AR080490A1 - FORMAS CRISTALINAS DE UN INHIBIDOR DE ELASTASA NEUTROFILA, COMPOSICIoN FARMACEUTICA QUE LAS COMPRENDE Y SU USO EN LA FABRICACION DE UN MEDICAMENTO PARA EL TRATAMIENTO DE LA DEFICIENCIA DE ALFA-1-ANTITRIPSINA - Google Patents
FORMAS CRISTALINAS DE UN INHIBIDOR DE ELASTASA NEUTROFILA, COMPOSICIoN FARMACEUTICA QUE LAS COMPRENDE Y SU USO EN LA FABRICACION DE UN MEDICAMENTO PARA EL TRATAMIENTO DE LA DEFICIENCIA DE ALFA-1-ANTITRIPSINAInfo
- Publication number
- AR080490A1 AR080490A1 ARP110100754A ARP110100754A AR080490A1 AR 080490 A1 AR080490 A1 AR 080490A1 AR P110100754 A ARP110100754 A AR P110100754A AR P110100754 A ARP110100754 A AR P110100754A AR 080490 A1 AR080490 A1 AR 080490A1
- Authority
- AR
- Argentina
- Prior art keywords
- neutrofila
- elastasa
- antitripsin
- alfa
- inhibitor
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000013078 crystal Substances 0.000 title 1
- 230000007812 deficiency Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 150000001875 compounds Chemical group 0.000 abstract 4
- -1 3-trifluoromethylphenyl Chemical group 0.000 abstract 2
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 abstract 2
- JLLYLQLDYORLBB-UHFFFAOYSA-N 5-bromo-n-methylthiophene-2-sulfonamide Chemical compound CNS(=O)(=O)C1=CC=C(Br)S1 JLLYLQLDYORLBB-UHFFFAOYSA-N 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- 230000005855 radiation Effects 0.000 abstract 2
- OJVSGRDEFLGKTN-UHFFFAOYSA-N CC1=C(N=CC(=O)N1C2=CC=CC(=C2)C(F)(F)F)C3=CC=NN3C4=CC=C(C=C4)C#N Chemical compound CC1=C(N=CC(=O)N1C2=CC=CC(=C2)C(F)(F)F)C3=CC=NN3C4=CC=C(C=C4)C#N OJVSGRDEFLGKTN-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen formas cristalinas de la etilamida del ácido 6-[2-(4-cianafenil)-2H-pirazol-3-il]-5-metil-3-oxo-4-(3-trifluorometilfenil)-3,4-dihidropirazin-2-carboxílico, junto con procesos para preparar dichas formas, composiciones farmacéuticas que contienen dichas formas y el uso de dichas formas en terapia. Reivindicacion 1: El compuesto Forma B de la etilamida del ácido 6-[2-(4-cianofenil)-2H-pirazol-3-il]-5-metil-3-oxo-4-(3-trifluorometilfenil)-3,4-dihidropirazin-2-carboxílico. Reivindicacion 2: Un compuesto de acuerdo con la reivindicacion 1, caracterizado porque dicha Forma B tiene un patron de difraccion de rayos X en polvo con al menos un pico especifico a 20 aproximadamente = 14.3 o 23.2°, registrado utilizando radiacion CuK a 1.5418 Amstrong. Reivindicacion 6: Un compuesto Forma A de la etilamida del ácido 6-[2-(4-cianofenil)-2H-pirazol-3-il]-5-metil-3-oxo-4-(3-trifluorometilfenil)-3,4-dihidropirazin-2-carboxílico. Reivindicacion 7: Un compuesto de acuerdo con la reivindicacion 1, caracterizado porque dicha Forma A tiene un patron de difraccion de rayos X en polvo con al menos un pico específico a 20 aproximadamente = 10.1 o 18.7°, registrado utilizando radiacion CuKalfa1 a 1.5406 Amstrong en condiciones de temperatura y humedad controladas de un 5% de humedad relativa y 25°C.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31242410P | 2010-03-10 | 2010-03-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080490A1 true AR080490A1 (es) | 2012-04-11 |
Family
ID=43828300
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100754A AR080490A1 (es) | 2010-03-10 | 2011-03-10 | FORMAS CRISTALINAS DE UN INHIBIDOR DE ELASTASA NEUTROFILA, COMPOSICIoN FARMACEUTICA QUE LAS COMPRENDE Y SU USO EN LA FABRICACION DE UN MEDICAMENTO PARA EL TRATAMIENTO DE LA DEFICIENCIA DE ALFA-1-ANTITRIPSINA |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US20110224229A1 (es) |
| AR (1) | AR080490A1 (es) |
| WO (1) | WO2011110852A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9102624B2 (en) | 2012-08-23 | 2015-08-11 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US20140057926A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US20140057920A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| AU2014298561B8 (en) | 2013-07-30 | 2018-06-14 | Janssen Sciences Ireland Uc | Substituted pyridine-piperazinyl analogues as RSV antiviral compounds |
| JOP20210060A1 (ar) | 2018-10-05 | 2023-01-30 | Vertex Pharma | معدلات لمضاد تريبسين ألفا-1 |
| US11884672B2 (en) | 2019-05-14 | 2024-01-30 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| AU2020349353A1 (en) | 2019-09-17 | 2022-04-14 | Duke University | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| TW202116303A (zh) * | 2019-10-02 | 2021-05-01 | 美商維泰克斯製藥公司 | α—１抗胰蛋白酶缺乏症之治療方法 |
| GB201918410D0 (en) * | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of alpha1-antitrypsin deficiency |
| JP7732999B2 (ja) | 2020-04-03 | 2025-09-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | アルファ１－アンチトリプシンのモジュレーター |
| CN115697969B (zh) | 2020-04-03 | 2026-08-11 | 弗特克斯药品有限公司 | α-1抗胰蛋白酶调节剂 |
| AU2021247285A1 (en) | 2020-04-03 | 2022-10-27 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| HUE064089T2 (hu) | 2020-04-16 | 2024-02-28 | Mereo Biopharma 4 Ltd | Alvelesztat neutrofil elasztáz inhibitort alkalmazó módszerek alfa-1-antitripszin hiány által közvetített légzõszervi megbetegedés kezelésére |
| WO2021253643A1 (zh) * | 2020-06-18 | 2021-12-23 | 大连工业大学 | 硫酸化多糖在抗新型冠状病毒中的应用 |
| EP4188931A2 (en) | 2020-07-27 | 2023-06-07 | Vertex Pharmaceuticals Incorporated | Processes for preparing modulators of alpha-1 antitrypsin |
| GB202108523D0 (en) | 2021-06-15 | 2021-07-28 | Z Factor Ltd | Compositions and their use for the treatment of alpha1-antitrypsin deficiency |
| AU2022373971A1 (en) | 2021-10-20 | 2024-04-04 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9302777D0 (sv) | 1993-08-27 | 1993-08-27 | Astra Ab | Process for conditioning substances |
| SE9101090D0 (sv) | 1991-04-11 | 1991-04-11 | Astra Ab | Process for conditioning of water-soluble substances |
| ES2166786T3 (es) | 1993-10-01 | 2002-05-01 | Astrazeneca Ab | Procedimiento i. |
| SE9700134D0 (sv) | 1997-01-20 | 1997-01-20 | Astra Ab | New formulation |
| SE9700133D0 (sv) | 1997-01-20 | 1997-01-20 | Astra Ab | New formulation |
| SE9700135D0 (sv) | 1997-01-20 | 1997-01-20 | Astra Ab | New formulation |
| TW200808771A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
| WO2009061271A1 (en) | 2007-11-06 | 2009-05-14 | Astrazeneca Ab | Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
-
2011
- 2011-03-09 WO PCT/GB2011/050466 patent/WO2011110852A1/en not_active Ceased
- 2011-03-09 US US13/043,697 patent/US20110224229A1/en not_active Abandoned
- 2011-03-10 AR ARP110100754A patent/AR080490A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20110224229A1 (en) | 2011-09-15 |
| WO2011110852A1 (en) | 2011-09-15 |
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