CN1324014C - 用作pde4抑制剂的哒嗪－3(2h)－酮衍生物、制备方法以及其组合物和用途 - Google Patents

用作pde4抑制剂的哒嗪－3(2h)－酮衍生物、制备方法以及其组合物和用途 Download PDF

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Publication number
CN1324014C
CN1324014C CNB03816342XA CN03816342A CN1324014C CN 1324014 C CN1324014 C CN 1324014C CN B03816342X A CNB03816342X A CN B03816342XA CN 03816342 A CN03816342 A CN 03816342A CN 1324014 C CN1324014 C CN 1324014C
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phenyl
amino
ethanoyl
ethyl
ketone
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Expired - Fee Related
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CN1668603A (zh
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V·达尔皮亚兹
M·P·乔瓦诺尼
C·韦尔杰利
N·阿吉拉伊斯基耶多
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Almirall SA
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Almirall Prodesfarma SA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-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
    • C07D237/22—Nitrogen and oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CNB03816342XA 2002-05-16 2003-05-14 用作pde4抑制剂的哒嗪－3(2h)－酮衍生物、制备方法以及其组合物和用途 Expired - Fee Related CN1324014C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ESP200201111 2002-05-16
ES200201111A ES2195785B1 (es) 2002-05-16 2002-05-16 Nuevos derivados de piridazin-3(2h)-ona.

Publications (2)

Publication Number Publication Date
CN1668603A CN1668603A (zh) 2005-09-14
CN1324014C true CN1324014C (zh) 2007-07-04

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CNB03816342XA Expired - Fee Related CN1324014C (zh) 2002-05-16 2003-05-14 用作pde4抑制剂的哒嗪－3(2h)－酮衍生物、制备方法以及其组合物和用途

Country Status (23)

Country Link
US (2) US7459453B2 (https=)
EP (1) EP1503992A1 (https=)
JP (1) JP2005533024A (https=)
KR (1) KR20040106536A (https=)
CN (1) CN1324014C (https=)
AR (1) AR040076A1 (https=)
AU (1) AU2003236648A1 (https=)
BR (1) BR0310106A (https=)
CA (1) CA2485896A1 (https=)
EC (1) ECSP045410A (https=)
ES (1) ES2195785B1 (https=)
IL (1) IL165173A0 (https=)
MX (1) MXPA04011209A (https=)
MY (1) MY132106A (https=)
NO (1) NO20045461L (https=)
NZ (1) NZ536604A (https=)
PE (1) PE20040689A1 (https=)
RU (1) RU2326869C2 (https=)
TW (1) TWI309981B (https=)
UA (1) UA77532C2 (https=)
UY (1) UY27807A1 (https=)
WO (1) WO2003097613A1 (https=)
ZA (1) ZA200409173B (https=)

Families Citing this family (62)

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US7214687B2 (en) 1999-07-14 2007-05-08 Almirall Ag Quinuclidine derivatives and medicinal compositions containing the same
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
ES2211344B1 (es) * 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
CN1938296A (zh) * 2004-04-01 2007-03-28 安斯泰来制药有限公司 作为腺苷拮抗剂的吡嗪衍生物及其制药用途
BRPI0510486A (pt) * 2004-05-19 2007-11-20 Basf Ag composto, processo para preparar o mesmo, agente pesticida, e, processo para combater fungos nocivos fitopatogênicos
ATE474601T1 (de) 2004-05-31 2010-08-15 Almirall Sa Kombinationen mit antimuskarin-wirkstoffen und pde4-hemmern
ES2257152B1 (es) 2004-05-31 2007-07-01 Laboratorios Almirall S.A. Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos.
ES2251866B1 (es) * 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2251867B1 (es) * 2004-06-21 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
ES2298049B1 (es) 2006-07-21 2009-10-20 Laboratorios Almirall S.A. Procedimiento para fabricar bromuro de 3(r)-(2-hidroxi-2,2-ditien-2-ilacetoxi)-1-(3-fenoxipropil)-1-azoniabiciclo (2.2.2) octano.
AU2008219166B2 (en) * 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
ES2320954B1 (es) * 2007-03-02 2010-03-16 Laboratorio Almirall S.A. Nuevo procedimiento de preparacion de 3-metil-4-fenilisoxazolo (3,4-d)iridazin-7(6h)-ona.
ES2320955B1 (es) 2007-03-02 2010-03-16 Laboratorios Almirall S.A. Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida.
EP2096105A1 (en) 2008-02-28 2009-09-02 Laboratorios Almirall, S.A. Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the b2 adrenergic receptor
EP2100599A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2100598A1 (en) 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
EP2113503A1 (en) 2008-04-28 2009-11-04 Laboratorios Almirall, S.A. New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
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EP2226323A1 (en) 2009-02-27 2010-09-08 Almirall, S.A. New tetrahydropyrazolo[3,4-c]isoquinolin-5-amine derivatives
EP2228368A1 (en) 2009-03-12 2010-09-15 Almirall, S.A. Process for manufacturing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one
EP2322176A1 (en) 2009-11-11 2011-05-18 Almirall, S.A. New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
EP2360158A1 (en) 2010-02-18 2011-08-24 Almirall, S.A. Pyrazole derivatives as jak inhibitors
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
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EP2386555A1 (en) 2010-05-13 2011-11-16 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
EP2394998A1 (en) 2010-05-31 2011-12-14 Almirall, S.A. 3-(5-Amino-6-oxo-1,6-dihydropyridazin-3-yl)-biphenyl derivatives as PDE4 inhibitors
EP2397482A1 (en) 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
EP2441755A1 (en) 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
EP2457900A1 (en) 2010-11-25 2012-05-30 Almirall, S.A. New pyrazole derivatives having CRTh2 antagonistic behaviour
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
EP2510928A1 (en) 2011-04-15 2012-10-17 Almirall, S.A. Aclidinium for use in improving the quality of sleep in respiratory patients
EP2518070A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
EP2518071A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
EP2526945A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. New CRTH2 Antagonists
EP2548863A1 (en) 2011-07-18 2013-01-23 Almirall, S.A. New CRTh2 antagonists.
EP2548876A1 (en) 2011-07-18 2013-01-23 Almirall, S.A. New CRTh2 antagonists
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
EP2578570A1 (en) 2011-10-07 2013-04-10 Almirall, S.A. Novel process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one via novel intermediates of synthesis.
EP2592077A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
EP2592078A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
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EP2647627A1 (en) 2012-04-02 2013-10-09 Almirall, S.A. Salts of 5-[(1r)-2-({2-[4-(2,2-difluoro-2-phenylethoxy)phenyl] ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1h)-one.
EP2666465A1 (en) 2012-05-25 2013-11-27 Almirall, S.A. Novel dosage and formulation
EP2668941A1 (en) 2012-05-31 2013-12-04 Almirall, S.A. Novel dosage form and formulation of abediterol
JP6215315B2 (ja) 2012-06-12 2017-10-18 アッヴィ・インコーポレイテッド ピリジノンおよびピリダジノン誘導体
WO2014060431A1 (en) 2012-10-16 2014-04-24 Almirall, S.A. Pyrrolotriazinone derivatives as pi3k inhibitors
EP2738172A1 (en) 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
LT2931275T (lt) 2012-12-17 2022-06-27 Almirall S.A. Aklidiniumas, skirtas naudoti fizinio aktyvumo kasdieniniame gyvenime padidinimui pacientui, sergančiam lėtine obstrukcine plaučių liga
ES2750523T3 (es) 2012-12-18 2020-03-26 Almirall Sa Derivados de ciclohexil y quinuclidinil carbamato que tienen actividades de agonista beta2 adrenérgicos y antagonistas muscarínicos M3
TW201446767A (zh) 2013-02-15 2014-12-16 Almirall Sa 作為磷脂肌醇3-激酶抑製劑之吡咯並三嗪衍生物
EP2848615A1 (en) 2013-07-03 2015-03-18 Almirall, S.A. New pyrazole derivatives as CRAC channel modulators
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RU2004136977A (ru) 2005-07-10
KR20040106536A (ko) 2004-12-17
BR0310106A (pt) 2005-02-22
ECSP045410A (es) 2005-01-03
US20060052379A1 (en) 2006-03-09
CN1668603A (zh) 2005-09-14
ZA200409173B (en) 2005-07-29
AU2003236648A1 (en) 2003-12-02
CA2485896A1 (en) 2003-11-27
TW200400033A (en) 2004-01-01
TWI309981B (en) 2009-05-21
UY27807A1 (es) 2003-11-28
NZ536604A (en) 2006-07-28
RU2326869C2 (ru) 2008-06-20
US7459453B2 (en) 2008-12-02
US20080269235A1 (en) 2008-10-30
NO20045461L (no) 2005-01-19
JP2005533024A (ja) 2005-11-04
ES2195785A1 (es) 2003-12-01
AR040076A1 (es) 2005-03-16
IL165173A0 (en) 2005-12-18
UA77532C2 (en) 2006-12-15
MY132106A (en) 2007-09-28
WO2003097613A1 (en) 2003-11-27
MXPA04011209A (es) 2005-02-14
ES2195785B1 (es) 2005-03-16
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