TW200726769A - Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates - Google Patents

Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates

Info

Publication number: TW200726769A
Authority: TW; Taiwan
Prior art keywords: intermediates; pyrimidines; compositions; processes; compounds
Prior art date: 2005-06-21

Application number

TW095121824A

Other languages

English (en)

Other versions

TWI382985B (zh

Inventor

Luis Anglada

Albert Palomer

Antonio Guglietta

Original Assignee

Ferrer Int

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.)

2005-06-21

Filing date

2006-06-19

Publication date

2007-07-16

2006-06-19 Application filed by Ferrer Int filed Critical Ferrer Int

2007-07-16 Publication of TW200726769A publication Critical patent/TW200726769A/zh

2013-01-21 Application granted granted Critical

2013-01-21 Publication of TWI382985B publication Critical patent/TWI382985B/zh

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
- C07D471/04—Ortho-condensed systems
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- 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
- A61P25/08—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
- A61P25/20—Hypnotics; Sedatives
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/30—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
- C07C233/33—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
- C07C303/40—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Neurology (AREA)
Epidemiology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Anesthesiology (AREA)
Pain & Pain Management (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

TW095121824A 2005-06-21 2006-06-19 鹵化的吡唑并〔１．５-ａ〕嘧啶，方法，用途，組成物和中間物 TWI382985B (zh)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US69286605P	2005-06-21	2005-06-21
EP05105478A EP1736475A1 (en)	2005-06-21	2005-06-21	Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates

Publications (2)

Publication Number	Publication Date
TW200726769A true TW200726769A (en)	2007-07-16
TWI382985B TWI382985B (zh)	2013-01-21

Family

ID=35311853

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
TW095121824A TWI382985B (zh)	2005-06-21	2006-06-19	鹵化的吡唑并〔１．５-ａ〕嘧啶，方法，用途，組成物和中間物

Country Status (24)

Country	Link
US (3)	US8530482B2 (zh)
EP (2)	EP1736475A1 (zh)
JP (1)	JP5010591B2 (zh)
KR (1)	KR101465802B1 (zh)
CN (1)	CN101243089B (zh)
AR (1)	AR054785A1 (zh)
AT (1)	ATE467635T1 (zh)
AU (1)	AU2006261025B2 (zh)
BR (1)	BRPI0612075A2 (zh)
CA (1)	CA2612726C (zh)
CY (1)	CY1111452T1 (zh)
DE (1)	DE602006014272D1 (zh)
DK (1)	DK1899343T3 (zh)
ES (1)	ES2345999T3 (zh)
MX (1)	MX2007016340A (zh)
NO (1)	NO339973B1 (zh)
PE (1)	PE20070071A1 (zh)
PL (1)	PL1899343T3 (zh)
PT (1)	PT1899343E (zh)
RU (1)	RU2478101C2 (zh)
SI (1)	SI1899343T1 (zh)
TW (1)	TWI382985B (zh)
UY (1)	UY29618A1 (zh)
WO (1)	WO2006136530A1 (zh)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP1736475A1 (en)	2005-06-21	2006-12-27	Ferrer Internacional, S.A.	Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
BRPI0708813A2 (pt) *	2006-03-17	2011-05-24	Wyeth Corp	composto; composição; método de tratamento, inibição do crescimento ou erradicaçõ de neoplasias em um mamìfero necessitado; método de tratamento dse cáncer em um mamìfero necessitado; e mistura
EP1884516A1 (en)	2006-08-04	2008-02-06	Ferrer Internacional, S.A.	Pyrazolo[1,5-a]pyrimidines, processes, uses and compositions
EP1956021A1 (en)	2006-10-11	2008-08-13	Ferrer Internacional, S.A.	Process for the manufacture of a crystalline pyrazolo[1,5-a]pyrimidine compound
EP1918290A1 (en)	2006-10-11	2008-05-07	Ferrer Internacional, S.A.	Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide
EP1921079A1 (en) *	2006-11-08	2008-05-14	Ferrer Internacional, S.A.	Amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide
JP5507579B2 (ja)	2009-01-13	2014-05-28	インテルキム、ソシエダッドアノニマ	Ｎ−［５−（３−ジメチルアミノ−アクリロイル）−２−フルオロ−フェニル］−ｎ−メチル−アセトアミドの調製方法
JP6272833B2 (ja)	2013-04-04	2018-01-31	武田薬品工業株式会社	複素環化合物
JP2018199623A (ja) *	2015-10-22	2018-12-20	大正製薬株式会社	含窒素縮合複素環化合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4521422A (en) *	1983-06-23	1985-06-04	American Cyanamid Company	Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones
US6399621B1 (en) *	1999-08-10	2002-06-04	American Cyanamid Company	N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
KR20030082982A (ko) *	2001-03-14	2003-10-23	그뤼넨탈 게엠베하	치환된 피라졸로피리미딘 및 티아졸로피리미딘
DE60206072T2 (de) *	2001-12-21	2006-07-13	Bayer Healthcare Ag	Aroylpyridinone
ES2222813B1 (es) *	2003-07-24	2005-12-16	Ferrer Internacional, S.A.	N-(3-(3-sustituidas-pirazolo(1,5-a)pirimidin-7-il)-fenil)-sulfonamidas y composiciones y metodos relacionados.
WO2006033795A2 (en) *	2004-09-17	2006-03-30	Wyeth	Substituted pyrazolo [1, 5-a] pyrimidines for inhibiting abnormal cell growth
WO2006033796A1 (en) *	2004-09-17	2006-03-30	Wyeth	SUBSTITUTED PYRAZOLO [1,5-a] PYRIMIDINES AND PROCESS FOR MAKING SAME
CN100528875C (zh) *	2005-02-18	2009-08-19	美德（江西）生物科技有限公司	无结晶型态的印地普隆及其制备方法
EP1736475A1 (en) *	2005-06-21	2006-12-27	Ferrer Internacional, S.A.	Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates

2005
- 2005-06-21 EP EP05105478A patent/EP1736475A1/en not_active Withdrawn
2006
- 2006-06-15 US US11/922,602 patent/US8530482B2/en not_active Expired - Fee Related
- 2006-06-15 CA CA2612726A patent/CA2612726C/en not_active Expired - Fee Related
- 2006-06-15 AU AU2006261025A patent/AU2006261025B2/en not_active Ceased
- 2006-06-15 AT AT06763737T patent/ATE467635T1/de active
- 2006-06-15 RU RU2008101371/04A patent/RU2478101C2/ru not_active IP Right Cessation
- 2006-06-15 EP EP06763737A patent/EP1899343B1/en not_active Not-in-force
- 2006-06-15 KR KR1020087001565A patent/KR101465802B1/ko not_active Expired - Fee Related
- 2006-06-15 CN CN2006800303968A patent/CN101243089B/zh not_active Expired - Fee Related
- 2006-06-15 BR BRPI0612075-0A patent/BRPI0612075A2/pt not_active Application Discontinuation
- 2006-06-15 ES ES06763737T patent/ES2345999T3/es active Active
- 2006-06-15 JP JP2008517470A patent/JP5010591B2/ja not_active Expired - Fee Related
- 2006-06-15 PT PT06763737T patent/PT1899343E/pt unknown
- 2006-06-15 DE DE602006014272T patent/DE602006014272D1/de active Active
- 2006-06-15 MX MX2007016340A patent/MX2007016340A/es active IP Right Grant
- 2006-06-15 WO PCT/EP2006/063243 patent/WO2006136530A1/en not_active Ceased
- 2006-06-15 SI SI200630735T patent/SI1899343T1/sl unknown
- 2006-06-15 PL PL06763737T patent/PL1899343T3/pl unknown
- 2006-06-15 DK DK06763737.1T patent/DK1899343T3/da active
- 2006-06-19 TW TW095121824A patent/TWI382985B/zh not_active IP Right Cessation
- 2006-06-19 PE PE2006000684A patent/PE20070071A1/es active IP Right Grant
- 2006-06-20 AR ARP060102604A patent/AR054785A1/es active IP Right Grant
- 2006-06-21 UY UY29618A patent/UY29618A1/es active IP Right Grant
2008
- 2008-01-21 NO NO20080393A patent/NO339973B1/no not_active IP Right Cessation
2010
- 2010-08-11 CY CY20101100750T patent/CY1111452T1/el unknown
2013
- 2013-08-13 US US13/965,516 patent/US10072000B2/en not_active Expired - Fee Related
- 2013-08-13 US US13/965,383 patent/US20130331610A1/en not_active Abandoned

Also Published As

Publication number	Publication date
KR101465802B1 (ko)	2014-11-27
PT1899343E (pt)	2010-08-17
NO339973B1 (no)	2017-02-27
AR054785A1 (es)	2007-07-18
CA2612726A1 (en)	2006-12-28
US20130331401A1 (en)	2013-12-12
CA2612726C (en)	2013-10-01
KR20080032104A (ko)	2008-04-14
ATE467635T1 (de)	2010-05-15
WO2006136530A1 (en)	2006-12-28
CN101243089A (zh)	2008-08-13
JP5010591B2 (ja)	2012-08-29
HK1116184A1 (zh)	2008-12-19
CN101243089B (zh)	2011-07-06
DK1899343T3 (da)	2010-09-06
MX2007016340A (es)	2008-03-10
US10072000B2 (en)	2018-09-11
EP1899343A1 (en)	2008-03-19
UY29618A1 (es)	2006-10-31
US8530482B2 (en)	2013-09-10
CY1111452T1 (el)	2015-08-05
EP1899343B1 (en)	2010-05-12
EP1736475A1 (en)	2006-12-27
US20090111848A1 (en)	2009-04-30
DE602006014272D1 (de)	2010-06-24
PE20070071A1 (es)	2007-02-01
US20160368912A9 (en)	2016-12-22
SI1899343T1 (sl)	2010-09-30
NO20080393L (no)	2008-03-10
US20130331610A1 (en)	2013-12-12
PL1899343T3 (pl)	2010-10-29
JP2008543913A (ja)	2008-12-04
AU2006261025B2 (en)	2011-09-08
BRPI0612075A2 (pt)	2010-10-19
AU2006261025A1 (en)	2006-12-28
TWI382985B (zh)	2013-01-21
RU2478101C2 (ru)	2013-03-27
RU2008101371A (ru)	2009-07-27
ES2345999T3 (es)	2010-10-07

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TW200517109A (en)	2005-06-01	Substituted pyridinones
CY1111452T1 (el)	2015-08-05	Αλογονωμενες πυραζολο [1,5-α]πυριμιδινες, διεργασιες, χρησεις ως προσδεμα υποδοχεα gaba-a, συνθεσεις και ενδιαμεσα
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MX2009006885A (es)	2009-08-28	Derivados de pirrolo[3,2-a]piridina para inhibir la actividad de la proteina cinesina del huso.
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Legal Events

Date	Code	Title	Description
2020-10-21	MM4A	Annulment or lapse of patent due to non-payment of fees