MX2017006412A - Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida. - Google Patents
Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida.Info
- Publication number
- MX2017006412A MX2017006412A MX2017006412A MX2017006412A MX2017006412A MX 2017006412 A MX2017006412 A MX 2017006412A MX 2017006412 A MX2017006412 A MX 2017006412A MX 2017006412 A MX2017006412 A MX 2017006412A MX 2017006412 A MX2017006412 A MX 2017006412A
- Authority
- MX
- Mexico
- Prior art keywords
- crystalline form
- hydroxypyrrolidine
- pyrazolo
- difluorophenyl
- pyrimidin
- Prior art date
Links
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 title 1
- NYNZQNWKBKUAII-KBXCAEBGSA-N (3s)-n-[5-[(2r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide Chemical compound C1[C@@H](O)CCN1C(=O)NC1=C2N=C(N3[C@H](CCC3)C=3C(=CC=C(F)C=3)F)C=CN2N=C1 NYNZQNWKBKUAII-KBXCAEBGSA-N 0.000 abstract 1
- 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 abstract 1
- 206010001935 American trypanosomiasis Diseases 0.000 abstract 1
- 208000024699 Chagas disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 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
- 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
- A61P25/04—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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- 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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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2800/00—Detection or diagnosis of diseases
- G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
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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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- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
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- General Engineering & Computer Science (AREA)
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- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención se refiere a una novedosa forma cristalina de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-iI)-pirazolo[1 ,5-a]-pirimidin-3-iI)-3-hidroxipirrolidina-1-carboxamida, a composiciones farmacéuticas que contienen dicha forma cristalina, y al uso de la forma cristalina en el tratamiento del dolor, cáncer, inflamación, enfermedad neurodegenerativa o infección por Trypanosoma cruzi. En algunas modalidades, la novedosa forma cristalina comprende una forma polimórfica estable de sulfato ácido de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-iI)-pira zolo[1,5-a]-pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida. La presente invención se refiere además a un proceso para la preparación de la novedosa forma cristalina.
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 | |
PCT/US2015/060953 WO2016077841A1 (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 |
---|---|
MX2017006412A true MX2017006412A (es) | 2017-09-12 |
Family
ID=54848892
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2017006412A MX2017006412A (es) | 2014-11-16 | 2015-11-16 | Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida. |
MX2020011079A MX2020011079A (es) | 2014-11-16 | 2017-05-16 | Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida. |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2020011079A MX2020011079A (es) | 2014-11-16 | 2017-05-16 | Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida. |
Country Status (30)
Country | Link |
---|---|
US (5) | US10799505B2 (es) |
EP (2) | EP3699181B1 (es) |
JP (2) | JP6914834B2 (es) |
KR (1) | KR102649887B1 (es) |
CN (2) | CN113354649A (es) |
AU (1) | AU2015346046B2 (es) |
BR (1) | BR112017010141A2 (es) |
CA (1) | CA2967951C (es) |
CL (1) | CL2017001249A1 (es) |
CO (1) | CO2017005483A2 (es) |
CR (1) | CR20170263A (es) |
DK (1) | DK3699181T3 (es) |
ES (1) | ES2941630T3 (es) |
FI (1) | FI3699181T3 (es) |
HK (1) | HK1244483A1 (es) |
HR (1) | HRP20230271T1 (es) |
HU (1) | HUE061448T2 (es) |
IL (2) | IL290905B2 (es) |
LT (1) | LT3699181T (es) |
MX (2) | MX2017006412A (es) |
PH (2) | PH12017500900A1 (es) |
PL (1) | PL3699181T3 (es) |
PT (1) | PT3699181T (es) |
RS (1) | RS64122B1 (es) |
SG (1) | SG11201703962XA (es) |
SI (1) | SI3699181T1 (es) |
TW (2) | TWI767858B (es) |
UA (1) | UA123044C2 (es) |
WO (1) | WO2016077841A1 (es) |
ZA (1) | ZA201703501B (es) |
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AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
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