CZ295381B6 - Morfoliny antagonizující tachykininové receptory, způsob jejich výroby a farmaceutické prostředky s jejich obsahem - Google Patents

Morfoliny antagonizující tachykininové receptory, způsob jejich výroby a farmaceutické prostředky s jejich obsahem Download PDF

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Publication number
CZ295381B6
CZ295381B6 CZ19961772A CZ177296A CZ295381B6 CZ 295381 B6 CZ295381 B6 CZ 295381B6 CZ 19961772 A CZ19961772 A CZ 19961772A CZ 177296 A CZ177296 A CZ 177296A CZ 295381 B6 CZ295381 B6 CZ 295381B6
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CZ
Czechia
Prior art keywords
defined above
phenyl
trifluoromethyl
carbon atoms
cor
Prior art date
Application number
CZ19961772A
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Czech (cs)
English (en)
Other versions
CZ177296A3 (en
Inventor
Conrad P. Dorn
Paul E. Finke
Jeffrey J. Hale
Malcolm Maccoss
Sander G. Mills
Shrenik K. Shah
Mark Stuart Chambers
Timothy Harrison
Tamara Ladduwahetty
Brian John Williams
Original Assignee
Merck & Co., Inc.
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.)
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22617632&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CZ295381(B6) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Publication of CZ177296A3 publication Critical patent/CZ177296A3/cs
Publication of CZ295381B6 publication Critical patent/CZ295381B6/cs

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • A61P1/08—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
CZ19961772A 1993-12-17 1994-12-13 Morfoliny antagonizující tachykininové receptory, způsob jejich výroby a farmaceutické prostředky s jejich obsahem CZ295381B6 (cs)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16988993A 1993-12-17 1993-12-17

Publications (2)

Publication Number Publication Date
CZ177296A3 CZ177296A3 (en) 1996-12-11
CZ295381B6 true CZ295381B6 (cs) 2005-07-13

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
CZ19961772A CZ295381B6 (cs) 1993-12-17 1994-12-13 Morfoliny antagonizující tachykininové receptory, způsob jejich výroby a farmaceutické prostředky s jejich obsahem

Country Status (40)

Country Link
EP (1) EP0734381B1 (forum.php)
JP (1) JP3245424B2 (forum.php)
KR (1) KR100335704B1 (forum.php)
CN (1) CN1057296C (forum.php)
AT (1) ATE194336T1 (forum.php)
AU (1) AU701862B2 (forum.php)
BG (1) BG64775B1 (forum.php)
BR (1) BR9408351A (forum.php)
CA (1) CA2178949C (forum.php)
CO (1) CO4340628A1 (forum.php)
CY (2) CY2203B1 (forum.php)
CZ (1) CZ295381B6 (forum.php)
DE (2) DE122004000019I1 (forum.php)
DK (1) DK0734381T3 (forum.php)
ES (1) ES2147840T3 (forum.php)
FI (1) FI109532B (forum.php)
FR (1) FR04C0010I2 (forum.php)
GR (1) GR3034095T3 (forum.php)
HR (1) HRP941000B9 (forum.php)
HU (1) HU224014B1 (forum.php)
IL (1) IL111960A (forum.php)
LT (1) LTC0734381I2 (forum.php)
LU (1) LU91069I9 (forum.php)
LV (1) LV11617B (forum.php)
MY (1) MY115164A (forum.php)
NL (1) NL300146I2 (forum.php)
NO (3) NO308742B1 (forum.php)
NZ (1) NZ278222A (forum.php)
PL (1) PL182521B1 (forum.php)
PT (1) PT734381E (forum.php)
RO (1) RO118203B1 (forum.php)
RU (1) RU2201924C2 (forum.php)
SA (1) SA95150523B1 (forum.php)
SI (1) SI0734381T1 (forum.php)
SK (1) SK282800B6 (forum.php)
TW (1) TW419471B (forum.php)
UA (1) UA47397C2 (forum.php)
WO (1) WO1995016679A1 (forum.php)
YU (1) YU49037B (forum.php)
ZA (1) ZA9410008B (forum.php)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ299286B6 (cs) * 1999-11-29 2008-06-04 F. Hoffmann-La Roche Ag 2-(3,5-bis-Trifluormethylfenyl)-N-methyl-N-(6-morfolin-4-yl-4-o-tolylpyridin-3-yl)izobutyramid, zpusob jeho prípravy, použití a lécivo s jeho obsahem

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TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
EP0758329A1 (en) * 1994-05-05 1997-02-19 MERCK SHARP & DOHME LTD. Morpholine derivatives and their use as antagonists of tachikinins
AU691327B2 (en) * 1994-08-15 1998-05-14 Merck Sharp & Dohme Limited Morpholine derivatives and their use as therapeutic agents
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US5750549A (en) * 1996-10-15 1998-05-12 Merck & Co., Inc. Cycloalkyl tachykinin receptor antagonists
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RU2309953C2 (ru) 1999-11-03 2007-11-10 Эймр Текнолоджи, Инк. Арил- и гетероарилзамещенные тетрагидроизохинолины, фармацевтическая композиция и способ лечения на их основе
US6452001B2 (en) 2000-05-25 2002-09-17 Hoffmann-La Roche Inc. Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
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KR100501608B1 (ko) 2000-07-14 2005-07-18 에프. 호프만-라 로슈 아게 4-페닐-피리딘 유도체의 ｎｋ1 수용체의 길항성선구약물로서의 ｎ-산화물
TWI287003B (en) 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
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ES2290666T3 (es) * 2003-01-31 2008-02-16 F. Hoffmann-La Roche Ag Nueva modificacion cristalina de la 2-(3,5-bis-trifluormetil-fenil)-n-(6-(1,1-dioxo-1landa6-tiomorfolin-4-il)-4-(4-fluor-2-metil-fenil)-piridin-3-il)-n-metil-isobutiramida.
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
ATE371451T1 (de) 2003-07-03 2007-09-15 Hoffmann La Roche Duale nk1/nk3 antagonisten zur behandlung von schizophrenie
US7288658B2 (en) 2003-07-15 2007-10-30 Hoffmann-La Roche Inc. Process for preparation of pyridine derivatives
ES2246687B2 (es) 2004-02-11 2006-11-16 Miguel Muñoz Saez Utilizacion de antagonistas no peptidicos de receptores nk1 para la produccion de apoptosis en celulas tumorales.
NZ552397A (en) 2004-07-15 2011-04-29 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
DE602006008900D1 (de) 2005-02-22 2009-10-15 Hoffmann La Roche Nk1-antagonisten
EP1863767B1 (en) 2005-03-23 2009-03-11 F. Hoffmann-Roche AG Metabolites for nk-i antagonists for emesis
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
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JP5489333B2 (ja) 2006-09-22 2014-05-14 メルク・シャープ・アンド・ドーム・コーポレーション 脂肪酸合成阻害剤を用いた治療の方法
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
CN101190330A (zh) 2006-11-30 2008-06-04 深圳市鼎兴生物医药技术开发有限公司 胆碱酯酶在拮抗速激肽药物中的应用
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JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
KR101163847B1 (ko) 2007-04-20 2012-07-09 에프. 호프만-라 로슈 아게 이중 ｎｋ1/ｎｋ3 수용체 길항제로서의 피롤리딘 유도체
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