AR106830A1 - Usos de piridazinonas para tratar el cáncer - Google Patents
Usos de piridazinonas para tratar el cáncerInfo
- Publication number
- AR106830A1 AR106830A1 ARP160103628A ARP160103628A AR106830A1 AR 106830 A1 AR106830 A1 AR 106830A1 AR P160103628 A ARP160103628 A AR P160103628A AR P160103628 A ARP160103628 A AR P160103628A AR 106830 A1 AR106830 A1 AR 106830A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- optionally substituted
- cycloalkyl
- membered
- alkyl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 7
- 201000011510 cancer Diseases 0.000 title abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 abstract 3
- 150000002148 esters Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 230000012010 growth Effects 0.000 abstract 2
- 230000035755 proliferation Effects 0.000 abstract 2
- 230000004614 tumor growth Effects 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se revelan métodos de tratamiento del cáncer, que incluyen administrar una cantidad terapéuticamente efectiva de un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable o éster del mismo, a un sujeto que lo necesite. Además se revelan métodos de inhibición del crecimiento y proliferación de células cancerosas in vitro o in vivo, que incluyen poner en contacto las células con una cantidad del compuesto de la fórmula (1) eficaz para inhibir el crecimiento o proliferación de las células cancerosas. Además se revelan métodos de inhibición del crecimiento tumoral, que incluyen poner en contacto el tumor con una cantidad del compuesto de la fórmula (1) eficaz para inhibir el crecimiento del tumor. Reivindicación 1: Un método de tratamiento de un sujeto que padece cáncer, caracterizado porque comprende administrar a un sujeto con cáncer que la necesita, una cantidad terapéuticamente efectiva de un compuesto de la fórmula (1), en la cual: R¹ es NR⁴R⁵, alcoxi C₁₋₆ opcionalmente sustituido, arilo C₆₋₁₄ opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo monocíclico o bicíclico de 3 a 10 miembros opcionalmente sustituido, o heterociclilo monocíclico bicíclico de 3 a 10 miembros opcionalmente sustituido, en tanto: (i) el cicloalquilo y heterociclilo de 3 a 4 miembros son saturados; (ii) átomos de hidrógeno en el mismo átomo de carbono de dicho cicloalquilo o heterociclilo opcionalmente se reemplazan con un cicloalquilo o heterociclilo opcionalmente sustituido de 3 a 6 miembros para formar un espirocicloalquilo o espiro heterociclilo; y (iii) átomos de hidrógeno en el mismo átomo de dicho cicloalquilo o heterociclilo opcionalmente se reemplazan con O para formar un sustituyente oxo; R² es fenilo opcionalmente sustituido, -O-(alquilo C₁₋₆)-fenilo opcionalmente sustituido, o heteroarilo, de 5 - 6 miembros opcionalmente sustituido, con la condición que cuando R² es 4-piridilo, el 4-piridilo carece de un sustituyente carbonilo en la segunda posición; R⁴ y R⁵ son: (a) independientemente seleccionados del grupo integrado por H, alquilo C₁₋₆, hidroxialquilo C₁₋₆, cicloalquilo C₃₋₈, y -(alquilo C₁₋₆)N(alquilo C₁₋₆)(alquilo C₁₋₆); (b) unidos para formar un heterociclilo de 3 a 8 miembros opcionalmente sustituido, en donde; (bi) átomos de hidrógeno en el mismo átomo de carbono de dicho heterociclilo opcionalmente se reemplazan con un cicloalquilo o heterociclilo opcionalmente sustituido de 3 a 6 miembros para formar un espirocicloalquilo o espiroheterociclilo; y (bii) átomos de hidrógeno en el mismo átomo de dicho heterociclilo (b), cicloalquilo (bi), o heterociclilo (bi), opcionalmente se reemplazan con O para formar un sustituyente oxo; o una sal farmacéuticamente aceptable o éster del mismo. Reivindicación 20: El método de cualquiera de las reivindicaciones 1 - 19, caracterizado porque el compuesto de la formula (1) es 2-(1-(4-((4-(4-hidroxipiperidin-1-il)fenil)amino)-5-oxo-5,6-dihidropirimido[4,5-d]piridazin-2-il)piperidin-4-il)acetonitrilo, o una sal farmacéuticamente aceptable o éster del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562263398P | 2015-12-04 | 2015-12-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR106830A1 true AR106830A1 (es) | 2018-02-21 |
Family
ID=57570591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160103628A AR106830A1 (es) | 2015-12-04 | 2016-11-25 | Usos de piridazinonas para tratar el cáncer |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US10188654B2 (es) |
| EP (1) | EP3383399A1 (es) |
| JP (1) | JP2018535995A (es) |
| KR (1) | KR20180084983A (es) |
| CN (1) | CN108601785A (es) |
| AR (1) | AR106830A1 (es) |
| AU (1) | AU2016365215A1 (es) |
| BR (1) | BR112018011196A2 (es) |
| CA (1) | CA3006762A1 (es) |
| IL (1) | IL259781A (es) |
| MX (1) | MX2018006776A (es) |
| RU (1) | RU2018124289A (es) |
| TW (1) | TW201726141A (es) |
| WO (1) | WO2017095898A1 (es) |
| ZA (1) | ZA201803593B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX361458B (es) * | 2011-08-23 | 2018-12-06 | Asana Biosciences Llc | Compuestos de pirimido-piridazinona y uso de los mismos. |
| WO2018201131A1 (en) | 2017-04-28 | 2018-11-01 | Asana Biosciences, Llc | Formulations, methods, kits, and dosage forms for treating atopic dermatitis and for improved stability of an active pharmaceutical ingredient |
| CN111961035B (zh) * | 2019-05-20 | 2022-11-01 | 南京科技职业学院 | 一类含有羟基异喹啉类结构的化合物、药物组合物以及其应用 |
| US20250195524A1 (en) * | 2022-03-22 | 2025-06-19 | Shanghai Visonpharma Co., Ltd. | Pyrimido-pyridazinone compound as toll-like receptor agonist |
| WO2025020171A1 (en) * | 2023-07-27 | 2025-01-30 | Libertas Bio, Inc. | Crystalline forms of a jak/syk inhibitor |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA024109B1 (ru) | 2008-04-16 | 2016-08-31 | Портола Фармасьютиклз, Инк. | Ингибиторы протеинкиназ |
| JP5634995B2 (ja) * | 2008-08-12 | 2014-12-03 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | 化学化合物 |
| MX2012004846A (es) * | 2009-10-29 | 2012-10-05 | Genosco | Inhibidores de cinasa. |
| WO2013013031A1 (en) * | 2011-07-19 | 2013-01-24 | Abbvie Inc. | Pyridazino [4, 5 -d] pyrimidin- (6h) -one inhibitors of wee - 1 kinase |
| MX361458B (es) * | 2011-08-23 | 2018-12-06 | Asana Biosciences Llc | Compuestos de pirimido-piridazinona y uso de los mismos. |
-
2016
- 2016-11-25 AR ARP160103628A patent/AR106830A1/es unknown
- 2016-11-28 TW TW105138865A patent/TW201726141A/zh unknown
- 2016-11-30 CN CN201680081107.0A patent/CN108601785A/zh active Pending
- 2016-11-30 WO PCT/US2016/064178 patent/WO2017095898A1/en not_active Ceased
- 2016-11-30 RU RU2018124289A patent/RU2018124289A/ru not_active Application Discontinuation
- 2016-11-30 JP JP2018528583A patent/JP2018535995A/ja active Pending
- 2016-11-30 BR BR112018011196A patent/BR112018011196A2/pt not_active IP Right Cessation
- 2016-11-30 KR KR1020187017697A patent/KR20180084983A/ko not_active Withdrawn
- 2016-11-30 MX MX2018006776A patent/MX2018006776A/es unknown
- 2016-11-30 AU AU2016365215A patent/AU2016365215A1/en not_active Abandoned
- 2016-11-30 EP EP16813264.5A patent/EP3383399A1/en not_active Withdrawn
- 2016-11-30 US US15/365,222 patent/US10188654B2/en active Active
- 2016-11-30 CA CA3006762A patent/CA3006762A1/en not_active Abandoned
-
2018
- 2018-05-30 ZA ZA2018/03593A patent/ZA201803593B/en unknown
- 2018-06-03 IL IL259781A patent/IL259781A/en unknown
- 2018-11-02 US US16/179,274 patent/US20190070182A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| IL259781A (en) | 2018-07-31 |
| CA3006762A1 (en) | 2017-06-08 |
| KR20180084983A (ko) | 2018-07-25 |
| TW201726141A (zh) | 2017-08-01 |
| JP2018535995A (ja) | 2018-12-06 |
| ZA201803593B (en) | 2019-04-24 |
| MX2018006776A (es) | 2018-08-15 |
| US20190070182A1 (en) | 2019-03-07 |
| CN108601785A (zh) | 2018-09-28 |
| RU2018124289A (ru) | 2020-01-14 |
| BR112018011196A2 (pt) | 2018-11-21 |
| WO2017095898A1 (en) | 2017-06-08 |
| EP3383399A1 (en) | 2018-10-10 |
| US10188654B2 (en) | 2019-01-29 |
| US20170157126A1 (en) | 2017-06-08 |
| AU2016365215A1 (en) | 2018-07-05 |
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| FB | Suspension of granting procedure |