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AR044829A1 - Derivados de bis-4-cloro fenil pirazinas - Google Patents

Derivados de bis-4-cloro fenil pirazinas

Info

Publication number
AR044829A1
AR044829A1 ARP040102139A ARP040102139A AR044829A1 AR 044829 A1 AR044829 A1 AR 044829A1 AR P040102139 A ARP040102139 A AR P040102139A AR P040102139 A ARP040102139 A AR P040102139A AR 044829 A1 AR044829 A1 AR 044829A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
optionally substituted
formula
hydroxy
Prior art date
Application number
ARP040102139A
Other languages
English (en)
Inventor
Kristina Berggren
Leifeng Cheng
Stig Elebring
Henrik Sorensen
Original Assignee
Schuckmann Alfred Von
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
Priority claimed from GB0314061A external-priority patent/GB0314061D0/en
Priority claimed from GB0314059A external-priority patent/GB0314059D0/en
Application filed by Schuckmann Alfred Von filed Critical Schuckmann Alfred Von
Publication of AR044829A1 publication Critical patent/AR044829A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/10Antiepileptics; Anticonvulsants for petit-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/12Antiepileptics; Anticonvulsants for grand-mal
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/06Antihyperlipidemics
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de bis-4-cloro fenil pirazinas, procesos para preparar dichos compuestos, su uso en el tratamiento de obesidad, trastornos psiquiátricos y neurológicos, métodos para su uso terapéutico y composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1) donde R1 y R2 representan en forma independiente fenilo, tienilo o piridilo donde cada uno de los cuales está sustituido opcionalmente en forma independiente con uno o más grupos representados por Z; Z representa un grupo C1-8 alquilo, un grupo C1-6 alcoxi, hidroxi, halo, trifluorometilo, trifluorometiltio, trifluorometoxi, trifluorometilsulfonilo, nitro, mono o di C1-3 alquilamino, C1-3 alquilsulfonilo, C1-3 alquilsulfoniloxi, C1-3 alcoxicarbonilo, carboxi, ciano, carbamoilo, mono o di C1-3 alquilo carbamoilo, sulfamoilo, acetilo, un grupo aromático heterocíclico, opcionalmente sustituido con halo, alquilo, trifluorometilo o trifluorometoxi y un grupo heterocíclico saturado o parcialmente insaturado de entre 5 y 8 miembros que contiene uno o más heteroátomos seleccionados entre N, O o S donde el grupo heterocíclico está sustituido opcionalmente con uno o más grupos C1-3alquilo, hidroxi, fluoro, bencilo o un grupo amino-NRxRy en donde Rx y Ry representan en forma independiente H o C1-4 alquilo; R3 representa un grupo de la fórmula (CH2)nCOOR7 en donde n es 0, 1, 2, 3 o 4 y R7 representa un grupo C4-12 alquilo, un grupo C3-12 cicloalquilo o un grupo (C3-12 cicloalquil)C1-3 alquilo donde cada uno de los cuales está sustituido opcionalmente con uno o más de los siguientes: un grupo C1-6 alquilo, fluoro, amino o hidroxi, o R7 representa un grupo -(CH2)afenilo en donde a es 0, 1, 2, 3 o 4 y el grupo fenilo está sustituido opcionalmente con uno o más grupos representados por Z que pueden ser iguales o diferentes o R7 representa un grupo heterocíclico saturado o parcialmente insaturado de entre 5 y 8 miembros que contiene uno o más de los siguientes: O, S o N; donde el grupo heterocíclico está sustituido opcionalmente con uno o más grupos C1-3 alquilo, grupos C1-3 acilo, hidroxi, amino o bencilo; o R3 representa un grupo de la fórmula -(CH2)o-O-(CH2)p-R8 en donde o representa un entero 1, 2, 3 o 4 y p representa un entero 0, 1, 2, 3 o 4 y R8 representa un grupo C1-12 alquilo opcionalmente sustituido con uno o más de los siguientes: un grupo C1-6 alquilo, fluoro, hidroxi, o un grupo amino NRxRy en donde Rx y Ry representan en forma independiente H o C1-4 alquilo; o R8 representa fenilo sustituido opcionalmente en forma independiente con uno o más grupos Z o R8 representa un grupo aromático heterocíclico o un grupo heterocíclico saturado o parcialmente insaturado de entre 5 y 8 miembros que contiene uno o más de los siguientes: O, S o N donde cada uno de estos anillos está sustituido opcionalmente con uno o más grupos representados por Z que pueden ser iguales o diferentes; R3 representa un grupo de fórmula -(CH2)qR9 en donde q es 2, 3 o 4 y R9 representa un grupo C3-12 cicloalquilo, fenilo, un grupo aromático heterocíclico o un grupo heterocíclico saturado o parcialmente insaturado de entre 5 y 8 miembros que contiene uno o más de los siguientes: O, S o N donde cada uno de estos anillos está sustituido opcionalmente con uno o más grupos representados por Z que pueden ser iguales o diferentes; o R3 representa un grupo de la fórmula -(CH2)m-O-(CO)-R10 en donde m representa un entero 0, 1, 2, 3 o 4, y en donde R10 representa un grupo C1-12 alquilo opcionalmente sustituido con uno o más fluoro, hidroxi, o amino o R10 representa un grupo de la fórmula -(CH2)qR9 en donde q y R9 son como se ha descrito, o R3 tiene la siguiente fórmula (2); R11 representa hidroxi, fluoro, carboxi, un grupo C1-6 alcoxicarbonilo o un grupo amino NRxRy en donde Rx y Ry representan en forma independiente H o C1-4 alquilo; d es 1, 2 o 3; y R12 representa H o un grupo C1-3 alquilo, o R3 representa un grupo de la fórmula CONH-Rz, en donde Rz es un anillo piperidinilo sustituido con un grupo C1-6 alcanoilo o R3 representa un grupo -COG en donde G es un dihidroindol o un dihidroisoindol, unido a través de N al carbonilo, y sales aceptables para uso farmacéutico del mismo
ARP040102139A 2003-06-18 2004-06-18 Derivados de bis-4-cloro fenil pirazinas AR044829A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0314061A GB0314061D0 (en) 2003-06-18 2003-06-18 Therapeutic agents
GB0314059A GB0314059D0 (en) 2003-06-18 2003-06-18 Therapeutic agents

Publications (1)

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AR044829A1 true AR044829A1 (es) 2005-10-05

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ID=33554154

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102139A AR044829A1 (es) 2003-06-18 2004-06-18 Derivados de bis-4-cloro fenil pirazinas

Country Status (9)

Country Link
US (1) US20060135523A1 (es)
EP (1) EP1641779A1 (es)
JP (1) JP2006527770A (es)
AR (1) AR044829A1 (es)
AU (1) AU2004247615B2 (es)
CA (1) CA2527033A1 (es)
TW (1) TW200504034A (es)
UY (1) UY28374A1 (es)
WO (1) WO2004111033A1 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1546115A4 (en) 2002-09-27 2010-08-04 Merck Sharp & Dohme Substituted pyrimidines
GB0230087D0 (en) * 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
GB0230088D0 (en) * 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
GB0302672D0 (en) * 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
GB0314057D0 (en) * 2003-06-18 2003-07-23 Astrazeneca Ab Therapeutic agents
WO2006106054A1 (en) 2005-04-06 2006-10-12 F. Hoffmann-La Roche Ag Pyridine-3-carboxamide derivatives as cb1 inverse agonists
CA2606288A1 (en) * 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
US7629346B2 (en) * 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
AU2007283113A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use
US7781593B2 (en) 2006-09-14 2010-08-24 Hoffmann-La Roche Inc. 5-phenyl-nicotinamide derivatives
WO2008040651A1 (en) 2006-10-04 2008-04-10 F. Hoffmann-La Roche Ag 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents
EP2076499B1 (en) * 2006-10-04 2010-05-12 F.Hoffmann-La Roche Ag Pyrazine-2-carboxamide derivatives as cb2 receptor modulators
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
JO3465B1 (ar) 2008-06-19 2020-07-05 Takeda Pharmaceuticals Co مركب متغاير الحلقه واستخدامه
EP2310372B1 (en) 2008-07-09 2012-05-23 Sanofi Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
EP2348857B1 (en) 2008-10-22 2016-02-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
AU2009309037A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
EA022094B1 (ru) 2010-06-16 2015-10-30 Такеда Фармасьютикал Компани Лимитед Кристаллическая форма амидного соединения
US8410107B2 (en) 2010-10-15 2013-04-02 Hoffmann-La Roche Inc. N-pyridin-3-yl or N-pyrazin-2-yl carboxamides
US8669254B2 (en) 2010-12-15 2014-03-11 Hoffman-La Roche Inc. Pyridine, pyridazine, pyrimidine or pyrazine carboxamides as HDL-cholesterol raising agents
JP5728099B2 (ja) 2011-02-25 2015-06-03 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 抗糖尿病剤として有用な新規環状アザベンゾイミダゾール誘導体
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683700B1 (de) 2011-03-08 2015-02-18 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683705B1 (de) 2011-03-08 2015-04-22 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2766349B1 (de) 2011-03-08 2016-06-01 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120057A1 (de) 2011-03-08 2012-09-13 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8809324B2 (en) 2011-03-08 2014-08-19 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
RU2015106909A (ru) 2012-08-02 2016-09-27 Мерк Шарп И Доум Корп. Антидиабетические трициклические соединения
WO2014130608A1 (en) 2013-02-22 2014-08-28 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX381180B (es) * 2014-11-18 2025-03-12 Merck Sharp & Dohme Compuestos aminopirazina con propiedades antagonistas a2a.
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4348385A (en) * 1980-11-17 1982-09-07 Mobay Chemical Corporation Flowable pesticides
US4610868A (en) * 1984-03-20 1986-09-09 The Liposome Company, Inc. Lipid matrix carriers for use in drug delivery systems
US4826689A (en) * 1984-05-21 1989-05-02 University Of Rochester Method for making uniformly sized particles from water-insoluble organic compounds
FR2608988B1 (fr) * 1986-12-31 1991-01-11 Centre Nat Rech Scient Procede de preparation de systemes colloidaux dispersibles d'une substance, sous forme de nanoparticules
EP0379591B1 (en) * 1988-06-28 1994-01-19 Matsushita Electric Industrial Co., Ltd. Exhaust smoke purifier apparatus
FR2651680B1 (fr) * 1989-09-14 1991-12-27 Medgenix Group Sa Nouveau procede de preparation de microparticules lipidiques.
JP3282731B2 (ja) * 1990-06-15 2002-05-20 メルク エンド カムパニー インコーポレーテッド 結晶の構造および大きさを改良する結晶化方法
JPH06501926A (ja) * 1990-08-06 1994-03-03 藤沢薬品工業株式会社 複素環式化合物
US5145684A (en) * 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
ATE137962T1 (de) * 1991-12-05 1996-06-15 Alfatec Pharma Gmbh Pharmazeutisch applizierbares nanosol und verfahren zu seiner herstellung
FR2692575B1 (fr) * 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2713225B1 (fr) * 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
US5468604A (en) * 1992-11-18 1995-11-21 Eastman Kodak Company Photographic dispersion
GB9319129D0 (en) * 1993-09-15 1993-11-03 Dowelanco Ltd Storage and dilution of stable aqueous dispersions
SE9303281D0 (sv) * 1993-10-07 1993-10-07 Astra Ab New formulation
SE9403846D0 (sv) * 1994-11-09 1994-11-09 Univ Ohio State Res Found Small particle formation
DE4440337A1 (de) * 1994-11-11 1996-05-15 Dds Drug Delivery Services Ges Pharmazeutische Nanosuspensionen zur Arzneistoffapplikation als Systeme mit erhöhter Sättigungslöslichkeit und Lösungsgeschwindigkeit
US5665331A (en) * 1995-01-10 1997-09-09 Nanosystems L.L.C. Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers
WO1998014180A1 (en) * 1996-10-03 1998-04-09 Dmitri Kirpotin Hydrophilic microparticles and methods to prepare same
US6127520A (en) * 1997-04-15 2000-10-03 Regents Of The University Of Michigan Compositions and methods for the inhibition of neurotransmitter uptake of synaptic vesicles
FR2766368B1 (fr) * 1997-07-24 2000-03-31 Univ Claude Bernard Lyon Procede de preparation de nanocapsules de type vesiculaire, utilisables notamment comme vecteurs colloidaux de principes actifs pharmaceutiques ou autres
US6375986B1 (en) * 2000-09-21 2002-04-23 Elan Pharma International Ltd. Solid dose nanoparticulate compositions comprising a synergistic combination of a polymeric surface stabilizer and dioctyl sodium sulfosuccinate
FR2789079B3 (fr) * 1999-02-01 2001-03-02 Sanofi Synthelabo Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant
US6383471B1 (en) * 1999-04-06 2002-05-07 Lipocine, Inc. Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents
CN1205188C (zh) * 2000-03-23 2005-06-08 索尔瓦药物有限公司 具有cb1-拮抗活性的4,5-二氢-1h-吡唑衍生物
JP4714412B2 (ja) * 2001-08-06 2011-06-29 アストラゼネカ・アクチエボラーグ 水不溶性の活性でかつ賦形剤様の中鎖トリグリセリド(mct)の安定なナノ粒子を含む水性分散液
US20060003012A9 (en) * 2001-09-26 2006-01-05 Sean Brynjelsen Preparation of submicron solid particle suspensions by sonication of multiphase systems
SE0104330D0 (sv) * 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
SE0104332D0 (sv) * 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
GB0216700D0 (en) * 2002-07-18 2002-08-28 Astrazeneca Ab Process
GB0302673D0 (en) * 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
GB0302672D0 (en) * 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
GB0302671D0 (en) * 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
GB0314057D0 (en) * 2003-06-18 2003-07-23 Astrazeneca Ab Therapeutic agents

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TW200504034A (en) 2005-02-01
WO2004111033A1 (en) 2004-12-23
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EP1641779A1 (en) 2006-04-05
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