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RU2006143758A - BY THE EXISTENCE PURE 2 - {[2- (2-METHYLAMINOPYRIMIDIN-4-IL) -1H-INDOL-5-CARBONIL] -AMINO} -3- (Phenylpyridin-2-ILAMINO) PROPIONIC ACID IN CASIUM - Google Patents

BY THE EXISTENCE PURE 2 - {[2- (2-METHYLAMINOPYRIMIDIN-4-IL) -1H-INDOL-5-CARBONIL] -AMINO} -3- (Phenylpyridin-2-ILAMINO) PROPIONIC ACID IN CASIUM Download PDF

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Publication number
RU2006143758A
RU2006143758A RU2006143758/04A RU2006143758A RU2006143758A RU 2006143758 A RU2006143758 A RU 2006143758A RU 2006143758/04 A RU2006143758/04 A RU 2006143758/04A RU 2006143758 A RU2006143758 A RU 2006143758A RU 2006143758 A RU2006143758 A RU 2006143758A
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Russia
Prior art keywords
effective amount
patient
agonist
administering
pharmaceutically effective
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RU2006143758/04A
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Russian (ru)
Inventor
Эль-Бдауи АДДАД (US)
Эль-Бдауи Аддад
Олаф РИТЦЕЛЕР (DE)
Олаф Ритцелер
Дэвид Дж. ОЛДОУС (US)
Дэвид Дж. ОЛДОУС
Пол Джозеф КОКС (US)
Пол Джозеф Кокс
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Авентис Фармасьютикалз Инк. (Us)
Авентис Фармасьютикалз Инк.
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Publication of RU2006143758A publication Critical patent/RU2006143758A/en

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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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (14)

1. По существу чистое соединение формулы (A)1. Essentially pure compound of the formula (A)
Figure 00000001
Figure 00000001
 или его фармацевтически приемлемая соль или сольват.or a pharmaceutically acceptable salt or solvate thereof. 2. Фармацевтическая композиция, содержащая фармацевтически эффективное количество соединения формулы (A) и фармацевтически приемлемый носитель.2. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of formula (A) and a pharmaceutically acceptable carrier. 3. Способ лечения пациента, страдающего патологическим состоянием или подверженному патологическим состоянием, которое может быть облегчено ингибированием IKK-2 путем введения указанному пациенту фармацевтически эффективного количества соединения по п.1.3. A method of treating a patient suffering from a pathological condition or susceptible to a pathological condition that can be alleviated by inhibiting IKK-2 by administering to said patient a pharmaceutically effective amount of a compound according to claim 1. 4. Способ по п.3, где введение проводят с получением локализованного действия.4. The method according to claim 3, where the introduction is carried out with obtaining a localized action. 5. Способ по п.3, где патологическим состоянием является астма, ринит, хроническое обструктивное заболевание легких или обострения хронического обструктивного заболевания легких.5. The method according to claim 3, where the pathological condition is asthma, rhinitis, chronic obstructive pulmonary disease or exacerbation of chronic obstructive pulmonary disease. 6. Способ по п.3, где введение проводят интратрахеально, интраназально, ингаляционно или при помощи аэрозоля.6. The method according to claim 3, where the introduction is carried out intratracheally, intranasally, inhalation or by aerosol. 7. Способ лечения пациента, страдающего от астмы, включающий введение пациенту фармацевтически эффективного количества соединения по п.1.7. A method of treating a patient suffering from asthma, comprising administering to the patient a pharmaceutically effective amount of a compound according to claim 1. 8. Способ лечения пациента, страдающего от ринита, включающий введение пациенту фармацевтически эффективного количества соединения по п.1.8. A method of treating a patient suffering from rhinitis, comprising administering to the patient a pharmaceutically effective amount of a compound according to claim 1. 9. Способ лечения пациента, страдающего от хронического обструктивного заболевания легких, включающий введение пациенту фармацевтически эффективного количества соединения по п.1.9. A method of treating a patient suffering from chronic obstructive pulmonary disease, comprising administering to the patient a pharmaceutically effective amount of a compound according to claim 1. 10. Способ лечения пациента, страдающего от обострений хронического обструктивного заболевания легких, включающий введение пациенту фармацевтически эффективного количества соединения по п.1.10. A method of treating a patient suffering from exacerbations of chronic obstructive pulmonary disease, comprising administering to the patient a pharmaceutically effective amount of a compound according to claim 1. 11. Фармацевтическая композиция по п.2, дополнительно содержащая фармацевтически эффективное количество соединения, выбранное из группы, включающей бронходилатор, бета 2-агонист длительного действия, антихолинергические средства, метилксантин и противовоспалительное средство, в смеси с фармацевтически приемлемым носителем.11. The pharmaceutical composition according to claim 2, further comprising a pharmaceutically effective amount of a compound selected from the group consisting of a bronchodilator, long-acting beta 2 agonist, anticholinergics, methylxanthine and an anti-inflammatory agent, in admixture with a pharmaceutically acceptable carrier. 12. Фармацевтическая композиция по п.11, в котором бронходилатором является бета 2-агонист кратковременного действия; бета 2-агонистом длительного действия может быть салметерол или формотерол; антихолинергическим средством может быть бромид ипратропия и бромид тиотропия; метилксантином является теофиллин; противовоспалительным средством могут быть ингибиторы рекрутинга клеток и медиаторы токсического воспаления, ингибиторы протеолитических ферментов, антиоксиданты, ингибиторы выделения слизи и антибиотики.12. The pharmaceutical composition according to claim 11, in which the bronchodilator is a short-acting beta 2-agonist; long-acting beta 2-agonist may be salmeterol or formoterol; the anticholinergic agent may be ipratropium bromide and tiotropium bromide; methylxanthine is theophylline; anti-inflammatory agents can be cell recruitment inhibitors and toxic inflammation mediators, proteolytic enzyme inhibitors, antioxidants, mucus secretion inhibitors and antibiotics. 13. Способ лечения по п.3, дополнительно включающий введение фармакологически эффективного количества соединения, выбранное из группы, включающей бронходилатор, бета-2 агонист длительного действия, антихолинергические средства, метилксантин и противовоспалительное средство, в смеси с фармацевтически приемлемым носителем.13. The treatment method according to claim 3, further comprising administering a pharmacologically effective amount of a compound selected from the group consisting of a bronchodilator, long-acting beta-2 agonist, anticholinergics, methylxanthine and an anti-inflammatory agent, in admixture with a pharmaceutically acceptable carrier. 14. Способ лечения по п.13, в котором бронходилатором является бета 2-агонист кратковременного действия; бета 2-агонистом длительного действия может быть салметерол или формотерол; антихолинергическим средством может быть бромид ипратропия и бромид тиотропия; метилксантином является теофиллин; противовоспалительным средством могут быть ингибиторы рекрутинга клеток и медиаторы токсического воспаления, ингибиторы протеолитических ферментов, антиоксиданты, ингибиторы выделения слизи и антибиотики.14. The treatment method according to item 13, in which the bronchodilator is a short-acting beta 2-agonist; long-acting beta 2-agonist may be salmeterol or formoterol; the anticholinergic agent may be ipratropium bromide and tiotropium bromide; methylxanthine is theophylline; anti-inflammatory agents can be cell recruitment inhibitors and toxic inflammation mediators, proteolytic enzyme inhibitors, antioxidants, mucus secretion inhibitors and antibiotics.
RU2006143758/04A 2004-05-12 2005-05-11 BY THE EXISTENCE PURE 2 - {[2- (2-METHYLAMINOPYRIMIDIN-4-IL) -1H-INDOL-5-CARBONIL] -AMINO} -3- (Phenylpyridin-2-ILAMINO) PROPIONIC ACID IN CASIUM RU2006143758A (en)

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US60/570,146 2004-05-12

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EP (1) EP1747215A1 (en)
JP (1) JP2007537266A (en)
KR (1) KR20070011483A (en)
CN (1) CN1950359A (en)
AR (1) AR049274A1 (en)
AU (1) AU2005245834A1 (en)
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CA (1) CA2566213A1 (en)
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MA (1) MA28553B1 (en)
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PA (1) PA8633101A1 (en)
PE (1) PE20060269A1 (en)
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SV (1) SV2006002111A (en)
TN (1) TNSN06338A1 (en)
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UY (1) UY28897A1 (en)
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KR102340754B1 (en) 2008-04-21 2021-12-16 오토노미, 인코포레이티드 Auris formulations for treating otic diseases and conditions
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RU2552999C2 (en) 2010-04-27 2015-06-10 Хатчисон Медифарма Лимитед Pyrimidine indole compounds
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TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
EP2766349B1 (en) 2011-03-08 2016-06-01 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120056A1 (en) 2011-03-08 2012-09-13 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
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
WO2012120055A1 (en) 2011-03-08 2012-09-13 Sanofi Di- and tri-substituted oxathiazine derivates, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP3478269A4 (en) 2016-06-29 2020-04-08 Otonomy, Inc. TRICLYCERIDE FORMULAS FOR THE EAR AND USE THEREOF
CN106588803A (en) * 2016-11-16 2017-04-26 西南科技大学 Novel method for preparing 5-acetylisoxazole

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ECSP066992A (en) 2006-12-29
NO20065719L (en) 2006-12-12
AU2005245834A1 (en) 2005-12-01
GT200500111A (en) 2006-05-09
KR20070011483A (en) 2007-01-24
AR049274A1 (en) 2006-07-12
JP2007537266A (en) 2007-12-20
BRPI0511029A (en) 2007-11-27
CN1950359A (en) 2007-04-18
PA8633101A1 (en) 2006-01-23
PE20060269A1 (en) 2006-05-11
MXPA06012870A (en) 2007-02-15
SV2006002111A (en) 2006-01-30
IL178992A0 (en) 2007-03-08
TNSN06338A1 (en) 2008-02-22
CA2566213A1 (en) 2005-12-11
TW200605881A (en) 2006-02-16
WO2005113544A1 (en) 2005-12-01
EP1747215A1 (en) 2007-01-31
MA28553B1 (en) 2007-04-03
UY28897A1 (en) 2005-12-30
ZA200608712B (en) 2008-06-25

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