HRP20170564T1 - Derivati aminociklobutana, metoda njihove priprave i njihova upotreba za lijekove - Google Patents

Derivati aminociklobutana, metoda njihove priprave i njihova upotreba za lijekove Download PDF

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Publication number
HRP20170564T1
HRP20170564T1 HRP20170564TT HRP20170564T HRP20170564T1 HR P20170564 T1 HRP20170564 T1 HR P20170564T1 HR P20170564T T HRP20170564T T HR P20170564TT HR P20170564 T HRP20170564 T HR P20170564T HR P20170564 T1 HRP20170564 T1 HR P20170564T1
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HR
Croatia
Prior art keywords
trans
amino
diethyl
cyclobutanecarboxamide
compound
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HRP20170564TT
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English (en)
Inventor
Bernard Vacher
Elodie BLANC
Ronan DEPOORTERE
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Pierre Fabre Médicament
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Application filed by Pierre Fabre Médicament filed Critical Pierre Fabre Médicament
Publication of HRP20170564T1 publication Critical patent/HRP20170564T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/14Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/40Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Furan Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (15)

1. Spoj sljedeće opće formule (1): (1) ili odgovarajuća famaceutski prihvatljiva sol ili solvat, gdje: - X1 predstavlja vodikov atom ili fluorov atom; - X2 je vodikov atom ili fluorov atom ili klorov atom; - R1 predstavlja vodikov atom ili fluorov atom ili klorov atom ili metilnu skupinu ili metoksi-skupinu ili cijano-skupinu; - R2 predstavlja neovisno ili zajedno metilnu skupinu ili etilnu skupinu.
2. Spoj prema patentnom zahtjevu 1, naznačeno time da: - X1 predstavlja vodikov atom ili fluorov atom; - X2 je vodikov atom ili fluorov atom ili klorov atom; - R1 je vodikov atom ili fluorov atom ili klorov atom ili metilnu skupinu ili metoksi-skupinu ili cijano-skupinu; - R2 je etilna skupina.
3. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2, naznačeno time da je odabran od sljedećih spojeva: - trans-3-amino-N,N-dietill-1-fenilciklobutankarboksamid, - trans-3-amino-N,N-dimetill-1-fenilciklobutankarboksamid - trans-3-amino-N,N-dietill-1-(2-fluorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3-methoxyfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3-fluorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3-klorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3-metillfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3-cijanofenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(2-fluor-3-klorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(2,5-difluorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3,5-difluorfenil)-ciklobutankarboksamid, - trans-3-amino-N,N-dietill-1-(3,5-diklorfenil)-ciklobutankarboksamid.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3 za upotrebu kao lijek.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3 za upotrebu kao lijek za liječenje depresije.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3 za upotrebu kao lijek za liječenje boli, posebno boli od jake nocicepcije, neuropatske boli i miješane boli.
7. Farmaceutski pripravak koji sadržava najmanje jedan spoj opće formule (1) prema bilo kojem od patentnih zahtjeva 1 do 3 te najmanje jedan farmaceutski prihvatljiv ekscipijens.
8. Farmaceutski pripravak prema patentnom zahtjevu 7 za upotrebu kao lijek za liječenje i/ili sprječavanje depresije.
9. Farmaceutski pripravak prema patentnom zahtjevu 7 za upotrebu kao lijek za liječenje boli, posebno boli od jake nocicepcije, neuropatske boli i miješane boli.
10. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 7 do 9, naznačeno time da je formuliran za oralno davanje.
11. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 7 do 9, naznačeno time da je formuliran za topikalno davanje.
12. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 8 do 11, naznačeno time da dolazi u obliku jedinice dnevne doze s između 1 i 1000 mg spoja opće formule (1).
13. Metoda priprave spojeva opće formule (1) kako su definirani u jednom od patentnih zahtjeva 1 do 3, naznačeno time da je sekundarni amin formule (R2)2NH reagirao sa spojem formule (C) dajući spoj formule (D) te da je spoj formule (D) zatim pretvoren u amin formule (1), a R1, R2, X1 i X2 radikali prisutni u reagensima jesu kako su iznad definirani u patentnom zahtjevu 1.
14. Sinteza međuprodukata formule (D) gdje R1, R2, X1 i X2 jesu kako su definirani u patentnom zahtjevu 1, koji se koriste za pripravu spojeva opće formule (1) kako su definirani u patentnim zahtjevima 1 do 3.
15. Sinteza međuprodukata formule (C) gdje R1, X1 i X2 jesu kako su definirani u patentnom zahtjevu 1, koji se koriste za pripravu spojeva opće formule (D), kako su definirani u patentnom zahtjevu 14.
HRP20170564TT 2012-12-04 2017-04-10 Derivati aminociklobutana, metoda njihove priprave i njihova upotreba za lijekove HRP20170564T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR1261621A FR2998892B1 (fr) 2012-12-04 2012-12-04 Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments
PCT/EP2013/075481 WO2014086825A1 (fr) 2012-12-04 2013-12-04 Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments
EP13811402.0A EP2928861B1 (fr) 2012-12-04 2013-12-04 Dérivés d'aminocyclobutane, leur procédé de préparation et leur utilisation à titre de médicaments

Publications (1)

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HRP20170564T1 true HRP20170564T1 (hr) 2017-06-16

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HRP20170564TT HRP20170564T1 (hr) 2012-12-04 2017-04-10 Derivati aminociklobutana, metoda njihove priprave i njihova upotreba za lijekove

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US (2) US9469601B2 (hr)
EP (1) EP2928861B1 (hr)
JP (1) JP6391586B2 (hr)
KR (1) KR102221928B1 (hr)
CN (2) CN106957285B (hr)
AR (1) AR093787A1 (hr)
AU (1) AU2013354133B2 (hr)
BR (1) BR112015012752B1 (hr)
CA (1) CA2893216C (hr)
CY (1) CY1118841T1 (hr)
DK (1) DK2928861T3 (hr)
ES (1) ES2621896T3 (hr)
FR (1) FR2998892B1 (hr)
HK (1) HK1212968A1 (hr)
HR (1) HRP20170564T1 (hr)
IL (1) IL239146A (hr)
LT (1) LT2928861T (hr)
MA (1) MA38229B1 (hr)
MX (1) MX364556B (hr)
MY (1) MY179886A (hr)
NZ (1) NZ709572A (hr)
PL (1) PL2928861T3 (hr)
PT (1) PT2928861T (hr)
RS (1) RS55916B1 (hr)
RU (1) RU2655919C2 (hr)
SA (1) SA515360518B1 (hr)
SI (1) SI2928861T1 (hr)
TN (1) TN2015000240A1 (hr)
TW (1) TWI603947B (hr)
UA (1) UA114017C2 (hr)
WO (1) WO2014086825A1 (hr)

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EP3774800A1 (en) 2018-03-28 2021-02-17 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
JP2021050161A (ja) 2019-09-25 2021-04-01 武田薬品工業株式会社 複素環化合物及びその用途
CN114269747B (zh) * 2019-11-18 2023-04-18 苏州恩华生物医药科技有限公司 一种1’,2’-二氢-3’h-螺[环丁烷1,4’-异喹啉]-3’-酮衍生物及其应用

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Publication number Publication date
KR102221928B1 (ko) 2021-03-02
US9469601B2 (en) 2016-10-18
HK1212968A1 (zh) 2016-06-24
PL2928861T3 (pl) 2017-08-31
RS55916B1 (sr) 2017-09-29
BR112015012752B1 (pt) 2020-10-27
MY179886A (en) 2020-11-18
JP2016502555A (ja) 2016-01-28
RU2655919C2 (ru) 2018-05-30
WO2014086825A1 (fr) 2014-06-12
EP2928861B1 (fr) 2017-01-11
EP2928861A1 (fr) 2015-10-14
AU2013354133A1 (en) 2015-07-23
SI2928861T1 (sl) 2017-05-31
FR2998892B1 (fr) 2015-01-02
US9687459B2 (en) 2017-06-27
AU2013354133B2 (en) 2017-07-06
AR093787A1 (es) 2015-06-24
UA114017C2 (xx) 2017-04-10
JP6391586B2 (ja) 2018-09-19
PT2928861T (pt) 2017-04-24
CN104854083A (zh) 2015-08-19
FR2998892A1 (fr) 2014-06-06
CA2893216C (fr) 2021-01-26
IL239146A (en) 2017-06-29
IL239146A0 (en) 2015-07-30
MA38229B1 (fr) 2016-09-30
RU2015126104A (ru) 2017-01-10
BR112015012752A2 (pt) 2017-07-11
MX364556B (es) 2019-04-30
MX2015006686A (es) 2015-08-10
DK2928861T3 (en) 2017-04-24
SA515360518B1 (ar) 2017-05-17
TW201427930A (zh) 2014-07-16
US20170065543A1 (en) 2017-03-09
CN104854083B (zh) 2017-05-24
TN2015000240A1 (fr) 2016-10-03
KR20150091163A (ko) 2015-08-07
CA2893216A1 (fr) 2014-06-12
CN106957285A (zh) 2017-07-18
CN106957285B (zh) 2019-05-03
CY1118841T1 (el) 2018-01-10
US20150315132A1 (en) 2015-11-05
LT2928861T (lt) 2017-04-25
MA38229A1 (fr) 2016-01-29
ES2621896T3 (es) 2017-07-05
NZ709572A (en) 2019-02-22
TWI603947B (zh) 2017-11-01

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