ME02814B - Nova so abeksinostata, sa njom povezani kristalni oblik, postupak pripreme i farmaceutske supstance koje ih sadrže - Google Patents

Nova so abeksinostata, sa njom povezani kristalni oblik, postupak pripreme i farmaceutske supstance koje ih sadrže

Info

Publication number
ME02814B
ME02814B MEP-2017-139A MEP2017139A ME02814B ME 02814 B ME02814 B ME 02814B ME P2017139 A MEP2017139 A ME P2017139A ME 02814 B ME02814 B ME 02814B
Authority
ME
Montenegro
Prior art keywords
abexinostat
crystalline form
tosylate
expressed
water
Prior art date
Application number
MEP-2017-139A
Other languages
German (de)
English (en)
French (fr)
Inventor
Anne Pimont-Garro
Philippe Letellier
Original Assignee
Pharmacyclics Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48521256&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02814(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmacyclics Llc filed Critical Pharmacyclics Llc
Publication of ME02814B publication Critical patent/ME02814B/me

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Claims (18)

1. Tozilat N-hidroksi-4-{2-[3-(N,N-dimetilaminometil)benzofuran- 2- ilkarbonilamino]etoksi}benzamida ili jedan od njegovih solvata.
2. So prema patenom zahtjevu 1 iz op!te formule (ll): H3C-oSO,H ..N \ (TI) o HN \ OH
3. Kristalini oblik l tozilata abeksinostata prema jednom od patentnih zahtjeva 1 ili 2, naznačen time što ima dijagram rendgenske difrakcije praha sa sledećim linijama difrakcije (Bragov ugao 2 teta, izraženo u stepenima ± 0,2•): 6,50; 9,94; 11,35; 12,33; 14,08; 18,95; 21,08; 27,05.
4. Kristalni oblik l tozilata abeksinostata prema patentnom zahtjevu 3, naznačen time što ima dijagram rendgenske difrakcije praha sa sledećim linijama difrakcije (Bragov ugao 2 teta, izraženo u stepenima± 0,2•): 6,50; 9,94; 11,35; 12,33; 14,08; 18,95; 19,61; 19,96; 21,08; 22,82; 23,61; 27,05.
5. Kristalni oblik l tozilata abeksinostata prema patentnom zahtjevu 3 ili 4, naznačen time što ima sljedeći dijagram rendgenske difrakcije praha izmeren na PANalytical X'Pert Pro MPD difraktometru sa detektorom X'Celerator i izražen u smislu položaja linije (Bragov ugao 2, izraženo u stepenima ± 0,2•) i d interretikularno rastojanje d (izraženo u A): • Linija br. Ugao 2 teta (stepeni) lnterretlkularno rastojanje (A) 1 2 3 4 5 6 7 8 9 10 11 12 6,50 9,94 11,35 12,33 14,08 18,95 19,61 19,96 21,08 22,82 23,61 27,05 13,581 8,894 7,789 7,173 6,285 4,683 4,526 4,449 4,215 3,897 3,768 3,296
6. Kristalni oblik l tozilata abeksinostata prema jednom od patentnih zahtjeva 3 do 5, naznačen time što ima Ramanov spektar sa značajnim vršnim vrednostima na poziciji 1608 cm·1.
7. Kristalni oblik l tozilata abeksinostata prema jednom od patentnih zahtjeva 1 do 6, naznačen time što ima Ramanov spektar sa značajnim vršnim vrednostima na pozicijama 940 cm·1, 1088 cm-1, 1132 cm·1, 1242 cm-1, 1360 cm·1, 1608 cm-1.
8. Kristalni oblik l tozilata abeksinostata prema jednom od patentnih zahtjeva 1 ili 2, naznačen time što ima 13c CP/MAS NMR spektar čvrstog stanja sa sledećim vršnim vrednostima (izraženimuppm±0,2ppm): 121,2ppm,122,1 ppm,123,5ppm 126,0ppm,126,8ppm,128,2 ppm, 128,9 ppm, 143,4 ppm, 144,6 ppm, 153,8 ppm, 159 ppm, 161,2 ppm i 162,1 ppm.
9. Kristalni oblik l tozilata abeksinostata prema patentnom zahtevu 8, naznačen time što ima 13c CP/MAS NMR spektar čvrstog stanja sa sledećim vršnim vrednostima (izraženo u ppm ± 0,2 ppm): Vr na vrednost Hemljskl pomak (ppm) Vr na vrednost Hemijskl pomak (ppm) 1 2 3 4 5 6 7 8 g 162,1 161,2 159,0 153,8 144,6 143,4 128,9 128,2 126,8 10 11 12 13 14 15 16 17 18 126,0 123,5 122,1 121,3 65,9 50,6 46,9 45,0 21,9 • •
10.Farmaceutska supstanca koja sadrži tozilat abeksinostata prema jednom od patentnih zahtjeva 1 ili 2 kao aktivni sastojak u vezi sa jednim ili više farmaceutski prihvatljivih ekscipijenata.
11.Farmaceutska supstanca koja sadržikristalni oblik l tozilata abeksinostata prema jednom od patentnih zahtjeva 3 do 9 kao aktivni sastojak u vezi sa jednim ili više farmaceutski prihvatljivih ekscipijenata.
12.Farmaceutska supstanca prema patentnom zahtjevu 1O do 11 za upotrebu u lečenju kancera.
13.Farmaceutska supstanca predviđena da se koristi prema jednom od patentnih zahtjeva 1O do12 u kojima je kancer karcinom, tumor, neoplazam, limfom, melanom, gliom, sarkom ili blastom.
14.Postupak za pripremu kristalnog oblika l tozilata abeksinostata prema jednom od patentnih zahtjeva 3 do 9, u kojima je abeksinostat kristalizovan u prisustvu paratoluensulfonske kiseline u polarnom medijumu.
15.Postupak za pripremu kristalnog oblika l tozilata abeksinostata prema patentnom zahtjevu 14, u kom se polarni medijum sastoji od jednog ili više rastvarača izabranih iz vode, alkohola, ketona i estara.
16.Postupak za pripremu kristalnog oblika l tozilata abeksinostata prema patentnom zahtevu 15, u kom je polarni medijum binarna mešavina, u kojoj je jedan od sastavnih delova voda.
17.Postupak za pripremu kristalnog oblika l tozilata abeksinostata prema patentnom zahljevu 16, u kom je polarni medijum binarna mešavina izabrana iz: acetona/vode, etanola/vode, izopropanola/vode i metil etil ketona/vode.
18.Postupak za pripremu kristalnog oblika l tozilata abeksinostata prema jednom od patentnih zahtjeva 14 do 17, u kom je kristalizacija aktivirana veoma malom količinom kristalnog oblika l tozilata abeksinostata. l
MEP-2017-139A 2013-03-04 2014-03-03 Nova so abeksinostata, sa njom povezani kristalni oblik, postupak pripreme i farmaceutske supstance koje ih sadrže ME02814B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361772191P 2013-03-04 2013-03-04
FR1351898A FR3002733B1 (fr) 2013-03-04 2013-03-04 Nouveau sel de l'abexinostat, forme cristalline associee,leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP14711833.5A EP2964622B1 (fr) 2013-03-04 2014-03-03 Nouveau sel de l'abexinostat, forme cristalline associee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
PCT/FR2014/050455 WO2014135776A1 (fr) 2013-03-04 2014-03-03 Nouveau sel de l'abexinostat, forme cristalline associee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Publications (1)

Publication Number Publication Date
ME02814B true ME02814B (me) 2018-01-20

Family

ID=48521256

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2017-139A ME02814B (me) 2013-03-04 2014-03-03 Nova so abeksinostata, sa njom povezani kristalni oblik, postupak pripreme i farmaceutske supstance koje ih sadrže

Country Status (39)

Country Link
US (3) US9115108B2 (me)
EP (2) EP2964622B1 (me)
JP (2) JP6449177B2 (me)
CN (2) CN109734690B (me)
AR (1) AR094935A1 (me)
AU (2) AU2014224456B2 (me)
BR (1) BR112015021443A2 (me)
CA (1) CA2903369C (me)
CL (1) CL2015002488A1 (me)
CR (1) CR20150456A (me)
CY (1) CY1119147T1 (me)
DK (1) DK2964622T3 (me)
DO (1) DOP2015000215A (me)
EA (2) EA039113B1 (me)
ES (1) ES2632471T3 (me)
FR (1) FR3002733B1 (me)
GE (1) GEP201706760B (me)
HR (1) HRP20171041T1 (me)
HU (1) HUE035299T2 (me)
IL (1) IL241038B (me)
JO (1) JO3402B1 (me)
LT (1) LT2964622T (me)
MA (1) MA38423B1 (me)
ME (1) ME02814B (me)
MX (1) MX355436B (me)
MY (1) MY192027A (me)
NI (1) NI201500122A (me)
PE (1) PE20151591A1 (me)
PL (1) PL2964622T3 (me)
PT (1) PT2964622T (me)
RS (1) RS56224B1 (me)
SG (1) SG11201506952YA (me)
SI (1) SI2964622T1 (me)
SM (1) SMT201700351T1 (me)
TN (1) TN2015000367A1 (me)
TW (1) TWI506023B (me)
UA (1) UA118550C2 (me)
UY (1) UY35356A (me)
WO (1) WO2014135776A1 (me)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107898791A (zh) 2010-06-03 2018-04-13 药品循环有限责任公司 布鲁顿酪氨酸激酶(btk)抑制剂的应用
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
JP6178861B2 (ja) 2012-11-02 2017-08-09 ファイザー・インク ブルトン型チロシンキナーゼ阻害剤
FR3002733B1 (fr) 2013-03-04 2015-08-14 Servier Lab Nouveau sel de l'abexinostat, forme cristalline associee,leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2015143400A1 (en) 2014-03-20 2015-09-24 Pharmacyclics, Inc. Phospholipase c gamma 2 and resistance associated mutations
FR3025196B1 (fr) * 2014-09-03 2019-09-06 Pharmacyclics, Inc. Nouveaux sels de 3-[(dimethylamino)methyl]-n-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofurane-2-carboxamide, formes cristallines associees, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CN107001307A (zh) * 2014-09-03 2017-08-01 药品循环有限责任公司 3‑[(二甲基氨基)甲基]‑n‑{2‑[4‑(羟基氨基甲酰基)苯氧基]乙基}‑1‑苯并呋喃‑2‑甲酰胺的新颖的盐、有关的结晶形式、用于制备其的方法及包含其的药物组合物
FR3025197B1 (fr) * 2014-09-03 2019-09-06 Pharmacyclics, Inc. Nouveau sel de 3-[(dimethylamino)methyl]-n-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofurane-2-carboxamide, formes cristallines associees, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2017011314A1 (en) * 2015-07-10 2017-01-19 Paharmacyclics Llc Btk and hdac combinations
EP4351734A1 (en) 2021-06-10 2024-04-17 Teva Pharmaceuticals International GmbH Solid state forms of abexinostat and process for preparation thereof

Family Cites Families (8)

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US3038004A (en) * 1958-04-18 1962-06-05 Burroughs Wellcome Co Quaternary ammonium compounds
GB0020721D0 (en) * 2000-08-22 2000-10-11 Merck Sharp & Dohme Therapeutic agents
SI1611088T1 (sl) * 2003-04-07 2009-12-31 Pharmacyclics Inc Hidroksamati kot terapevtska sredstva
US20090270497A1 (en) * 2008-04-24 2009-10-29 Pharmacyclics, Inc. Treatment of Non-Localized Inflammation with pan-HDAC Inhibitors
US8603521B2 (en) * 2009-04-17 2013-12-10 Pharmacyclics, Inc. Formulations of histone deacetylase inhibitor and uses thereof
WO2011036647A1 (en) * 2009-09-24 2011-03-31 Ranbaxy Laboratories Limited Process for the preparation of sorafenib tosylate
WO2013039956A2 (en) * 2011-09-14 2013-03-21 The Trustees Of Columbia University In The City Of New York Compositions and methods for treating mood disorders
FR3002733B1 (fr) 2013-03-04 2015-08-14 Servier Lab Nouveau sel de l'abexinostat, forme cristalline associee,leur procede de preparation et les compositions pharmaceutiques qui les contiennent

Also Published As

Publication number Publication date
TW201434822A (zh) 2014-09-16
US9115108B2 (en) 2015-08-25
DOP2015000215A (es) 2015-09-30
JP6720280B2 (ja) 2020-07-08
MY192027A (en) 2022-07-23
NI201500122A (es) 2018-10-18
LT2964622T (lt) 2017-08-10
EP2964622B1 (fr) 2017-04-19
UY35356A (es) 2014-09-30
AU2014224456B2 (en) 2018-01-25
MA38423B1 (fr) 2017-10-31
HK1220965A1 (zh) 2017-05-19
EA201591530A1 (ru) 2016-01-29
GEP201706760B (en) 2017-10-25
JO3402B1 (ar) 2019-10-20
IL241038A0 (en) 2015-11-30
CY1119147T1 (el) 2018-02-14
UA118550C2 (uk) 2019-02-11
US20170313671A1 (en) 2017-11-02
PT2964622T (pt) 2017-07-13
RS56224B1 (sr) 2017-11-30
US20140249215A1 (en) 2014-09-04
CN105263917B (zh) 2018-11-20
PL2964622T3 (pl) 2017-10-31
EP3252044A1 (fr) 2017-12-06
PE20151591A1 (es) 2015-11-06
FR3002733B1 (fr) 2015-08-14
BR112015021443A2 (pt) 2017-07-18
HUE035299T2 (en) 2018-05-02
EA201891023A1 (ru) 2019-03-29
AU2014224456A8 (en) 2015-10-22
AU2014224456A1 (en) 2015-10-08
TN2015000367A1 (fr) 2017-01-03
CA2903369C (en) 2021-06-08
EA030689B1 (ru) 2018-09-28
AU2018202881A1 (en) 2018-05-17
DK2964622T3 (en) 2017-07-31
JP2019069955A (ja) 2019-05-09
WO2014135776A1 (fr) 2014-09-12
IL241038B (en) 2019-09-26
EP2964622A1 (fr) 2016-01-13
SMT201700351T1 (it) 2017-09-07
ES2632471T3 (es) 2017-09-13
CN105263917A (zh) 2016-01-20
CA2903369A1 (en) 2014-09-12
CN109734690A (zh) 2019-05-10
SI2964622T1 (sl) 2017-10-30
FR3002733A1 (fr) 2014-09-05
MX355436B (es) 2018-04-18
NZ712380A (en) 2020-10-30
CN109734690B (zh) 2023-08-11
US10150748B2 (en) 2018-12-11
JP2016510735A (ja) 2016-04-11
MA38423A1 (fr) 2017-02-28
CR20150456A (es) 2015-10-21
JP6449177B2 (ja) 2019-01-09
AR094935A1 (es) 2015-09-09
CL2015002488A1 (es) 2016-03-11
AU2018202881B2 (en) 2020-02-27
MX2015011566A (es) 2016-06-24
EA039113B1 (ru) 2021-12-06
SG11201506952YA (en) 2015-10-29
TWI506023B (zh) 2015-11-01
HRP20171041T1 (hr) 2017-10-06
US20150315167A1 (en) 2015-11-05

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