BR112021022685A2 - Formas cristalinas de n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamida - Google Patents
Formas cristalinas de n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamidaInfo
- Publication number
- BR112021022685A2 BR112021022685A2 BR112021022685A BR112021022685A BR112021022685A2 BR 112021022685 A2 BR112021022685 A2 BR 112021022685A2 BR 112021022685 A BR112021022685 A BR 112021022685A BR 112021022685 A BR112021022685 A BR 112021022685A BR 112021022685 A2 BR112021022685 A2 BR 112021022685A2
- Authority
- BR
- Brazil
- Prior art keywords
- fluorocyclopropyl
- imidazo
- methylphenyl
- carboxamide
- pyridine
- Prior art date
Links
- RHNJOZCVGSBEAG-KBPBESRZSA-N n-[5-[5-[(1r,2s)-2-fluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@H]1C[C@@H]1F RHNJOZCVGSBEAG-KBPBESRZSA-N 0.000 title abstract 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000001530 fumaric acid Substances 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 1
- 208000016097 disease of metabolism Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 210000003630 histaminocyte Anatomy 0.000 abstract 1
- ZMBYQTGAXZOMOO-UHFFFAOYSA-N imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=CC=CN2C(C(=O)N)=CN=C21 ZMBYQTGAXZOMOO-UHFFFAOYSA-N 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
formas cristalinas de n-(5-(5-((1r,2s)- 2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamida. a presente invenção refere-se a formas cristalinas de n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamida, em particular a forma a e um n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamida, cocristal de ácido fumárico. a presente invenção também se refere aos processos para a preparação de tais formas cristalinas. além disso, a invenção refere-se a uma composição farmacêutica que compreende a referida n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo-[1,2-a]piridina-3-carboxamida forma a, ou o referido n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridi-na-3-carboxamida, cocristal de ácido fumárico e pelo menos um excipiente farmaceuticamente aceitável. a composição farmacêutica pode ser usada como um medicamento, em particular para o tratamento e/ou profilaxia de uma doença associada a mastócitos, uma doença respiratória, um distúrbio inflamatório, síndrome do intestino irritável (ibs), doença inflamatória do intestino (ibd), um distúrbio autoimune, uma doença metabólica, uma doença fibrótica.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019086582 | 2019-05-13 | ||
| PCT/CN2020/090060 WO2020228746A1 (en) | 2019-05-13 | 2020-05-13 | Crystalline forms of n- (5- (5- ( (1r, 2s) -2-fluorocyclopropyl) -1, 2, 4-oxadiazol-3-yl) -2-methylphenyl) imidazo [1, 2-a] pyridine-3-carboxamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021022685A2 true BR112021022685A2 (pt) | 2022-03-29 |
Family
ID=73289607
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021022685A BR112021022685A2 (pt) | 2019-05-13 | 2020-05-13 | Formas cristalinas de n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4-oxadiazol-3-il)-2-metilfenil)imidazo[1,2-a]piridina-3-carboxamida |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20220194936A1 (pt) |
| EP (1) | EP3969453A4 (pt) |
| JP (1) | JP2022533340A (pt) |
| KR (1) | KR20220007650A (pt) |
| CN (1) | CN114096538A (pt) |
| AU (1) | AU2020274564A1 (pt) |
| BR (1) | BR112021022685A2 (pt) |
| CA (1) | CA3139552A1 (pt) |
| IL (1) | IL287877A (pt) |
| MA (1) | MA55976A (pt) |
| MX (1) | MX2021013814A (pt) |
| SG (1) | SG11202112281UA (pt) |
| TW (1) | TW202108581A (pt) |
| WO (1) | WO2020228746A1 (pt) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4181921A1 (en) * | 2020-07-15 | 2023-05-24 | Third Harmonic Bio, Inc. | Crystalline forms of a selective c-kit kinase inhibitor |
| US11744823B2 (en) * | 2020-11-19 | 2023-09-05 | Third Harmonic Bio, Inc. | Pharmaceutical compositions of a selective c-kit kinase inhibitor and methods for making and using same |
| US20220175740A1 (en) * | 2020-11-19 | 2022-06-09 | Novartis Ag | Pharmaceutical compositions of a selective c-kit kinase inhibitor and methods for making and using same |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2845785A1 (en) * | 2011-09-01 | 2013-03-07 | Irm Llc | Compounds and compositions as c-kit kinase inhibitors |
| BR112014003963A2 (pt) * | 2011-09-01 | 2017-03-21 | Irm Llc | compostos e composições como inibidores de quinase c-kit |
| US9199981B2 (en) * | 2011-09-01 | 2015-12-01 | Novartis Ag | Compounds and compositions as C-kit kinase inhibitors |
| BR112014004560A2 (pt) * | 2011-09-01 | 2017-04-04 | Irm Llc | compostos e composições como inibidores de c-kit quinase |
-
2020
- 2020-05-13 MA MA055976A patent/MA55976A/fr unknown
- 2020-05-13 SG SG11202112281UA patent/SG11202112281UA/en unknown
- 2020-05-13 WO PCT/CN2020/090060 patent/WO2020228746A1/en unknown
- 2020-05-13 MX MX2021013814A patent/MX2021013814A/es unknown
- 2020-05-13 KR KR1020217040220A patent/KR20220007650A/ko unknown
- 2020-05-13 TW TW109115939A patent/TW202108581A/zh unknown
- 2020-05-13 JP JP2021567913A patent/JP2022533340A/ja active Pending
- 2020-05-13 EP EP20805948.5A patent/EP3969453A4/en active Pending
- 2020-05-13 CN CN202080050607.4A patent/CN114096538A/zh active Pending
- 2020-05-13 CA CA3139552A patent/CA3139552A1/en active Pending
- 2020-05-13 BR BR112021022685A patent/BR112021022685A2/pt unknown
- 2020-05-13 US US17/595,260 patent/US20220194936A1/en active Pending
- 2020-05-13 AU AU2020274564A patent/AU2020274564A1/en active Pending
-
2021
- 2021-11-07 IL IL287877A patent/IL287877A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW202108581A (zh) | 2021-03-01 |
| KR20220007650A (ko) | 2022-01-18 |
| EP3969453A1 (en) | 2022-03-23 |
| CA3139552A1 (en) | 2020-11-19 |
| MX2021013814A (es) | 2022-02-10 |
| MA55976A (fr) | 2022-03-23 |
| US20220194936A1 (en) | 2022-06-23 |
| SG11202112281UA (en) | 2021-12-30 |
| JP2022533340A (ja) | 2022-07-22 |
| AU2020274564A1 (en) | 2021-12-09 |
| IL287877A (en) | 2022-01-01 |
| CN114096538A (zh) | 2022-02-25 |
| EP3969453A4 (en) | 2023-01-18 |
| WO2020228746A1 (en) | 2020-11-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |