HRP20230271T1 - Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogen sulfata - Google Patents
Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogen sulfata Download PDFInfo
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- HRP20230271T1 HRP20230271T1 HRP20230271TT HRP20230271T HRP20230271T1 HR P20230271 T1 HRP20230271 T1 HR P20230271T1 HR P20230271T T HRP20230271T T HR P20230271TT HR P20230271 T HRP20230271 T HR P20230271T HR P20230271 T1 HRP20230271 T1 HR P20230271T1
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- PXHANKVTFWSDSG-QLOBERJESA-N (3s)-n-[5-[(2r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide;sulfuric acid Chemical compound OS(O)(=O)=O.C1[C@@H](O)CCN1C(=O)NC1=C2N=C(N3[C@H](CCC3)C=3C(=CC=C(F)C=3)F)C=CN2N=C1 PXHANKVTFWSDSG-QLOBERJESA-N 0.000 title 1
- 101150111783 NTRK1 gene Proteins 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- 230000035772 mutation Effects 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 230000008482 dysregulation Effects 0.000 claims 3
- 230000014509 gene expression Effects 0.000 claims 3
- 101150056950 Ntrk2 gene Proteins 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 230000003321 amplification Effects 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 108020001507 fusion proteins Proteins 0.000 claims 2
- 102000037865 fusion proteins Human genes 0.000 claims 2
- 238000003199 nucleic acid amplification method Methods 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 241000223109 Trypanosoma cruzi Species 0.000 claims 1
- 230000002759 chromosomal effect Effects 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 244000045947 parasite Species 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 102200049395 rs2070863 Human genes 0.000 claims 1
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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
- A61K31/495—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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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]
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- 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
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
- C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/10—Protein-tyrosine kinases (2.7.10)
- C12Y207/10001—Receptor protein-tyrosine kinase (2.7.10.1)
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/91—Transferases (2.)
- G01N2333/912—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- G01N2333/91205—Phosphotransferases in general
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- G01N2800/00—Detection or diagnosis of diseases
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (22)
1. Kristalni oblik (I-HS) koji ima formulu:
[image]
naznačen time, što ima difrakcijske pikove XRPD (2θ stupnjeva) na 18.4±0.2, 20.7±0.2, 23.1±0.2 i 24.0±0.2, pri čemu kristalni oblik suštinski ne sadrži druge amorfne, polimorfne ili kristalne oblike, što znači da je molni postotak drugog/drugih amorfnih, polimorfnih ili kristalnih oblika izolirane baze kristalnog oblika (I-HS) manji od oko 5 molnih postotaka.
2. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, što ima difrakcijske pikove XRPD (2θ stupnjeva) na 10.7±0.2, 18.4±0.2, 20.7±0.2, 23.1±0.2 i 24.0±0.2.
3. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, što ima difrakcijske pikove XRPD (2θ stupnjeva) na 10.7±0.2, 18.4±0.2, 19.2±0.2, 20.2±0.2, 20.7±0.2, 21.5±0.2, 23.1±0.2 i 24.0±0.2.
4. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, što ima difrakcijske pikove XRPD (2θ stupnjeva) na 10.7±0.2, 15.3±0.2, 16.5±0.2, 18.4±0.2, 19.2±0.2, 19.9±0.2, 20.2±0.2, 20.7±0.2, 21.5±0.2, 22.1±0.2, 23.1±0.2, 24.0±0.2, 24.4±0.2, 25.6±0.2, 26.5±0.2, 27.6±0.2, 28.2±0.2, 28.7±0.2, 30.8±0.2 i 38.5±0.2.
5. Kristalni oblik prema patentnom zahtjevu 1, gdje kristalni oblik pokazuje početak do maksimuma od oko 193 do oko 205° Celzijusa, mjereno diferencijalnom skenirajućom kalorimetrijom.
6. Kristalni oblik prema patentnom zahtjevu 1, gdje kristalni oblik pokazuje toplinu topljenja od oko 2 415 mW, mjereno diferencijalnom skenirajućom kalorimetrijom.
7. Kristalni oblik prema patentnom zahtjevu 1, gdje kristalni oblik nije higroskpan.
8. Farmaceutski pripravak koji sadrži farmaceutski prihvatljiv nosač i kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7.
9. Postupak za izradu farmaceutskog pripravka koji obuhvaća miješanje kristalnog oblika prema bilo kojem od patentnih zahtjeva 1-7 i farmaceutski prihvatljivog nosača.
10. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju poremećaja izabranog iz grupe koja se sastoji od raka, bola, upale, neurodegenerativne bolesti ili infekcije parazitom Trypanosoma cruzi.
11. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju raka posredovanog Trk kinazom.
12. Kristalni oblik za uporabu prema patentnom zahtjevu 11, gdje je rak posredovan kinazom TrkA.
13. Kristalni oblik za uporabu prema patentnom zahtjevu 11, gdje je rak posredovan kinazom TrkB.
14. Kristalni oblik za uporabu prema patentnom zahtjevu 11, gdje je rak posredovan kinazom TrkA i TrkB.
15. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju pacijenta kojem je dijagnosticiran, ili je identificirano da ima, rak povezan sa Trk.
16. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju raka povezanog sa jednim ili više od prekomjerne ekspresije, aktivacije, amplifikacije i mutacije Trk kinaze, pri čemu uporaba prvo obuhvaća određivanje da li je rak povezan sa jednim ili više od prekomjerne ekspresije, aktivacije, amplifikacije i mutacije Trk kinaze.
17. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1-7 za uporabu u liječenju pacijenta koji ima disregulaciju gena NTRK, proteina Trk, ili njihove ekspresije ili nivoa.
18. Kristalni oblik za uporabu prema patentnom zahtjevu 15 ili 17, gdje je disregulacija gena NTRK, proteina Trk, ili njihove ekspresije ili nivoa kromosomska translacija koja rezultira translacijom fuzijskog proteina Trk.
19. Kristalni oblik za uporabu prema patentnom zahtjevu 18, gdje je fuzijski protein Trk izabran iz grupe koja se sastoji od: TP53-TrkA, LMNA-TrkA, CD74-TrkA, TFG-TrkA, TPM3-TrkA, NFASC-TrkA, BCAN-TrkA, MPRIP-TrkA, TPR-TrkA, RFWD2-TrkA, IRF2BP2-TrkA, SQSTM1-TrkA, SSBP2-TrkA, RABGAP1L-TrkA, C18ORF8-TrkA, RNF213-TrkA, TBC1D22A-TrkA, C20ORF112-TrkA, DNER-TrkA, ARHGEF2-TrkA, CHTOP-TrkA, PPL-TrkA, PLEKHA6-TrkA, PEAR1-TrkA, MRPL24-TrkA, MDM4-TrkA, LRRC71-TrkA, GRIPAP1-TrkA, EPS15-TrkA, DYNC2H1-TrkA, CEL-TrkA, EPHB2-TrkA, TGF-TrkA, NACC2-TrkB, QKI-TrkB, AFAP1-TrkB, PAN3-TrkB, SQSTM1-TrkB, TRIM24-TrkB, VCL-TrkB, AGBL4-TrkB, DAB2IP-TrkB, ETV6-TrkC, BTBD1-TrkC, LYN-TrkC, RBPMS-TrkC, EML4-TrkC, HOMER2-TrkC, TFG-TrkC, FAT1-TrkC i TEL-TrkC.
20. Kristalni oblik za uporabu prema patentnom zahtjevu 15 ili 18, gdje je disregulacija gena NTRK, proteina Trk, ili njihove ekspresije ili aktivnosti, jedna ili više točkastih mutacija u genu.
21. Kristalni oblik za uporabu prema patentnom zahtjevu 20, gdje je gen NTRK gen NTRK1, i jedna ili više točkastih mutacija u genu NTRK1 rezultira translacijom proteina TrkA koji ima supstitucije na jednoj ili više od sljedećih aminokiselinskih pozicija: 33, 336, 337, 324, 420, 444, 517, 538, 649, 682, 683, 702 i 1879.
22. Kristalni oblik za uporabu prema patentnom zahtjevu 21, gdje jedna ili više točkastih mutacija u genu NTRK1 rezultira translacijom proteina TrkA koji ima jednu ili više od sljedećih aminokiselinskih supstitucija: R33W, A336E, A337T, R324Q, R324W, V420M, R444Q, R444W, G517R, G517V, K538A, R649W, R649L, R682S, V683G, R702C i C1879T.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462080374P | 2014-11-16 | 2014-11-16 | |
| US201562169545P | 2015-06-01 | 2015-06-01 | |
| EP20169707.5A EP3699181B1 (en) | 2014-11-16 | 2015-11-16 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230271T1 true HRP20230271T1 (hr) | 2023-06-09 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20230271TT HRP20230271T1 (hr) | 2014-11-16 | 2015-11-16 | Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogen sulfata |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US10799505B2 (hr) |
| EP (2) | EP3218380B1 (hr) |
| JP (2) | JP6914834B2 (hr) |
| KR (1) | KR102649887B1 (hr) |
| CN (2) | CN113354649A (hr) |
| AU (1) | AU2015346046B2 (hr) |
| BR (1) | BR112017010141A2 (hr) |
| CA (1) | CA2967951C (hr) |
| CL (1) | CL2017001249A1 (hr) |
| CO (1) | CO2017005483A2 (hr) |
| CR (1) | CR20170263A (hr) |
| DK (1) | DK3699181T3 (hr) |
| ES (1) | ES2941630T3 (hr) |
| FI (1) | FI3699181T3 (hr) |
| HK (1) | HK1244483A1 (hr) |
| HR (1) | HRP20230271T1 (hr) |
| HU (1) | HUE061448T2 (hr) |
| IL (2) | IL290905B2 (hr) |
| LT (1) | LT3699181T (hr) |
| MX (2) | MX2017006412A (hr) |
| PH (2) | PH12017500900A1 (hr) |
| PL (1) | PL3699181T3 (hr) |
| PT (1) | PT3699181T (hr) |
| RS (1) | RS64122B1 (hr) |
| SG (1) | SG11201703962XA (hr) |
| SI (1) | SI3699181T1 (hr) |
| TW (2) | TWI767858B (hr) |
| UA (1) | UA123044C2 (hr) |
| WO (1) | WO2016077841A1 (hr) |
| ZA (1) | ZA201703501B (hr) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| RU2523544C2 (ru) | 2008-10-22 | 2014-07-20 | Эррэй Биофарма Инк. | ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ КАК ИНГИБИТОРЫ ТРК КИНАЗЫ |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| SI3205654T1 (sl) | 2010-05-20 | 2019-07-31 | Array Biopharma, Inc. | Makrociklične spojine kot inhibitorji TRK kinaze |
| WO2015017533A1 (en) * | 2013-07-30 | 2015-02-05 | Blueprint Medicines Corporation | Ntrk2 fusions |
| SI3699181T1 (sl) | 2014-11-16 | 2023-06-30 | Array Biopharma, Inc. | Kristalinična oblika(s)-n-(5-((r)-2-(2,5-difluorofenil)- pirolidin-1-il)-pirazolo(1,5-a)pirimidin-3-il)-3-hidroksipirolidin-1 -karboksamid hidrogen sulfata |
| KR20180021745A (ko) | 2015-06-01 | 2018-03-05 | 록쏘 온콜로지, 인코포레이티드 | 암을 진단하고 치료하는 방법 |
| ES2857081T3 (es) | 2015-07-16 | 2021-09-28 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret |
| WO2017075107A1 (en) | 2015-10-26 | 2017-05-04 | Nanda Nisha | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| CA3019661A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3439662A1 (en) * | 2016-04-04 | 2019-02-13 | 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 |
| US11214571B2 (en) * | 2016-05-18 | 2022-01-04 | Array Biopharma Inc. | Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof |
| 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 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
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