AR073079A1 - Compuestos triazolopiridina como inhibidores de pim cinasa - Google Patents
Compuestos triazolopiridina como inhibidores de pim cinasaInfo
- Publication number
- AR073079A1 AR073079A1 ARP090103170A ARP090103170A AR073079A1 AR 073079 A1 AR073079 A1 AR 073079A1 AR P090103170 A ARP090103170 A AR P090103170A AR P090103170 A ARP090103170 A AR P090103170A AR 073079 A1 AR073079 A1 AR 073079A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- ring
- optionally substituted
- membered
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 19
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 229910052731 fluorine Inorganic materials 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 229910052794 bromium Inorganic materials 0.000 abstract 4
- 229910052801 chlorine Inorganic materials 0.000 abstract 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 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
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 210000002865 immune cell Anatomy 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- 125000001424 substituent group Chemical group 0.000 abstract 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- 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
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Estos compuestos son inhibidores de tirosina de receptor utiles en el tratamiento de enfermedades asociadas con células inmunes, tales como enfermedades inflamatorias y autoinmunes. Se proveen además una composicion farmacéutica que los comprende y un método para su preparacion. Reivindicacion 1: Un compuesto de la formula general (1) o una sal farmacéuticamente aceptable de él, en donde: A es OR10 o NR11R12; B es H, F, Cl, ORa, alquilo C1-6NRbRc, alquilo C1-6OH, CH(OH)CH2OH o alquilo C1-4; R1 es H, F, Cl, Br, Me, ciclopropilo o CN; R1a, R2, R3 y R4 son independientemente H, F, Cl, Br, Me o CN; R5 y R7 son independientemente H, F, Me o CN; R6 es H, F, Me, Br, CN, ciclopropilo, fenilo, MeO- o MeOCH2CH2O-; R10 es H, hetCyc1, alquilo C1-3hetCyc1a, hetCyc2, (CR17R18)p(CR13R14)CH2NR15R16, -(CR17R18)p(CR13R14)CH2OH, alquilo C1-6, hetAr1, alquilo C1-3hetAr1a, o cicloalquilo C3-7 sustituido con NH2, NH-alquilo C1-6 o N(alquilo C1-6)2; R11 es H o alquilo C1-6; R12 es hetCyc3, alquilo C1-6NR15R16, C(O)alquilo C1-6NR15R16, alquilo C1-6NHC(O)O-alquilo C1-6, o cicloalquilo C4-7 optativamente sustituido con OH, NH2, NH-alquilo C1-6 o N(alquilo C1-6)2; R13 es H, alquilo C1-6, F o OH, y R14 es H, alquilo C1-6 o F, o R13 y R14 junto con el átomo de carbono al cual están unidos forman un anillo carbocíclico de 3-6 miembros; cada R15, R16, R17 y R18 es independientemente H o alquilo C1-6, o cada R15, R17, y R18 es independientemente H o alquilo C1-6 y R16 es H, alquilo C1-6, C(=O)CH2F, CH2CHF2 o CH2CF3; o NR15R16 forma un anillo heterocíclico de 5-6 miembros que tiene un primer heteroátomo del anillo que es N y que optativamente tiene un segundo heteroátomo del anillo que es N y O; hetCyc1, hetCyc1a y hetCyc3 son independientemente un heterociclo de 4-7 miembros que tiene un átomo del anillo de nitrogeno y optativamente sustituido con uno o más grupos R9, o hetCyc1 y hetCyc3 son independientemente un heterociclo de 4-7 miembros que tiene un átomo de N y optativamente sustituido con uno o más grupos R9, y hetCyc1a se selecciona de un morfolinilo y un anillo azacíclico de 4-7 miembros optativamente sustituido con uno o más grupos R9; cada R9 se selecciona independientemente de halogeno, alquilo C1-6, ciclopropilmetilo, bencilo, NRfRg, alquilo C1-6NRhRi, ORj, alquilo C1-6ORk, fluoroalquilo C1-6, C(O)NRmRn, alquilo C1-6C(O)NRpRq, y C(O)O-alquilo C1-6; hetCyc2 es un heterociclo de puente de 8 miembros que tiene un átomo de nitrogeno del anillo; hetAr1 y hetAr1a son independientemente un heteroarilo de 5 o 6 miembros que tiene 1-2 átomos de nitrogeno del anillo y optativamente sustituido con uno o más sustituyentes, que se seleccionan independientemente de F, Cl, Br, Me, ciclopropilo, CN, NH2, NH-alquilo C1-6 y N(alquilo C1-6)2; Ra es H, alquilo C1-6, alquilo C1-6-O-alquilo C1-6, o alquilo C1-6-O-cicloalquilo C3-6; cada Rb, Rf, Rg, Rh, Ri, Rk, Rm, Rp, y Rq se selecciona independientemente de H y alquilo C1-6; Rj es H, alquilo C1-6 o ciclopropilo; Rn es H, alquilo C1-6, -O-alquilo C1-6 o -O-cicloalquilo C3-6; y p es 0, 1 o 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8995208P | 2008-08-19 | 2008-08-19 | |
| US17527709P | 2009-05-04 | 2009-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073079A1 true AR073079A1 (es) | 2010-10-13 |
Family
ID=41227138
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103170A AR073079A1 (es) | 2008-08-19 | 2009-08-18 | Compuestos triazolopiridina como inhibidores de pim cinasa |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8575145B2 (es) |
| EP (1) | EP2334677B1 (es) |
| JP (2) | JP5518072B2 (es) |
| CN (1) | CN102186851B (es) |
| AR (1) | AR073079A1 (es) |
| CA (1) | CA2734831C (es) |
| DK (1) | DK2334677T3 (es) |
| ES (1) | ES2439501T3 (es) |
| HR (1) | HRP20131140T1 (es) |
| PL (1) | PL2334677T3 (es) |
| PT (1) | PT2334677E (es) |
| RS (1) | RS53079B (es) |
| SI (1) | SI2334677T1 (es) |
| SM (1) | SMT201400154B (es) |
| TW (1) | TWI496779B (es) |
| UY (1) | UY32057A (es) |
| WO (1) | WO2010022076A1 (es) |
Families Citing this family (73)
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|---|---|---|---|---|
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| EP3838903B1 (en) | 2005-12-13 | 2023-11-22 | Incyte Holdings Corporation | Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor |
| AR059898A1 (es) | 2006-03-15 | 2008-05-07 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2 |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| CN101932582B (zh) | 2007-06-13 | 2013-09-25 | 因塞特公司 | 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐 |
| NZ584148A (en) | 2007-09-14 | 2011-05-27 | Ortho Mcneil Janssen Pharm | 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones |
| CA2696948C (en) | 2007-09-14 | 2013-04-30 | Jose Maria Cid-Nunez | 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones |
| EP2200985B1 (en) | 2007-09-14 | 2011-07-13 | Ortho-McNeil-Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones |
| CN101861316B (zh) | 2007-11-14 | 2013-08-21 | 奥梅-杨森制药有限公司 | 咪唑并[1,2-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| US8987251B2 (en) | 2008-08-19 | 2015-03-24 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| CN102143955B (zh) | 2008-09-02 | 2013-08-14 | Omj制药公司 | 作为代谢型谷氨酸受体调节剂的3-氮杂二环[3.1.0]己烷衍生物 |
| WO2010043396A1 (en) | 2008-10-16 | 2010-04-22 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| JP5690277B2 (ja) | 2008-11-28 | 2015-03-25 | ジャンセン ファーマシューティカルズ， インコーポレイテッド． | 代謝型グルタミン酸受容体の調節因子としてのインドールおよびベンゾオキサジン誘導体 |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| CN102439015B (zh) | 2009-05-12 | 2015-05-13 | 杨森制药有限公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物和其作为mGluR2受体的正向变构调节剂的用途 |
| ES2440001T3 (es) | 2009-05-12 | 2014-01-27 | Janssen Pharmaceuticals, Inc. | Derivados de 1,2,4-triazolo[4,3-A]piridina y su uso para el tratamiento o prevención de trastornos neurológicos y psiquiátricos |
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| RS59632B1 (sr) | 2009-05-22 | 2020-01-31 | Incyte Holdings Corp | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori |
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| ME02386B (me) | 2010-03-10 | 2016-09-20 | Incyte Holdings Corp | Derivati piperidin-4-il azetidina kao inhibitori jak1 |
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| CA2814998C (en) | 2010-11-08 | 2019-10-29 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| US9271967B2 (en) | 2010-11-08 | 2016-03-01 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
| WO2012065297A1 (en) | 2010-11-16 | 2012-05-24 | Impact Therapeutics, Inc. | 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF |
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| DK2964650T3 (en) | 2013-03-06 | 2019-02-11 | Incyte Holdings Corp | PROCEDURES AND INTERMEDIATES FOR THE MANUFACTURE OF A JAK INHIBITOR |
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2009
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- 2009-08-18 AR ARP090103170A patent/AR073079A1/es active IP Right Grant
- 2009-08-18 PL PL09791625T patent/PL2334677T3/pl unknown
- 2009-08-18 SI SI200930782T patent/SI2334677T1/sl unknown
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- 2009-08-18 ES ES09791625.8T patent/ES2439501T3/es active Active
- 2009-08-18 US US13/059,902 patent/US8575145B2/en not_active Expired - Fee Related
- 2009-08-18 EP EP09791625.8A patent/EP2334677B1/en active Active
- 2009-08-18 DK DK09791625.8T patent/DK2334677T3/da active
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- 2009-08-18 HR HRP20131140AT patent/HRP20131140T1/hr unknown
- 2009-08-18 JP JP2011523939A patent/JP5518072B2/ja not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| EP2334677A1 (en) | 2011-06-22 |
| HRP20131140T1 (hr) | 2014-01-03 |
| EP2334677B1 (en) | 2013-10-09 |
| CN102186851A (zh) | 2011-09-14 |
| US8575145B2 (en) | 2013-11-05 |
| WO2010022076A1 (en) | 2010-02-25 |
| TWI496779B (zh) | 2015-08-21 |
| DK2334677T3 (da) | 2013-11-18 |
| PT2334677E (pt) | 2013-11-26 |
| UY32057A (es) | 2011-01-31 |
| SMT201400154B (it) | 2015-01-15 |
| CA2734831C (en) | 2017-04-18 |
| TW201008940A (en) | 2010-03-01 |
| CN102186851B (zh) | 2013-06-12 |
| SI2334677T1 (sl) | 2013-12-31 |
| RS53079B (sr) | 2014-06-30 |
| JP2012500277A (ja) | 2012-01-05 |
| CA2734831A1 (en) | 2010-02-25 |
| JP2014129409A (ja) | 2014-07-10 |
| JP5518072B2 (ja) | 2014-06-11 |
| US20110144085A1 (en) | 2011-06-16 |
| PL2334677T3 (pl) | 2014-03-31 |
| ES2439501T3 (es) | 2014-01-23 |
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