CA2542140C - Crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone - Google Patents

Crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone Download PDF

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Publication number
CA2542140C
CA2542140C CA2542140A CA2542140A CA2542140C CA 2542140 C CA2542140 C CA 2542140C CA 2542140 A CA2542140 A CA 2542140A CA 2542140 A CA2542140 A CA 2542140A CA 2542140 C CA2542140 C CA 2542140C
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Prior art keywords
pyridin
chlorophenyl
methanone
triazol
bistrifluoromethylbenzyl
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Expired - Lifetime
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CA2542140A
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English (en)
French (fr)
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CA2542140A1 (en
Inventor
Alfio Borghese
David Scott Coffey
Pamela Kaye Footman
Steven Wayne Pedersen
Susan Marie Reutzel-Edens
Shella Lenyonga Tameze
Carsten Weber
Carsten Timpe
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Eli Lilly and Co
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Eli Lilly and Co
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    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46Oxygen atoms
    • C07D213/50Ketonic radicals
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
CA2542140A 2003-10-24 2004-10-12 Crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone Expired - Lifetime CA2542140C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US51430003P 2003-10-24 2003-10-24
US60/514,300 2003-10-24
PCT/US2004/030914 WO2005042515A1 (en) 2003-10-24 2004-10-12 Novel crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone

Publications (2)

Publication Number Publication Date
CA2542140A1 CA2542140A1 (en) 2005-05-12
CA2542140C true CA2542140C (en) 2012-05-29

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CA2542140A Expired - Lifetime CA2542140C (en) 2003-10-24 2004-10-12 Crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone

Country Status (28)

Country Link
US (1) US7381826B2 (enExample)
JP (1) JP4959336B2 (enExample)
KR (1) KR100848407B1 (enExample)
CN (1) CN1863791B (enExample)
AR (1) AR046131A1 (enExample)
AT (1) ATE462700T1 (enExample)
AU (1) AU2004285855B8 (enExample)
BR (1) BRPI0415010B8 (enExample)
CA (1) CA2542140C (enExample)
CL (2) CL2009001310A1 (enExample)
CR (1) CR8353A (enExample)
DE (1) DE602004026333D1 (enExample)
DK (1) DK1675846T3 (enExample)
EA (1) EA008881B1 (enExample)
EC (1) ECSP066517A (enExample)
ES (1) ES2340772T3 (enExample)
HR (1) HRP20100207T1 (enExample)
IL (1) IL174926A0 (enExample)
MA (1) MA28329A1 (enExample)
MY (1) MY157375A (enExample)
NO (1) NO335090B1 (enExample)
NZ (2) NZ580480A (enExample)
PE (1) PE20050481A1 (enExample)
PT (1) PT1675846E (enExample)
TW (1) TW200524906A (enExample)
UA (1) UA82901C2 (enExample)
WO (1) WO2005042515A1 (enExample)
ZA (1) ZA200603234B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2121610B1 (en) * 2006-12-20 2014-04-02 Eli Lilly & Company Novel intermediate and process useful in the preparation of {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone
WO2009075778A2 (en) * 2007-12-06 2009-06-18 The Regents Of The University Of California Nonpeptidic inhibitors of cruzain
US8080568B1 (en) * 2010-06-29 2011-12-20 Ewha University - Industry Collaboration Foundation 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
KR20170122777A (ko) 2015-03-04 2017-11-06 반다 파마슈티칼즈, 인코퍼레이티드. 트라디피턴트에 의한 치료 방법
US10287287B2 (en) 2015-08-17 2019-05-14 Eli Lilly And Company Process development of a pyridine-containing NK-1 receptor antagonist
KR20200054232A (ko) 2017-09-13 2020-05-19 반다 파마슈티칼즈, 인코퍼레이티드. 트라디피탄트를 이용한 아토피 피부염의 개선된 치료
KR20250140655A (ko) * 2017-11-17 2025-09-25 반다 파마슈티칼즈, 인코퍼레이티드. 트라디피탄트를 이용한 위장 질환의 치료 방법
US20210228555A1 (en) 2018-06-08 2021-07-29 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant
US10821099B2 (en) 2018-09-28 2020-11-03 Vanda Pharmaceuticals Inc. Use of tradipitant in motion sickness
CN111918701B (zh) 2018-09-28 2024-08-02 万达制药公司 曲地匹坦在晕动病中的用途
WO2020117811A1 (en) * 2018-12-03 2020-06-11 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant
WO2021173641A1 (en) 2020-02-25 2021-09-02 Vanda Pharmaceuticals Inc. Improved treatment of atopic dermatitis with tradipitant
WO2021195205A1 (en) 2020-03-26 2021-09-30 Vanda Pharmaceuticals Inc. Treatment of lower respiratory tract infection with tradipitant
WO2023019084A1 (en) 2021-08-12 2023-02-16 Vanda Pharmaceuticals Inc. Treatment of gastric accommodation with tradipitant
US20240350469A1 (en) 2021-08-31 2024-10-24 Vanda Pharmaceuticals Inc. Treatment of lower respiratory tract infection with tradipitant
WO2024138040A1 (en) 2022-12-21 2024-06-27 Vanda Pharmaceuticals Inc. Methods of treatment with tradipitant
US20250255855A1 (en) 2024-02-09 2025-08-14 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020099067A1 (en) 1993-07-08 2002-07-25 Ulrich Posanski Pharmaceutical compositions for sparingly soluble therapeutic agents
GB9505492D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9525296D0 (en) * 1995-12-11 1996-02-07 Merck Sharp & Dohme Therapeutic agents
JP2001502311A (ja) * 1996-10-07 2001-02-20 メルク シヤープ エンド ドーム リミテツド 抗鬱及び/又は抗不安薬としてのcns浸透性nk―1受容体拮抗薬
AR032130A1 (es) * 1999-08-13 2003-10-29 Vertex Pharma Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto
EP1228068A1 (en) * 1999-10-29 2002-08-07 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
US20020044971A1 (en) 2000-07-07 2002-04-18 Amidon Gordon L. Dissolution rate of poorly soluble drugs
JP4559087B2 (ja) * 2002-04-26 2010-10-06 イーライ リリー アンド カンパニー タキキニン受容体アンタゴニストとしてのトリアゾール誘導体

Also Published As

Publication number Publication date
AR046131A1 (es) 2005-11-23
JP4959336B2 (ja) 2012-06-20
CL2009001311A1 (es) 2009-10-02
NZ545917A (en) 2009-11-27
MY157375A (en) 2016-06-15
NZ580480A (en) 2010-02-26
KR100848407B1 (ko) 2008-07-28
ES2340772T3 (es) 2010-06-09
MA28329A1 (fr) 2006-12-01
CN1863791B (zh) 2011-12-07
HRP20100207T1 (hr) 2010-05-31
CR8353A (es) 2006-06-06
ATE462700T1 (de) 2010-04-15
CL2009001310A1 (es) 2009-12-04
US7381826B2 (en) 2008-06-03
DK1675846T3 (da) 2010-05-31
AU2004285855A1 (en) 2005-05-12
AU2004285855B8 (en) 2011-04-28
TW200524906A (en) 2005-08-01
PT1675846E (pt) 2010-04-20
PE20050481A1 (es) 2005-09-20
NO20062371L (no) 2006-05-24
AU2004285855B2 (en) 2010-12-23
CN1863791A (zh) 2006-11-15
EA008881B1 (ru) 2007-08-31
KR20060061388A (ko) 2006-06-07
ZA200603234B (en) 2007-07-25
BRPI0415010A8 (pt) 2018-05-08
IL174926A0 (en) 2006-08-20
NO335090B1 (no) 2014-09-08
DE602004026333D1 (de) 2010-05-12
EA200600829A1 (ru) 2006-08-25
WO2005042515A1 (en) 2005-05-12
CA2542140A1 (en) 2005-05-12
UA82901C2 (en) 2008-05-26
BRPI0415010B1 (pt) 2019-07-09
US20070078166A1 (en) 2007-04-05
ECSP066517A (es) 2006-10-10
BRPI0415010B8 (pt) 2021-05-25
BRPI0415010A (pt) 2006-11-07
JP2007509143A (ja) 2007-04-12

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