AR107526A1 - Derivados de pirazol como inhibidores de las fosfoinositido 3-quinasas - Google Patents
Derivados de pirazol como inhibidores de las fosfoinositido 3-quinasasInfo
- Publication number
- AR107526A1 AR107526A1 ARP170100271A ARP170100271A AR107526A1 AR 107526 A1 AR107526 A1 AR 107526A1 AR P170100271 A ARP170100271 A AR P170100271A AR P170100271 A ARP170100271 A AR P170100271A AR 107526 A1 AR107526 A1 AR 107526A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- haloalkyl
- hydroxyalkyl
- aryl
- independently
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 108091007960 PI3Ks Proteins 0.000 abstract 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- -1 pyrazolo [3,4-d] pyrimidinyl Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000005016 hydroxyalkynyl group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pulmonology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos que inhiben las fosfoinositido 3-quinasas (PI3K), composiciones farmacéuticas que los comprenden y su uso terapéutico en el tratamiento de los trastornos asociados a las enzimas PI3K. Reivindicación 1: Compuestos caracterizados porque responden a la fórmula (1), donde R¹, R⁴ y R⁵ pueden ser idénticos o diferentes, se seleccionan independientemente del grupo que consiste en C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo o arilo y pueden estar sustituidos independientemente con uno o más grupos seleccionados entre halógenos, -OH, -(CH₂)ₚNR⁶R⁷, -CN, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo o C₂₋₆ hidroxialquinilo; R² se selecciona entre H y C₁₋₆ alquilo; R³ es H; Cy es un heteroarilo seleccionado del grupo que consiste en l-1 a l-3, donde (l-1) es purinilo, (l-2) es pirazolo[3,4-d]pirimidinilo e (l-3) es pirimidinilo, donde cada uno de l-1 a l-3 puede estar sustituido independientemente con uno o más grupos seleccionados entre halógenos, -OH, -(CH₂)ₚNR⁶R⁷, -CN, -CH=NOH, -C(O)NR⁶R⁷, -C(O)OR⁶, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ alcanilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₂₋₆ hidroxialquinilo, arilo, heteroarilo o heterocicloalquilo, y donde los grupos arilo, heteroarilo y heterocicloalquilo pueden estar sustituidos independientemente con uno o más grupos seleccionados entre -OH, halógenos, -CN, -S(O)₂NR⁶R⁷, -NR⁶S(O)₂R⁷, -NR⁶R⁷, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo o C₁₋₆ alcoxilo; en cada caso, R⁶ y R⁷ pueden ser idénticos o diferentes y se seleccionan independientemente del grupo que consiste en -H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₁₋₆ alcanilo o aril-C₁₋₆ alcanilo, o cuando R⁶ y R⁷ están unidos a un átomo de nitrógeno, pueden formar con él un heterociclo con entre 4 y 6 miembros que puede contener uno o más heteroátomos o grupos heteroatómicos seleccionados entre O, S, N o NH; en cada caso, p es independientemente cero o un número entero entre 1 y 3; o sales o solvatos farmacéuticamente aceptables de éstos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16154299 | 2016-02-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR107526A1 true AR107526A1 (es) | 2018-05-09 |
Family
ID=55299403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170100271A AR107526A1 (es) | 2016-02-04 | 2017-02-02 | Derivados de pirazol como inhibidores de las fosfoinositido 3-quinasas |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10189844B2 (es) |
| EP (1) | EP3411375B1 (es) |
| AR (1) | AR107526A1 (es) |
| WO (1) | WO2017134053A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3691620T (pt) | 2017-10-05 | 2022-10-06 | Fulcrum Therapeutics Inc | Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| SG11202110801XA (en) | 2019-04-04 | 2021-10-28 | Chiesi Farm Spa | Isochromene derivatives as phosphoinositide 3-kinases inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2338716T3 (es) | 2006-01-27 | 2010-05-11 | F.Hoffmann-La Roche Ag | Uso de derivados de 4-imidazol para trastornos del snc. |
| CA2909277A1 (en) | 2006-04-04 | 2007-10-11 | Kevan M. Shokat | Kinase antagonists |
| JP6297582B2 (ja) * | 2012-11-16 | 2018-03-20 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 |
| TWI672297B (zh) | 2013-12-18 | 2019-09-21 | 義大利商吉斯藥品公司 | 作為磷脂肌醇－３－激酶抑制劑之異唏衍生物 |
| TN2016000555A1 (en) * | 2014-06-17 | 2018-04-04 | Chiesi Farm Spa | Indolizine derivatives as phosphoinositide 3-kinases inhibitors |
-
2017
- 2017-01-31 WO PCT/EP2017/052054 patent/WO2017134053A1/en not_active Ceased
- 2017-01-31 EP EP17705804.7A patent/EP3411375B1/en active Active
- 2017-01-31 US US15/420,513 patent/US10189844B2/en active Active
- 2017-02-02 AR ARP170100271A patent/AR107526A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3411375A1 (en) | 2018-12-12 |
| US20170226109A1 (en) | 2017-08-10 |
| WO2017134053A1 (en) | 2017-08-10 |
| EP3411375B1 (en) | 2020-08-05 |
| US10189844B2 (en) | 2019-01-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |