CA2882410A1 - Dihydropyrrolidino-pyrimidines as kinase inhibitors - Google Patents
Dihydropyrrolidino-pyrimidines as kinase inhibitors Download PDFInfo
- Publication number
- CA2882410A1 CA2882410A1 CA2882410A CA2882410A CA2882410A1 CA 2882410 A1 CA2882410 A1 CA 2882410A1 CA 2882410 A CA2882410 A CA 2882410A CA 2882410 A CA2882410 A CA 2882410A CA 2882410 A1 CA2882410 A1 CA 2882410A1
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- Prior art keywords
- alkyl
- compound
- optionally substituted
- amino
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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- 229950001603 taplitumomab paptox Drugs 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
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- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 description 1
- 229960001278 teniposide Drugs 0.000 description 1
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- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
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- 238000003354 tissue distribution assay Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 239000012443 tonicity enhancing agent Substances 0.000 description 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 description 1
- 229960000303 topotecan Drugs 0.000 description 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
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- 230000037317 transdermal delivery Effects 0.000 description 1
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- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 125000004385 trihaloalkyl group Chemical group 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
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- 238000004704 ultra performance liquid chromatography Methods 0.000 description 1
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 description 1
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- UGGWPQSBPIFKDZ-KOTLKJBCSA-N vindesine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(N)=O)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1N=C1[C]2C=CC=C1 UGGWPQSBPIFKDZ-KOTLKJBCSA-N 0.000 description 1
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Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
- C07D207/36—Oxygen or sulfur atoms
-
- 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
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702981P | 2012-09-19 | 2012-09-19 | |
| US61/702,981 | 2012-09-19 | ||
| PCT/US2013/060032 WO2014047020A1 (en) | 2012-09-19 | 2013-09-17 | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2882410A1 true CA2882410A1 (en) | 2014-03-27 |
Family
ID=49274870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2882410A Abandoned CA2882410A1 (en) | 2012-09-19 | 2013-09-17 | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9546173B2 (OSRAM) |
| EP (1) | EP2897961B1 (OSRAM) |
| JP (1) | JP6186440B2 (OSRAM) |
| KR (1) | KR20150056550A (OSRAM) |
| CN (1) | CN104640865B (OSRAM) |
| AU (1) | AU2013318283A1 (OSRAM) |
| BR (1) | BR112015005982A2 (OSRAM) |
| CA (1) | CA2882410A1 (OSRAM) |
| EA (1) | EA201590600A1 (OSRAM) |
| ES (1) | ES2612885T3 (OSRAM) |
| IN (1) | IN2015DN01328A (OSRAM) |
| MX (1) | MX2015003535A (OSRAM) |
| WO (1) | WO2014047020A1 (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150274733A1 (en) * | 2012-09-19 | 2015-10-01 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7349491B2 (ja) | 2018-07-12 | 2023-09-22 | ユーシービー バイオファルマ エスアールエル | Ｉｌ－１７モジュレーターとしてのスピロ環状インダン類似体 |
| WO2020243457A1 (en) * | 2019-05-29 | 2020-12-03 | Viogen Biosciences, Llc | Compounds and therapeutic uses thereof |
| CN114502546A (zh) * | 2019-08-01 | 2022-05-13 | 普拉特戈公司 | 晚期糖基化终产物的抑制剂 |
| WO2021116055A1 (en) | 2019-12-10 | 2021-06-17 | F. Hoffmann-La Roche Ag | New methylquinazolinone derivatives |
| MX2022006711A (es) * | 2019-12-10 | 2022-07-12 | Hoffmann La Roche | Nuevos inhibidores de braf como rompedores de la paradoja. |
| WO2021218912A1 (zh) | 2020-04-30 | 2021-11-04 | 南京明德新药研发有限公司 | 含苯基并内磺酰胺的化合物 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7208498B2 (en) * | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| US7244735B2 (en) * | 2003-12-02 | 2007-07-17 | Vertex Pharmaceuticals Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| AP2007004061A0 (en) | 2005-01-10 | 2007-08-31 | Galloway & Company | Pyrrolopyrazoles, potent kinase inhibitors |
| CA2633023C (en) | 2005-12-13 | 2015-11-24 | Schering Corporation | Polycyclic indazole derivatives that are erk inhibitors |
| KR20100025553A (ko) | 2007-06-05 | 2010-03-09 | 쉐링 코포레이션 | 암 치료용 ｅｒｋ 억제제로서의 폴리사이클릭 인다졸 유도체 및 이의 용도 |
| US8946216B2 (en) | 2010-09-01 | 2015-02-03 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as ERK inhibitors |
| EP2615916B1 (en) * | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel erk inhibitors |
| KR20130121122A (ko) | 2010-11-17 | 2013-11-05 | 에프. 호프만-라 로슈 아게 | 종양의 치료 방법 |
| CA2828478C (en) * | 2011-02-28 | 2019-12-31 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| AU2013225531A1 (en) | 2012-03-02 | 2014-09-25 | Forma Tm, Llc. | Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives |
| EP2897961B1 (en) * | 2012-09-19 | 2016-10-26 | Novartis AG | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
-
2013
- 2013-09-17 EP EP13771007.5A patent/EP2897961B1/en active Active
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
- 2013-09-17 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 BR BR112015005982A patent/BR112015005982A2/pt not_active IP Right Cessation
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 2013-09-17 ES ES13771007.5T patent/ES2612885T3/es active Active
- 2013-09-17 CA CA2882410A patent/CA2882410A1/en not_active Abandoned
- 2013-09-17 JP JP2015533126A patent/JP6186440B2/ja active Active
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 2013-09-17 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150274733A1 (en) * | 2012-09-19 | 2015-10-01 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| US9546173B2 (en) * | 2012-09-19 | 2017-01-17 | Novartis Ag | Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2612885T3 (es) | 2017-05-19 |
| US9546173B2 (en) | 2017-01-17 |
| IN2015DN01328A (OSRAM) | 2015-07-03 |
| EP2897961B1 (en) | 2016-10-26 |
| BR112015005982A2 (pt) | 2017-07-04 |
| EP2897961A1 (en) | 2015-07-29 |
| EA201590600A1 (ru) | 2015-07-30 |
| KR20150056550A (ko) | 2015-05-26 |
| US20150274733A1 (en) | 2015-10-01 |
| JP6186440B2 (ja) | 2017-08-23 |
| CN104640865B (zh) | 2018-05-11 |
| AU2013318283A1 (en) | 2015-03-05 |
| JP2015529248A (ja) | 2015-10-05 |
| MX2015003535A (es) | 2015-07-14 |
| CN104640865A (zh) | 2015-05-20 |
| WO2014047020A1 (en) | 2014-03-27 |
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