CO5700743A2 - Formas polimorficas de un agonista de gaba a - Google Patents

Formas polimorficas de un agonista de gaba a

Info

Publication number
CO5700743A2
CO5700743A2 CO06073254A CO06073254A CO5700743A2 CO 5700743 A2 CO5700743 A2 CO 5700743A2 CO 06073254 A CO06073254 A CO 06073254A CO 06073254 A CO06073254 A CO 06073254A CO 5700743 A2 CO5700743 A2 CO 5700743A2
Authority
CO
Colombia
Prior art keywords
peak
powder
values
ray diffraction
cuka radiation
Prior art date
Application number
CO06073254A
Other languages
English (en)
Inventor
Vincent Brett Cooper
Original Assignee
Merck Sharp & Dohme
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=31971783&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO5700743(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of CO5700743A2 publication Critical patent/CO5700743A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

1.- El compuesto monohidrato de gaboxadol en una forma cristalina.2.- El compuesto de acuerdo con la reivindicación 1 en una forma cristalina seleccionada de: (a) forma I la cual se caracteriza por un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a 11,5°; y (b) forma II la cual se caracteriza por un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a 25,2°.3.- El compuesto de acuerdo con la reivindicación 2 el cual es monohidrato de gaboxadol cristalino de forma II el cual se caracteriza por un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a 25,2°.4.- El compuesto de acuerdo con la reivindicación 3 el cual se caracteriza adicionalmente mediante cambios químicos en RMN 13C en el estado sólido de 17,5, 40,3, 102,2, 158,5 y 172,5 ppm con referencia a un valor de 176,03 ppm para el pico carbonilo de glicina.5.- El compuesto anhidrato de gaboxadol en una forma cristalina seleccionada de: (a) forma I la cual se caracteriza por un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a 12,8°; y (b) forma II la cual se caracteriza por un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a uno o más de 16,0°, 24,7° y 28,4°.6.- El compuesto de acuerdo con reivindicación 5 el cual es anhidrato de gaboxadol cristalino de forma II el cual se caracteriza mediante un espectro de difracción de rayos X en polvo en valores de 2? usando radiación CuKa que tiene un pico a uno o más de 16,0°, 24,7° y 28,4° en la ausencia de un pico a 12,8°.
CO06073254A 2004-01-30 2006-07-26 Formas polimorficas de un agonista de gaba a CO5700743A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0402118.4A GB0402118D0 (en) 2004-01-30 2004-01-30 Polymorphic forms of a GABAA agonist

Publications (1)

Publication Number Publication Date
CO5700743A2 true CO5700743A2 (es) 2006-11-30

Family

ID=31971783

Family Applications (1)

Application Number Title Priority Date Filing Date
CO06073254A CO5700743A2 (es) 2004-01-30 2006-07-26 Formas polimorficas de un agonista de gaba a

Country Status (35)

Country Link
US (2) US7262300B2 (es)
EP (2) EP1713813B1 (es)
JP (1) JP4917440B2 (es)
KR (1) KR101210361B1 (es)
CN (1) CN1914212B (es)
AR (1) AR047511A1 (es)
AT (1) ATE414088T1 (es)
AU (1) AU2005209473B2 (es)
BR (1) BRPI0506858A (es)
CA (1) CA2554536C (es)
CO (1) CO5700743A2 (es)
CY (1) CY1108647T1 (es)
DE (1) DE602005010975D1 (es)
DK (1) DK1713813T3 (es)
DO (1) DOP2005000013A (es)
EA (1) EA009413B1 (es)
EC (1) ECSP066735A (es)
ES (1) ES2314613T3 (es)
GB (2) GB0402118D0 (es)
HK (1) HK1096547A1 (es)
HR (1) HRP20080614T3 (es)
IL (1) IL176863A0 (es)
MA (1) MA28364A1 (es)
MX (1) MXPA06008595A (es)
MY (1) MY139525A (es)
NO (1) NO20063843L (es)
NZ (1) NZ548191A (es)
PE (1) PE20050769A1 (es)
PL (1) PL1713813T3 (es)
PT (1) PT1713813E (es)
SI (1) SI1713813T1 (es)
TW (1) TWI345972B (es)
UA (1) UA87487C2 (es)
WO (1) WO2005073237A2 (es)
ZA (1) ZA200605307B (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0402118D0 (en) 2004-01-30 2004-03-03 Merck Sharp & Dohme Polymorphic forms of a GABAA agonist
US20060063802A1 (en) 2004-03-29 2006-03-23 Matthieu Guitton Methods for the treatment of tinnitus induced by cochlear excitotoxicity
US9072662B2 (en) 2004-03-29 2015-07-07 Auris Medical Ag Methods for the treatment of tinnitus induced by cochlear excitotoxicity
US8268866B2 (en) 2004-03-29 2012-09-18 Matthieu Guitton Methods for the treatment of tinnitus induced by cochlear excitotoxicity
DE102005004343A1 (de) * 2005-01-25 2006-08-10 Eberhard-Karls-Universität Tübingen Universitätsklinikum Behandlung von Phantomphänomenen
US8022084B2 (en) 2005-01-28 2011-09-20 H. Lundbeck A/S Polymorphic forms of a GABAA agonist
SI1928405T1 (sl) 2005-09-28 2014-12-31 Auris Medical Ag Farmacevtski sestavki za zdravljenje motenj notranjega ušesa
CN102093387B (zh) * 2009-12-10 2012-07-25 天津泰普医药知识产权流转储备中心有限公司 4,5,6,7-四氢异噁唑并[5,4-c]吡啶-3-醇一水合物的晶型化合物
US20150044200A1 (en) 2011-12-12 2015-02-12 Otolanum Ag Treatment of tinnitus through modulation of chloride co-transporter nkcc1 in the auditory system
KR20180031721A (ko) * 2015-07-17 2018-03-28 오비드 테라퓨틱스 인크. 가복사돌로 발달장애들을 치료하는 방법들
KR102518846B1 (ko) 2016-08-11 2023-04-05 오비드 테라퓨틱스 인크. 간질 장애의 치료를 위한 방법 및 조성물
EP3528807A4 (en) * 2016-11-22 2020-06-17 Ovid Therapeutics Inc METHOD FOR TREATING DEVELOPMENT DISORDERS AND / OR FALLS WITH FLUPIRTIN
US10071083B2 (en) * 2017-02-03 2018-09-11 Ovid Therapeutics Inc Use of gaboxadol in the treatment of tinnitus
WO2019028234A1 (en) 2017-08-04 2019-02-07 Ovid Therapeutics Inc. USE OF GABOXADOL IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS
MX2021003302A (es) 2018-09-20 2021-05-13 Ovid Therapeutics Inc Uso de gaboxadol para el tratamiento del sindrome de tourette, los tics y la tartamudez.
EP3883566A4 (en) 2018-11-21 2022-09-07 Certego Therapeutics Inc. GABOXADOL FOR SUICIDE RISK REDUCTION AND RAPID DEPRESSION RELIEF
CA3123876A1 (en) 2018-12-17 2020-06-25 Ovid Therapeutics Inc. Use of gaboxadol for the treatment of non-24 hour sleep-wake disorder
EP4051272A4 (en) 2019-12-18 2023-01-04 Ovid Therapeutics Inc. GABOXADOL FOR THE THERAPEUTIC TREATMENT OF 1p36 DELETION SYNDROME
CA3182508A1 (en) 2020-05-20 2021-11-25 Certego Therapeutics Inc. Ring deuterated gaboxadol and its use for the treatment of psychiatric disorders

Family Cites Families (22)

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Publication number Priority date Publication date Assignee Title
DK270278A (da) 1977-06-20 1978-12-21 Krogsgaard Larsen P Cycliske aminosyrer
US4315934A (en) 1979-09-24 1982-02-16 Sandoz Ltd. Organic compounds
US4362731A (en) 1980-09-01 1982-12-07 Sandoz Ltd. Myotonolytic use of 4,5,6,7-tetrahydroisoxazolo [5,4-c] pyridin-3-ol and derivatives thereof
US4352731A (en) * 1980-11-03 1982-10-05 Occidental Research Corporation Apparatus for selective wetting of particles
DE19525598C2 (de) 1995-07-13 1997-09-25 Max Planck Gesellschaft Schlafmittel
UA52661C2 (uk) * 1996-06-14 2003-01-15 Ново Нордіск А/С Безводна кристалічна форма гідрохлориду r(-)-n-(4,4-ди(3-метилтієн-2-іл)бут-3-еніл) ніпекотинової кислоти
CA2385749A1 (en) 1999-09-28 2001-04-05 H. Lundbeck A/S Melt granulated composition and modified release dosage form prepared from said composition
AR031473A1 (es) 2000-11-20 2003-09-24 Lundbeck & Co As H Intensificadores de gaba en el tratamiento de enfermedades relacionadas con una reducida actividad neuroesteroide
WO2002094255A1 (de) 2001-05-18 2002-11-28 Lonza Ag Verfahren zur herstellung fester formulierungen von natrium-3-hydroxy-3-methylbutyrat
AR033896A1 (es) 2001-05-21 2004-01-07 Lundbeck & Co As H Preparaciones granuladas de gaboxadol.
WO2004022550A1 (en) * 2002-09-03 2004-03-18 Naturon Limited Compound for treatment of anxiety and methods of preparation and use thereof
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ES2341004T3 (es) * 2003-06-25 2010-06-14 H. Lundbeck A/S Gaboxadol para tratar la depresion y otros trastornos afectivos.
AR045540A1 (es) 2003-09-05 2005-11-02 Lundbeck & Co As H Metodo de elaboracion de 4,5,6,7 tetrahidroisoxazol [5,4-c] piridin-3-ol (thip)
EP1663218A1 (en) 2003-09-10 2006-06-07 MERCK SHARP & DOHME LTD. Use of gabaa receptor agonists for the treatment of hearing, vestibular and attention disorders, intention tremor and restless leg syndrome
TW200528098A (en) 2003-12-18 2005-09-01 Lundbeck & Co As H Treatment of insomnia in human patients
GB0402118D0 (en) 2004-01-30 2004-03-03 Merck Sharp & Dohme Polymorphic forms of a GABAA agonist
EA200700102A1 (ru) 2004-06-29 2007-06-29 Х.Лундбекк А/С Лечение невропатической боли, фибромиалгии или ревматоидного артрита
GB0417558D0 (en) 2004-08-06 2004-09-08 Merck Sharp & Dohme Novel combination therapy
US8022084B2 (en) * 2005-01-28 2011-09-20 H. Lundbeck A/S Polymorphic forms of a GABAA agonist
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EP1906953A4 (en) 2005-04-29 2009-05-20 Lundbeck & Co As H FORMS OF ACID SALTS AND BASIC SALTS OF GABOXADOL

Also Published As

Publication number Publication date
PE20050769A1 (es) 2005-10-04
KR101210361B1 (ko) 2012-12-10
AU2005209473B2 (en) 2010-03-04
US7262300B2 (en) 2007-08-28
CY1108647T1 (el) 2014-04-09
PT1713813E (pt) 2008-12-26
HK1096547A1 (en) 2007-06-01
GB0501847D0 (en) 2005-03-09
NZ548191A (en) 2010-04-30
CA2554536C (en) 2012-09-18
UA87487C2 (ru) 2009-07-27
DE602005010975D1 (de) 2008-12-24
NO20063843L (no) 2006-08-29
MY139525A (en) 2009-10-30
AR047511A1 (es) 2006-01-25
MA28364A1 (fr) 2006-12-01
DK1713813T3 (da) 2009-02-16
KR20070007070A (ko) 2007-01-12
US20050171142A1 (en) 2005-08-04
MXPA06008595A (es) 2006-08-28
JP4917440B2 (ja) 2012-04-18
WO2005073237A3 (en) 2005-10-20
CN1914212B (zh) 2010-10-06
US8236958B2 (en) 2012-08-07
IL176863A0 (en) 2006-10-31
BRPI0506858A (pt) 2007-05-29
GB0402118D0 (en) 2004-03-03
ZA200605307B (en) 2007-11-28
WO2005073237A2 (en) 2005-08-11
EA009413B1 (ru) 2007-12-28
TW200534856A (en) 2005-11-01
AU2005209473A1 (en) 2005-08-11
PL1713813T3 (pl) 2009-04-30
SI1713813T1 (sl) 2009-02-28
ES2314613T3 (es) 2009-03-16
EP1713813B1 (en) 2008-11-12
EP1713813A2 (en) 2006-10-25
ATE414088T1 (de) 2008-11-15
JP2007519697A (ja) 2007-07-19
CA2554536A1 (en) 2005-08-11
ECSP066735A (es) 2006-10-31
CN1914212A (zh) 2007-02-14
GB2410434A (en) 2005-08-03
HRP20080614T3 (en) 2009-01-31
TWI345972B (en) 2011-08-01
DOP2005000013A (es) 2005-08-15
EA200601404A1 (ru) 2006-12-29
EP2042505A1 (en) 2009-04-01
US20070259912A1 (en) 2007-11-08

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