TW200843757A - Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors - Google Patents
Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors Download PDFInfo
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- TW200843757A TW200843757A TW097111546A TW97111546A TW200843757A TW 200843757 A TW200843757 A TW 200843757A TW 097111546 A TW097111546 A TW 097111546A TW 97111546 A TW97111546 A TW 97111546A TW 200843757 A TW200843757 A TW 200843757A
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- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 title description 2
- 150000005234 imidazo[1,2-a]pyridines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 154
- 230000001404 mediated effect Effects 0.000 claims abstract description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 222
- -1 C(0)NHMe Chemical compound 0.000 claims description 155
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 120
- 238000000034 method Methods 0.000 claims description 51
- 150000003839 salts Chemical class 0.000 claims description 31
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 26
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 125000004076 pyridyl group Chemical group 0.000 claims description 23
- 229910052731 fluorine Inorganic materials 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 18
- 150000002923 oximes Chemical class 0.000 claims description 18
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 17
- 229910003827 NRaRb Inorganic materials 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 15
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 15
- 125000004429 atom Chemical group 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 229910052763 palladium Inorganic materials 0.000 claims description 12
- 229910052801 chlorine Inorganic materials 0.000 claims description 11
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 11
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 9
- 229910052707 ruthenium Inorganic materials 0.000 claims description 9
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims description 8
- 208000024891 symptom Diseases 0.000 claims description 8
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 7
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- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims description 6
- 125000000468 ketone group Chemical group 0.000 claims description 6
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- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 5
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 claims description 4
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- 238000005859 coupling reaction Methods 0.000 claims description 4
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims description 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 3
- 150000001335 aliphatic alkanes Chemical class 0.000 claims description 3
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims description 3
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- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 2
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- 125000005843 halogen group Chemical group 0.000 claims description 2
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- MWPLVEDNUUSJAV-UHFFFAOYSA-N anthracene Chemical compound C1=CC=CC2=CC3=CC=CC=C3C=C21 MWPLVEDNUUSJAV-UHFFFAOYSA-N 0.000 claims 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 1
- ZRALSGWEFCBTJO-UHFFFAOYSA-N anhydrous guanidine Natural products NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 1
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- 230000009615 deamination Effects 0.000 claims 1
- 238000006481 deamination reaction Methods 0.000 claims 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims 1
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- 101001001642 Xenopus laevis Serine/threonine-protein kinase pim-3 Proteins 0.000 abstract description 5
- 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
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
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- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
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- Pain & Pain Management (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90855607P | 2007-03-28 | 2007-03-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW200843757A true TW200843757A (en) | 2008-11-16 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW097111546A TW200843757A (en) | 2007-03-28 | 2008-03-28 | Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20100144751A1 (enExample) |
| EP (1) | EP2139888A2 (enExample) |
| JP (1) | JP2010522765A (enExample) |
| CN (1) | CN101679422A (enExample) |
| CA (1) | CA2682231A1 (enExample) |
| TW (1) | TW200843757A (enExample) |
| WO (1) | WO2008121687A2 (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2008124323A1 (en) * | 2007-04-03 | 2008-10-16 | Array Biopharma Inc. | Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors |
| WO2009068567A1 (en) | 2007-11-30 | 2009-06-04 | Novartis Ag | C2-c5-alkyl-imidazole-bisphosphonates |
| US8987251B2 (en) | 2008-08-19 | 2015-03-24 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| TWI496779B (zh) | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為pim激酶抑制劑之三唑吡啶化合物 |
| US8557809B2 (en) | 2008-08-19 | 2013-10-15 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| US8895550B2 (en) | 2008-08-19 | 2014-11-25 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| US8377924B2 (en) | 2009-01-21 | 2013-02-19 | Rigel Pharmaceuticals Inc. | Protein kinase C inhibitors and uses thereof |
| AP2799A (en) | 2009-06-05 | 2013-11-30 | Pfizer | 1-(Piperidin-4-YL)-pyrazole derivatives as GPR 119modulators |
| JP5641664B2 (ja) | 2009-10-30 | 2014-12-17 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | イミダゾ[1,2−b]ピリダジン誘導体およびPDE10阻害剤としてのそれらの使用 |
| EP2332917B1 (en) * | 2009-11-11 | 2012-08-01 | Sygnis Bioscience GmbH & Co. KG | Compounds for PIM kinase inhibition and for treating malignancy |
| FR2952934B1 (fr) * | 2009-11-23 | 2012-06-22 | Sanofi Aventis | Derives de pyridino-pyridinones, leur preparation et leur application en therapeutique |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| WO2012066488A2 (en) | 2010-11-17 | 2012-05-24 | Actelion Pharmaceuticals Ltd | Bridged spiro[2.4]heptane ester derivatives |
| PH12013501754A1 (en) * | 2011-02-25 | 2013-10-14 | Array Biopharma Inc | Triazolopyridine compounds as pim kinase inhibitors |
| EP2524915A1 (en) | 2011-05-20 | 2012-11-21 | Sanofi | 2-Amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors |
| BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
| WO2013005057A1 (en) | 2011-07-07 | 2013-01-10 | Centro Nacional De Investigaciones Oncológicas (Cnio) | New compounds |
| WO2013007768A1 (en) | 2011-07-13 | 2013-01-17 | F. Hoffmann-La Roche Ag | Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors |
| CA2851155C (en) | 2011-10-14 | 2021-02-23 | Ambit Biosciences Corporation | Heterocyclic compounds and methods of use thereof |
| MA37618B1 (fr) | 2012-05-16 | 2017-08-31 | Actelion Pharmaceuticals Ltd | Dérivés pontés fluorés de spiro[2.4]heptane en tant qu'agonistes de récepteur alx |
| AU2013283426B2 (en) | 2012-06-26 | 2018-02-22 | Janssen Pharmaceutica Nv | Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| WO2014009305A1 (en) | 2012-07-09 | 2014-01-16 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| DK2900238T3 (en) | 2012-09-28 | 2018-03-12 | Univ Vanderbilt | CONDENSED HETEROCYCLIC COMPOUNDS AS SELECTIVE BMP INHIBITORS |
| CA2897200C (en) | 2013-01-14 | 2021-07-06 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| PE20191245A1 (es) | 2013-01-15 | 2019-09-18 | Incyte Holdings Corp | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim |
| CN105658653A (zh) | 2013-08-23 | 2016-06-08 | 因赛特公司 | 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物 |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | 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 |
| CN104597194B (zh) * | 2015-01-15 | 2016-07-06 | 武汉轻工大学 | 3-氯-1,2-丙二醇的高效液相色谱-荧光检测方法 |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | 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 |
| BR112020005489A2 (pt) | 2017-09-22 | 2020-09-24 | Jubilant Epipad Llc, | composto da fórmula (i), composto de fórmula (ii), composto de fórmula (iii), processo de preparação de compostos de fórmula (i), processo de preparação de compostos de fórmula (ii), processo de preparação de compostos de fórmula (iii), composição farmacêutica, método para inibir uma ou mais famílias pad em uma célula, método para tratar uma afeção mediada por um ou mais pads, utilização do composto, método para o tratamento e/ou prevenção de uma afeção mediada por um ou mais distúrbios da família pad, método para o tratamento de artrite reumatoide e método de tratamento de câncer |
| CN111225915B (zh) | 2017-10-18 | 2023-03-07 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的咪唑并吡啶化合物 |
| EP3707135A1 (en) | 2017-11-06 | 2020-09-16 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation |
| IL274762B2 (en) | 2017-11-24 | 2023-10-01 | Jubilant Episcribe Llc | Novel heterocyclic compounds as prmt5 inhibitors |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3765453A1 (en) | 2018-03-13 | 2021-01-20 | Jubilant Prodel LLC | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| US10745400B2 (en) | 2018-03-14 | 2020-08-18 | Vanderbuilt University | Inhibition of BMP signaling, compounds, compositions and uses thereof |
| CN110833556A (zh) * | 2018-08-15 | 2020-02-25 | 广西梧州制药(集团)股份有限公司 | 吡唑并嘧啶衍生物在治疗肝纤维化的用途 |
| EP4660192A1 (en) * | 2020-08-05 | 2025-12-10 | The General Hospital Corporation | Salt inducible kinase inhibitors |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA75055C2 (uk) * | 1999-11-30 | 2006-03-15 | Пфайзер Продактс Інк. | Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі |
| DE60318198T2 (de) * | 2002-05-02 | 2008-12-04 | Merck & Co., Inc. | Tyrosinkinase-hemmer |
| US20050124637A1 (en) * | 2003-08-15 | 2005-06-09 | Irm Llc | Compounds and compositions as inhibitors of receptor tyrosine kinase activity |
| US20050256309A1 (en) * | 2004-05-12 | 2005-11-17 | Altenbach Robert J | Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands |
-
2008
- 2008-03-27 EP EP08732914A patent/EP2139888A2/en not_active Withdrawn
- 2008-03-27 JP JP2010501214A patent/JP2010522765A/ja active Pending
- 2008-03-27 WO PCT/US2008/058385 patent/WO2008121687A2/en not_active Ceased
- 2008-03-27 CN CN200880017972A patent/CN101679422A/zh active Pending
- 2008-03-27 US US12/593,041 patent/US20100144751A1/en not_active Abandoned
- 2008-03-27 CA CA002682231A patent/CA2682231A1/en not_active Abandoned
- 2008-03-28 TW TW097111546A patent/TW200843757A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2010522765A (ja) | 2010-07-08 |
| WO2008121687A2 (en) | 2008-10-09 |
| US20100144751A1 (en) | 2010-06-10 |
| CN101679422A (zh) | 2010-03-24 |
| EP2139888A2 (en) | 2010-01-06 |
| WO2008121687A3 (en) | 2008-11-20 |
| CA2682231A1 (en) | 2008-10-09 |
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