AR079570A1 - Compuestos de pirrolo(2,3-d)pirazin-7-il-pirimidina - Google Patents
Compuestos de pirrolo(2,3-d)pirazin-7-il-pirimidinaInfo
- Publication number
- AR079570A1 AR079570A1 ARP100104797A ARP100104797A AR079570A1 AR 079570 A1 AR079570 A1 AR 079570A1 AR P100104797 A ARP100104797 A AR P100104797A AR P100104797 A ARP100104797 A AR P100104797A AR 079570 A1 AR079570 A1 AR 079570A1
- Authority
- AR
- Argentina
- Prior art keywords
- hal
- mono
- mhet2
- atoms
- unsubstituted
- Prior art date
Links
Classifications
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- 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
- A61K31/4985—Pyrazines or piperazines 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Hematology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los compuestos de pirrolo[2,3-d]pirazin-7-il-pirimidina son inhibidores de la proliferacion celular/actividad celular y pueden ser utilizados para el tratamiento de tumores. Procedimiento de obtencion, medicamentos y usos. Reivindicacion 1: Compuestos de la formula (1) en donde significan R1 H, A, Hal, [C(R3)2]mCN, [C(R3)2]mHet1, [C(R3)2]mAr', [C(R3)2]mCyc, [C(R3)2]mR3 o [C(R3)2]mN(R3)2, R2 A, C(R3)(R4)Ar, C(R3)(R4)Het o C(R3)(R4)Cyc, R3 H o A', R4 H, A, [C(R3)2]mOH, [C(R3)2]mOA, [C(R3)2]mN(R3)2 o [C(R3)2]mHet, R5 H, A, N(R3)2, OR3 o SR3, R6 H o Hal, Ar fenilo, naftilo o bifenilo insustituido o mono, bi o trisustituido por Hal, A, (CH2)mOR3, (CH2)mN(R3)2, SR3, NO2, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, COR3, (CH2)nCN y/o S(O)nA, Ar' fenilo, naftilo o bifenilo insustituido o mono, bi o trisustituido por Hal, A, (CH2)mOR3, SR3, NO2, (CH2)mCN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, [C(R3)2]nCOHet2, [C(R3)2]mN(R3)2, [C(R3)2]mHet2, O[C(R3)2]mHet2, O[C(R3)2]pN(R3)2, O[C(R3)2]mHet2, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]pN(R3)2, NHCOO[C(R3)2]pHet2, OCONH[C(R3)2]nN(R3)2, CHO y/o COA, Het un heterociclo mono o binuclear, saturado, insaturado o aromático, insustituido o mono o bisustituido por Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3 y/o S(O)nA, con 1 a 4 átomos de N, y/o O y/o S, Het1 un heterociclo mono, bi o trinuclear saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede ser insustituido o mono o bisustituido por Hal, A, OR3, SR3, NO2, [C(R3)2]nCOOR3, [C(R3)2]mCON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COR3, [C(R3)2]mCOHet2, (CH2)nCN, [C(R3)2]mN(R3)2, [C(R3)2]mHet2, O[C(R3)2]mHet2, O[C(R3)2]pN(R3)2, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]pN(R3)2, NHCOO[C(R3)2]nHet2, CHO, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]mHet2, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]mHet2, COA, C(R3)2]mCONH[C(R3)2]mN(R3)2, =S, =NH, =NA y/o =O (oxígeno carbonilo); Het2 un heterociclo mono o binuclear aromático, insaturado o saturado con 1 a 2 átomos N y/u O, insustituido o mono, bi o trisustituido por A, OA, OH, Hal y/o =O (oxígeno carbonilo), A alquilo no ramificado o de cadena ramificada, C1-10, en donde 1-7 átomos de H pueden estar reemplazados por F, CI y/o Br, y/o en donde uno o dos grupos no adyacentes de grupos CH y/o CH2 pueden estar reemplazados por NR3, O, S, SO, SO2, C:::C y/o grupos CH=CH, o alquilo cíclico C3-7; A' alquilo no ramificado o de cadena ramificada, C1-6, en donde 1-5 átomos de H pueden estar reemplazados por F, Cyc cicloalquilo C3-7, Hal F, CI, Br o I, n 0,1 o 2, m 0, 1, 2, 3 o 4, p 1, 2, 3 o 4 así como sus sales de uso farmacéutico, tautomeros y estereoisomeros, inclusive sus mezclas en todas las proporciones.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102009060175A DE102009060175A1 (de) | 2009-12-23 | 2009-12-23 | Pyrrolo[2,3-d] pyrazin-7-yl-pyrimidin-Verbindungen |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079570A1 true AR079570A1 (es) | 2012-02-01 |
Family
ID=43638852
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104797A AR079570A1 (es) | 2009-12-23 | 2010-12-20 | Compuestos de pirrolo(2,3-d)pirazin-7-il-pirimidina |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8999986B2 (es) |
| EP (1) | EP2516442B1 (es) |
| JP (1) | JP5718359B2 (es) |
| CN (1) | CN102666544B (es) |
| AR (1) | AR079570A1 (es) |
| AU (1) | AU2010335639B2 (es) |
| CA (1) | CA2785329C (es) |
| DE (1) | DE102009060175A1 (es) |
| ES (1) | ES2449697T3 (es) |
| WO (1) | WO2011076327A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102010049877A1 (de) * | 2010-11-01 | 2012-05-03 | Merck Patent Gmbh | 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate |
| CA2850551A1 (en) * | 2011-09-30 | 2013-04-04 | Endo Pharmaceuticals Inc. | Pyridine derivatives |
| US8809372B2 (en) | 2011-09-30 | 2014-08-19 | Asana Biosciences, Llc | Pyridine derivatives |
| CN106349217B (zh) | 2012-03-01 | 2020-08-28 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP2015533151A (ja) * | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| CA2992945A1 (en) | 2015-07-17 | 2017-01-26 | Memorial Sloan-Kettering Cancer Center | Combination therapy using pdk1 and pi3k inhibitors |
| EP4067351A4 (en) * | 2019-11-29 | 2023-11-22 | Medshine Discovery Inc. | DIAZAINDOLE DERIVATIVE AND ITS USE AS CHK1 INHIBITOR |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5747469A (en) | 1991-03-06 | 1998-05-05 | Board Of Regents, The University Of Texas System | Methods and compositions comprising DNA damaging agents and p53 |
| GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| RU2394825C2 (ru) | 2004-11-22 | 2010-07-20 | Вертекс Фармасьютикалз Инкорпорейтед | Пирролопиразины, пригодные в качестве ингибиторов киназы аврора а |
| EP1896470B1 (en) | 2005-05-16 | 2010-05-26 | Irm Llc | Pyrrolopyridine derivatives as protein kinase inhibitors |
| DE102006012617A1 (de) * | 2006-03-20 | 2007-09-27 | Merck Patent Gmbh | 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate |
| DE102007028515A1 (de) | 2007-06-21 | 2008-12-24 | Merck Patent Gmbh | 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate |
-
2009
- 2009-12-23 DE DE102009060175A patent/DE102009060175A1/de not_active Withdrawn
-
2010
- 2010-11-24 AU AU2010335639A patent/AU2010335639B2/en not_active Ceased
- 2010-11-24 JP JP2012545119A patent/JP5718359B2/ja not_active Expired - Fee Related
- 2010-11-24 WO PCT/EP2010/007134 patent/WO2011076327A1/de active Application Filing
- 2010-11-24 ES ES10788014.8T patent/ES2449697T3/es active Active
- 2010-11-24 US US13/518,419 patent/US8999986B2/en not_active Expired - Fee Related
- 2010-11-24 CA CA2785329A patent/CA2785329C/en not_active Expired - Fee Related
- 2010-11-24 EP EP10788014.8A patent/EP2516442B1/de not_active Not-in-force
- 2010-11-24 CN CN201080057854.3A patent/CN102666544B/zh not_active Expired - Fee Related
- 2010-12-20 AR ARP100104797A patent/AR079570A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011076327A1 (de) | 2011-06-30 |
| CA2785329A1 (en) | 2011-06-30 |
| ES2449697T3 (es) | 2014-03-20 |
| CA2785329C (en) | 2017-09-05 |
| CN102666544B (zh) | 2014-11-26 |
| AU2010335639A1 (en) | 2012-08-09 |
| EP2516442A1 (de) | 2012-10-31 |
| JP2013515686A (ja) | 2013-05-09 |
| JP5718359B2 (ja) | 2015-05-13 |
| DE102009060175A1 (de) | 2011-06-30 |
| US20120270880A1 (en) | 2012-10-25 |
| EP2516442B1 (de) | 2013-12-25 |
| CN102666544A (zh) | 2012-09-12 |
| AU2010335639B2 (en) | 2016-03-03 |
| US8999986B2 (en) | 2015-04-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |