UA82901C2 - 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

Info

Publication number: UA82901C2
Authority: UA; Ukraine
Prior art keywords: pyridin; chlorophenyl; methanone; peaks; compound
Prior art date: 2003-10-24

Application number

UAA200604473A

Other languages

English (en)

Ukrainian (uk)

Inventor

Suzanne Maria Ruttsel-Idens

Carsten Timpe

Original Assignee

Lilly Co Eli

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.)

2003-10-24

Filing date

2004-12-10

Publication date

2008-05-26

2004-12-10 Application filed by Lilly Co Eli filed Critical Lilly Co Eli

2008-05-26 Publication of UA82901C2 publication Critical patent/UA82901C2/uk

Links

CAVRKWRKTNINFF-UHFFFAOYSA-N [2-[1-[[3,5-bis(trifluoromethyl)phenyl]methyl]-5-pyridin-4-yltriazol-4-yl]pyridin-3-yl]-(2-chlorophenyl)methanone Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(CN2C(=C(N=N2)C=2C(=CC=CN=2)C(=O)C=2C(=CC=CC=2)Cl)C=2C=CN=CC=2)=C1 CAVRKWRKTNINFF-UHFFFAOYSA-N 0.000 title abstract 2
238000000034 method Methods 0.000 claims abstract description 68
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OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 42
IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 39
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 38
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 33
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 30
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 26
YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 21
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Classifications

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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
- C07D213/50—Ketonic radicals
- 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
- C07D401/04—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 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)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Pyridine Compounds (AREA)
Medicinal Preparation (AREA)

UAA200604473A 2003-10-24 2004-12-10 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 UA82901C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US51430003P	2003-10-24	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 (1)

Publication Number	Publication Date
UA82901C2 true UA82901C2 (en)	2008-05-26

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Application Number	Title	Priority Date	Filing Date
UAA200604473A UA82901C2 (en)	2003-10-24	2004-12-10	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 (pt)
JP (1)	JP4959336B2 (pt)
KR (1)	KR100848407B1 (pt)
CN (1)	CN1863791B (pt)
AR (1)	AR046131A1 (pt)
AT (1)	ATE462700T1 (pt)
AU (1)	AU2004285855B8 (pt)
BR (1)	BRPI0415010B8 (pt)
CA (1)	CA2542140C (pt)
CL (2)	CL2009001311A1 (pt)
CR (1)	CR8353A (pt)
DE (1)	DE602004026333D1 (pt)
DK (1)	DK1675846T3 (pt)
EA (1)	EA008881B1 (pt)
EC (1)	ECSP066517A (pt)
ES (1)	ES2340772T3 (pt)
HR (1)	HRP20100207T1 (pt)
IL (1)	IL174926A0 (pt)
MA (1)	MA28329A1 (pt)
MY (1)	MY157375A (pt)
NO (1)	NO335090B1 (pt)
NZ (2)	NZ545917A (pt)
PE (1)	PE20050481A1 (pt)
PT (1)	PT1675846E (pt)
TW (1)	TW200524906A (pt)
UA (1)	UA82901C2 (pt)
WO (1)	WO2005042515A1 (pt)
ZA (1)	ZA200603234B (pt)

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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
RU2770050C2 (ru)	2015-03-04	2022-04-14	Ванда Фармасьютиклз Инк.	Способ лечения с применением традипитанта
WO2017031215A1 (en) *	2015-08-17	2017-02-23	Eli Lilly And Company	Process development of a pyridine-containing nk-1 receptor antagonist
CA3073998A1 (en)	2017-09-13	2019-03-21	Vanda Pharmaceuticals Inc.	Improved treatment of atopic dermatitis with tradipitant
DK3710000T3 (da) *	2017-11-17	2025-06-16	Vanda Pharmaceuticals Inc	Tradipitant til anvendelse til behandling af gastroparese
CN112218636B (zh) *	2018-06-08	2025-05-06	万达制药公司	使用川地匹坦进行治疗的方法
IL281569B2 (en)	2018-09-28	2025-04-01	Vanda Pharmaceuticals Inc	Use of tradipient in motion sickness
US20220096449A1 (en)	2018-12-03	2022-03-31	Vanda Pharmaceuticals Inc.	Method of treatment with tradipitant
KR20220145844A (ko)	2020-02-25	2022-10-31	반다 파마슈티칼즈, 인코퍼레이티드.	트라디피탄트를 이용한 아토피 피부염의 개선된 치료
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
AU2023413130A1 (en)	2022-12-21	2025-06-05	Vanda Pharmaceuticals Inc.	Methods of treatment with tradipitant
EP4599831A1 (en)	2024-02-09	2025-08-13	Vanda Pharmaceuticals Inc.	Treatment of gastroparesis with tradipitant
WO2026152024A1 (en)	2025-01-09	2026-07-16	Vanda Pharmaceuticals Inc.	Method of treating nausea and vomiting after glp-1r agonist administration

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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
AU726745B2 (en) *	1996-10-07	2000-11-16	Merck Sharp & Dohme Limited	CNS-penetrant NK-1 receptor antagonists as antidepressant and/or an anti-anxiety agent
DE60039616D1 (de) *	1999-08-13	2008-09-04	Vertex Pharma	INHIBITOREN DER c-JUN N-TERMINALEN KINASE (JNK) UND ANDERE PROTEIN-KINASEN
WO2001032656A1 (en) *	1999-10-29	2001-05-10	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
AU2003230829B8 (en) *	2002-04-26	2008-12-11	Eli Lilly And Company	Triazole derivatives as tachykinin receptor antagonists

2004
- 2004-10-12 WO PCT/US2004/030914 patent/WO2005042515A1/en not_active Ceased
- 2004-10-12 KR KR1020067007751A patent/KR100848407B1/ko not_active Expired - Lifetime
- 2004-10-12 US US10/574,712 patent/US7381826B2/en not_active Expired - Lifetime
- 2004-10-12 NZ NZ545917A patent/NZ545917A/en unknown
- 2004-10-12 AU AU2004285855A patent/AU2004285855B8/en not_active Expired
- 2004-10-12 HR HR20100207T patent/HRP20100207T1/hr unknown
- 2004-10-12 DK DK04793893.1T patent/DK1675846T3/da active
- 2004-10-12 BR BRPI0415010A patent/BRPI0415010B8/pt not_active IP Right Cessation
- 2004-10-12 AT AT04793893T patent/ATE462700T1/de active
- 2004-10-12 PT PT04793893T patent/PT1675846E/pt unknown
- 2004-10-12 CA CA2542140A patent/CA2542140C/en not_active Expired - Lifetime
- 2004-10-12 CN CN2004800291393A patent/CN1863791B/zh not_active Expired - Lifetime
- 2004-10-12 DE DE602004026333T patent/DE602004026333D1/de not_active Expired - Lifetime
- 2004-10-12 ES ES04793893T patent/ES2340772T3/es not_active Expired - Lifetime
- 2004-10-12 NZ NZ580480A patent/NZ580480A/en unknown
- 2004-10-12 EA EA200600829A patent/EA008881B1/ru not_active IP Right Cessation
- 2004-10-12 JP JP2006536635A patent/JP4959336B2/ja not_active Expired - Lifetime
- 2004-10-20 AR ARP040103801A patent/AR046131A1/es not_active Application Discontinuation
- 2004-10-20 PE PE2004001008A patent/PE20050481A1/es not_active Application Discontinuation
- 2004-10-21 MY MYPI20044338A patent/MY157375A/en unknown
- 2004-10-22 TW TW093132097A patent/TW200524906A/zh unknown
- 2004-12-10 UA UAA200604473A patent/UA82901C2/uk unknown
2006
- 2006-04-11 IL IL174926A patent/IL174926A0/en unknown
- 2006-04-21 EC EC2006006517A patent/ECSP066517A/es unknown
- 2006-04-21 ZA ZA200603234A patent/ZA200603234B/en unknown
- 2006-04-21 CR CR8353A patent/CR8353A/es not_active Application Discontinuation
- 2006-05-22 MA MA29043A patent/MA28329A1/fr unknown
- 2006-05-24 NO NO20062371A patent/NO335090B1/no unknown
2009
- 2009-05-29 CL CL2009001311A patent/CL2009001311A1/es unknown
- 2009-05-29 CL CL2009001310A patent/CL2009001310A1/es unknown

Also Published As

Publication number	Publication date
NZ580480A (en)	2010-02-26
CA2542140A1 (en)	2005-05-12
KR100848407B1 (ko)	2008-07-28
AR046131A1 (es)	2005-11-23
DE602004026333D1 (de)	2010-05-12
PT1675846E (pt)	2010-04-20
EA008881B1 (ru)	2007-08-31
US20070078166A1 (en)	2007-04-05
CL2009001310A1 (es)	2009-12-04
CN1863791B (zh)	2011-12-07
DK1675846T3 (da)	2010-05-31
NZ545917A (en)	2009-11-27
BRPI0415010B8 (pt)	2021-05-25
AU2004285855A1 (en)	2005-05-12
NO20062371L (no)	2006-05-24
EA200600829A1 (ru)	2006-08-25
AU2004285855B8 (en)	2011-04-28
NO335090B1 (no)	2014-09-08
JP4959336B2 (ja)	2012-06-20
CL2009001311A1 (es)	2009-10-02
TW200524906A (en)	2005-08-01
ZA200603234B (en)	2007-07-25
IL174926A0 (en)	2006-08-20
BRPI0415010B1 (pt)	2019-07-09
WO2005042515A1 (en)	2005-05-12
PE20050481A1 (es)	2005-09-20
ATE462700T1 (de)	2010-04-15
US7381826B2 (en)	2008-06-03
HRP20100207T1 (hr)	2010-05-31
CN1863791A (zh)	2006-11-15
ES2340772T3 (es)	2010-06-09
JP2007509143A (ja)	2007-04-12
ECSP066517A (es)	2006-10-10
BRPI0415010A8 (pt)	2018-05-08
CR8353A (es)	2006-06-06
MA28329A1 (fr)	2006-12-01
MY157375A (en)	2016-06-15
KR20060061388A (ko)	2006-06-07
BRPI0415010A (pt)	2006-11-07
AU2004285855B2 (en)	2010-12-23
CA2542140C (en)	2012-05-29

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