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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (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 |
---|---|---|---|---|
AU2005288866B2 (en) | 2004-09-30 | 2012-07-26 | Janssen Sciences Ireland Uc | HIV inhibiting 5-substituted pyrimidines |
ES2371923T3 (es) | 2004-09-30 | 2012-01-11 | Tibotec Pharmaceuticals | 5-heterociclil-pirimidinas que inhiben el vih. |
WO2006087387A1 (en) * | 2005-02-18 | 2006-08-24 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 2-(4-cyanophenylamino) pyrimidine oxide derivatives |
EP2004632B1 (en) | 2006-03-30 | 2014-03-12 | Janssen R&D Ireland | Hiv inhibiting 5-amido substituted pyrimidines |
EP2089384B1 (en) | 2006-12-13 | 2015-08-05 | F. Hoffmann-La Roche AG | 2-(piperidin-4-yl)-4-phenoxy-or phenylamino-pyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors |
ES2470570T3 (es) | 2006-12-29 | 2014-06-24 | Janssen R&D Ireland | Pirimidinas sustituidas en posición 6 inhibidoras del HIV |
KR20090094084A (ko) | 2006-12-29 | 2009-09-03 | 티보텍 파마슈티칼즈 리미티드 | Hiv를 억제하는 5,6-치환된 피리미딘 |
US20100137313A1 (en) * | 2008-10-03 | 2010-06-03 | Astrazeneca Ab | Heterocyclic derivatives and methods of use thereof |
EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
JP5993010B2 (ja) | 2011-08-23 | 2016-09-14 | エンドゥ ファーマシューティカルズ,インコーポレイティド | ピリミド−ピリダジノン化合物及びその使用 |
JP2014532060A (ja) | 2011-10-03 | 2014-12-04 | ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル | 癌を治療するためのピロロピリミジン化合物 |
US9567326B2 (en) * | 2012-05-22 | 2017-02-14 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
EP2909211A4 (en) | 2012-10-17 | 2016-06-22 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
US9771330B2 (en) | 2012-11-27 | 2017-09-26 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
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 |
MX2016014166A (es) * | 2014-04-28 | 2017-02-14 | Medicines For Malaria Venture Mmv | Compuestos de triaminopirimidina utiles para evitar o tratar la malaria. |
TWI831347B (zh) * | 2014-08-08 | 2024-02-01 | 日商中外製藥股份有限公司 | 包含4環性化合物的非晶質體之固體分散體及製劑 |
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 |
AU2021224460A1 (en) | 2020-02-19 | 2022-12-15 | Pharmasyntez, Joint Stock Company | Pyrimidine-based bicycles as antiviral agents for the treatment and prevention of HIV infection |
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 |
PL189122B1 (pl) | 1995-11-23 | 2005-06-30 | Janssen Pharmaceutica Nv | Sposób wytwarzania mieszaniny stałej zawierającejjedną lub wiele cyklodekstryn, mieszanina stała ikompozycja farmaceutyczna |
NO311614B1 (no) | 1996-10-01 | 2001-12-17 | Janssen Pharmaceutica Nv | Substituerte diamino-1,3,5-triazinderivater |
TR200002760T2 (tr) | 1998-03-27 | 2000-12-21 | Janssen Pharmaceutica N.V. | HIV engelleyici pirimidin türevleri |
EP0945447A1 (en) | 1998-03-27 | 1999-09-29 | Janssen Pharmaceutica N.V. | Trisubstituted 1,3,5-triazine derivatives for treatment of HIV infections |
EA004049B1 (ru) | 1998-11-10 | 2003-12-25 | Янссен Фармацевтика Н.В. | Пиримидины, ингибирующие репликацию вич |
GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
WO2001058700A1 (de) | 2000-02-14 | 2001-08-16 | Claus Rayhle | Klammer |
US7276510B2 (en) * | 2000-05-08 | 2007-10-02 | Janssen Pharmaceutica, Inc. | HIV replication inhibitors |
US20030105090A1 (en) * | 2000-12-21 | 2003-06-05 | David Bebbington | Pyrazole compounds useful as protein kinase inhibitors |
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 |
EA009871B1 (ru) | 2002-11-15 | 2008-04-28 | Тиботек Фармасьютикалз Лтд. | Замещённые индолпиридиниевые соединения в качестве противоинфекционного средства |
US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
ES2371923T3 (es) | 2004-09-30 | 2012-01-11 | Tibotec Pharmaceuticals | 5-heterociclil-pirimidinas que inhiben el vih. |
WO2006035068A2 (en) * | 2004-09-30 | 2006-04-06 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
AU2005288866B2 (en) * | 2004-09-30 | 2012-07-26 | Janssen Sciences Ireland Uc | HIV inhibiting 5-substituted pyrimidines |
EP2004632B1 (en) * | 2006-03-30 | 2014-03-12 | Janssen R&D Ireland | Hiv inhibiting 5-amido substituted pyrimidines |
ES2470570T3 (es) | 2006-12-29 | 2014-06-24 | Janssen R&D Ireland | Pirimidinas sustituidas en posición 6 inhibidoras del HIV |
KR20090094084A (ko) | 2006-12-29 | 2009-09-03 | 티보텍 파마슈티칼즈 리미티드 | Hiv를 억제하는 5,6-치환된 피리미딘 |
-
2005
- 2005-09-29 ES ES05794656T patent/ES2371923T3/es active Active
- 2005-09-29 WO PCT/EP2005/054930 patent/WO2006035067A2/en active Application Filing
- 2005-09-29 JP JP2007534026A patent/JP5008567B2/ja not_active Expired - Fee Related
- 2005-09-29 EP EP05794656A patent/EP1797069B1/en active Active
- 2005-09-29 CN CN2005800331107A patent/CN101031558B/zh not_active Expired - Fee Related
- 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 MX MX2007003797A patent/MX2007003797A/es active IP Right Grant
- 2005-09-29 CA CA2577467A patent/CA2577467C/en not_active Expired - Fee Related
- 2005-09-29 BR BRPI0516746-9A patent/BRPI0516746A/pt active Search and Examination
- 2005-09-29 AU AU2005288864A patent/AU2005288864B2/en not_active Ceased
- 2005-09-29 TW TW094134107A patent/TW200626574A/zh unknown
- 2005-09-29 AT AT05794656T patent/ATE520680T1/de not_active IP Right Cessation
- 2005-09-29 KR KR1020077007388A patent/KR20070057899A/ko not_active Application Discontinuation
- 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 |
---|---|
JP5008567B2 (ja) | 2012-08-22 |
US8575342B2 (en) | 2013-11-05 |
CA2577467A1 (en) | 2006-04-06 |
ES2371923T3 (es) | 2012-01-11 |
US20090181993A1 (en) | 2009-07-16 |
MX2007003797A (es) | 2007-04-23 |
EP1797069B1 (en) | 2011-08-17 |
AU2005288864A1 (en) | 2006-04-06 |
WO2006035067A2 (en) | 2006-04-06 |
IL180959A (en) | 2012-08-30 |
ZA200702653B (en) | 2008-08-27 |
RU2007116152A (ru) | 2008-11-10 |
AU2005288864B2 (en) | 2012-08-23 |
RU2405778C2 (ru) | 2010-12-10 |
CN101031558B (zh) | 2011-10-05 |
AR050969A1 (es) | 2006-12-06 |
CA2577467C (en) | 2013-05-28 |
EP1797069A2 (en) | 2007-06-20 |
KR20070057899A (ko) | 2007-06-07 |
IL180959A0 (en) | 2007-07-04 |
TW200626574A (en) | 2006-08-01 |
JP2008514679A (ja) | 2008-05-08 |
CN101031558A (zh) | 2007-09-05 |
WO2006035067A3 (en) | 2006-08-24 |
ATE520680T1 (de) | 2011-09-15 |
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