AR085602A1 - Inhibidores de quinasas, composiciones farmaceuticas y su aplicacion en el tratamiento de canceres y trastornos autoinmunes - Google Patents
Inhibidores de quinasas, composiciones farmaceuticas y su aplicacion en el tratamiento de canceres y trastornos autoinmunesInfo
- Publication number
- AR085602A1 AR085602A1 ARP120100685A ARP120100685A AR085602A1 AR 085602 A1 AR085602 A1 AR 085602A1 AR P120100685 A ARP120100685 A AR P120100685A AR P120100685 A ARP120100685 A AR P120100685A AR 085602 A1 AR085602 A1 AR 085602A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- optionally substituted
- halo
- cycloalkyl
- alkyl
- Prior art date
Links
- 208000023275 Autoimmune disease Diseases 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 102000001253 Protein Kinase Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 108060006633 protein kinase Proteins 0.000 title 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 1
- -1 CONMe2 Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 150000004292 cyclic ethers Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
Classifications
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- 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
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
Composiciones farmacéuticas que comprenden estos compuestos. La presente proporciona además métodos para utilizar estos compuestos y composiciones para el tratamiento de trastornos asociados con niveles no deseados de la actividad de la PIM quinasa, incluyendo cánceres y trastornos autoinmunes.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: Z es N o CH; Q es H, Me u -OH; R3 es H, Me o alquilo C2-4; X es H o F; J es H o NH2; Y2 e Y6 son cada uno independientemente F o Cl, preferiblemente F; Y3 es H o se selecciona del grupo formado por CN, OEt, S(O)pR, -O(CH2)q-OH, -O(CH2)q-OR, -(CH2)q-OH, -C(CH3)2OH, -(CH2)q-OR, -(CR’2)1-3-OR’ u O-(CR’2)1-3-OR’, donde cada R’ es independientemente H o Me, y opcionalmente un miembro sustituido seleccionado del grupo que consiste de alquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxilo C1-4, alqueniloxilo C2-4, alquiniloxilo C2-4, alquiltio C1-4, alquilsulfonilo C1-4, hidroxialquilo C1-4, hidroxialquiloxilo C1-4, cicloalquilo C3-7, heterocicloalquilo C3-7, heteroarilo C5-10, y arilo C6-10, cada uno de los cuales es opcionalmente sustituido con hasta tres grupos seleccionados independientemente entre halo, hidroxilo, amino, OMe, CN, oxo, R y OR; cuando Y3 es H, Y4 se selecciona del grupo que consta CN, R, vinilo, COOH, COOR, S(O)qR, -O(CH2)q-OH, -O(CH2)q-O, -(CH2)q-OH, -C(CH3)2OH, -(CH2)pOR, (CH2)qR, -O-(CH2)qR, -(CR’2)1-3-OR’ u -O-(CR’2)1-3-OR’ en donde cada R’ es independientemente H o Me, y un miembro opcionalmente sustituido seleccionado del grupo que consiste de alquilo C1-4, alcoxilo C1-4, alquiltio C1-4, alquilsulfonilo C1-4, hidroxialquilo C1-4, hidroxialquiloxilo C1-4, cicloalquilo C3-7, heterocicloalquilo C3-7, heteroarilo C5-10, y arilo C6-10, cada uno de los cuales es opcionalmente sustituido con hasta dos grupos seleccionados independientemente entre halo, hidroxilo, amino, OMe, CN, oxo, R y OR; e Y4 puede ser H, cuando Y3 no es H; o Y3 e Y4 tomados juntos forman un anillo de 5 - 6 miembros seleccionado entre cicloalquilo, cicloalquenilo, heterociclilo, heteroarilo y arilo, tal anillo es opcionalmente sustituido con hasta dos grupos seleccionados independientemente entre R, halo, -OH, -OR, -(CH2)1-3-OR, -O-(CH2)1-3-OR, -(CH2)q-OH, y (CH2)q-OH; cada R es independientemente un alquilo C1-4, cicloalquilo C3-7, cicloalquenilo C5-6, heterociclilo C5-6, o éter cíclico de 3 - 7 miembros opcionalmente sustituido, en donde los sustituyentes opcionales para R se seleccionan independientemente entre OH, Me, -CH2OH, COOH, COOMe, CONH2, CONHMe, CONMe2, CF3, OMe, CN, NH2, halo, oxo, y CN; cada q es independientemente 1 ó 2; y cada p es independientemente 0, 1 ó 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161449229P | 2011-03-04 | 2011-03-04 | |
| US201161480015P | 2011-04-28 | 2011-04-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR085602A1 true AR085602A1 (es) | 2013-10-16 |
Family
ID=45873194
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100685A AR085602A1 (es) | 2011-03-04 | 2012-03-02 | Inhibidores de quinasas, composiciones farmaceuticas y su aplicacion en el tratamiento de canceres y trastornos autoinmunes |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20120225062A1 (es) |
| EP (1) | EP2681195A1 (es) |
| JP (1) | JP2014506917A (es) |
| CN (1) | CN103402984A (es) |
| AR (1) | AR085602A1 (es) |
| TW (1) | TW201240986A (es) |
| UY (1) | UY33930A (es) |
| WO (1) | WO2012120428A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008221263B2 (en) * | 2007-03-01 | 2012-02-23 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| US9173883B2 (en) * | 2012-05-21 | 2015-11-03 | Novartis Ag | Ring-substituted N-pyridinyl amides as kinase inhibitors |
| WO2014043633A1 (en) | 2012-09-17 | 2014-03-20 | Agios Pharmaceuticals, Inc. | Use of e-cadherin and vimentin for selection of treatment responsive patients |
| KR102281288B1 (ko) | 2012-09-26 | 2021-07-26 | 에프. 호프만-라 로슈 아게 | 환형 에터 피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 이의 사용 방법 |
| SG11201504022RA (en) | 2012-11-21 | 2015-06-29 | Agios Pharmaceuticals Inc | Glutamase inhibitors and method of use |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
| WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| ES2790419T3 (es) | 2013-01-15 | 2020-10-27 | Incyte Holdings Corp | Los compuestos de tiazolcarboxamidas y piridinacarboxamida útiles como inhibidores de quinasa de PIM |
| US9556197B2 (en) | 2013-08-23 | 2017-01-31 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| KR20160127140A (ko) | 2014-03-18 | 2016-11-02 | 에프. 호프만-라 로슈 아게 | 옥세판-2-일-피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 사용 방법 |
| JP6602364B2 (ja) * | 2014-03-21 | 2019-11-06 | アジオス ファーマシューティカルズ， インコーポレイテッド | 化合物及びそれらの使用の方法 |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| JO3589B1 (ar) * | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| GB201702221D0 (en) | 2017-02-10 | 2017-03-29 | Univ Of Sussex | Compounds |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| GB201803340D0 (en) | 2018-03-01 | 2018-04-18 | Univ Of Sussex | Compounds |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2061762B1 (en) | 2006-08-16 | 2011-07-27 | Boehringer Ingelheim International GmbH | Pyrazine compounds, their use and methods of preparation |
| AU2008221263B2 (en) * | 2007-03-01 | 2012-02-23 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| NZ582708A (en) * | 2007-07-19 | 2012-04-27 | Schering Corp | Heterocyclic amide compounds as protein kinase inhibitors |
| UY31679A1 (es) * | 2008-03-03 | 2009-09-30 | Inhibidores de cinasa pim y metodos para su uso | |
| RS54506B1 (sr) * | 2008-09-02 | 2016-06-30 | Novartis Ag | Derivati pikolinamida kao inhibitori kinaza |
| EP2590968A1 (en) * | 2010-07-06 | 2013-05-15 | Novartis AG | Cyclic ether compounds useful as kinase inhibitors |
-
2012
- 2012-03-01 UY UY0001033930A patent/UY33930A/es not_active Application Discontinuation
- 2012-03-02 EP EP12709966.1A patent/EP2681195A1/en not_active Withdrawn
- 2012-03-02 US US13/410,845 patent/US20120225062A1/en not_active Abandoned
- 2012-03-02 WO PCT/IB2012/051005 patent/WO2012120428A1/en not_active Ceased
- 2012-03-02 JP JP2013555986A patent/JP2014506917A/ja active Pending
- 2012-03-02 CN CN2012800117264A patent/CN103402984A/zh active Pending
- 2012-03-02 AR ARP120100685A patent/AR085602A1/es unknown
- 2012-03-03 TW TW101107234A patent/TW201240986A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN103402984A (zh) | 2013-11-20 |
| TW201240986A (en) | 2012-10-16 |
| EP2681195A1 (en) | 2014-01-08 |
| US20120225062A1 (en) | 2012-09-06 |
| JP2014506917A (ja) | 2014-03-20 |
| UY33930A (es) | 2012-10-31 |
| WO2012120428A1 (en) | 2012-09-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |