HRP20120837T1 - Derivati piperidina - Google Patents

Derivati piperidina Download PDF

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Publication number
HRP20120837T1
HRP20120837T1 HRP20120837AT HRP20120837T HRP20120837T1 HR P20120837 T1 HRP20120837 T1 HR P20120837T1 HR P20120837A T HRP20120837A T HR P20120837AT HR P20120837 T HRP20120837 T HR P20120837T HR P20120837 T1 HRP20120837 T1 HR P20120837T1
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HR
Croatia
Prior art keywords
indol
piperidin
carbonyl
alkyl
methylpropan
Prior art date
Application number
HRP20120837AT
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English (en)
Inventor
Akio Kakefuda
Kazushi Watanabe
Akio Kamikawa
Kentaro Enjo
Takashi Furutani
Minoru Yasuda
Original Assignee
Astellas Pharma Inc.
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Publication date
Application filed by Astellas Pharma Inc. filed Critical Astellas Pharma Inc.
Publication of HRP20120837T1 publication Critical patent/HRP20120837T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4465Non condensed piperidines, e.g. piperocaine only substituted in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (11)

1. Spoj, naznačen time, da ima formulu (Ia) ili njegova sol: [image] gdje: R1, R2 i R3, koji su međusobno isti ili različiti, predstavljaju H ili C1-6 alkil; R4, R5, R6, R7 i R8, koji su međusobno isti ili različiti, predstavljaju sljedeće: H, C1-6 alkil, halogen, halogen-C1-6alkil, nitro, -X-cikloalkil, koji može biti supstituiran, -X-aril, koji može biti supstituiran, -X-heterociklička skupina, koja može biti supstituirana, -X-COOR0, -X-CONR10R11, -X-CN, -X-OR0, -X-SR0, -X-S(O)-C1-6 alkil, -X-S (O)2-C1-6 alkil, -X-NR10R11, -X-NR0C(O)R10, -X-NR0C(O)OR10, -X-NR0C(O)NR10R11, -X-NR0S(O)2R10, -X-O-halogen-C1-6 alkil, -X-O-X-cikloalkil, koji može biti supstituiran, -X-O-X-aril, koji može biti supstituiran, -X-O-X-heterociklička skupina, koja može biti supstituirana, ili -X-O-C1-6 alkilen-OR0; ili R6 i R7 su kombinirani za tvorbu -O-C1-6 alkilen-O-; R0, koji može biti isti ili različit, predstavlja H ili C1-6 alkil; R10 i R11, koji su međusobno isti ili različiti, predstavljaju H, C1-6alkil, halogen-C1-6alkil, -X-cikloalkil, -X-aril ili -X-heterocikličku skupinu; ili R10 i R11, zajedno s N na koji su vezani, tvore zasićenu heterocikličku skupinu, koja može biti supstituirana; i X, koji može biti isti ili različit, predstavlja vezu ili C1-6 alkilen.
2. Spoj prema zahtjevu 1 ili njegova sol, naznačen time, da R1 i R2 su C1-6 alkil, a R3 je H.
3. Spoj prema zahtjevu 2 ili njegova sol, naznačen time, da R4, R5, R7 i R8, koji su međusobno isti ili različiti, predstavljaju H, C1-6 alkil, halogen ili -O-C1-6 alkil.
4. Spoj prema zahtjevu 2 ili 3 ili njegova sol, naznačen time, da R6 je H, C1-6 alkil, halogen, halogen-C1-6 alkil, nitro, cikloalkil, OH ili -O-C1-6 alkil.
5. Spoj prema zahtjevu 4 ili njegova sol, naznačen time, da R6 je C1-6 alkil, halogen ili -O-C1-6 alkil.
6. Spoj prema zahtjevu 2, naznačen time, da je odabran iz skupine koju čine: 1-[1-(1H-indol-2-ilkarbonil)piperidin-4-il]-2-metilpropan-2-ol; 2-metil-1-{1-[(4-metil-1H-indol-2-il)karbonil]piperidin-4-il}propan-2-ol; 2-metil-1-{1-[(5-metil-1H-indol-2-il)karbonil]piperidin-4-il}propan-2-ol; 1-{1-[(3,5-dimetil-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(5-tert-butil-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(4-fluoro-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(5-fluoro-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(4-kloro-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(5-kloro-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(5-bromo-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(7-kloro-5-fluoro-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 2-{[4-(2-hidroksi-2-metilpropil)piperidin-1-il]karbonil}-1H-indol-5-ol; 1-{1-[(4-metoksi-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(5-metoksi-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 1-{1-[(6-metoksi-1H-indol-2-il)karbonil]piperidin-4-il}-2-metilpropan-2-ol; 2-metil-1-(1-{[5-(trifluorometoksi)-1H-indol-2-il]karbonil}piperidin-4-il)propan-2-ol; i 2-metil-1-{1-[(5-nitro-1H-indol-2-il)karbonil]piperidin-4-il}propan-2-ol, ili njegova sol.
7. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema zahtjevu 1 ili njegovu sol, te farmaceutski prihvatljivo pomoćno sredstvo.
8. Uporaba spoja prema zahtjevu 1 ili njegove soli, naznačena time, da je za proizvodnju farmaceutskog sastava za prevenciju ili liječenje bolesti povezane s 17βHSD tip 5.
9. Uporaba spoja prema zahtjevu 1 ili njegove soli, naznačena time, da je za proizvodnju farmaceutskog sastava za prevenciju ili liječenje raka prostate, benigne prostatske hiperplazije, akni, seboreje, hirzutizma, ćelavosti, alopecije, preuranjenog puberteta, adrenalne hipertrofije, sindroma policističnih jajnika, raka dojke, endometrioze, raka pluća ili lejomioma.
10. Komercijalni paket, naznačen time, da sadrži farmaceutski sastav, koji obuhvaća spoj prema zahtjevu 1 ili njegovu sol; te uputstvo da je spoj prema zahtjevu 1, ili njegova sol, pogodan za upotrebu ili bi ga trebalo upotrebljavati za liječenje i/ili prevenciju raka prostate, benigne prostatske hiperplazije, akni, seboreje, hirzutizma, ćelavosti, alopecije, preuranjenog puberteta, adrenalne hipertrofije, sindroma policističnih jajnika, raka dojke, endometrioze, raka pluća ili lejomioma.
11. Spoj prema zahtjevu 1 ili njegova sol, naznačen time, da je za uporabu u liječenju raka prostate, benigne prostatske hiperplazije, akni, seboreje, hirzutizma, ćelavosti, alopecije, preuranjenog puberteta, adrenalne hipertrofije, sindroma policističnih jajnika, raka dojke, endometrioze, raka pluća ili lejomioma.
HRP20120837AT 2007-08-31 2012-10-18 Derivati piperidina HRP20120837T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007225378 2007-08-31
PCT/JP2008/065429 WO2009028618A1 (ja) 2007-08-31 2008-08-28 ピペリジン誘導体

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HRP20120837T1 true HRP20120837T1 (hr) 2012-11-30

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Country Status (20)

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US (1) US8513422B2 (hr)
EP (1) EP2181990B1 (hr)
JP (1) JP5327051B2 (hr)
KR (1) KR20100050444A (hr)
CN (1) CN101821253B (hr)
AU (1) AU2008292420A1 (hr)
BR (1) BRPI0815787A2 (hr)
CA (1) CA2696799A1 (hr)
CY (1) CY1113417T1 (hr)
DK (1) DK2181990T3 (hr)
ES (1) ES2392120T3 (hr)
HR (1) HRP20120837T1 (hr)
MX (1) MX2010002268A (hr)
PL (1) PL2181990T3 (hr)
PT (1) PT2181990E (hr)
RU (1) RU2470020C2 (hr)
SI (1) SI2181990T1 (hr)
TW (1) TW200924765A (hr)
WO (1) WO2009028618A1 (hr)
ZA (1) ZA201000917B (hr)

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JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
JP2012102017A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc インドール化合物
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Also Published As

Publication number Publication date
BRPI0815787A2 (pt) 2015-02-24
EP2181990A1 (en) 2010-05-05
EP2181990A4 (en) 2011-09-07
PL2181990T3 (pl) 2013-01-31
JP5327051B2 (ja) 2013-10-30
AU2008292420A1 (en) 2009-03-05
RU2010112412A (ru) 2011-10-10
JPWO2009028618A1 (ja) 2010-12-02
CY1113417T1 (el) 2016-06-22
EP2181990B1 (en) 2012-08-08
US8513422B2 (en) 2013-08-20
TW200924765A (en) 2009-06-16
CN101821253A (zh) 2010-09-01
WO2009028618A1 (ja) 2009-03-05
RU2470020C2 (ru) 2012-12-20
CA2696799A1 (en) 2009-03-05
PT2181990E (pt) 2012-10-16
KR20100050444A (ko) 2010-05-13
CN101821253B (zh) 2013-07-17
US20100256189A1 (en) 2010-10-07
ZA201000917B (en) 2011-04-28
ES2392120T3 (es) 2012-12-04
DK2181990T3 (da) 2012-09-10
MX2010002268A (es) 2010-03-25
SI2181990T1 (sl) 2012-10-30

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