AR070212A1 - Derivados de 4-(pirrolo[2,3-c]piridin-3-il)-pirimidinil-2-amina, proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores, metastasis tumoral y/o sida. - Google Patents
Derivados de 4-(pirrolo[2,3-c]piridin-3-il)-pirimidinil-2-amina, proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores, metastasis tumoral y/o sida.Info
- Publication number
- AR070212A1 AR070212A1 ARP090100174A ARP090100174A AR070212A1 AR 070212 A1 AR070212 A1 AR 070212A1 AR P090100174 A ARP090100174 A AR P090100174A AR P090100174 A ARP090100174 A AR P090100174A AR 070212 A1 AR070212 A1 AR 070212A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hal
- tumor
- pirimidinil
- pirrolo
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 208000030507 AIDS Diseases 0.000 title 1
- 206010027476 Metastases Diseases 0.000 title 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 230000009401 metastasis Effects 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los compuestos de la formula 1 en donde R1 es H, A, -[C(R6)2]nAr, -[C(R6)2]nHet o -[C(R6)2]ncicloalquilo, R2 es H, A, bencilo o CH2CH2OR6, R3, R4 son cada uno, de modo independiente entre sí, H, A, Hal, CN, -[C(R6)2]nAr, -[C(R6)2]nHet o -[C(R6)2]ncicloalquilo; R5 es H o alquilo C1-6, R6 es H o alquilo C1-6; A es alquilo no ramificado o ramificado C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupas -CH=CH y/o también 1-7 atamos de H pueden estar reemplazados por F, cicloalquilo es alquilo cíclico C3-7, que adicionalmente puede estar sustituido con alquilo C1-6; Hal es F, Cl, Br o I; Ar es fenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2N(R6)2 y/o S(O)pA, Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico no sustituido o mono- o disustituido con Hal, A, OR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2NR6, S(O)pA y/u =O (oxigeno del carbonilo) con 1 a 4 átomos de N y/u O y/o S, n es 0, 1, 2, 3 o 4; p es 0, 1 o 2, así como sus sales, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la proliferacion celular / vitalidad celular y se pueden emplear para el tratamiento de tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008005493A DE102008005493A1 (de) | 2008-01-22 | 2008-01-22 | 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070212A1 true AR070212A1 (es) | 2010-03-25 |
Family
ID=40386204
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100174A AR070212A1 (es) | 2008-01-22 | 2009-01-21 | Derivados de 4-(pirrolo[2,3-c]piridin-3-il)-pirimidinil-2-amina, proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores, metastasis tumoral y/o sida. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20100292262A1 (es) |
| EP (1) | EP2231664A1 (es) |
| JP (1) | JP5524864B2 (es) |
| KR (1) | KR20100112626A (es) |
| CN (1) | CN101918404A (es) |
| AR (1) | AR070212A1 (es) |
| AU (1) | AU2008348816B2 (es) |
| BR (1) | BRPI0821936A2 (es) |
| CA (1) | CA2712612A1 (es) |
| DE (1) | DE102008005493A1 (es) |
| IL (1) | IL206905A0 (es) |
| MX (1) | MX2010007927A (es) |
| WO (1) | WO2009092431A1 (es) |
| ZA (1) | ZA201005959B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101723936B (zh) * | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
| EP2714688B1 (en) | 2011-05-26 | 2016-02-24 | Daiichi Sankyo Company, Limited | Heterocyclic compounds as protein kinase inhibitors |
| CN104918919A (zh) | 2012-11-21 | 2015-09-16 | Ptc医疗公司 | 取代的反向嘧啶Bmi-1抑制剂 |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| US10370371B2 (en) | 2013-08-30 | 2019-08-06 | Ptc Therapeutics, Inc. | Substituted pyrimidine Bmi-1 inhibitors |
| TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 |
| TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
| WO2015076800A1 (en) | 2013-11-21 | 2015-05-28 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine bmi-1 inhibitors |
| MX371152B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | Nuevos derivados de pirazolopirimidina como inhibidores de la cinasa inductora de nf-kb (nk). |
| AU2015334917B2 (en) * | 2014-10-23 | 2019-08-29 | Janssen Pharmaceutica Nv | New compounds as NIK inhibitors |
| BR112017008039B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| AU2015334914B2 (en) | 2014-10-23 | 2019-09-19 | Janssen Pharmaceutica Nv | New thienopyrimidine derivatives as NIK inhibitors |
| CA3109386A1 (en) | 2018-08-17 | 2020-03-19 | Ptc Therapeutics, Inc. | Use of 5-fluoro-2-(6-fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine in the treatment of pancreatic cancer |
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 |
| EP1773807A2 (en) * | 2004-06-14 | 2007-04-18 | Takeda San Diego, Inc. | Kinase inhibitors |
| WO2006050076A1 (en) | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| EP1931674B1 (en) * | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| DE102006012617A1 (de) * | 2006-03-20 | 2007-09-27 | Merck Patent Gmbh | 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate |
-
2008
- 2008-01-22 DE DE102008005493A patent/DE102008005493A1/de not_active Withdrawn
- 2008-12-23 EP EP08871371A patent/EP2231664A1/de not_active Withdrawn
- 2008-12-23 KR KR1020107018575A patent/KR20100112626A/ko not_active Withdrawn
- 2008-12-23 CA CA2712612A patent/CA2712612A1/en not_active Abandoned
- 2008-12-23 MX MX2010007927A patent/MX2010007927A/es not_active Application Discontinuation
- 2008-12-23 JP JP2010543386A patent/JP5524864B2/ja not_active Expired - Fee Related
- 2008-12-23 WO PCT/EP2008/011098 patent/WO2009092431A1/de not_active Ceased
- 2008-12-23 BR BRPI0821936-2A patent/BRPI0821936A2/pt not_active IP Right Cessation
- 2008-12-23 US US12/863,817 patent/US20100292262A1/en not_active Abandoned
- 2008-12-23 CN CN200880125171XA patent/CN101918404A/zh active Pending
- 2008-12-23 AU AU2008348816A patent/AU2008348816B2/en not_active Ceased
-
2009
- 2009-01-21 AR ARP090100174A patent/AR070212A1/es unknown
-
2010
- 2010-07-08 IL IL206905A patent/IL206905A0/en unknown
- 2010-08-20 ZA ZA2010/05959A patent/ZA201005959B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2712612A1 (en) | 2009-07-30 |
| US20100292262A1 (en) | 2010-11-18 |
| ZA201005959B (en) | 2011-04-28 |
| CN101918404A (zh) | 2010-12-15 |
| JP5524864B2 (ja) | 2014-06-18 |
| KR20100112626A (ko) | 2010-10-19 |
| EP2231664A1 (de) | 2010-09-29 |
| MX2010007927A (es) | 2010-08-09 |
| DE102008005493A1 (de) | 2009-07-23 |
| DE102008005493A8 (de) | 2010-03-25 |
| JP2011510028A (ja) | 2011-03-31 |
| AU2008348816A1 (en) | 2009-07-30 |
| AU2008348816B2 (en) | 2011-10-20 |
| BRPI0821936A2 (pt) | 2015-06-16 |
| WO2009092431A1 (de) | 2009-07-30 |
| IL206905A0 (en) | 2010-12-30 |
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Legal Events
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| FB | Suspension of granting procedure |