BRPI0516746A - 5-heterociclil pirimidinas para inibição de hiv - Google Patents
5-heterociclil pirimidinas para inibição de hivInfo
- Publication number
- BRPI0516746A BRPI0516746A BRPI0516746-9A BRPI0516746A BRPI0516746A BR PI0516746 A BRPI0516746 A BR PI0516746A BR PI0516746 A BRPI0516746 A BR PI0516746A BR PI0516746 A BRPI0516746 A BR PI0516746A
- Authority
- BR
- Brazil
- Prior art keywords
- substituted
- optionally substituted
- alkyl
- amino
- alkyloxy
- Prior art date
Links
Classifications
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
5-HETEROCICLIL PIRIMIDINAS PARA INIBIçãO DE HIV. Inibidores da replicação de HIV da fórmula (1), N-óxidos, sais de adição farmaceuticamente aceitáveis, aminas quaternárias ou formas estereoisoméricas dos mesmos, em que: a = a - a = a¬ 4¬ é CH=CH-CH=CH-, -N=CH-CH=CH, -N=CH-N=CH-, -N=CH-CH=N, -N=N-CH=CH-; -b = b - b = b¬ 4¬ é -CH=CH-CH=CH, -N=CH-CH=CH, -N=CH-N=CH, -N=CH-CH=N-, -N=N-CH=CH-; R é hidrogênio; arila; formila; C~ 1~-C~ 6~ alquilcarbonila; C~ 1~-C~ 6~ alquila opcionalmente substituída; C~ 1~-C~ 6~ alquilóxicarbonila; R é OH; halo; C~ 2~-C~ 6~ alquenila ou C~ 2~-C~ 6~ alquinila opcionalmente substituída; carbonila substituída; carboxila; CN; nitro; amino;amino substituído; polihalometila; poilhalometiltio; -S(=O)rR¬ 6¬; C(=NH)R¬ 6¬; R¬ 2a¬ é CN; amino; amino substituído; C~ 1~-C~ 6~ alquila opcionalmente substituída; halo; C~ 1-6~ alquilóxi opcionalmente substituído; carbonila substituída; -CH=N-NH-C (=O)-R16; C~ 1-6~ alquilóxi C~ 1-6~ alquila opcionalmente substituída; C~ 2-6~ alquenila ou C~ 2-6~ alquinila opcionalmente substituída; -C(=N-O-R8)-C~ 1-4~ alquila; R¬ 7¬ ou X~ 1~ é -NR-,-O-, -C(=))-, CH~ 2~, -CHOH-,-S-, -S(=O)r-; R é CN; amino; C~ 1~-C~ 6~ alquila; halo; C~ 1~-C~ 6~ alquilóxi opcionalmente substituído; carbonila substituída; -CH=N-NH-C(=O)-R¬ 16¬; C~ 1~-C~ 6~ alquila substituída; C~ 1~-C~ 6~ alquilóxi C~ 1~-C~ 6~ alquila opcionalmente substituída; -C~ 2~-C~ 6~ alquenila ou C~ 2~ -C~ 6~ alquinila opcionalmente substituída; -C(=N-O-R¬ 8)-C~ 1-4~ alquila; R¬ 7¬; -X~ 3~-R¬ 7¬; R¬ 4¬ é halo; OH; C~ 1-6~ alquila opcionalmente substituída; C~ 2-6~ alquenila ou C~ 2-6~ alquinila; C~ 3-7 cicloalquila; C~ 1-6~ alquilóxi; CN; nitro; polihalo C~ 1-6~ alquila; polihalo C~ 1-6~ alquilóxi; carbonila substituída; formila; amino; mono- ou di(C~ 1-4~ alquil)amino ou R¬ 7¬; R¬ 5¬ é um sistema de anel completamente insaturado de 5 ou 6 elementos, em que 1-4 elementos no anel são nitrogênio, oxigênio ou enxofre; anel o qual pode ser opcionalmente substituído e pode ser opcionalmente anelado a um anel de benzeno; métodos para seu preparo e composições farmacêuticas compreendendo os mesmos. A presente invenção também se refere ao uso desses compostos para a prevenção ou tratamento de infecção pelo HIV.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04104812 | 2004-09-30 | ||
PCT/EP2005/054930 WO2006035067A2 (en) | 2004-09-30 | 2005-09-29 | Hiv inhibiting 5-heterocyclyl pyrimidines |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0516746A true BRPI0516746A (pt) | 2008-09-23 |
Family
ID=34929638
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0516746-9A BRPI0516746A (pt) | 2004-09-30 | 2005-09-29 | 5-heterociclil pirimidinas para inibição de hiv |
Country Status (17)
Country | Link |
---|---|
US (1) | US8575342B2 (pt) |
EP (1) | EP1797069B1 (pt) |
JP (1) | JP5008567B2 (pt) |
KR (1) | KR20070057899A (pt) |
CN (1) | CN101031558B (pt) |
AR (1) | AR050969A1 (pt) |
AT (1) | ATE520680T1 (pt) |
AU (1) | AU2005288864B2 (pt) |
BR (1) | BRPI0516746A (pt) |
CA (1) | CA2577467C (pt) |
ES (1) | ES2371923T3 (pt) |
IL (1) | IL180959A (pt) |
MX (1) | MX2007003797A (pt) |
RU (1) | RU2405778C2 (pt) |
TW (1) | TW200626574A (pt) |
WO (1) | WO2006035067A2 (pt) |
ZA (1) | ZA200702653B (pt) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2410379C2 (ru) | 2004-09-30 | 2011-01-27 | Тиботек Фармасьютикалз Лтд. | 5-замещенные пиримидины, ингибирующие вич |
BRPI0516746A (pt) | 2004-09-30 | 2008-09-23 | Tibotec Pharm Ltd | 5-heterociclil pirimidinas para inibição de hiv |
CN101119976B (zh) * | 2005-02-18 | 2010-12-22 | 泰博特克药品有限公司 | 抑制hiv的2-(4-氰基苯氨基)嘧啶氧化物衍生物 |
AU2007233737B2 (en) | 2006-03-30 | 2012-11-29 | Janssen Sciences Ireland Uc | HIV inhibiting 5-amido substituted pyrimidines |
CN101553483B (zh) | 2006-12-13 | 2013-04-17 | 弗·哈夫曼-拉罗切有限公司 | 作为非核苷逆转录酶抑制剂的2-(哌啶-4-基)-4-苯氧基-或苯基氨基-嘧啶衍生物 |
EA020749B1 (ru) | 2006-12-29 | 2015-01-30 | Тиботек Фармасьютикалз Лтд. | Вич-ингибирующие 5,6-замещенные пиримидины |
DK2114901T3 (da) * | 2006-12-29 | 2014-06-30 | Janssen R & D Ireland | Hiv-inhiberende 6-substituerede pyrimidiner |
UY32158A (es) * | 2008-10-03 | 2010-04-30 | Astrazeneca Ab | Derivados heterociclicos y metodos de uso de los mismos |
WO2011146313A1 (en) | 2010-05-19 | 2011-11-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
US8729079B2 (en) | 2011-08-23 | 2014-05-20 | Endo Pharmaceuticals Inc. | Pyrimido-pyridazinone compounds and methods of use thereof |
US9273056B2 (en) | 2011-10-03 | 2016-03-01 | The University Of North Carolina At Chapel Hill | Pyrrolopyrimidine compounds for the treatment of cancer |
BR112014028424A2 (pt) | 2012-05-22 | 2018-04-24 | Univ North Carolina Chapel Hill | compostos de pirimidina para o tratamento de câncer |
WO2014062774A1 (en) | 2012-10-17 | 2014-04-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
EP2925752A4 (en) | 2012-11-27 | 2016-06-01 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
RU2547844C1 (ru) * | 2013-10-29 | 2015-04-10 | Федеральное государственное бюджетное учреждение науки Институт органического синтеза им. И.Я. Постовского Уральского отделения Российской академии наук | Способ получения 5-(гет)арил-4-(2-тиенил)-2-(тио)морфолилпиримидина |
CN106459063A (zh) | 2014-04-11 | 2017-02-22 | 北卡罗来纳-查佩尔山大学 | Mertk‑特异性嘧啶化合物 |
CA2946654C (en) * | 2014-04-28 | 2022-08-23 | Mmv Medicines For Malaria Venture | Triaminopyrimidine compounds useful for preventing or treating malaria |
TWI765410B (zh) * | 2014-08-08 | 2022-05-21 | 日商中外製藥股份有限公司 | 4環性化合物的非晶質體的用途 |
US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
WO2019222538A1 (en) * | 2018-05-16 | 2019-11-21 | The University Of North Carolina At Chapel Hill | Aminopyrimidines and aminopyridines as mertk inhibitors and their application in cancer treatment |
PE20230559A1 (es) | 2020-02-19 | 2023-03-31 | Pharmasyntez | Medicamentos antivirales para el tratamiento y prevencion de la infeccion por vih |
CN111875548A (zh) * | 2020-07-16 | 2020-11-03 | 山东大学 | 一种5位芳环取代的二芳基嘧啶类衍生物及其制备方法与应用 |
US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
WO2022059996A1 (ko) * | 2020-09-15 | 2022-03-24 | 서울대학교 기술지주 주식회사 | 혈액 순환 미세체외소체 매개 암 치료용 조성물 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3459731A (en) * | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
HUP9900730A3 (en) | 1995-11-23 | 2001-04-28 | Janssen Pharmaceutica Nv | Solid mixtures of cyclodextrins prepared via melt-extrusion |
NO311614B1 (no) | 1996-10-01 | 2001-12-17 | Janssen Pharmaceutica Nv | Substituerte diamino-1,3,5-triazinderivater |
EP0945447A1 (en) | 1998-03-27 | 1999-09-29 | Janssen Pharmaceutica N.V. | Trisubstituted 1,3,5-triazine derivatives for treatment of HIV infections |
TR200002760T2 (tr) | 1998-03-27 | 2000-12-21 | Janssen Pharmaceutica N.V. | HIV engelleyici pirimidin türevleri |
CN1214013C (zh) | 1998-11-10 | 2005-08-10 | 詹森药业有限公司 | 抑制hiv复制的嘧啶类 |
GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
AU4413201A (en) | 2000-02-14 | 2001-08-20 | Claus Rayhle | Clip |
ES2542326T3 (es) * | 2000-05-08 | 2015-08-04 | Janssen Pharmaceutica Nv | Inhibidores de la replicación del VIH |
PL210066B1 (pl) * | 2000-12-21 | 2011-11-30 | Vertex Pharma | Związek pirazolowy, kompozycja zawierająca ten związek i jego zastosowania |
JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
AP1927A (en) | 2002-11-15 | 2008-12-10 | Tibotec Pharm Ltd | Substituted indolepyridinium as anti-infective compounds |
US7504396B2 (en) * | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
CN101031550B (zh) * | 2004-09-30 | 2015-05-27 | 泰博特克药品有限公司 | 抑制hiv的5-碳环-或杂环取代的嘧啶类 |
RU2410379C2 (ru) | 2004-09-30 | 2011-01-27 | Тиботек Фармасьютикалз Лтд. | 5-замещенные пиримидины, ингибирующие вич |
BRPI0516746A (pt) | 2004-09-30 | 2008-09-23 | Tibotec Pharm Ltd | 5-heterociclil pirimidinas para inibição de hiv |
AU2007233737B2 (en) | 2006-03-30 | 2012-11-29 | Janssen Sciences Ireland Uc | HIV inhibiting 5-amido substituted pyrimidines |
EA020749B1 (ru) | 2006-12-29 | 2015-01-30 | Тиботек Фармасьютикалз Лтд. | Вич-ингибирующие 5,6-замещенные пиримидины |
DK2114901T3 (da) * | 2006-12-29 | 2014-06-30 | Janssen R & D Ireland | Hiv-inhiberende 6-substituerede pyrimidiner |
-
2005
- 2005-09-29 BR BRPI0516746-9A patent/BRPI0516746A/pt active Search and Examination
- 2005-09-29 AT AT05794656T patent/ATE520680T1/de not_active IP Right Cessation
- 2005-09-29 EP EP05794656A patent/EP1797069B1/en active Active
- 2005-09-29 RU RU2007116152/04A patent/RU2405778C2/ru active
- 2005-09-29 US US11/575,818 patent/US8575342B2/en not_active Expired - Fee Related
- 2005-09-29 CA CA2577467A patent/CA2577467C/en not_active Expired - Fee Related
- 2005-09-29 KR KR1020077007388A patent/KR20070057899A/ko not_active Application Discontinuation
- 2005-09-29 AU AU2005288864A patent/AU2005288864B2/en not_active Ceased
- 2005-09-29 WO PCT/EP2005/054930 patent/WO2006035067A2/en active Application Filing
- 2005-09-29 MX MX2007003797A patent/MX2007003797A/es active IP Right Grant
- 2005-09-29 ES ES05794656T patent/ES2371923T3/es active Active
- 2005-09-29 TW TW094134107A patent/TW200626574A/zh unknown
- 2005-09-29 CN CN2005800331107A patent/CN101031558B/zh not_active Expired - Fee Related
- 2005-09-29 JP JP2007534026A patent/JP5008567B2/ja not_active Expired - Fee Related
- 2005-09-30 AR ARP050104153A patent/AR050969A1/es not_active Application Discontinuation
-
2007
- 2007-01-25 IL IL180959A patent/IL180959A/en active IP Right Grant
- 2007-03-29 ZA ZA200702653A patent/ZA200702653B/xx unknown
Also Published As
Publication number | Publication date |
---|---|
ZA200702653B (en) | 2008-08-27 |
WO2006035067A3 (en) | 2006-08-24 |
EP1797069B1 (en) | 2011-08-17 |
IL180959A (en) | 2012-08-30 |
CN101031558A (zh) | 2007-09-05 |
AU2005288864B2 (en) | 2012-08-23 |
JP5008567B2 (ja) | 2012-08-22 |
CA2577467A1 (en) | 2006-04-06 |
MX2007003797A (es) | 2007-04-23 |
IL180959A0 (en) | 2007-07-04 |
RU2405778C2 (ru) | 2010-12-10 |
EP1797069A2 (en) | 2007-06-20 |
TW200626574A (en) | 2006-08-01 |
JP2008514679A (ja) | 2008-05-08 |
CN101031558B (zh) | 2011-10-05 |
AR050969A1 (es) | 2006-12-06 |
ATE520680T1 (de) | 2011-09-15 |
KR20070057899A (ko) | 2007-06-07 |
WO2006035067A2 (en) | 2006-04-06 |
CA2577467C (en) | 2013-05-28 |
US20090181993A1 (en) | 2009-07-16 |
AU2005288864A1 (en) | 2006-04-06 |
RU2007116152A (ru) | 2008-11-10 |
US8575342B2 (en) | 2013-11-05 |
ES2371923T3 (es) | 2012-01-11 |
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