AR087148A1 - Imidazopiridazinas - Google Patents
ImidazopiridazinasInfo
- Publication number
- AR087148A1 AR087148A1 ARP120101200A ARP120101200A AR087148A1 AR 087148 A1 AR087148 A1 AR 087148A1 AR P120101200 A ARP120101200 A AR P120101200A AR P120101200 A ARP120101200 A AR P120101200A AR 087148 A1 AR087148 A1 AR 087148A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- nhc
- heteroaryl
- nr8r9
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Compuestos útiles para el tratamiento de enfermedades relacionadas con la proliferación desregulada de células.Reivindicación 1: Un compuesto de fórmula (1), en donde R1 es hidrógeno, hidroxi, NR5R6, halógeno, ciano, CO(NR8R9), C(O)OR8, C(O)(alquilo C1-6), NHC(O)(alquilo C1-6), NHS(O)2R11, NHC(O)NHR11, -S(O)n-alquilo C1-6, -S(O)2NR5R6 o un grupo seleccionado entre alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, arilo, heteroarilo, -(alquil C1-6)-arilo, -(alquil C1-6)-heteroarilo, -O-(cicloalquilo C3-7), -O-arilo, -O-(heterociclilo C3-7), -O-heteroarilo, -O-(alquil C1-6)-heteroarilo, -O-(alquil C1-6)-(heterociclilo C3-7), -O-(alquil C1-6)-arilo, alquenilo C2-6, alquinilo C2-6, donde dicho grupo está opcionalmente sustituido, una o más veces, en forma idéntica o diferente, con un sustituyente seleccionado entre: hidroxi, halógeno, alquilo C1-6, haloalquilo C1-4, alcoxi C1-6, -NR8R9, ciano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, cicloalquilo C3-7, heterociclilo C3-7, arilo; R2 es hidrógeno, hidroxi, NR5R6, halógeno, ciano, CO(NR8R9), C(O)OR8, C(O)(alquilo C1-6), NHC(alquilo C1-6), NHS(O)2R11, NHC(O)NHR11, -S(O)n-alquilo C1-6, -S(O)2NR5R6 o un grupo seleccionado entre alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, arilo, heteroarilo, -(alquil C1-6)-arilo, -(alquil C1-6)-heteroarilo, -O-(cicloalquilo C3-7), -O-arilo, -O-(heterociclilo C3-7), -O-heteroarilo, -O-(alquil C1-6)-heteroarilo, -O-(alquil C1-6)-(heterociclilo C3-7), -O-(alquil C1-6)-arilo, alquenilo C2-6, alquinilo C2-6, donde dicho grupo está opcionalmente sustituido, una o más veces, en forma idéntica o diferente, con un sustituyente seleccionado entre: hidroxi, halógeno, alquilo C1-6, haloalquilo C1-4, alcoxi C1-6, -NR8R9, ciano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, heterociclilo C3-7, arilo; R3 es hidrógeno, hidroxi, NR5R6, halógeno, ciano, CO(NR8R9), C(O)OR8, C(O)(alquilo C1-6), NHS(O)2R11, NHC(O)NHR11, -S(O)n-alquilo C1-6, -S(O)2NR5R6 o un grupo seleccionado entre alquilo C1-6, alcoxi C1-6, cicloalquilo C3-7, arilo, heteroarilo, (alquil C1-6)-arilo, -(alquil C1-6)-heteroarilo, -O-(cicloalquilo C3-7), -O-arilo, -O-(heterociclilo C3-7), -O-heteroarilo, -O-(alquil C1-6)-heteroarilo, -O-(alquil C1-6)-(heterociclilo C3-7), -O-(alquil C1-6)-arilo, NHC(O)(alquilo C1-6), alquenilo C2-6, alquinilo C2-6, donde dicho grupo está opcionalmente sustituido, una o más veces, en forma idéntica o diferente, con un sustituyente seleccionado entre: hidroxi, halógeno, alquilo C1-6, haloalquilo C1-4, alcoxi C1-6, -NR8R9, ciano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, heterociclilo C3-7, arilo; R4 es fenilo el cual está opcionalmente sustituido una, dos o tres veces, en forma idéntica o diferente, con un átomo de halógeno; R5 es hidrógeno, alquilo C1-6; R6 es hidrógeno, alquilo C1-6; R8 es hidrógeno, alquilo C1-6 que está opcionalmente sustituido con hidroxi; R9 es hidrógeno, alquilo C1-6; R10 es hidrógeno, alquilo C1-6; R11 es hidrógeno, alquilo C1-6; X, Y es CH2; n es 0, 1, 2; o un N-óxido, una sal, un tautómero o un estereoisómero de dicho compuesto, o una sal de dicho N-óxido, tautómero o estereoisómero.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161472732P | 2011-04-07 | 2011-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087148A1 true AR087148A1 (es) | 2014-02-26 |
Family
ID=45953129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101200A Pending AR087148A1 (es) | 2011-04-07 | 2012-04-09 | Imidazopiridazinas |
Country Status (42)
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| KR20170128623A (ko) | 2008-06-16 | 2017-11-22 | 유니버시티 오브 테네시 리서치 파운데이션 | 암 치료용 화합물 |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| WO2011109059A1 (en) | 2010-03-01 | 2011-09-09 | Gtx, Inc. | Compounds for treatment of cancer |
| US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
| DK2694510T3 (en) * | 2011-04-07 | 2016-01-18 | Bayer Ip Gmbh | IMIDAZOPYRIDAZINER AS AKT kinase inhibitors |
| CN104066736B (zh) * | 2012-01-10 | 2017-03-08 | 拜耳知识产权有限责任公司 | 作为akt激酶抑制剂的取代的吡唑并嘧啶 |
| CA2860723A1 (en) * | 2012-01-10 | 2013-07-18 | Bayer Intellectual Property Gmbh | Substituted imidazopyrazines as akt kinase inhibitors |
| CA2891346A1 (en) * | 2012-11-30 | 2014-06-05 | Gossett Campbell | Pharmaceutical composition comprising trametinib dimethyl sulfoxide |
| CN109568312A (zh) * | 2013-03-05 | 2019-04-05 | 田纳西大学研究基金会 | 用于治疗癌症的化合物 |
| WO2014158467A1 (en) * | 2013-03-12 | 2014-10-02 | Glaxosmithkline Llc | Combination |
| CA2903312A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2015104254A1 (en) * | 2014-01-09 | 2015-07-16 | Bayer Pharma Aktiengesellschaft | Amido-substituted imidazopyridazines useful in the treatment of hyper-proliferative and/or angiogenesis disorders |
| WO2018098411A1 (en) * | 2016-11-28 | 2018-05-31 | Bristol-Myers Squibb Company | Gsk-3 inhibitors |
| EP3453706A1 (en) | 2017-09-08 | 2019-03-13 | Basf Se | Pesticidal imidazole compounds |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1246621A4 (en) | 1999-12-23 | 2004-11-24 | Nitromed Inc | NITROSED AND NITROSYLATED CYCLOOXYGENASE-2 INHIBITORS, COMPOSITIONS AND METHODS FOR THEIR USE |
| ES2286114T3 (es) | 2000-03-31 | 2007-12-01 | Ortho-Mcneil Pharmaceutical, Inc. | Imidazopiridina fenil-substituidos. |
| DK1277754T3 (da) | 2000-04-27 | 2005-11-14 | Astellas Pharma Inc | Imidazopyridinderivater |
| US7381825B2 (en) | 2003-03-17 | 2008-06-03 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| ATE512957T1 (de) | 2003-04-24 | 2011-07-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| ES2298798T3 (es) | 2003-07-30 | 2008-05-16 | Laboratorios S.A.L.V.A.T., S.A. | Imidazopirimidinas sustituidas para la prevencion y el tratamiento del cancer. |
| EP1737843B1 (en) | 2004-04-09 | 2011-02-23 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| AU2005290081B2 (en) | 2004-08-23 | 2010-12-02 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| CN101006062A (zh) | 2004-08-24 | 2007-07-25 | 巴斯福股份公司 | 用作生产离子液体的起始化合物的咪唑甲基亚硫酸盐 |
| CN101242834A (zh) | 2004-12-15 | 2008-08-13 | 默克公司 | Akt活性抑制剂 |
| RU2007147382A (ru) | 2005-05-20 | 2009-06-27 | Эррэй Биофарма Инк. (Us) | Соединения, являющиеся ингибиторами raf, и способы их применения |
| JP5055494B2 (ja) | 2005-06-10 | 2012-10-24 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性阻害剤 |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| US7530313B2 (en) | 2006-05-12 | 2009-05-12 | Day & Zimmerman, Inc. | Self-destruct fuze delay mechanism |
| AR064010A1 (es) | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| CN101790526A (zh) * | 2007-06-08 | 2010-07-28 | 雅培制药有限公司 | 用作激酶抑制剂的5-杂芳基取代的吲唑化合物 |
| CN101835776A (zh) * | 2007-08-14 | 2010-09-15 | 拜耳先灵医药股份有限公司 | 用于癌症治疗的稠合的咪唑 |
| UY31293A1 (es) | 2007-08-14 | 2009-03-31 | Pirimidinas biciclicas fusionadas | |
| AU2008345688A1 (en) | 2007-12-21 | 2009-07-09 | Wyeth Llc | Imidazo [1,2-b] pyridazine compounds as modulators of liver X receptors |
| AU2009255358A1 (en) | 2008-06-03 | 2009-12-10 | Msd K.K. | Inhibitors of Akt activity |
| JP2011522047A (ja) | 2008-06-03 | 2011-07-28 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性の阻害剤 |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| JP2012516847A (ja) | 2009-02-02 | 2012-07-26 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性の阻害剤 |
| AU2010213192A1 (en) * | 2009-02-13 | 2011-08-04 | Bayer Intellectual Property Gmbh | Fused pyrimidines |
| EP2406250B1 (en) | 2009-03-11 | 2015-08-12 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| WO2010114780A1 (en) * | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| AR076936A1 (es) | 2009-06-02 | 2011-07-20 | Vitae Pharmaceuticals Inc | Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1 |
| US8546376B2 (en) * | 2009-09-18 | 2013-10-01 | Almac Discovery Limited | Pharmaceutical compounds |
| EP2593451B1 (en) * | 2010-07-12 | 2015-08-19 | Bayer Intellectual Property GmbH | Substituted imidazo[1,2-a]pyrimidines and -pyridines |
| CN103384670B (zh) * | 2010-07-28 | 2016-05-25 | 拜耳知识产权有限责任公司 | 取代的咪唑并[1,2-b]哒嗪 |
| DK2694510T3 (en) * | 2011-04-07 | 2016-01-18 | Bayer Ip Gmbh | IMIDAZOPYRIDAZINER AS AKT kinase inhibitors |
-
2012
- 2012-04-05 DK DK12713963.2T patent/DK2694510T3/en active
- 2012-04-05 WO PCT/EP2012/056300 patent/WO2012136776A1/en active Application Filing
- 2012-04-05 SI SI201230430T patent/SI2694510T1/sl unknown
- 2012-04-05 MX MX2013011699A patent/MX336865B/es active IP Right Grant
- 2012-04-05 JP JP2014503153A patent/JP5906303B2/ja not_active Expired - Fee Related
- 2012-04-05 HU HUE12713963A patent/HUE026323T2/en unknown
- 2012-04-05 MA MA36290A patent/MA35016B1/fr unknown
- 2012-04-05 CA CA2832374A patent/CA2832374A1/en not_active Abandoned
- 2012-04-05 EA EA201301130A patent/EA024890B1/ru not_active IP Right Cessation
- 2012-04-05 PL PL12713963T patent/PL2694510T3/pl unknown
- 2012-04-05 RS RS20160005A patent/RS54480B1/en unknown
- 2012-04-05 PT PT127139632T patent/PT2694510E/pt unknown
- 2012-04-05 CU CUP2013000135A patent/CU24263B1/es unknown
- 2012-04-05 SG SG2013072509A patent/SG193631A1/en unknown
- 2012-04-05 KR KR1020137029229A patent/KR20140022057A/ko not_active Application Discontinuation
- 2012-04-05 ME MEP-2016-1A patent/ME02316B/me unknown
- 2012-04-05 JO JOP/2012/0084A patent/JO3068B1/ar active
- 2012-04-05 US US14/007,427 patent/US9206185B2/en not_active Expired - Fee Related
- 2012-04-05 CN CN201280027994.5A patent/CN103596957B/zh not_active Expired - Fee Related
- 2012-04-05 PE PE2013002192A patent/PE20141380A1/es not_active Application Discontinuation
- 2012-04-05 EP EP12713963.2A patent/EP2694510B1/en active Active
- 2012-04-05 AU AU2012238589A patent/AU2012238589B2/en not_active Ceased
- 2012-04-05 ES ES12713963.2T patent/ES2558780T3/es active Active
- 2012-04-05 AP AP2013007215A patent/AP3597A/xx active
- 2012-04-05 BR BR112013025777A patent/BR112013025777A2/pt active Search and Examination
- 2012-04-06 TW TW101112356A patent/TWI535719B/zh not_active IP Right Cessation
- 2012-04-09 UY UY0001034006A patent/UY34006A/es not_active Application Discontinuation
- 2012-04-09 AR ARP120101200A patent/AR087148A1/es active Pending
- 2012-05-04 UA UAA201312894A patent/UA111739C2/uk unknown
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2013
- 2013-09-26 ZA ZA2013/07223A patent/ZA201307223B/en unknown
- 2013-09-29 IL IL228567A patent/IL228567A0/en unknown
- 2013-10-03 TN TNP2013000400A patent/TN2013000400A1/fr unknown
- 2013-10-07 CO CO13237923A patent/CO6862145A2/es active IP Right Grant
- 2013-10-07 CL CL2013002878A patent/CL2013002878A1/es unknown
- 2013-10-07 GT GT201300238A patent/GT201300238A/es unknown
- 2013-10-07 NI NI201300105A patent/NI201300105A/es unknown
- 2013-10-07 DO DO2013000226A patent/DOP2013000226A/es unknown
- 2013-10-07 CR CR20130515A patent/CR20130515A/es unknown
- 2013-11-04 EC ECSP13013008 patent/ECSP13013008A/es unknown
-
2015
- 2015-07-06 US US14/792,205 patent/US9604989B2/en not_active Expired - Fee Related
-
2016
- 2016-01-05 SM SM201600001T patent/SMT201600001B/it unknown
- 2016-01-05 HR HRP20160011TT patent/HRP20160011T1/hr unknown
- 2016-01-08 CY CY20161100011T patent/CY1117163T1/el unknown
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| FB | Suspension of granting procedure |