JP4700908B2 - ２−（３，５−ビス−トリフルオロメチル−フェニル）−Ｎ−〔６−（１，１−ジオキソ−１λ６−チオモルホリン−４−イル）−４−（２−メチル又は４−フルオロ−２−メチル置換）フェニル−ピリジン−３−イル〕−Ｎ−メチル−イソブチルアミド - Google Patents

２−（３，５−ビス−トリフルオロメチル−フェニル）−Ｎ−〔６−（１，１−ジオキソ−１λ６−チオモルホリン−４−イル）−４−（２−メチル又は４−フルオロ−２−メチル置換）フェニル−ピリジン−３−イル〕−Ｎ−メチル−イソブチルアミド Download PDF

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Publication number
JP4700908B2
JP4700908B2 JP2003517052A JP2003517052A JP4700908B2 JP 4700908 B2 JP4700908 B2 JP 4700908B2 JP 2003517052 A JP2003517052 A JP 2003517052A JP 2003517052 A JP2003517052 A JP 2003517052A JP 4700908 B2 JP4700908 B2 JP 4700908B2
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Prior art keywords
methyl
phenyl
compound
formula
thiomorpholin
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
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JP2003517052A
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Japanese (ja)
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JP2005500354A5 (https=
JP2005500354A (ja
Inventor
バラード，テレサ・マリア
ホフマン，トルシュテン
ポリ，ソニア・マリア
シュニダー，パトリック
スライト，アンドリュー
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P11/02—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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P25/04—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
    • A61P25/14—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
    • A61P25/22—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
JP2003517052A 2001-07-31 2002-07-26 ２−（３，５−ビス−トリフルオロメチル−フェニル）−Ｎ−〔６−（１，１−ジオキソ−１λ６−チオモルホリン−４−イル）−４−（２−メチル又は４−フルオロ−２−メチル置換）フェニル−ピリジン−３−イル〕−Ｎ−メチル−イソブチルアミド Expired - Fee Related JP4700908B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01118412 2001-07-31
EP01118412.4 2001-07-31
PCT/EP2002/008311 WO2003011860A2 (en) 2001-07-31 2002-07-26 2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1λ6-THIOMORPHOLIN-4-YL)-4-(2-METHYL OR 4-FLUORO-2-METHYL SUBSTITUTED)PHENYL-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE

Publications (3)

Publication Number Publication Date
JP2005500354A JP2005500354A (ja) 2005-01-06
JP2005500354A5 JP2005500354A5 (https=) 2005-11-17
JP4700908B2 true JP4700908B2 (ja) 2011-06-15

Family

ID=8178193

Family Applications (1)

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JP2003517052A Expired - Fee Related JP4700908B2 (ja) 2001-07-31 2002-07-26 ２−（３，５−ビス−トリフルオロメチル−フェニル）−Ｎ−〔６−（１，１−ジオキソ−１λ６−チオモルホリン−４−イル）−４−（２−メチル又は４−フルオロ−２−メチル置換）フェニル−ピリジン−３−イル〕−Ｎ−メチル−イソブチルアミド

Country Status (29)

Country Link
US (1) US6849624B2 (https=)
EP (1) EP1414525B1 (https=)
JP (1) JP4700908B2 (https=)
KR (1) KR100577101B1 (https=)
CN (1) CN1289497C (https=)
AR (1) AR034921A1 (https=)
AT (1) ATE430600T1 (https=)
BR (1) BR0211523A (https=)
CA (1) CA2452502C (https=)
DE (1) DE60232246D1 (https=)
EA (1) EA006238B1 (https=)
EC (1) ECSP044963A (https=)
ES (1) ES2324209T3 (https=)
GT (1) GT200200159A (https=)
HR (1) HRP20040039A2 (https=)
HU (1) HUP0400398A3 (https=)
MA (1) MA27055A1 (https=)
MX (1) MXPA04000917A (https=)
MY (1) MY128464A (https=)
NO (1) NO20040404L (https=)
NZ (1) NZ530579A (https=)
PA (1) PA8551601A1 (https=)
PE (1) PE20030276A1 (https=)
PL (1) PL366986A1 (https=)
UA (1) UA77685C2 (https=)
UY (1) UY27403A1 (https=)
WO (1) WO2003011860A2 (https=)
YU (1) YU2704A (https=)
ZA (1) ZA200400652B (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2444395C (en) * 2001-04-23 2010-12-21 F. Hoffmann-La Roche Ag Use of nk-1 receptor antagonists against benign prostatic hyperplasia
SE521512C2 (sv) * 2001-06-25 2003-11-11 Niconovum Ab Anordning för administrering av en substans till främre delen av en individs munhåla
PT1578422E (pt) 2002-12-20 2007-06-14 Niconovum Ab Material particulado contendo nicotina fisicamente e quimicamente estável
NZ541243A (en) * 2003-01-31 2008-04-30 Hoffmann La Roche New crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambda6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide
CN1984891B (zh) 2004-07-06 2012-08-08 弗·哈夫曼-拉罗切有限公司 用作合成nk-1受体拮抗剂的中间体的甲酰胺吡啶衍生物的制备方法
MX2007010034A (es) * 2005-02-22 2007-10-04 Hoffmann La Roche Antagonista de nk1.
KR20070094666A (ko) 2005-02-25 2007-09-20 에프. 호프만-라 로슈 아게 약제 물질 분산성이 향상된 정제
AU2007224584A1 (en) 2006-03-16 2007-09-20 Niconovum Ab Improved snuff composition
GB0808747D0 (en) 2008-05-14 2008-06-18 Glaxo Wellcome Mfg Pte Ltd Novel compounds
US10383894B2 (en) * 2010-03-17 2019-08-20 Lutran Industries, Inc. Human medicinal treatment using salt of peroxymonosulfuric acid
CA2930008A1 (en) 2013-11-08 2015-05-14 Kissei Pharmaceutical Co., Ltd. Carboxymethyl piperidine derivative
TWI649307B (zh) 2014-05-07 2019-02-01 日商橘生藥品工業股份有限公司 Cyclohexylpyridine derivative
ES2824552T3 (es) 2015-03-04 2021-05-12 Vanda Pharmaceuticals Inc Método de tratamiento con tradipitant
CA3101210A1 (en) * 2018-06-08 2019-12-12 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6435115A (en) * 1987-07-31 1989-02-06 Nippon Seiko Kk Bearing device
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
IL112134A (en) 1993-12-29 1999-12-22 Merck Sharp & Dohme Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
PT1035115E (pt) 1999-02-24 2005-01-31 Hoffmann La Roche Derivados de 4-fenilpiridina e a sua utilizacao como antagonistas do receptor nk-1
CA2444395C (en) * 2001-04-23 2010-12-21 F. Hoffmann-La Roche Ag Use of nk-1 receptor antagonists against benign prostatic hyperplasia

Also Published As

Publication number Publication date
YU2704A (sh) 2006-08-17
NZ530579A (en) 2006-02-24
ES2324209T3 (es) 2009-08-03
UA77685C2 (en) 2007-01-15
EA006238B1 (ru) 2005-10-27
EA200400109A1 (ru) 2004-08-26
CN1537025A (zh) 2004-10-13
ATE430600T1 (de) 2009-05-15
PE20030276A1 (es) 2003-03-29
AU2002355652B2 (en) 2007-07-05
WO2003011860A2 (en) 2003-02-13
BR0211523A (pt) 2004-09-14
HK1069136A1 (en) 2005-05-13
HUP0400398A3 (en) 2010-06-28
US20030064983A1 (en) 2003-04-03
HRP20040039A2 (en) 2004-06-30
AR034921A1 (es) 2004-03-24
CA2452502A1 (en) 2003-02-13
HUP0400398A2 (hu) 2004-09-28
UY27403A1 (es) 2003-04-30
EP1414525A2 (en) 2004-05-06
ECSP044963A (es) 2004-03-23
MY128464A (en) 2007-02-28
GT200200159A (es) 2003-05-16
PL366986A1 (en) 2005-02-07
JP2005500354A (ja) 2005-01-06
PA8551601A1 (es) 2003-06-30
KR100577101B1 (ko) 2006-05-10
MA27055A1 (fr) 2004-12-20
NO20040404L (no) 2004-01-29
DE60232246D1 (de) 2009-06-18
MXPA04000917A (es) 2004-04-02
WO2003011860A3 (en) 2003-09-04
US6849624B2 (en) 2005-02-01
ZA200400652B (en) 2005-04-28
KR20040029386A (ko) 2004-04-06
CN1289497C (zh) 2006-12-13
EP1414525B1 (en) 2009-05-06
CA2452502C (en) 2011-02-15

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