ME02990B - Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze - Google Patents
Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinazeInfo
- Publication number
- ME02990B ME02990B MEP-2018-76A MEP201876A ME02990B ME 02990 B ME02990 B ME 02990B ME P201876 A MEP201876 A ME P201876A ME 02990 B ME02990 B ME 02990B
- Authority
- ME
- Montenegro
- Prior art keywords
- thiourea
- pyrrolidinyl
- guanidine
- pyrazolyl
- race
- Prior art date
Links
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 title 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 title 2
- XAEGRAIWWBXIRR-UHFFFAOYSA-N 1h-pyrazol-5-ylurea Chemical compound NC(=O)NC=1C=CNN=1 XAEGRAIWWBXIRR-UHFFFAOYSA-N 0.000 title 1
- -1 N-Pyrrolidinyl Chemical group 0.000 title 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 title 1
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- QGBSISYHAICWAH-UHFFFAOYSA-N dicyandiamide Chemical class NC(N)=NC#N QGBSISYHAICWAH-UHFFFAOYSA-N 0.000 title 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
- C07C403/14—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by doubly-bound oxygen atoms
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Shaping Metal By Deep-Drawing, Or The Like (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261725913P | 2012-11-13 | 2012-11-13 | |
| EP13795946.6A EP2922844B1 (en) | 2012-11-13 | 2013-11-12 | N-pyrrolidinyl, n'-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| PCT/US2013/069729 WO2014078323A1 (en) | 2012-11-13 | 2013-11-12 | N-pyrrolidinyl, n'-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02990B true ME02990B (me) | 2018-10-20 |
Family
ID=49667600
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2018-76A ME02990B (me) | 2012-11-13 | 2013-11-12 | Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze |
Country Status (32)
Families Citing this family (60)
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| ES2464461T3 (es) | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
| SG196855A1 (en) | 2008-10-22 | 2014-02-13 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| AU2011256380C1 (en) | 2010-05-20 | 2016-09-08 | Array Biopharma Inc. | Macrocyclic compounds as Trk kinase inhibitors |
| HRP20161786T1 (hr) * | 2011-05-13 | 2017-03-10 | Array Biopharma, Inc. | Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze |
| US9828360B2 (en) | 2012-11-13 | 2017-11-28 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| UA117573C2 (uk) | 2012-11-13 | 2018-08-27 | Ерей Біофарма Інк. | Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю |
| WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| UA116455C2 (uk) * | 2012-11-13 | 2018-03-26 | Еррей Біофарма Інк. | Сполуки n-піролідинілсечовини, n'-піразолілсечовини, тіосечовини, гуанідину та ціаногуанідину як інгібітори кінази trka |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| SMT201800061T1 (it) | 2013-11-28 | 2018-05-02 | Kyorin Seiyaku Kk | Derivati dell'urea o loro sali farmacologicamente accettabili utili come io agonisti del recettore del peptide formile di tipo i (fprl-1) |
| CN109970614B (zh) | 2014-05-15 | 2023-01-13 | 阵列生物制药公司 | 作为trka激酶抑制剂的化合物及其用途 |
| WO2016021629A1 (ja) | 2014-08-06 | 2016-02-11 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する複素環および炭素環誘導体 |
| EP3699181B1 (en) | 2014-11-16 | 2023-03-01 | Array Biopharma, Inc. | Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| AU2016270803A1 (en) | 2015-06-01 | 2018-01-04 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
| JP6812059B2 (ja) | 2015-07-07 | 2021-01-13 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する複素環誘導体 |
| JP6816100B2 (ja) | 2015-07-16 | 2021-01-20 | アレイ バイオファーマ、インコーポレイテッド | ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物 |
| US10724102B2 (en) | 2015-10-26 | 2020-07-28 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
| WO2017135399A1 (ja) * | 2016-02-04 | 2017-08-10 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する含窒素複素環および炭素環誘導体 |
| PL3439663T3 (pl) | 2016-04-04 | 2024-11-18 | Loxo Oncology, Inc. | Sposoby leczenia nowotworów wieku dziecięcego |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| SG11201808559PA (en) | 2016-04-04 | 2018-10-30 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| FI3800189T3 (fi) | 2016-05-18 | 2023-07-31 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
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| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| JP2019026646A (ja) * | 2017-08-03 | 2019-02-21 | 塩野義製薬株式会社 | 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および／または予防用医薬組成物 |
| US11053217B2 (en) | 2017-09-29 | 2021-07-06 | Mitsubishi Tanabe Pharma Corporation | Optically active pyrrolidine compound and method for producing same |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
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| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
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| EP3773725A1 (en) | 2018-03-29 | 2021-02-17 | Loxo Oncology Inc. | Treatment of trk-associated cancers |
| EP3822266B1 (en) * | 2018-07-12 | 2024-11-06 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Pyrrolidinyl urea derivatives and application thereof in trka-related diseases |
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| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| CN112979615B (zh) * | 2019-12-17 | 2024-08-09 | 上海医药集团股份有限公司 | 一种喹唑啉脲类化合物、其制备方法、制备中间体、药物组合物及应用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
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| CN117836289A (zh) * | 2021-04-12 | 2024-04-05 | 上海睿跃生物科技有限公司 | 原肌球蛋白受体激酶(trk)降解化合物及其使用方法 |
| CN113278409B (zh) * | 2021-06-22 | 2022-04-29 | 西南石油大学 | 一种高温酸化缓蚀剂 |
| CN114031556B (zh) * | 2021-11-08 | 2023-03-31 | 温州大学 | 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法 |
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