AR035573A1 - Profarmacos de pirimidinas inhibitorias de la replicacion de hiv - Google Patents
Profarmacos de pirimidinas inhibitorias de la replicacion de hivInfo
- Publication number
- AR035573A1 AR035573A1 ARP010102148A ARP010102148A AR035573A1 AR 035573 A1 AR035573 A1 AR 035573A1 AR P010102148 A ARP010102148 A AR P010102148A AR P010102148 A ARP010102148 A AR P010102148A AR 035573 A1 AR035573 A1 AR 035573A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- hiv replication
- propharmaces
- pyrimidines
- inhibitory
- Prior art date
Links
- 230000010076 replication Effects 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
Compuestos de fórmula (A1)(A2)N-R1 (1), las formas de N-óxido, las sales de adición farmacéuticamente aceptables, las aminas cuaternarias y las formas estereoquímicamente isómeras de los mismos, en donde R1 es alquilo C1-6 sustituido, -S(=O)-R8, -S(=O)2-R8, alquilcarbonilo C7-12, alquiloxicarbonilo C1-6 alquilcarbonilo C1-6opcionalmente sustituido, siendo R8, alquilo C1-6, arilo1 o Het1; (A1)(A2)N- es la forma covalentemente enlazada del correspondiente intermediario de fórmula (A1)(A2)N-H, que es una pirimidina inhibitoria de la replicación de HIV de fórmula (2) (Ver los valores que toman los sustituyentes en la descripción) Y una composición farmacéutica, procedimiento de preparación del compuesto y de la composición y el uso para la preparación de un medicamento.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20247100P | 2000-05-08 | 2000-05-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035573A1 true AR035573A1 (es) | 2004-06-16 |
Family
ID=22749996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010102148A AR035573A1 (es) | 2000-05-08 | 2001-05-07 | Profarmacos de pirimidinas inhibitorias de la replicacion de hiv |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7034019B2 (es) |
| EP (1) | EP1282607B1 (es) |
| JP (1) | JP4969010B2 (es) |
| AR (1) | AR035573A1 (es) |
| AU (1) | AU782948B2 (es) |
| CA (1) | CA2407754C (es) |
| DK (1) | DK1282607T3 (es) |
| ES (1) | ES2559273T3 (es) |
| JO (1) | JO3079B1 (es) |
| MY (1) | MY136671A (es) |
| PA (1) | PA8516501A1 (es) |
| SA (1) | SA01220305B1 (es) |
| TW (1) | TWI292395B (es) |
| WO (1) | WO2001085699A2 (es) |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK287269B6 (sk) * | 1998-11-10 | 2010-05-07 | Janssen Pharmaceutica N. V. | Derivát pyrimidínu, jeho použitie, spôsob jeho prípravy a farmaceutická kompozícia, kombinácia a produkt s jeho obsahom |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| EP1438053B1 (de) * | 2001-10-17 | 2008-09-10 | Boehringer Ingelheim Pharma GmbH & Co.KG | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
| SE0104140D0 (sv) | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| AR039540A1 (es) * | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| HRP20050089B1 (hr) | 2002-07-29 | 2015-06-19 | Rigel Pharmaceuticals | Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti |
| EA200500721A1 (ru) * | 2002-11-28 | 2005-12-29 | Шеринг Акциенгезельшафт | Пиримидины, ингибирующие chk, pdk и акт, их получение и применение в качестве лекарственных средств |
| KR101078098B1 (ko) | 2003-01-14 | 2011-10-28 | 아레나 파마슈티칼스, 인크. | 대사 조절제로서의 1,2,3-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료 |
| AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
| JP4886511B2 (ja) | 2003-07-30 | 2012-02-29 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療または予防方法 |
| KR20060123164A (ko) | 2003-10-17 | 2006-12-01 | 아스트라제네카 아베 | 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체 |
| ES2519690T3 (es) * | 2004-09-24 | 2014-11-07 | University Of Maryland, Baltimore | Método de tratamiento de envenenamiento por organosfósforo |
| US9132135B2 (en) * | 2004-09-24 | 2015-09-15 | University Of Maryland, Baltimore | Method of treating organophosphorous poisoning |
| ATE540035T1 (de) | 2004-11-24 | 2012-01-15 | Rigel Pharmaceuticals Inc | Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| CN101115761B (zh) | 2005-01-19 | 2012-07-18 | 里格尔药品股份有限公司 | 2,4-嘧啶二胺化合物的前药及其应用 |
| US7216803B2 (en) | 2005-01-21 | 2007-05-15 | Kingsley Chukwudum Nwosu | Biometric delegation and authentication of financial transactions |
| NZ561145A (en) | 2005-02-04 | 2011-02-25 | Astrazeneca Ab | Pyrazolylaminopyridine derivatives useful as kinase inhibitors |
| SI1853588T1 (sl) | 2005-02-16 | 2008-10-31 | Astrazeneca Ab | Kemične spojine |
| ES2347815T3 (es) * | 2005-03-04 | 2010-11-04 | Tibotec Pharmaceuticals | 2-(4-cianofenil)-6-hidroxilaminopirimidinas inhibidoras de hiv. |
| BRPI0610184A2 (pt) | 2005-05-16 | 2012-09-25 | Astrazeneca Ab | composto, sal farmaceuticamente aceitável de um composto, processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, métodos para a inibição da atividade de trk, para o tratamento ou profilaxia de cáncer e para a produção de um efeito anti-proliferativo em um animal de sanque quente, e, composição farmacêutica |
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| KR101364277B1 (ko) | 2006-12-08 | 2014-02-21 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 |
| DK2146779T3 (en) | 2007-04-18 | 2016-11-28 | Pfizer Prod Inc | Sulfonylamid derivatives to treat abnormal cell growth. |
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| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
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| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| US8153790B2 (en) | 2009-07-27 | 2012-04-10 | Krizmanic Irena | Process for the preparation and purification of etravirine and intermediates thereof |
| EP2493863B1 (en) * | 2009-10-30 | 2015-02-25 | Janssen Pharmaceutica NV | Phenoxy-substituted pyrimidines as opioid receptor modulators |
| MY160734A (en) | 2010-08-10 | 2017-03-15 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| SG188548A1 (en) | 2010-09-22 | 2013-04-30 | Arena Pharm Inc | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012061303A1 (en) | 2010-11-01 | 2012-05-10 | Avila Therapeutics, Inc. | Heteroaryl compounds and uses thereof |
| NZ710636A (en) | 2010-11-01 | 2017-02-24 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| WO2012064706A1 (en) | 2010-11-10 | 2012-05-18 | Avila Therapeutics, Inc. | Mutant-selective egfr inhibitors and uses thereof |
| WO2012147091A2 (en) * | 2011-04-25 | 2012-11-01 | Hetero Research Foundation | Process for rilpivirine |
| BR112013027734A2 (pt) | 2011-05-04 | 2017-08-08 | Ariad Pharma Inc | compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica |
| EP2755959B1 (en) | 2011-09-16 | 2018-05-16 | Hetero Research Foundation | Rilpivirine hydrochloride |
| CA2853498A1 (en) | 2011-10-28 | 2013-05-02 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
| SMT201800571T1 (it) | 2012-03-15 | 2019-01-11 | Celgene Car Llc | Sali di un inibitore di chinasi del recettore del fattore di crescita dell’epidermide |
| BR112014022789B1 (pt) | 2012-03-15 | 2022-04-19 | Celgene Car Llc | Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US9561228B2 (en) | 2013-02-08 | 2017-02-07 | Celgene Avilomics Research, Inc. | ERK inhibitors and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US10005760B2 (en) | 2014-08-13 | 2018-06-26 | Celgene Car Llc | Forms and compositions of an ERK inhibitor |
| PL3242666T3 (pl) | 2015-01-06 | 2025-02-17 | Arena Pharmaceuticals, Inc. | Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1 |
| HUE060476T2 (hu) | 2015-06-22 | 2023-03-28 | Arena Pharm Inc | (R)-2-(7-(4-ciklopentil-3-(trifluormetil)benziloxi)-1,2,3,4- tetrahidrociklopenta[B]indol-3-il)ecetsav kristályos L-arginin-sója S1P1 receptorral kapcsolatos rendellenességek esetén való alkalmazásra |
| WO2018151873A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| CN107778255B (zh) * | 2017-11-16 | 2019-10-25 | 山东大学 | 一种二芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法和应用 |
| US12156866B2 (en) | 2018-06-06 | 2024-12-03 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
| 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 |
| CN112546969B (zh) * | 2020-12-07 | 2022-12-23 | 安徽贝克制药股份有限公司 | 催化加氢连续生产装置和利托那韦中间体的制备方法 |
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|---|---|---|---|---|
| US2748122A (en) * | 1954-05-06 | 1956-05-29 | Searle & Co | 2-anilino-4, 6-dimethylpyrimidines |
| DD236667A1 (de) * | 1984-05-21 | 1986-06-18 | Fahlberg List Veb | Fungizide mittel, die 2-amino-pyrimidine enthalten |
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| JPH02308248A (ja) | 1989-05-24 | 1990-12-21 | Fuji Photo Film Co Ltd | アミノピリミジン系色素形成カプラーおよび該カプラーを含有するハロゲン化銀カラー写真感光材料 |
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| WO1995010506A1 (en) | 1993-10-12 | 1995-04-20 | The Du Pont Merck Pharmaceutical Company | 1n-alkyl-n-arylpyrimidinamines and derivatives thereof |
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| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
-
2001
- 2001-05-03 DK DK01933925.8T patent/DK1282607T3/en active
- 2001-05-03 ES ES01933925.8T patent/ES2559273T3/es not_active Expired - Lifetime
- 2001-05-03 AU AU60277/01A patent/AU782948B2/en not_active Expired
- 2001-05-03 WO PCT/EP2001/004990 patent/WO2001085699A2/en not_active Ceased
- 2001-05-03 CA CA002407754A patent/CA2407754C/en not_active Expired - Lifetime
- 2001-05-03 US US10/275,333 patent/US7034019B2/en not_active Expired - Lifetime
- 2001-05-03 EP EP01933925.8A patent/EP1282607B1/en not_active Expired - Lifetime
- 2001-05-03 JP JP2001582300A patent/JP4969010B2/ja not_active Expired - Lifetime
- 2001-05-04 MY MYPI20012073A patent/MY136671A/en unknown
- 2001-05-07 AR ARP010102148A patent/AR035573A1/es not_active Application Discontinuation
- 2001-05-07 JO JOP/2001/0062A patent/JO3079B1/ar active
- 2001-05-07 TW TW090110799A patent/TWI292395B/zh not_active IP Right Cessation
- 2001-05-08 PA PA20018516501A patent/PA8516501A1/es unknown
- 2001-08-22 SA SA01220305A patent/SA01220305B1/ar unknown
-
2005
- 2005-09-13 US US11/225,839 patent/US7763631B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| DK1282607T3 (en) | 2016-02-01 |
| JP2003532713A (ja) | 2003-11-05 |
| MY136671A (en) | 2008-11-28 |
| PA8516501A1 (es) | 2002-08-26 |
| CA2407754C (en) | 2009-09-15 |
| TWI292395B (en) | 2008-01-11 |
| ES2559273T3 (es) | 2016-02-11 |
| US20060009474A1 (en) | 2006-01-12 |
| EP1282607A2 (en) | 2003-02-12 |
| EP1282607B1 (en) | 2015-11-11 |
| CA2407754A1 (en) | 2001-11-15 |
| US20030186990A1 (en) | 2003-10-02 |
| US7763631B2 (en) | 2010-07-27 |
| WO2001085699A3 (en) | 2002-02-28 |
| JP4969010B2 (ja) | 2012-07-04 |
| AU782948B2 (en) | 2005-09-15 |
| AU6027701A (en) | 2001-11-20 |
| SA01220305B1 (ar) | 2007-03-10 |
| WO2001085699A2 (en) | 2001-11-15 |
| US7034019B2 (en) | 2006-04-25 |
| JO3079B1 (ar) | 2017-03-15 |
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