OA12929A - Pyrazole derivatives as transforming growth (TGF) inhibitors. - Google Patents

Pyrazole derivatives as transforming growth (TGF) inhibitors. Download PDF

Info

Publication number: OA12929A
Authority: OA; OAPI
Prior art keywords: alkyl; cio; phenyl; cycloalkyl; heteroaryl
Prior art date: 2002-09-18

Application number

OA1200500078A

Other languages

English (en)

Inventor

Laura Cook Blumberg

Michael John Munchhof

Original Assignee

Pfizer Prod 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.)

2002-09-18

Filing date

2003-09-08

Publication date

2006-10-13

2003-09-08 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2006-10-13 Publication of OA12929A publication Critical patent/OA12929A/en

Links

239000003112 inhibitor Substances 0.000 title abstract description 9
150000003217 pyrazoles Chemical class 0.000 title abstract description 3
230000001131 transforming effect Effects 0.000 title 1
150000001875 compounds Chemical class 0.000 claims abstract description 156
-1 derivatives thereof Chemical class 0.000 claims abstract description 61
201000010099 disease Diseases 0.000 claims abstract description 18
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 18
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
206010028980 Neoplasm Diseases 0.000 claims abstract description 6
201000011510 cancer Diseases 0.000 claims abstract description 4
125000000217 alkyl group Chemical group 0.000 claims description 130
125000003545 alkoxy group Chemical group 0.000 claims description 42
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 32
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
125000001072 heteroaryl group Chemical group 0.000 claims description 23
125000000753 cycloalkyl group Chemical group 0.000 claims description 21
125000000623 heterocyclic group Chemical group 0.000 claims description 19
239000000651 prodrug Substances 0.000 claims description 19
229940002612 prodrug Drugs 0.000 claims description 19
125000003282 alkyl amino group Chemical group 0.000 claims description 18
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 12
125000003342 alkenyl group Chemical group 0.000 claims description 12
229910052739 hydrogen Inorganic materials 0.000 claims description 12
239000001257 hydrogen Substances 0.000 claims description 12
125000001424 substituent group Chemical group 0.000 claims description 11
RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 9
125000000304 alkynyl group Chemical group 0.000 claims description 9
125000003118 aryl group Chemical group 0.000 claims description 9
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 9
150000002148 esters Chemical class 0.000 claims description 8
125000005842 heteroatom Chemical group 0.000 claims description 8
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 7
241001465754 Metazoa Species 0.000 claims description 7
125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 7
GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 6
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
229910052760 oxygen Inorganic materials 0.000 claims description 5
229920006395 saturated elastomer Polymers 0.000 claims description 5
125000003368 amide group Chemical group 0.000 claims description 4
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UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 3
125000004457 alkyl amino carbonyl group Chemical group 0.000 claims description 3
125000004448 alkyl carbonyl group Chemical group 0.000 claims description 3
125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 3
125000004414 alkyl thio group Chemical group 0.000 claims description 3
125000005129 aryl carbonyl group Chemical group 0.000 claims description 3
125000005161 aryl oxy carbonyl group Chemical group 0.000 claims description 3
125000004391 aryl sulfonyl group Chemical group 0.000 claims description 3
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125000005553 heteroaryloxy group Chemical group 0.000 claims description 3
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206010019668 Hepatic fibrosis Diseases 0.000 claims description 2
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- 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
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
- C07D413/14—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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OA1200500078A 2002-09-18 2003-09-08 Pyrazole derivatives as transforming growth (TGF) inhibitors. OA12929A (en)

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US41214602P	2002-09-18	2002-09-18
US48454303P	2003-07-02	2003-07-02

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EP (2)	EP1542684B1 (pl)
JP (1)	JP4519657B2 (pl)
KR (1)	KR20050044807A (pl)
CN (1)	CN1681501A (pl)
AP (1)	AP2005003263A0 (pl)
AR (1)	AR041272A1 (pl)
AT (1)	ATE450258T1 (pl)
AU (1)	AU2003259475A1 (pl)
BR (1)	BR0314302A (pl)
CA (1)	CA2496295C (pl)
CO (1)	CO5550456A2 (pl)
DE (1)	DE60330362D1 (pl)
EA (1)	EA200500377A1 (pl)
EC (1)	ECSP055679A (pl)
ES (1)	ES2335099T3 (pl)
HR (1)	HRP20050247A2 (pl)
IS (1)	IS7698A (pl)
MA (1)	MA27440A1 (pl)
MX (1)	MXPA05002376A (pl)
NO (1)	NO20050838L (pl)
OA (1)	OA12929A (pl)
PA (1)	PA8583201A1 (pl)
PE (1)	PE20040988A1 (pl)
PL (1)	PL375979A1 (pl)
UY (1)	UY27985A1 (pl)
WO (1)	WO2004026306A2 (pl)

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2003
- 2003-09-08 WO PCT/IB2003/003933 patent/WO2004026306A2/en not_active Ceased
- 2003-09-08 AP AP2005003263A patent/AP2005003263A0/xx unknown
- 2003-09-08 EP EP03797443A patent/EP1542684B1/en not_active Expired - Lifetime
- 2003-09-08 DE DE60330362T patent/DE60330362D1/de not_active Expired - Lifetime
- 2003-09-08 EP EP09177298A patent/EP2165708A3/en not_active Withdrawn
- 2003-09-08 PL PL03375979A patent/PL375979A1/pl not_active Application Discontinuation
- 2003-09-08 EA EA200500377A patent/EA200500377A1/ru unknown
- 2003-09-08 ES ES03797443T patent/ES2335099T3/es not_active Expired - Lifetime
- 2003-09-08 HR HR20050247A patent/HRP20050247A2/hr not_active Application Discontinuation
- 2003-09-08 MX MXPA05002376A patent/MXPA05002376A/es active IP Right Grant
- 2003-09-08 BR BR0314302-3A patent/BR0314302A/pt not_active IP Right Cessation
- 2003-09-08 KR KR1020057004598A patent/KR20050044807A/ko not_active Ceased
- 2003-09-08 CN CNA038222655A patent/CN1681501A/zh active Pending
- 2003-09-08 OA OA1200500078A patent/OA12929A/en unknown
- 2003-09-08 CA CA2496295A patent/CA2496295C/en not_active Expired - Fee Related
- 2003-09-08 JP JP2004568904A patent/JP4519657B2/ja not_active Expired - Fee Related
- 2003-09-08 AT AT03797443T patent/ATE450258T1/de not_active IP Right Cessation
- 2003-09-08 AU AU2003259475A patent/AU2003259475A1/en not_active Abandoned
- 2003-09-15 PE PE2003000940A patent/PE20040988A1/es not_active Application Discontinuation
- 2003-09-16 AR ARP030103356A patent/AR041272A1/es unknown
- 2003-09-16 UY UY27985A patent/UY27985A1/es not_active Application Discontinuation
- 2003-09-17 US US10/667,189 patent/US6958354B2/en not_active Expired - Fee Related
- 2003-09-17 PA PA20038583201A patent/PA8583201A1/es unknown
2005
- 2005-02-16 NO NO20050838A patent/NO20050838L/no unknown
- 2005-02-17 IS IS7698A patent/IS7698A/is unknown
- 2005-03-16 EC EC2005005679A patent/ECSP055679A/es unknown
- 2005-03-16 CO CO05024529A patent/CO5550456A2/es not_active Application Discontinuation
- 2005-03-18 MA MA28154A patent/MA27440A1/fr unknown
- 2005-09-23 US US11/234,564 patent/US7151110B2/en not_active Expired - Fee Related
2006
- 2006-11-08 US US11/557,638 patent/US7638537B2/en not_active Expired - Fee Related
2009
- 2009-11-12 US US12/617,027 patent/US20100056571A1/en not_active Abandoned

Also Published As

Publication number	Publication date
WO2004026306A2 (en)	2004-04-01
WO2004026306A3 (en)	2004-07-01
CA2496295A1 (en)	2004-04-01
CN1681501A (zh)	2005-10-12
HRP20050247A2 (en)	2005-10-31
EP2165708A3 (en)	2010-07-28
AP2005003263A0 (en)	2005-03-31
ATE450258T1 (de)	2009-12-15
EP1542684A2 (en)	2005-06-22
US20070117850A1 (en)	2007-05-24
PA8583201A1 (es)	2004-04-23
BR0314302A (pt)	2005-07-05
EP1542684B1 (en)	2009-12-02
AU2003259475A1 (en)	2004-04-08
CO5550456A2 (es)	2005-08-31
EP2165708A2 (en)	2010-03-24
PE20040988A1 (es)	2004-12-25
KR20050044807A (ko)	2005-05-12
MXPA05002376A (es)	2005-05-23
JP2006507353A (ja)	2006-03-02
MA27440A1 (fr)	2005-07-01
US20060025451A1 (en)	2006-02-02
US20100056571A1 (en)	2010-03-04
IS7698A (is)	2005-02-17
NO20050838L (no)	2005-05-18
AR041272A1 (es)	2005-05-11
US20040116474A1 (en)	2004-06-17
PL375979A1 (pl)	2005-12-12
US6958354B2 (en)	2005-10-25
US7638537B2 (en)	2009-12-29
ECSP055679A (es)	2005-05-30
US7151110B2 (en)	2006-12-19
DE60330362D1 (de)	2010-01-14
UY27985A1 (es)	2004-04-30
EA200500377A1 (ru)	2005-08-25
CA2496295C (en)	2010-11-23
JP4519657B2 (ja)	2010-08-04
ES2335099T3 (es)	2010-03-22

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US7030125B2 (en)	2006-04-18	Isothiazole and isoxazole compounds as transforming growth factor (TGF) inhibitors
EP1606267B1 (en)	2008-07-30	Pyrazine compounds as transforming growth factor (tgf) inhibitors
ZA200502277B (en)	2006-02-22	Novel isothiazole and isoxazole compounds as transforming growth factor (TGF) inhibitors.