° C. under suitable conditions.6. The crystalline form of claim 5 , having a melting point of about 167.5° C. as determined by differential scanning calorimetry.7. The crystalline form of claim 4 , produced by adding said 4-((N-benzyl-8-chloro-1-methyl-1 claim 4 ,4-dihydrochromeno[4 claim 4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate to acetone in water solution; and heating reaction mixture at a temperature of about 50° C. under suitable conditions.8. The crystalline form of claim 7 , having a dehydration point at about 61° C. by differential scanning calorimetry.9. A crystalline form of 4-((N-benzyl-8-chloro-1-methyl-1 claim 7 ,4-dihydrochromeno[4 claim 7 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid claim 7 , produced by contacting 4-((N-benzyl-8- ...

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06-08-2020 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

Номер: US20200247757A1
Принадлежит:

The present invention relates to compounds of Formula I, 1. A method for preparing 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate , comprising contacting 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid in a solvent with meglumine in water solution under suitable conditions , thereby providing 4-((N-benzyl-8-chloro-1-methyl-1 ,4-dihydrochromeno[4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate.2. The method of claim 1 , comprising adding said meglumine in water solution to a suspension of said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido) methyl)benzoic acid in acetone.3. The method of claim 1 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate has a dehydration point at about 71° C. by differential scanning calorimetry.4. The method of claim 1 , further comprising heating said 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate at a temperature ranging from 60-90° C. under suitable conditions claim 1 , thereby providing a 4-((N-benzyl-8-chloro-1-methyl-1 claim 1 ,4-dihydrochromeno[4 claim 1 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine salt.5. The method of claim 4 , comprising heating said 4-((N-benzyl-8-chloro-1-methyl-1 claim 4 ,4-dihydrochromeno[4 claim 4 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate at about 80° C.6. The method of claim 5 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim 5 ,4-dihydrochromeno[4 claim 5 ,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine salt has a melting point of about 167.5° C. by differential scanning calorimetry.7. The method of claim 5 , wherein said 4-((N-benzyl-8-chloro-1-methyl-1 claim ...

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28-09-2017 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

Номер: US20170275256A1
Принадлежит:

The present invention relates to compounds of Formula I, 1. A compound selected from the group consisting of:4-fluoro-3-(2-(8-fluoro-N-(2-fluorobenzyl)-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)acetamido)benzoic acid L-arginine salt;4-fluoro-3-(2-(8-fluoro-N-(2-fluorobenzyl)-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)acetamido)benzoic acid sodium salt;4-fluoro-3-(2-(8-fluoro-N-(3-fluorobenzyl)-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)acetamido)benzoic acid L-arginine salt;4-fluoro-3-(2-(8-fluoro-N-(3-fluorobenzyl)-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)acetamido)benzoic acid L-lysine salt;4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid TRIS salt;4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine monohydrate; and4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid meglumine salt.2. A pharmaceutical composition comprising a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.3. A combination comprising a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof claim 1 , and a second therapeutic agent.4. A method for treating a condition mediated by farnesoid X receptors (FXR) in a subject suffering therefrom claim 1 , comprising administering to the subject a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof claim 1 , and optionally in combination with a second therapeutic agent.5. The method of claim 4 , wherein said condition mediated by FXR is a liver disease or a gastrointestinal disease.6. The method of claim 5 , wherein said condition mediated by FXR is a liver disease selected from intrahepatic cholestasis claim 5 , estrogen-induced cholestasis claim 5 , drug- ...

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18-10-2018 дата публикации

FUSED TRICYCLIC PYRAZOLE DERIVATIVES USEFUL FOR FARNESOID X RECEPTORS

Номер: US20180298018A1
Принадлежит:

The present invention relates to compounds of Formula I, 3. The compound according to claim 1 , wherein Lis *—(CRR)—; *—(CRR)—C(O)—NR—; *—(CRR)—O—; *—(CRR)—NR—SO—; *—(CRR)—NR—C(O)—; *—(CRR)—C(O)—NR—(CRR)—; or *—(CRR)—NR—C(O)—NR—(CRR)-1; wherein “*” indicates the point of attachment of Lto N.4. The compound according to claim 1 , wherein Ris Calkyl; Chaloalkyl; Chydroxyalkyl; or halo-substituted Chydroxyalkyl.5. The compound according to claim 1 , wherein Ris cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl; each of which is unsubstituted or substituted by 1-2 substituents independently represented by R; wherein Ris halo or hydroxyl.6. The compound according to claim 1 , wherein Ris tetrahydofuranyl claim 1 , tetrapyranyl claim 1 , N-methyl pyrazolyl claim 1 , thiazolyl or 1 claim 1 ,1-dioxidotetrahydrothiophen-3-yl.7. The compound according to claim 1 , wherein{'sup': 0', '6', '7', '4', '5', '4', '5', '4', '5', '4', '5', '4', '5, 'sub': 2', '2-3', '2, 'Ris phenyl optionally substituted with halo, —C(O)NRR; —S(O)—NRN; —C(O)O—(CRCR)NRR; —N(R)—C(O)O—R; —SOR; —NRRor —(CRR)—C(O)OR;'}{'sup': 4', '5', '6', '7', '6', '7, 'sub': '1-6', 'wherein R, R, R, Rand Rare independently hydrogen or Calkyl; alternatively Rand Rtogether with N may form morpholinyl.'}8. The compound according to claim 1 , wherein Ring B is phenyl optionally substituted with 1-2 halo; tetrahydropyranyl claim 1 , cyclopentyl claim 1 , cyclohexyl or thiazolyl.9. The compound according to claim 1 , wherein X is —(CRR)—; and Rand R claim 1 , are independently hydrogen or methyl.10. The compound according to claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , sec-butyl claim 1 , vinyl or cyclopropyl11. The compound according to selected from:2-(1-{8-chloro-1-methyl-1H,4H-chromeno[4,3-c]pyrazol-3-yl}-N-[(3-fluorophenyl)methyl]formamido)-N-(cyclopropylmethyl)acetamide;2-(1-{8-chloro-1-methyl-1H,4H-chromeno[4,3-c]pyrazol-3-yl}-N-[(3-fluorophenyl)methyl]formamido)-N-(3,3,3- ...

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24-11-2016 дата публикации

Compositions and methods for modulating farnesoid x receptors

Номер: US20160340317A1
Принадлежит: NOVARTIS AG

The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

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01-06-2021 дата публикации

Compositions and methods for modulating farnesoid X receptors

Номер: US11021446B2
Принадлежит: NOVARTIS AG

The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

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19-01-2023 дата публикации

Antiviral pyridopyrazinedione compounds

Номер: AU2022279408A1
Принадлежит: NOVARTIS AG

The invention provides compounds of Formula (I) R4 0 R2 R1 N Cy 0 H N 0 N4 W R3 as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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26-09-2022 дата публикации

Antiviral pyridopyrazinedione compounds

Номер: JP2022140642A
Принадлежит: NOVARTIS AG

【課題】 疾患の処置及び防止のための化合物を提供すること【解決手段】 本発明は明細書に記載の式(I)の化合物を薬学的に許容される塩と共に提供し、そのような化合物を含む医薬組成物並びにこれらの化合物、塩及び組成物をウイルス感染、特にヘルペスウイルスに引き起こされる感染を処置するために使用する方法を提供する。本発明は、ヘルペスウイルス複製の阻害剤であり、したがってヘルペスウイルス感染を処置するのに有用な新規の二環式ピリドン化合物に関する。化合物はサイトメガロウイルス(CMV)、単純ヘルペスウイルスなどを含む種々のヘルペスウイルスのウイルスDNAポリメラーゼを阻害する。本発明は本明細書に開示される新規二環式ピリドン化合物、そのような化合物を含有する医薬組成物並びにこれらの化合物及び組成物をヘルペスウイルス疾患の処置及び防止に使用する方法を提供する。【選択図】図1

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07-03-2024 дата публикации

Antiviral pyrazolopyridinone compounds

Номер: AU2020353055B2
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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07-03-2018 дата публикации

Fused tricyclic pyrazole derivatives useful for modulating farnesoid x receptors

Номер: EP3288948A1
Принадлежит: NOVARTIS AG

The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

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16-11-2023 дата публикации

Antiviral Pyrazolopiridinone Compounds

Номер: US20230365511A1
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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06-05-2021 дата публикации

Antiviral Pyrazolopyridinone Compounds

Номер: US20210130302A1
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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26-01-2023 дата публикации

Substituted pyridone compounds useful to treat orthomyxovirus infections

Номер: CA3227169A1
Принадлежит: NOVARTIS AG

The disclosure provides compounds of Formula (I): (I) as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.

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27-03-2024 дата публикации

抗ウイルスピラゾロピリジノン化合物

Номер: JP2024041852A
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

【課題】疾患を処置する方法を提供すること。 【解決手段】式(I)の化合物を、薬学的に許容される塩、そのような化合物を含有する医薬組成物、並びにウイルス感染症、特にヘルペスウイルスによって引き起こされる感染症を治療するためのこれらの化合物、塩、及び組成物を使用するための方法と一緒に提供する。本発明は、ヘルペスウイルス複製の阻害剤であり、したがって、ヘルペスウイルス感染症を治療するのに有用である、新規の二環式ピラゾロピリジオン(pyrazolopyridione)化合物に関する。この化合物は、サイトメガロウイルス(cytomegalovirus:CMV)及び単純ヘルペスウイルスなどを含む、様々なヘルペスウイルスのウイルスDNAポリメラーゼを阻害する。 【選択図】なし

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29-05-2024 дата публикации

Substituted pyridone compounds useful to treat orthomyxovirus infections

Номер: EP4373809A1
Принадлежит: NOVARTIS AG

The disclosure provides compounds of Formula (I): (I) as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.

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07-12-2023 дата публикации

Antiviral naphthyridinone compounds

Номер: WO2023154905A8
Принадлежит: Gilead Sciences, Inc., NOVARTIS AG

The disclosure provides compounds of Formulae (I) or (II), or a pharmaceutically acceptable salt thereof, (I), or (II) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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08-02-2024 дата публикации

Substituted pyridone compounds useful to treat orthomyxovirus infections

Номер: AU2022313600A1
Принадлежит: NOVARTIS AG

The disclosure provides compounds of Formula (I): (I) as further described herein, as well as pharmaceutical compositions comprising such compounds, and methods to use the compounds and pharmaceutical compositions for treatment of certain viral disorders, including influenza.

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27-06-2024 дата публикации

Antiviral pyrazolopyridinone compounds

Номер: AU2024203782A1
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

The invention provides compounds of formula (1) as described herein, along with pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds and salts, and methods of using said compounds, salts and compositions in the treatment of viral infections, particularly herpesvirus infections.

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15-05-2024 дата публикации

Compuestos antivirales de pirazolopiridinona

Номер: AR128504A1
Принадлежит: Gilead Sciences Inc, NOVARTIS AG

La descripción proporciona compuestos de la fórmula (1) o (2), o una sal farmacéuticamente aceptable de este, como se describe en la presente descripción, junto con sales farmacéuticamente aceptables, composiciones farmacéuticas que contienen tales compuestos, y métodos para usar estos compuestos, sales y composiciones para tratar infecciones virales, particularmente infecciones causadas por el herpesvirus.

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15-08-2024 дата публикации

Antiviral pyridopyrazinedione compounds

Номер: AU2024205050A1
Принадлежит: NOVARTIS AG

The invention provides compounds of Formula (I) R4 0 R2 R1 N Cy 0 H N 0 N4 W R3 as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

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