PE20160593A1 - Tienopirimidinas como inhibidores mknk1 y mknk2 - Google Patents
Tienopirimidinas como inhibidores mknk1 y mknk2Info
- Publication number
- PE20160593A1 PE20160593A1 PE2016000657A PE2016000657A PE20160593A1 PE 20160593 A1 PE20160593 A1 PE 20160593A1 PE 2016000657 A PE2016000657 A PE 2016000657A PE 2016000657 A PE2016000657 A PE 2016000657A PE 20160593 A1 PE20160593 A1 PE 20160593A1
- Authority
- PE
- Peru
- Prior art keywords
- mknk2
- mknk1
- pyrimidines
- inhibitors
- benzothieno
- Prior art date
Links
- 101000573522 Homo sapiens MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 title abstract 2
- 101001018978 Homo sapiens MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 title abstract 2
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 title abstract 2
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- FSHHAIJBKKRUTN-NSHDSACASA-N (7S)-4-(1H-indazol-5-ylamino)-N,N-dimethyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidine-7-carboxamide Chemical compound N1N=CC2=CC(=CC=C12)NC=1C2=C(N=CN1)SC1=C2CC[C@@H](C1)C(=O)N(C)C FSHHAIJBKKRUTN-NSHDSACASA-N 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- BJBQPIYJUJWWNQ-LBPRGKRZSA-N azetidin-1-yl-[(7S)-4-(1H-indazol-5-ylamino)-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-7-yl]methanone Chemical compound N1(CCC1)C(=O)[C@@H]1CC2=C(CC1)C1=C(N=CN=C1NC=1C=C3C=NNC3=CC1)S2 BJBQPIYJUJWWNQ-LBPRGKRZSA-N 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- RBNBDIMXFJYDLQ-UHFFFAOYSA-N thieno[3,2-d]pyrimidine Chemical class C1=NC=C2SC=CC2=N1 RBNBDIMXFJYDLQ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Referida a derivados de tienopirimidina de formula I, donde: R1 es C(=O)N(R3)(R4); R2a y R2b son H; R2c es H o halogeno; R2d es H, halogeno, entre otros.; R3 es C1-C6alquilo, C1-C6 alcoxi, entre otros; R4 es C1-C4alquilo, entre otros. Son compuestos preferidos: (7S)-4-(1H-indazol-5-ilamino)-N,N-dimetil-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidin-7-carboxamida; azetidin-1-il[(7S)-4-(1H-indazol-5-ilamino)-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidin-7-il]metanona, entre otros. dichos compuestos inhiben MKNK1 Y MKNK2, siendo utiles en el tratamiento de trastornos hiperproliferativos y/o angiogenesis.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13193665 | 2013-11-20 | ||
| EP14174731 | 2014-06-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160593A1 true PE20160593A1 (es) | 2016-07-13 |
Family
ID=52000798
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000657A PE20160593A1 (es) | 2013-11-20 | 2014-11-17 | Tienopirimidinas como inhibidores mknk1 y mknk2 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20160297833A1 (es) |
| EP (1) | EP3071577A1 (es) |
| JP (1) | JP2016539113A (es) |
| KR (1) | KR20160086404A (es) |
| CN (1) | CN106061980A (es) |
| AP (1) | AP2016009225A0 (es) |
| AU (1) | AU2014352066A1 (es) |
| BR (1) | BR112016011472A2 (es) |
| CA (1) | CA2930873A1 (es) |
| CL (1) | CL2016001218A1 (es) |
| CR (1) | CR20160235A (es) |
| CU (1) | CU20160072A7 (es) |
| DO (1) | DOP2016000118A (es) |
| EA (1) | EA201600398A1 (es) |
| IL (1) | IL245404A0 (es) |
| MX (1) | MX2016006631A (es) |
| PE (1) | PE20160593A1 (es) |
| PH (1) | PH12016500931A1 (es) |
| TN (1) | TN2016000194A1 (es) |
| TW (1) | TW201605867A (es) |
| UY (1) | UY35848A (es) |
| WO (1) | WO2015074986A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI713455B (zh) | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | ＭｎＫ抑制劑及其相關方法 |
| EP3368530A1 (en) | 2015-10-29 | 2018-09-05 | Effector Therapeutics Inc. | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
| EP3368533A1 (en) * | 2015-10-29 | 2018-09-05 | Effector Therapeutics Inc. | Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit mnk1 and mnk2 |
| US10000487B2 (en) | 2015-11-20 | 2018-06-19 | Effector Therapeutics, Inc. | Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers |
| CN106727587A (zh) * | 2016-11-28 | 2017-05-31 | 李娜 | 一种治疗心律失常的药物组合物 |
| CA3050599A1 (en) | 2017-01-20 | 2018-07-26 | Bayer Pharma Aktiengesellschaft | Substituted imidazopyridinpyrimidines |
| EA201991894A1 (ru) | 2017-02-14 | 2020-02-05 | Эффектор Терапьютикс, Инк. | ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ |
| JP2022505846A (ja) | 2018-10-24 | 2022-01-14 | イーフェクター セラピューティクス， インコーポレイテッド | Ｍｎｋ阻害剤の結晶形態 |
| CN110981903A (zh) * | 2019-11-28 | 2020-04-10 | 南京正济医药研究有限公司 | 一种艾日布林中间体化合物提高光学纯度的精制方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005503345A (ja) * | 2001-04-30 | 2005-02-03 | バイエル・コーポレーシヨン | 新規な４−アミノ−５，６−置換チオフェノ［２，３−ｄ］ピリミジン |
| ES2305435T3 (es) * | 2002-01-10 | 2008-11-01 | Bayer Healthcare Ag | Inhibidores de la rho-quinasa. |
| DE602004003952T2 (de) * | 2003-07-24 | 2007-11-08 | Bayer Pharmaceuticals Corp., West Haven | Substituierte tetrahydrobenzothienopyrimidinamine verbindungen geeignet zur behandlung von hyper-proliferative disorders |
| US8207172B2 (en) * | 2004-08-20 | 2012-06-26 | Bayer Intellectual Property Gmbh | Pyrimidinothienoindazoles useful for the treatment of hyperproliferative disorders |
| AR052019A1 (es) * | 2004-10-15 | 2007-02-28 | Bayer Pharmaceuticals Corp | COMPUESTOS HETEROCICLICOS, PROCESOS DE PREPARACIoN Y MÉTODO PARA TRATAR ENFERMEDADES HIPERPROLIFERATIVAS |
| EP1899353A1 (en) * | 2005-06-22 | 2008-03-19 | DeveloGen Aktiengesellschaft | Thienopyrimidines for pharmaceutical compositions |
| WO2007059905A2 (en) * | 2005-11-25 | 2007-05-31 | Develogen Aktiengesellschaft | Thienopyrimidines treating inflammatory diseases |
| EA201201191A1 (ru) * | 2010-02-26 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций |
| BR112014017021A8 (pt) * | 2012-01-10 | 2017-07-04 | Nimbus Iris Inc | inibidores de irak e usos dos mesmos |
| US9540392B2 (en) * | 2012-05-21 | 2017-01-10 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| CA2873971A1 (en) * | 2012-05-21 | 2013-11-28 | Bayer Pharma Aktiengesellschaft | Substituted pyrrolopyrimidines |
| EP2852595B1 (en) * | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Substituted benzothienopyrimidines |
| EP2951187A1 (en) * | 2013-02-01 | 2015-12-09 | Bayer Pharma Aktiengesellschaft | Substituted thienopyrimidines and pharmaceutical use thereof |
| CN105531279A (zh) * | 2013-07-08 | 2016-04-27 | 拜耳制药股份公司 | 取代的吡唑并吡啶胺 |
-
2014
- 2014-11-05 TW TW103138437A patent/TW201605867A/zh unknown
- 2014-11-17 WO PCT/EP2014/074722 patent/WO2015074986A1/en not_active Ceased
- 2014-11-17 EA EA201600398A patent/EA201600398A1/ru unknown
- 2014-11-17 JP JP2016532533A patent/JP2016539113A/ja active Pending
- 2014-11-17 KR KR1020167015876A patent/KR20160086404A/ko not_active Withdrawn
- 2014-11-17 TN TN2016000194A patent/TN2016000194A1/en unknown
- 2014-11-17 BR BR112016011472A patent/BR112016011472A2/pt not_active IP Right Cessation
- 2014-11-17 MX MX2016006631A patent/MX2016006631A/es unknown
- 2014-11-17 EP EP14805505.6A patent/EP3071577A1/en not_active Withdrawn
- 2014-11-17 AU AU2014352066A patent/AU2014352066A1/en not_active Abandoned
- 2014-11-17 PE PE2016000657A patent/PE20160593A1/es not_active Application Discontinuation
- 2014-11-17 CA CA2930873A patent/CA2930873A1/en not_active Abandoned
- 2014-11-17 US US15/037,949 patent/US20160297833A1/en not_active Abandoned
- 2014-11-17 AP AP2016009225A patent/AP2016009225A0/en unknown
- 2014-11-17 CN CN201480072749.5A patent/CN106061980A/zh active Pending
- 2014-11-19 UY UY0001035848A patent/UY35848A/es not_active Application Discontinuation
-
2016
- 2016-05-02 IL IL245404A patent/IL245404A0/en unknown
- 2016-05-19 PH PH12016500931A patent/PH12016500931A1/en unknown
- 2016-05-20 CL CL2016001218A patent/CL2016001218A1/es unknown
- 2016-05-20 CU CUP2016000072A patent/CU20160072A7/es unknown
- 2016-05-20 DO DO2016000118A patent/DOP2016000118A/es unknown
- 2016-05-20 CR CR20160235A patent/CR20160235A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20160297833A1 (en) | 2016-10-13 |
| DOP2016000118A (es) | 2016-06-30 |
| JP2016539113A (ja) | 2016-12-15 |
| CA2930873A1 (en) | 2015-05-28 |
| CR20160235A (es) | 2016-07-20 |
| TW201605867A (zh) | 2016-02-16 |
| TN2016000194A1 (en) | 2017-10-06 |
| MX2016006631A (es) | 2016-08-17 |
| IL245404A0 (en) | 2016-06-30 |
| CU20160072A7 (es) | 2016-10-28 |
| CN106061980A (zh) | 2016-10-26 |
| EP3071577A1 (en) | 2016-09-28 |
| CL2016001218A1 (es) | 2016-12-16 |
| KR20160086404A (ko) | 2016-07-19 |
| WO2015074986A1 (en) | 2015-05-28 |
| AU2014352066A1 (en) | 2016-05-26 |
| UY35848A (es) | 2015-06-30 |
| PH12016500931A1 (en) | 2016-06-27 |
| EA201600398A1 (ru) | 2016-10-31 |
| BR112016011472A2 (pt) | 2017-09-26 |
| AP2016009225A0 (en) | 2016-05-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |