AR075951A1 - Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mek - Google Patents
Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mekInfo
- Publication number
- AR075951A1 AR075951A1 ARP100100964A ARP100100964A AR075951A1 AR 075951 A1 AR075951 A1 AR 075951A1 AR P100100964 A ARP100100964 A AR P100100964A AR P100100964 A ARP100100964 A AR P100100964A AR 075951 A1 AR075951 A1 AR 075951A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydroxy
- independently selected
- alkenyl
- halogen
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/76—Nitrogen atoms to which a second hetero atom is attached
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
N-(orto fenilamino dihidropiridil)sulfonamidas y N-(orto fenilamino dihidropiridil), N'-alquilsulfamidas que son inhibidores de MEK y de utilidad en el tratamiento de cáncer y otras enfermedades hiperproliferativas. Reivindicacion 1: Un compuesto caracterizado porque es de formula 1, o una sal, solvato, polimorfo, éster, tautomero o prodroga farmacéuticamente aceptable del mismo donde B es H, alquilo C1-6 o alquenilo C26; donde dicho alquilo C1-6 está opcionalmente sustituido con uno o dos grupos seleccionados en forma independiente entre hidroxi, alcoxi, oxi, amina y amina sustituida; A y A' son en forma independiente entre sí H, alquilo C1-6, o alquenilo C2-6; donde cada alquilo C1-6 está opcionalmente sustituido con uno o dos grupos seleccionados en forma independiente entre hidroxi, alcoxi, oxi, amina y amina sustituida; o A y A' junto con el átomo de carbono al cual se encuentran unidos, forman un grupo ciclopropilo, ciclobutilo, o ciclopentilo, donde cada grupo ciclopropilo, ciclobutilo, o ciclopentilo está opcionalmente sustituido con uno o dos grupos seleccionados en forma independiente entre metilo, hidroxi, y halogeno; X e Y son en forma independiente entre sí halogeno, metilo, SCH3 o trifluorometilo; R1 es H, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, cicloalquenilo C5-6 o alquinilo C2-6; donde cada grupo alquilo, cicloalquilo, alquenilo, cicloalquenilo o alquinilo está opcionalmente sustituido con 1-3 sustituyentes seleccionados en forma independiente entre halogeno, hidroxi, alquilo C1-4, alcoxi C1-4, ciano, cianometilo, nitro, azido, trifluorometilo difluorometoxi y fenilo, y uno o dos átomos de carbono del anillo de dichos grupos cicloalquilo C3-6 se reemplazan opcionalmente en forma independiente por O, N, o S; o R1 es un grupo heterocíclico de 5 o 6 átomos, que puede ser saturado, insaturado, o aromático, que contiene 1-5 heteroátomos seleccionados en forma independiente entre O, N, y S, donde el grupo heterocíclico está opcionalmente sustituido con 1-3 sustituyentes seleccionados en forma independiente entre halogeno, hidroxi, alquilo C1-4, alcoxi C1-4, ciano, cianometilo, nitro, azido, trifluorometil difluorometoxi y fenilo; y R2 es H, halogeno, hidroxi, azido, ciano, cianometilo, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, cicloalquenilo C5-6 o alquinilo C2-6, donde cada grupo alquilo, cicloalquilo, alquenilo, cicloalquenilo o alquinilo está opcionalmente sustituido con 1-3 sustituyentes seleccionados en forma independiente entre halogeno, hidroxi, alcoxi C1-4, ciano, cianometilo, nitro, azido, trifluorometilo y fenilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16431909P | 2009-03-27 | 2009-03-27 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR075951A1 true AR075951A1 (es) | 2011-05-04 |
Family
ID=42112300
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100100964A AR075951A1 (es) | 2009-03-27 | 2010-03-26 | Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mek |
Country Status (8)
Country | Link |
---|---|
US (1) | US8673919B2 (es) |
EP (1) | EP2411366B8 (es) |
JP (1) | JP5844727B2 (es) |
CN (2) | CN106478496A (es) |
AR (1) | AR075951A1 (es) |
CA (1) | CA2756566A1 (es) |
ES (1) | ES2543608T3 (es) |
WO (1) | WO2010108652A1 (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2567283T3 (es) | 2008-06-03 | 2016-04-21 | Intermune, Inc. | Compuestos y métodos para tratar trastornos inflamatorios y fibróticos |
AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
CA2890238A1 (en) | 2012-11-02 | 2014-05-08 | Merck Patent Gmbh | Method of reducing adverse effects in a cancer patient undergoing treatment with a mek inhibitor |
EP3126362B1 (en) | 2014-04-02 | 2022-01-12 | Intermune, Inc. | Anti-fibrotic pyridinones |
FR3032496B1 (fr) | 2015-02-10 | 2017-08-18 | Monestrol Georges De | Dispositif pour le blocage d'un premier tube exterieur et d'un deuxieme tube interieur montes telescopiques entre eux. |
US20190008859A1 (en) | 2015-08-21 | 2019-01-10 | Acerta Pharma B.V. | Therapeutic Combinations of a MEK Inhibitor and a BTK Inhibitor |
AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
IL299206A (en) * | 2020-06-23 | 2023-02-01 | Chemocentryx Inc | Methods for treating cancer using heteroaryl-biphenyl amide derivatives |
Family Cites Families (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8607683D0 (en) | 1986-03-27 | 1986-04-30 | Ici Plc | Anti-tumor agents |
GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
JPH06135934A (ja) * | 1991-12-27 | 1994-05-17 | Ishihara Sangyo Kaisha Ltd | ピリジン誘導体又はその塩を含有するホスホリパーゼ▲a2▼阻害剤、抗炎症剤又は抗膵炎剤 |
US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
ES2153031T4 (es) | 1995-04-20 | 2001-05-16 | Pfizer | Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf. |
DE69624081T2 (de) | 1995-12-20 | 2003-06-12 | Agouron Pharmaceuticals, Inc. | Matrix-metalloprotease Inhibitoren |
EP0923585B1 (en) | 1996-07-18 | 2002-05-08 | Pfizer Inc. | Phosphinate based inhibitors of matrix metalloproteases |
AU711585B2 (en) | 1996-08-23 | 1999-10-14 | Pfizer Inc. | Arylsulfonylamino hydroxamic acid derivatives |
BR9714266A (pt) | 1997-01-06 | 2000-04-18 | Pfizer | Derivados de sulfona cìclicos. |
PT977733E (pt) | 1997-02-03 | 2003-12-31 | Pfizer Prod Inc | Derivados de acido arilsulfonilamino-hidroxamico |
AU5493598A (en) | 1997-02-07 | 1998-08-26 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
PL334997A1 (en) | 1997-02-11 | 2000-03-27 | Pfizer | Derivatives or arylosulphonyl-hydroxamic acid |
US6310060B1 (en) | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
AU2002210714A1 (en) | 2000-11-02 | 2002-06-11 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
TW200303742A (en) | 2001-11-21 | 2003-09-16 | Novartis Ag | Organic compounds |
WO2005051302A2 (en) * | 2003-11-19 | 2005-06-09 | Array Biopharma Inc. | Bicyclic inhibitors of mek and methods of use thereof |
SA06270141B1 (ar) | 2005-05-18 | 2009-11-15 | اراي بيوفارما انك | مثبطات حلقية غير متجانسة لـmek وطرق استخدامها |
CA2618218C (en) * | 2005-07-21 | 2015-06-30 | Ardea Biosciences, Inc. | N-(arylamino)-sulfonamide inhibitors of mek |
DE602007009663D1 (de) | 2006-04-18 | 2010-11-18 | Ardea Biosciences Inc | Pyridonsulfonamide und pyridonsulfamide als mek-hemmer |
CN102134218A (zh) * | 2009-06-15 | 2011-07-27 | 凯美隆(北京)药业技术有限公司 | 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂 |
-
2010
- 2010-03-23 JP JP2012501180A patent/JP5844727B2/ja not_active Expired - Fee Related
- 2010-03-23 CN CN201610768696.1A patent/CN106478496A/zh active Pending
- 2010-03-23 US US13/259,239 patent/US8673919B2/en not_active Expired - Fee Related
- 2010-03-23 WO PCT/EP2010/001808 patent/WO2010108652A1/en active Application Filing
- 2010-03-23 EP EP10711012.4A patent/EP2411366B8/en not_active Not-in-force
- 2010-03-23 ES ES10711012.4T patent/ES2543608T3/es active Active
- 2010-03-23 CN CN2010800227265A patent/CN102448938A/zh active Pending
- 2010-03-23 CA CA2756566A patent/CA2756566A1/en not_active Abandoned
- 2010-03-26 AR ARP100100964A patent/AR075951A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
CN102448938A (zh) | 2012-05-09 |
CN106478496A (zh) | 2017-03-08 |
EP2411366A1 (en) | 2012-02-01 |
US20120107307A1 (en) | 2012-05-03 |
JP2012521968A (ja) | 2012-09-20 |
CA2756566A1 (en) | 2010-09-30 |
US8673919B2 (en) | 2014-03-18 |
WO2010108652A1 (en) | 2010-09-30 |
JP5844727B2 (ja) | 2016-01-20 |
ES2543608T3 (es) | 2015-08-20 |
EP2411366B1 (en) | 2015-05-20 |
EP2411366B8 (en) | 2015-07-15 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR075951A1 (es) | Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mek | |
PE20212247A1 (es) | Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos | |
AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
AR059622A1 (es) | Quinolonas utiles como inhibidores de la sintetasa del oxido nitrico inducibles | |
AR066043A1 (es) | Derivados de benzamida sustituida como inhibidores de la 11-beta-hidroxi esteroide deshidrogenasa tipo 1(11betahsd1) | |
AR086983A1 (es) | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak | |
PE20141598A1 (es) | Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina | |
PE20191245A1 (es) | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim | |
PE20181298A1 (es) | Inhibidores de bromodominio bivalentes y usos de los mismos | |
PE20181093A1 (es) | Compuestos heterociclicos y usos de los mismos | |
AR098912A1 (es) | Inhibidores de syk | |
EA201591000A1 (ru) | Пирролобензодиазепины | |
AR075635A1 (es) | N-alcoxiamidas de 6-(fenil sustituido)-4-aminopicolinatos y 2-(fenil sustituido)-6-amino-4-pirimidina carboxilatos, su uso como herbicidas selectivos para las cosechas y proceso de preparacion de dichos compuestos | |
AR085004A1 (es) | Inhibidores selectivos de glicosidasas y usos de los mismos | |
AR099379A1 (es) | Compuestos tricíclicos como agentes antineoplásicos | |
ES2570756T3 (es) | Derivados pirimidinilpirrolopiridinona sustituidos, proceso para su preparación y su uso como inhibidores de cinasa | |
AR079226A1 (es) | Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancer | |
AR062074A1 (es) | Derivados de alcoholes 1-fenil-2-piridinil alquilenicos como inhibidores de fosfodiesterasa | |
AR060489A1 (es) | Derivados del acido benzoazepin - oxi- acetico como agonistas de ppar - delta usados para aumentar hdl- c, reducir ldl-c y reducir colesterol | |
AR101177A1 (es) | Inhibidores de la syk | |
PE20131165A1 (es) | Analogos de carba-nucleosidos sustituidos con 2'-fluoro para tratamiento antiviral | |
AR101815A1 (es) | Compuestos y composiciones como inhibidores de quinasa | |
AR080596A1 (es) | Compuestos alquilamido y composiciones farmaceuticas | |
AR074608A1 (es) | Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas | |
AR087915A1 (es) | N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |