SG11201909059XA - Solid form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol - Google Patents
Solid form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanolInfo
- Publication number
- SG11201909059XA SG11201909059XA SG11201909059XA SG11201909059XA SG 11201909059X A SG11201909059X A SG 11201909059XA SG 11201909059X A SG11201909059X A SG 11201909059XA SG 11201909059X A SG11201909059X A SG 11201909059XA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- darmstadt
- pyridazin
- morpholin
- fluoro
- Prior art date
Links
- 239000007787 solid Substances 0.000 title abstract 2
- MOWXJLUYGFNTAL-DEOSSOPVSA-N (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxypyridazin-3-yl)methanol Chemical compound N1=NC(OC)=CC=C1[C@@H](O)C1=CC(C=2C3=CC=C(C=C3N=CN=2)N2CCOCC2)=C(F)C=C1Cl MOWXJLUYGFNTAL-DEOSSOPVSA-N 0.000 title 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 2
- -1 METHOXY-PYRIDAZIN-3-YL Chemical class 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 235000015244 frankfurter Nutrition 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
Classifications
-
- 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
- C07D403/10—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 carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01D—SEPARATION
- B01D9/00—Crystallisation
- B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
- B01D9/0054—Use of anti-solvent
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Crystallography & Structural Chemistry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 04 October 2018 (04.10.2018) W I PO I PCT o °nolo VIII n mum oimiE (10) International Publication Number WO 2018/178133 Al (51) International Patent Classification: C07D 403/10 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2018/057875 (22) International Filing Date: 28 March 2018 (28.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 17163826.5 30 March 2017 (30.03.2017) EP (71) Applicant: MERCK PATENT GMBH [DE/DE]; Frank- furter Strasse 250, 64293 DARMSTADT (DE). (72) Inventors: LANGE, Michael; Am Blauen Stein 4, 64295 DARMSTADT (DE). KUEHN, Clemens; Im Appensee 19, 64291 DARMSTADT (DE). FUCHSS, Thomas; Jahn- strasse 12, 64625 BENSHEIM-AUERBACH (DE). MAIL- LARD, David; Martinstrasse 81, 64285 DARMSTADT (DE). BREUNING, Marcel; Uhlandstrasse 11, 60314 FRANKFURT AM MAIN (DE). POMA, Marco; Via E. Q. Visconti 60, 00193 ROME (IT). BURINI, Edoardo; Via Puglie 5, 00012 GUIDONIA MONTECELIO (IT). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). It Published: with international search report (Art. 21(3)) 00 N 1-1 (54) Title: SOLID FORM OF (S)-[2-CHLORO-4-FLUORO-5-(7-MORPHOLIN-4-YLQUINAZOLIN-4-YL)PHENYL]-(6- 00 METHOXY-PYRIDAZIN-3-YL)METHANOL 1-1 0 (57) : The present invention relates to anhydrous disordered crystalline (S)42-chloro-4-fluoro-5-(7-morpholin-4-ylquina- \" zolin-4-yl)pheny1]-(6-methoxy-pyridazin-3-yl)methanol, as well as a method of making same, and pharmaceutical compositions and 0 medical uses thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17163826 | 2017-03-30 | ||
| PCT/EP2018/057875 WO2018178133A1 (en) | 2017-03-30 | 2018-03-28 | Solid form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201909059XA true SG11201909059XA (en) | 2019-10-30 |
Family
ID=58461171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201909059X SG11201909059XA (en) | 2017-03-30 | 2018-03-28 | Solid form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US11053233B2 (en) |
| EP (1) | EP3601265B1 (en) |
| JP (1) | JP7365904B2 (en) |
| KR (1) | KR20190136037A (en) |
| CN (1) | CN110446705B (en) |
| AU (1) | AU2018246257B2 (en) |
| CA (1) | CA3058285C (en) |
| DK (1) | DK3601265T3 (en) |
| ES (1) | ES2956036T3 (en) |
| IL (1) | IL269667B1 (en) |
| MX (1) | MX2019011649A (en) |
| RU (1) | RU2019133577A (en) |
| SG (1) | SG11201909059XA (en) |
| TW (1) | TWI781161B (en) |
| WO (1) | WO2018178133A1 (en) |
| ZA (1) | ZA201907144B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102013008118A1 (en) * | 2013-05-11 | 2014-11-13 | Merck Patent Gmbh | Arylchinazoline |
| WO2018178129A1 (en) * | 2017-03-30 | 2018-10-04 | Merck Patent Gmbh | Crystalline form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol |
| WO2020259613A1 (en) | 2019-06-27 | 2020-12-30 | 南京明德新药研发有限公司 | Quinazoline and cinnoline derivatives as dna-pk inhibitor |
| CN116670128A (en) * | 2020-12-28 | 2023-08-29 | 南京明德新药研发有限公司 | Crystal form of morpholine-substituted benzopyrimidine compound and preparation method thereof |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN191496B (en) * | 1999-07-30 | 2003-12-06 | Ranbaxy Lab Ltd | |
| GB2383042A (en) * | 2001-10-18 | 2003-06-18 | Cipla Ltd | Amorphous alendronate sodium |
| US7655692B2 (en) * | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
| EP2123641A4 (en) * | 2007-02-16 | 2011-06-22 | Eisai R&D Man Co Ltd | Crystal, amorphous form and salt of methyl n-ý3-(6,7-dimethoxy- 2-methylaminoquinazolin-4-yl)phenyl¨terephthalamic acid |
| WO2009100258A1 (en) * | 2008-02-05 | 2009-08-13 | Hollis-Eden Pharmaceuticals, Inc. | Pharmaceutical solid state forms |
| IT1404157B1 (en) * | 2010-12-30 | 2013-11-15 | Nano Active Film S R L | NANOPOROSAL CRYSTALLINE FORM DISORDERED WITH SINDIOTACTIC POLYSTYRENE, ITS PREPARATION PROCESS AND ITEMS INCLUDING THE SAME. |
| DE102013008118A1 (en) * | 2013-05-11 | 2014-11-13 | Merck Patent Gmbh | Arylchinazoline |
| CA2914284A1 (en) * | 2013-05-30 | 2014-12-04 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| US10905146B2 (en) * | 2013-07-12 | 2021-02-02 | The Coca-Cola Company | Compositions for improving rebaudioside M solubility |
| BR122023025347A2 (en) * | 2015-06-12 | 2024-01-16 | Gb006, Inc. | MEGLUMINE OR TROMETHAMINE SALT OF A COMPOUND, CRYSTALLINE FORMS AND PHARMACEUTICAL FORMULATIONS THEREOF AND THEIR USES |
-
2018
- 2018-03-28 JP JP2019553242A patent/JP7365904B2/en active Active
- 2018-03-28 CN CN201880022210.7A patent/CN110446705B/en active Active
- 2018-03-28 ES ES18714751T patent/ES2956036T3/en active Active
- 2018-03-28 MX MX2019011649A patent/MX2019011649A/en unknown
- 2018-03-28 EP EP18714751.7A patent/EP3601265B1/en active Active
- 2018-03-28 WO PCT/EP2018/057875 patent/WO2018178133A1/en unknown
- 2018-03-28 RU RU2019133577A patent/RU2019133577A/en unknown
- 2018-03-28 CA CA3058285A patent/CA3058285C/en active Active
- 2018-03-28 KR KR1020197031923A patent/KR20190136037A/en not_active Application Discontinuation
- 2018-03-28 SG SG11201909059X patent/SG11201909059XA/en unknown
- 2018-03-28 DK DK18714751.7T patent/DK3601265T3/en active
- 2018-03-28 IL IL269667A patent/IL269667B1/en unknown
- 2018-03-28 AU AU2018246257A patent/AU2018246257B2/en active Active
- 2018-03-28 US US16/498,905 patent/US11053233B2/en active Active
- 2018-03-30 TW TW107111176A patent/TWI781161B/en active
-
2019
- 2019-10-29 ZA ZA2019/07144A patent/ZA201907144B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2019011649A (en) | 2019-12-19 |
| AU2018246257A1 (en) | 2019-11-14 |
| CA3058285A1 (en) | 2018-10-04 |
| CA3058285C (en) | 2024-02-06 |
| EP3601265B1 (en) | 2023-06-21 |
| US11053233B2 (en) | 2021-07-06 |
| WO2018178133A1 (en) | 2018-10-04 |
| JP7365904B2 (en) | 2023-10-20 |
| IL269667B1 (en) | 2024-05-01 |
| ES2956036T3 (en) | 2023-12-12 |
| EP3601265A1 (en) | 2020-02-05 |
| RU2019133577A3 (en) | 2021-07-30 |
| TWI781161B (en) | 2022-10-21 |
| KR20190136037A (en) | 2019-12-09 |
| CN110446705B (en) | 2023-04-14 |
| AU2018246257A8 (en) | 2019-11-28 |
| AU2018246257B2 (en) | 2022-05-12 |
| TW201900634A (en) | 2019-01-01 |
| DK3601265T3 (en) | 2023-09-18 |
| RU2019133577A (en) | 2021-04-30 |
| JP2020512362A (en) | 2020-04-23 |
| ZA201907144B (en) | 2023-10-25 |
| CN110446705A (en) | 2019-11-12 |
| IL269667A (en) | 2019-11-28 |
| US20200123144A1 (en) | 2020-04-23 |
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