AR054785A1 - Compuesto que comprende pirazolo (1,5-a) pirimidinas halogenadas, procedimiento para prepararlo uso de dicho compuesto composicion farmaceutica que lo comprende, procedimiento para preparar sus intermedios y compuesto intermedio - Google Patents
Compuesto que comprende pirazolo (1,5-a) pirimidinas halogenadas, procedimiento para prepararlo uso de dicho compuesto composicion farmaceutica que lo comprende, procedimiento para preparar sus intermedios y compuesto intermedioInfo
- Publication number
- AR054785A1 AR054785A1 ARP060102604A ARP060102604A AR054785A1 AR 054785 A1 AR054785 A1 AR 054785A1 AR P060102604 A ARP060102604 A AR P060102604A AR P060102604 A ARP060102604 A AR P060102604A AR 054785 A1 AR054785 A1 AR 054785A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- prepare
- procedure
- intermediates
- halogened
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 239000000543 intermediate Substances 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 206010002091 Anaesthesia Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 206010021118 Hypotonia Diseases 0.000 abstract 1
- 206010039897 Sedation Diseases 0.000 abstract 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 230000037005 anaesthesia Effects 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 206010022437 insomnia Diseases 0.000 abstract 1
- 230000036640 muscle relaxation Effects 0.000 abstract 1
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000007958 sleep Effects 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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)
Abstract
Los compuestos de formula (1) son utiles para tratar o prevenir la ansiedad, epilepsia y los trastornos del sueno incluyendo el insomnio, y para inducir sedacion-hipnosis, anestesia, sueno y relajacion muscular, también se refiere a procesos de síntesis para preparar dichos compuestos y ciertos intermedios, así como los mismos intermedios. Reivindicacion 1: Un compuesto caracterizado porque comprende pirazolo[1,5-a]pirimidinas halogenadas de formula (1) donde: R significa un grupo alquil C1-6; R1 se selecciona del grupo que consiste en alquil C1-6 y alquinil C1-6; X significa un átomo de halogeno; e Y se selecciona del grupo que consiste en -CO- y -SO2-; y una sal correspondiente farmacéuticamente aceptable.
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 (1)
| Publication Number | Publication Date |
|---|---|
| AR054785A1 true AR054785A1 (es) | 2007-07-18 |
Family
ID=35311853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102604A AR054785A1 (es) | 2005-06-21 | 2006-06-20 | Compuesto que comprende pirazolo (1,5-a) pirimidinas halogenadas, procedimiento para prepararlo uso de dicho compuesto composicion farmaceutica que lo comprende, procedimiento para preparar sus intermedios y compuesto intermedio |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US8530482B2 (es) |
| EP (2) | EP1736475A1 (es) |
| JP (1) | JP5010591B2 (es) |
| KR (1) | KR101465802B1 (es) |
| CN (1) | CN101243089B (es) |
| AR (1) | AR054785A1 (es) |
| AT (1) | ATE467635T1 (es) |
| AU (1) | AU2006261025B2 (es) |
| BR (1) | BRPI0612075A2 (es) |
| CA (1) | CA2612726C (es) |
| CY (1) | CY1111452T1 (es) |
| DE (1) | DE602006014272D1 (es) |
| DK (1) | DK1899343T3 (es) |
| ES (1) | ES2345999T3 (es) |
| MX (1) | MX2007016340A (es) |
| NO (1) | NO339973B1 (es) |
| PE (1) | PE20070071A1 (es) |
| PL (1) | PL1899343T3 (es) |
| PT (1) | PT1899343E (es) |
| RU (1) | RU2478101C2 (es) |
| SI (1) | SI1899343T1 (es) |
| TW (1) | TWI382985B (es) |
| UY (1) | UY29618A1 (es) |
| WO (1) | WO2006136530A1 (es) |
Families Citing this family (9)
| 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 |
| AU2007227557A1 (en) * | 2006-03-17 | 2007-09-27 | Wyeth | Pyrazolo[1,5-a]pyrimidine derivatives and methods of use thereof |
| EP1884516A1 (en) * | 2006-08-04 | 2008-02-06 | Ferrer Internacional, S.A. | Pyrazolo[1,5-a]pyrimidines, processes, uses and compositions |
| 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 |
| 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 |
| 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 |
| BRPI1006150A2 (pt) | 2009-01-13 | 2018-01-16 | Interquim Sa | Processo para preparação de n-[5-(3-dimetilamino- acriloil)-2fluorofenil]-n-metil-acetamida |
| WO2014163162A1 (ja) | 2013-04-04 | 2014-10-09 | 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)
| 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 |
| ES2311920T3 (es) * | 2001-03-14 | 2009-02-16 | Grunenthal Gmbh | Tiazolopirimidinas sustituidas como analgesicos. |
| JP2005516955A (ja) * | 2001-12-21 | 2005-06-09 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | アロイル・ピリジノン化合物 |
| 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 BR BRPI0612075-0A patent/BRPI0612075A2/pt not_active Application Discontinuation
- 2006-06-15 MX MX2007016340A patent/MX2007016340A/es active IP Right Grant
- 2006-06-15 CA CA2612726A patent/CA2612726C/en not_active Expired - Fee Related
- 2006-06-15 ES ES06763737T patent/ES2345999T3/es active Active
- 2006-06-15 PT PT06763737T patent/PT1899343E/pt unknown
- 2006-06-15 US US11/922,602 patent/US8530482B2/en not_active Expired - Fee Related
- 2006-06-15 AT AT06763737T patent/ATE467635T1/de active
- 2006-06-15 DE DE602006014272T patent/DE602006014272D1/de active Active
- 2006-06-15 JP JP2008517470A patent/JP5010591B2/ja not_active Expired - Fee Related
- 2006-06-15 CN CN2006800303968A patent/CN101243089B/zh not_active Expired - Fee Related
- 2006-06-15 RU RU2008101371/04A patent/RU2478101C2/ru not_active IP Right Cessation
- 2006-06-15 PL PL06763737T patent/PL1899343T3/pl unknown
- 2006-06-15 SI SI200630735T patent/SI1899343T1/sl unknown
- 2006-06-15 KR KR1020087001565A patent/KR101465802B1/ko not_active Expired - Fee Related
- 2006-06-15 WO PCT/EP2006/063243 patent/WO2006136530A1/en not_active Ceased
- 2006-06-15 AU AU2006261025A patent/AU2006261025B2/en not_active Ceased
- 2006-06-15 DK DK06763737.1T patent/DK1899343T3/da active
- 2006-06-15 EP EP06763737A patent/EP1899343B1/en not_active Not-in-force
- 2006-06-19 PE PE2006000684A patent/PE20070071A1/es active IP Right Grant
- 2006-06-19 TW TW095121824A patent/TWI382985B/zh not_active IP Right Cessation
- 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 US13/965,383 patent/US20130331610A1/en not_active Abandoned
- 2013-08-13 US US13/965,516 patent/US10072000B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |