AR123884A1 - Compuestos moduladores del cftr, composiciones y usos de estos - Google Patents
Compuestos moduladores del cftr, composiciones y usos de estosInfo
- Publication number
- AR123884A1 AR123884A1 ARP210102922A ARP210102922A AR123884A1 AR 123884 A1 AR123884 A1 AR 123884A1 AR P210102922 A ARP210102922 A AR P210102922A AR P210102922 A ARP210102922 A AR P210102922A AR 123884 A1 AR123884 A1 AR 123884A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- compounds
- alkyl
- compositions
- methods
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 11
- 239000000203 mixture Substances 0.000 title abstract 6
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 2
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 abstract 2
- 208000022873 Ocular disease Diseases 0.000 abstract 2
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000001620 monocyclic carbocycle group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se proporcionan compuestos moduladores de CFTR y composiciones que incluyen dichos compuestos. La presente divulgación también proporciona compuestos inhibidores de PDE4 y composiciones que incluyen dichos compuestos. También se proporcionan métodos para utilizar dichos compuestos y composiciones para modular CFTR, métodos para tratar una enfermedad o trastorno ocular y métodos para tratar indicaciones relacionadas con CFTR. La presente divulgación también proporciona métodos para utilizar dichos compuestos y composiciones para inhibir la PDE4, para tratar una enfermedad o trastorno inflamatorio y para tratar otras indicaciones relacionadas con la PDE4. También se proporcionan métodos de preparación de dichos compuestos y composiciones, y precursores sintéticos de dichos compuestos. Reivindicación 1: Un compuesto de fórmula (1), o una sal, un solvato, un hidrato, un profármaco o un estereoisómero farmacéuticamente aceptable de este, caracterizado porque: R¹ se selecciona de H, halógeno, arilo opcionalmente sustituido, alquilo (C₁₋₁₀) opcionalmente sustituido y alcoxi (C₁₋₁₀) opcionalmente sustituido; R² se selecciona de H, alquilo (C₁₋₁₀) opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido y heterociclo opcionalmente sustituido, y los sustituyentes opcionales en arilo, heteroarilo y heterociclo se seleccionan independientemente de entre los siguientes: H, OH, NH₂, NO₂, OCF₃, CF₃, halógeno, amina opcionalmente sustituida, alquilo (C₁₋₅) opcionalmente sustituido, y alcoxi (C₁₋₅) opcionalmente sustituido; R⁴ se selecciona de los compuestos del grupo de fórmulas (2); R⁵ y R⁶ se seleccionan independientemente de H, alquilo (C₁₋₁₀) opcionalmente sustituido, alquenilo (C₁₋₁₀) opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, arilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, carbociclo monocíclico o bicíclico opcionalmente sustituido y heterociclo monocíclico o bicíclico opcionalmente sustituido; o R⁵ y R⁶ juntos con el átomo nitrógeno, al cual están unidos, están cíclicamente unidos para formar un heterociclo monocíclico o bicíclico opcionalmente sustituido; R⁷ se selecciona de NR⁵R⁶, alquilo (C₁₋₁₀) opcionalmente sustituido, alcoxi (C₁₋₁₀) opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, arilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido y heterocicloalquilo opcionalmente sustituido; R⁸ se selecciona de H y alquilo (C₁₋₁₀) opcionalmente sustituido; y R⁹ se selecciona de H y halógeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063104979P | 2020-10-23 | 2020-10-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR123884A1 true AR123884A1 (es) | 2023-01-18 |
Family
ID=81290147
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210102922A AR123884A1 (es) | 2020-10-23 | 2021-10-22 | Compuestos moduladores del cftr, composiciones y usos de estos |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11827640B2 (es) |
| EP (1) | EP4232451A1 (es) |
| JP (1) | JP2023547389A (es) |
| KR (1) | KR20230096026A (es) |
| CN (1) | CN116348468A (es) |
| AR (1) | AR123884A1 (es) |
| AU (1) | AU2021363703A1 (es) |
| CA (1) | CA3196061A1 (es) |
| CL (1) | CL2023001139A1 (es) |
| CO (1) | CO2023006647A2 (es) |
| IL (1) | IL302247A (es) |
| MX (1) | MX2023004712A (es) |
| TW (1) | TW202233620A (es) |
| UY (1) | UY39482A (es) |
| WO (1) | WO2022084741A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114380835B (zh) * | 2022-01-06 | 2022-12-27 | 南京桦冠生物技术有限公司 | 一种7-(3,4-二甲氧苯基)-2-吡唑[1,5-a]嘧啶羧酸的制备方法 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4178449A (en) | 1978-04-17 | 1979-12-11 | American Cyanamid Company | Pyrazolo[1,5-a]pyrimidines and imidazo-[1,5-a]pyrimidines |
| US4281000A (en) | 1979-07-09 | 1981-07-28 | American Cyanamid Company | Substituted pyrazolo (1,5-a)pyrimidines and their use as anxiolytic agents |
| US5688949A (en) | 1991-04-22 | 1997-11-18 | Otsuka Pharmaceutical Factory, Inc. | Pyrazolo 1,5-A!pyrimidine derivatives and anti-inflammatory agent containing the same |
| AU2003240488A1 (en) | 2002-06-04 | 2003-12-19 | Neogenesis Pharmaceuticals, Inc. | Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents |
| JP2004170323A (ja) | 2002-11-22 | 2004-06-17 | Sumitomo Pharmaceut Co Ltd | 皮膚疾患治療剤のスクリーニング方法 |
| US7893096B2 (en) | 2003-03-28 | 2011-02-22 | Novartis Vaccines And Diagnostics, Inc. | Use of small molecule compounds for immunopotentiation |
| US20070270408A1 (en) | 2003-04-11 | 2007-11-22 | Novo Nordisk A/S | Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines |
| EP1615697A2 (en) | 2003-04-11 | 2006-01-18 | Novo Nordisk A/S | New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof |
| JPWO2005037837A1 (ja) * | 2003-10-17 | 2006-12-28 | 日本化薬株式会社 | 置換２−アミノ−［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体及びその用途 |
| JP2007517876A (ja) | 2004-01-14 | 2007-07-05 | マリンクロッド・インコーポレイテッド | 選択的ピラゾロピリミジン類の合成のための２相法 |
| KR20070045254A (ko) | 2004-08-02 | 2007-05-02 | 슈바르츠 파르마 악티엔게젤샤프트 | 인돌리진 카르복사미드 및 그 아자 및 디아자유도체 |
| WO2006088246A1 (ja) | 2005-02-18 | 2006-08-24 | Takeda Pharmaceutical Company Limited | Ｇｐｒ３４受容体機能調節剤 |
| AU2006305104B2 (en) | 2005-10-21 | 2009-10-22 | Mitsubishi Tanabe Pharma Corporation | Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists |
| AR061793A1 (es) | 2006-07-05 | 2008-09-24 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica |
| WO2008045664A2 (en) | 2006-10-06 | 2008-04-17 | Kalypsys, Inc. | Heterocyclic pde4 inhibitors as antiinflammatory agents |
| WO2008056176A1 (en) | 2006-11-10 | 2008-05-15 | Scottish Biomedical Limited | Pyrazolopyrimidines as phosphodiesterase inhibitors |
| WO2010074284A1 (ja) | 2008-12-26 | 2010-07-01 | 味の素株式会社 | ピラゾロピリミジン化合物 |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| WO2011050245A1 (en) | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
| WO2012000970A1 (en) | 2010-07-01 | 2012-01-05 | Cellzome Limited | Triazolopyridines as tyk2 inhibitors |
| US8883789B2 (en) * | 2011-12-14 | 2014-11-11 | Boehringer Ingelheim International Gmbh | Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors |
| EP2970266B1 (en) | 2013-03-15 | 2018-01-31 | Epizyme, Inc. | 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof |
| CN103923105B (zh) | 2014-04-17 | 2016-08-24 | 北京大学 | 2-中氮茚甲酰胺类化合物及其制备和用途 |
| JP2018076234A (ja) | 2015-03-16 | 2018-05-17 | 大正製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| CN108699107B (zh) | 2015-12-24 | 2022-05-10 | 加利福尼亚大学董事会 | Cftr调节剂及其使用方法 |
| CN107286156A (zh) | 2016-04-05 | 2017-10-24 | 江苏新元素医药科技有限公司 | 新型urat1抑制剂及其在医药上的应用 |
| WO2018145080A1 (en) * | 2017-02-06 | 2018-08-09 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| WO2018226150A1 (en) | 2017-06-05 | 2018-12-13 | Medivir Aktiebolag | Pyrazolopyrimidine as malt-1 inhibitors |
-
2021
- 2021-10-22 US US17/508,198 patent/US11827640B2/en active Active
- 2021-10-22 CA CA3196061A patent/CA3196061A1/en active Pending
- 2021-10-22 JP JP2023524685A patent/JP2023547389A/ja active Pending
- 2021-10-22 UY UY0001039482A patent/UY39482A/es unknown
- 2021-10-22 KR KR1020237017551A patent/KR20230096026A/ko unknown
- 2021-10-22 AR ARP210102922A patent/AR123884A1/es unknown
- 2021-10-22 AU AU2021363703A patent/AU2021363703A1/en active Pending
- 2021-10-22 IL IL302247A patent/IL302247A/en unknown
- 2021-10-22 MX MX2023004712A patent/MX2023004712A/es unknown
- 2021-10-22 TW TW110139341A patent/TW202233620A/zh unknown
- 2021-10-22 EP EP21882228.6A patent/EP4232451A1/en active Pending
- 2021-10-22 CN CN202180072298.5A patent/CN116348468A/zh active Pending
- 2021-10-22 WO PCT/IB2021/000710 patent/WO2022084741A1/en active Application Filing
-
2023
- 2023-04-20 CL CL2023001139A patent/CL2023001139A1/es unknown
- 2023-05-19 CO CONC2023/0006647A patent/CO2023006647A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2023004712A (es) | 2023-05-09 |
| EP4232451A1 (en) | 2023-08-30 |
| UY39482A (es) | 2022-05-31 |
| CO2023006647A2 (es) | 2023-05-29 |
| US11827640B2 (en) | 2023-11-28 |
| AU2021363703A1 (en) | 2023-06-22 |
| TW202233620A (zh) | 2022-09-01 |
| CL2023001139A1 (es) | 2023-11-17 |
| CA3196061A1 (en) | 2022-04-28 |
| JP2023547389A (ja) | 2023-11-10 |
| CN116348468A (zh) | 2023-06-27 |
| IL302247A (en) | 2023-06-01 |
| WO2022084741A1 (en) | 2022-04-28 |
| US20230080486A1 (en) | 2023-03-16 |
| KR20230096026A (ko) | 2023-06-29 |
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