HRP20120073T1 - NOVI KRISTALNI OBLIK DERIVATA PIRIDAZINO[ b]INDOLA - Google Patents

NOVI KRISTALNI OBLIK DERIVATA PIRIDAZINO[ b]INDOLA Download PDF

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HRP20120073T1
HRP20120073T1 HRP20120073TT HRP20120073T HRP20120073T1 HR P20120073 T1 HRP20120073 T1 HR P20120073T1 HR P20120073T T HRP20120073T T HR P20120073TT HR P20120073 T HRP20120073 T HR P20120073T HR P20120073 T1 HRP20120073 T1 HR P20120073T1
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prevention
treatment
intended
crystalline form
pharmaceutical preparation
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HRP20120073TT
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William@L@@Rocco
John@D@@Higgins
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Sanofi@Aventis@U@S@@LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Kristalni oblik spoja Formule A označen kao Oblik II naznačen time što mu uzorak difrakcije rendgenskih zraka sadrži pikove na ± ° ° i ° gdje su uzorci XRPDdobiveni difraktometrom rendgenskih zraka na prahu uz pomoć zračenja K a uzorci su skenirani brzinom od ° u minuti od do ° pod uglom od Patent sadrži još patentnih zahtjeva

Claims (21)

1. Kristalni oblik spoja Formule (A): [image] označen kao Oblik II, naznačen time što mu uzorak difrakcije rendgenskih zraka sadrži pikove na (± 0,15° 2θ): 5.71°, 11,47 i 9,97° 2θ, gdje su uzorci XRPD dobiveni difraktometrom rendgenskih zraka na prahu, uz pomoć zračenja Kα, a uzorci su skenirani brzinom od 1,0° u minuti, od 2 do 40°, pod uglom od 2θ.
2. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što uzorak difrakcije rendgenskih zraka također sadrži pikove na (± 0,15° 2θ): 19,21, 18,43, 15,95, te 11,97° 2θ.
3. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je uglavnom čist od bilo kojeg drugog polimorfa.
4. Farmaceutski pripravak, naznačen time što sadrži kristalni oblik u skladu s patentnim zahtjevom 1 i jednu ili više farmaceutski prihvatljivih pomoćnih tvari.
5. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju bolesti ili poremećaja povezanog s disfunkcijom perifernog tipa benzodiazepinskih receptora.
6. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju bolesti ili poremećaja povezanog s disfunkcijom perifernog tipa benzodiazepinskih receptora.
7. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju neurodegenerativne bolesti.
8. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju neurodegenerativne bolesti.
9. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju neuropatije.
10. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju neuropatije.
11. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju raka ili tumora.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju raka ili tumora.
13. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju kutanog stresa.
14. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju kutanog stresa.
15. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju reumatoidnog artritisa.
16. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju reumatoidnog artritisa.
17. Kristalni oblik u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen liječenju ili sprječavanju bolesti srca ili poremećaja srca.
18. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen liječenju ili sprječavanju bolesti srca ili poremećaja srca.
19. Postupak dobivanja kristalnog oblika u skladu s patentnim zahtjevom 1, naznačen time što se navedeni postupak sastoji u koracima miješanja 7-klor-N,N,5-trimetil-4-okso-3-fenil-3,5-dihidro-4H-piridazino[4,5-b]indol-1-acetamida s nižim alkoholom, primjerice metanolom ili etanolom, u koncentraciji od otprilike 1 mg/ml do otprilike 4 mg/ml, kako bi se dobilo smjesu, grijanja smjese do temperature između otprilike 45 °C i otprilike 60 °C, filtriranja smjese, te otparavanja nižeg alkohola iz filtrata strujom inertnog plina kako bi se dobilo krutinu.
20. Postupak dobivanja kristalnog oblika u skladu s patentnim zahtjevom 1, naznačen time što se navedeni postupak sastoji u koracima otapanja 7-klor-N,N,5-trimetil-4-okso-3-fenil-3,5-dihidro-4H-piridazino[4,5-b]indol-1-acetamida u diklormetanu, u koncentraciji od otprilike 30 mg/ml do otprilike 50 mg/ml, kako bi se dobilo otopinu; dodavanja otopine u etanol, u omjeru od otprilike 1:3 do otprilike 1:4, volumno, u odnosu na količinu diklormetana, zatim koncentriranja otopine, smanjivanja volumena za otprilike 10% do otprilike 40% strujom inertnog plina dok se krutina ne iskristalizira, te izdvajanja krutine.
21. Postupak dobivanja kristalnog oblika u skladu s patentnim zahtjevom 1, naznačen time što se navedeni postupak sastoji u koracima otapanja 7-klor-N,N,5-trimetil-4-okso-3-fenil-3,5-dihidro-4H-piridazino[4,5-b]indol-1-acetamida u diklormetanu, u koncentraciji od otprilike 20 mg/ml do otprilike 50 mg/ml, kako bi se dobilo otopinu, dodavanja otopine u heksane kako bi došlo do taloženja krutine, te izdvajanja krutine.
HRP20120073TT 2005-08-29 2012-01-23 NOVI KRISTALNI OBLIK DERIVATA PIRIDAZINO[ b]INDOLA HRP20120073T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US71215305P 2005-08-29 2005-08-29
PCT/US2006/033254 WO2007027525A1 (en) 2005-08-29 2006-08-24 Novel crystalline form of a pyridazino [4 , 5-b] indole derivative

Publications (1)

Publication Number Publication Date
HRP20120073T1 true HRP20120073T1 (hr) 2012-07-31

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ID=37546937

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HRP20120073TT HRP20120073T1 (hr) 2005-08-29 2012-01-23 NOVI KRISTALNI OBLIK DERIVATA PIRIDAZINO[ b]INDOLA

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Country Link
US (1) US7683062B2 (hr)
EP (1) EP1924585B1 (hr)
JP (1) JP5063600B2 (hr)
KR (2) KR20080050577A (hr)
CN (1) CN101253176B (hr)
AR (1) AR057099A1 (hr)
AT (1) ATE531717T1 (hr)
AU (1) AU2006285142B2 (hr)
BR (1) BRPI0615259A2 (hr)
CA (1) CA2619284C (hr)
CR (1) CR9723A (hr)
CY (1) CY1112317T1 (hr)
DK (1) DK1924585T3 (hr)
EA (1) EA014164B1 (hr)
EC (1) ECSP088209A (hr)
ES (1) ES2375841T3 (hr)
HK (1) HK1123794A1 (hr)
HR (1) HRP20120073T1 (hr)
IL (1) IL189276A (hr)
MA (1) MA30000B1 (hr)
NO (1) NO20081365L (hr)
NZ (1) NZ566087A (hr)
PL (1) PL1924585T3 (hr)
PT (1) PT1924585E (hr)
RS (1) RS52318B (hr)
SI (1) SI1924585T1 (hr)
TN (1) TNSN08059A1 (hr)
TW (1) TW200813060A (hr)
UA (1) UA91716C2 (hr)
UY (1) UY29771A1 (hr)
WO (1) WO2007027525A1 (hr)
ZA (1) ZA200801890B (hr)

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JP2007536210A (ja) * 2003-11-17 2007-12-13 メルック・エプロバ・アクチエンゲゼルシヤフト (6r)−l−エリスロ−テトラヒドロビオプテリンジヒドロクロライドの結晶形
JP2008501657A (ja) * 2004-06-02 2008-01-24 サンド・アクチエンゲゼルシヤフト 結晶形態のメロペネム中間体
BRPI0616040A2 (pt) * 2005-09-21 2011-06-07 Nycomed Gmbh cloridrato de sulfonilpirról como inibidor de histona desacetilases
EP1951700A2 (en) * 2005-10-31 2008-08-06 Janssen Pharmaceutica N.V. Novel processes for the preparation of piperazinyl and diazapanyl benzamide derivatives
EP2044020B1 (en) * 2006-06-16 2011-05-04 H. Lundbeck A/S Crystalline forms of 4- [2- (4-methylphenylsulfanyl) -phenyl]piperidine with combined serotonin and norepinephrine reuptake inhibition for the treatment of neuropathic pain
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EP2085397A1 (en) * 2008-01-21 2009-08-05 Esteve Quimica, S.A. Crystalline form of abacavir
US7935817B2 (en) * 2008-03-31 2011-05-03 Apotex Pharmachem Inc. Salt form and cocrystals of adefovir dipivoxil and processes for preparation thereof
AR071318A1 (es) * 2008-04-15 2010-06-09 Basilea Pharmaceutica Ag Benzhidril ester del acido (6r,7r)-7-{2-(5-amino-[1,2,4]tiadiazol-3-il)-2-[(z)-tritiloxiimino]-acetilamino}-3-[(r)-1'-terc-butoxicarbonil-2-oxo-[1,3']bipirrolidinil-(3e)-ilidenometil]-8-oxo-5-tia-1-aza-biciclo[4.2.0]oct-2-eno-2-carboxilico cristalino; su elaboracion y uso
US8097719B2 (en) * 2008-07-15 2012-01-17 Genesen Labs Meropenem intermediate in novel crystalline form and a method of manufacture of meropenem
KR20110052640A (ko) * 2008-08-18 2011-05-18 사노피-아벤티스 유.에스. 엘엘씨 7-클로로-N,N,5-트리메틸-4-옥소-3-페닐-3,5-디하이드로-4H-피리다지노[4,5-b]인돌-1-아세트아미드의 다형체의 제조방법
NZ601967A (en) 2010-03-12 2015-03-27 Omeros Corp Pde10 inhibitors and related compositions and methods
EP2611433A2 (en) * 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Non-hygroscopic salts of 5-ht2c agonists
WO2013044816A1 (en) * 2011-09-30 2013-04-04 Sunshine Lake Pharma Co., Ltd. Crystalline forms of azilsartan and preparation and uses thereof
NZ716462A (en) * 2014-04-28 2017-11-24 Omeros Corp Optically active pde10 inhibitor
NZ630810A (en) 2014-04-28 2016-03-31 Omeros Corp Processes and intermediates for the preparation of a pde10 inhibitor
EP3285760A4 (en) 2015-04-24 2018-09-26 Omeros Corporation Pde10 inhibitors and related compositions and methods
JP2018535969A (ja) 2015-11-04 2018-12-06 オメロス コーポレーション Pde10阻害剤の固体状態形態
CN111303230B (zh) * 2020-03-09 2021-07-13 中国食品药品检定研究院 一种黄体酮共晶物及其制备方法和用途

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FR2766823B1 (fr) * 1997-07-30 1999-10-08 Synthelabo Derives de 4-oxo-3,5-dihydro-4h-pyridazino[4,5-b] indole-1-acetamide, leur preparation et leur application en therapeutique
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Also Published As

Publication number Publication date
CR9723A (es) 2008-06-18
DK1924585T3 (da) 2012-02-27
IL189276A (en) 2012-07-31
EP1924585B1 (en) 2011-11-02
ES2375841T3 (es) 2012-03-06
ATE531717T1 (de) 2011-11-15
EA200800716A1 (ru) 2008-08-29
HK1123794A1 (en) 2009-06-26
US7683062B2 (en) 2010-03-23
CA2619284A1 (en) 2007-03-08
JP2009506116A (ja) 2009-02-12
EP1924585A1 (en) 2008-05-28
EA014164B1 (ru) 2010-10-29
CY1112317T1 (el) 2015-12-09
KR20080050577A (ko) 2008-06-09
PL1924585T3 (pl) 2012-08-31
SI1924585T1 (sl) 2012-09-28
UA91716C2 (ru) 2010-08-25
JP5063600B2 (ja) 2012-10-31
US20080139569A1 (en) 2008-06-12
NO20081365L (no) 2008-04-03
CN101253176A (zh) 2008-08-27
ECSP088209A (es) 2008-06-30
AU2006285142B2 (en) 2012-06-14
MA30000B1 (fr) 2008-12-01
ZA200801890B (en) 2009-11-25
CN101253176B (zh) 2012-04-18
PT1924585E (pt) 2012-01-19
AR057099A1 (es) 2007-11-14
UY29771A1 (es) 2007-03-30
CA2619284C (en) 2014-04-29
KR20130087059A (ko) 2013-08-05
NZ566087A (en) 2011-03-31
TW200813060A (en) 2008-03-16
BRPI0615259A2 (pt) 2011-05-17
RS52318B (en) 2012-12-31
IL189276A0 (en) 2008-08-07
AU2006285142A1 (en) 2007-03-08
WO2007027525A1 (en) 2007-03-08
TNSN08059A1 (en) 2009-07-14

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