ES2193664T3 - Pirimidinas inhibidoras de la replicacion del vih. - Google Patents
Pirimidinas inhibidoras de la replicacion del vih.Info
- Publication number
- ES2193664T3 ES2193664T3 ES99203590T ES99203590T ES2193664T3 ES 2193664 T3 ES2193664 T3 ES 2193664T3 ES 99203590 T ES99203590 T ES 99203590T ES 99203590 T ES99203590 T ES 99203590T ES 2193664 T3 ES2193664 T3 ES 2193664T3
- Authority
- ES
- Spain
- Prior art keywords
- sub
- sup
- alkyl
- optionally substituted
- nhc
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 230000010076 replication Effects 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- -1 cyano, nitro, amino Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000006684 polyhaloalkyl group Polymers 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
Classifications
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10779298P | 1998-11-10 | 1998-11-10 | |
| US14396299P | 1999-07-15 | 1999-07-15 | |
| PCT/EP1999/007417 WO2000027825A1 (en) | 1998-11-10 | 1999-09-24 | Hiv replication inhibiting pyrimidines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2193664T3 true ES2193664T3 (es) | 2003-11-01 |
Family
ID=26805159
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99203590T Expired - Lifetime ES2193664T3 (es) | 1998-11-10 | 1999-11-01 | Pirimidinas inhibidoras de la replicacion del vih. |
| ES02018455T Expired - Lifetime ES2338760T3 (es) | 1998-11-10 | 1999-11-01 | Pirimidinas inhibidoras de la replicacion del vih. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES02018455T Expired - Lifetime ES2338760T3 (es) | 1998-11-10 | 1999-11-01 | Pirimidinas inhibidoras de la replicacion del vih. |
Country Status (41)
Families Citing this family (129)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ID28376A (id) * | 1998-11-10 | 2001-05-17 | Janssen Pharmaceutica Nv | Pirimidina yang menghambat replikasi hiv |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| BRPI0014271B1 (pt) * | 1999-09-24 | 2021-06-22 | Janssen Pharmaceutica N.V. | Partícula consistindo em uma dispersão de sólidos, uso da dita partícula, dispersão de sólidos, forma de dosagem farmacêutica, bem como processos de preparação de dita partícula, dispersão e forma de dosagem |
| DE19945982A1 (de) | 1999-09-24 | 2001-03-29 | Knoll Ag | Geschwindigkeitsbestimmte Partikel |
| AU770600B2 (en) | 1999-10-07 | 2004-02-26 | Amgen, Inc. | Triazine kinase inhibitors |
| US20030004174A9 (en) | 2000-02-17 | 2003-01-02 | Armistead David M. | Kinase inhibitors |
| WO2001085699A2 (en) * | 2000-05-08 | 2001-11-15 | Janssen Pharmaceutica N.V. | Prodrugs of hiv replication inhibiting pyrimidines |
| WO2001085700A2 (en) | 2000-05-08 | 2001-11-15 | Janssen Pharmaceutica N.V. | Hiv replication inhibiting pyrimidines and triazines |
| EP1337931A4 (en) * | 2000-11-01 | 2005-05-11 | Snapnames Com Inc | DOMAIN NAME ACQUISITION AND MANAGEMENT SYSTEM AND METHOD |
| KR100874791B1 (ko) | 2001-05-29 | 2008-12-18 | 바이엘 쉐링 파마 악티엔게젤샤프트 | Ｃｄｋ-억제 피리미딘, 그의 제조방법 및 약제로서의 용도 |
| US6958211B2 (en) | 2001-08-08 | 2005-10-25 | Tibotech Bvba | Methods of assessing HIV integrase inhibitor therapy |
| US8101629B2 (en) | 2001-08-13 | 2012-01-24 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| US7638522B2 (en) | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
| US7115617B2 (en) | 2001-08-22 | 2006-10-03 | Amgen Inc. | Amino-substituted pyrimidinyl derivatives and methods of use |
| US6939874B2 (en) | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
| WO2003032994A2 (de) | 2001-10-17 | 2003-04-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren |
| 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 |
| KR20040048920A (ko) | 2001-11-01 | 2004-06-10 | 얀센 파마슈티카 엔.브이. | 글리코겐 신타아제 키나제 3-베타 저해제(ｇｓｋ저해제)로서의 헤테로아릴 아민 |
| WO2003037869A1 (en) | 2001-11-01 | 2003-05-08 | Janssen Pharmaceutica N.V. | Amide derivatives as glycogen synthase kinase 3-beta inhibitors |
| 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 |
| WO2003076401A1 (en) | 2002-03-13 | 2003-09-18 | Janssen Pharmaceutica N.V. | Sulfonylamino-derivatives as novel inhibitors of histone deacetylase |
| IL164005A0 (en) | 2002-03-13 | 2005-12-18 | Janssen Pharmaceutica Nv | Carbonylamino-derivatives as novel inhibitiors of histone deacetylase |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| DE60318035T2 (de) * | 2002-05-03 | 2008-12-11 | Janssen Pharmaceutica N.V. | Polymermikroemulsionen |
| AR039540A1 (es) * | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| AR040456A1 (es) | 2002-06-27 | 2005-04-06 | Bristol Myers Squibb Co | Piridina n-oxidos 2,4 -disubstituidos utiles como inhibidores de transcriptasa inversa del virus de inmunodeficiencia humana |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| CA2686429C (en) | 2002-08-09 | 2010-11-16 | Janssen Pharmaceutica N.V. | Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
| PT1551372T (pt) | 2002-09-20 | 2018-07-23 | Alpharma Pharmaceuticals Llc | Subunidade de sequestração e composições e métodos relacionados |
| BR0316680A (pt) * | 2002-11-28 | 2005-10-18 | Schering Ag | Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos |
| PT1599468E (pt) | 2003-01-14 | 2008-01-14 | Arena Pharm Inc | Derivados de arilo e heteroarilo 1,2,3.-trissubstituídos comomoduladores do metabolismo, e profilaxia e tratamento dedesordens relacionadas tais como diabetes e hiperglicemia |
| KR101185048B1 (ko) | 2003-02-07 | 2012-09-21 | 얀센 파마슈티카 엔.브이. | Ｈｉｖ 감염 예방용 피리미딘 유도체 |
| CN1747941A (zh) * | 2003-02-07 | 2006-03-15 | 詹森药业有限公司 | 抑制hiv的1,2,4－三嗪 |
| CL2004000303A1 (es) * | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih. |
| ATE433447T1 (de) | 2003-02-20 | 2009-06-15 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| 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 |
| CN1822843B (zh) * | 2003-07-17 | 2010-04-28 | 泰博特克药品有限公司 | 制备含有抗病毒药物颗粒的方法 |
| NZ545270A (en) | 2003-07-30 | 2010-04-30 | Rigel Pharmaceuticals Inc | 2,4-Pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| WO2005028479A2 (en) | 2003-09-25 | 2005-03-31 | Janssen Pharmaceutica N.V. | Hiv replication inhibiting purine derivatives |
| AU2005218183B2 (en) | 2004-03-02 | 2012-06-07 | Virco Bvba | Estimation of clinical cut-offs |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| SG156687A1 (en) | 2004-07-28 | 2009-11-26 | Janssen Pharmaceutica Nv | Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase |
| WO2006015985A1 (en) | 2004-08-10 | 2006-02-16 | Janssen Pharmaceutica N.V. | Hiv inhibiting 1,2,4-triazin-6-one derivatives |
| ES2371923T3 (es) | 2004-09-30 | 2012-01-11 | Tibotec Pharmaceuticals | 5-heterociclil-pirimidinas que inhiben el vih. |
| EP1797047B1 (en) * | 2004-09-30 | 2012-01-25 | Tibotec Pharmaceuticals | Hiv inhibiting 5-substituted pyrimidines |
| EP1797048B1 (en) * | 2004-09-30 | 2011-08-17 | Tibotec Pharmaceuticals | Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
| KR20070085286A (ko) * | 2004-10-29 | 2007-08-27 | 티보텍 파마슈티칼즈 리미티드 | Ｈｉｖ를 저해하는 바이사이클릭 피리미딘 유도체 |
| US20060106043A1 (en) * | 2004-11-08 | 2006-05-18 | Boehringer Ingelheim International Gmbh | Method for treating HIV infection through co-administration of tipranavir and etravirine |
| EP1814878B1 (en) | 2004-11-24 | 2012-01-04 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
| BRPI0606318B8 (pt) | 2005-01-19 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, composição, e, uso de um composto |
| EP2388249A1 (en) * | 2005-01-27 | 2011-11-23 | Tibotec Pharmaceuticals | HIV inhibiting 2-(4-cyanophenylamino) pyrimidine derivatives |
| ES2308731T3 (es) | 2005-02-16 | 2008-12-01 | Astrazeneca Ab | Compuestos quimicos. |
| RU2398768C2 (ru) * | 2005-02-18 | 2010-09-10 | Тиботек Фармасьютикалз Лтд. | Ингибирующие вич производные 2-(4-цианофениламино)-пиримидин-оксида |
| EP1858861B1 (en) * | 2005-03-04 | 2010-07-07 | Tibotec Pharmaceuticals | Hiv inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines |
| KR20080015409A (ko) | 2005-05-16 | 2008-02-19 | 아스트라제네카 아베 | 티로신 키나제 억제제로서 유용한 피라졸릴아미노피리미딘 유도체 |
| RU2458056C2 (ru) | 2005-05-26 | 2012-08-10 | Тиботек Фармасьютикалз Лтд | Способ получения 4-(1,6-дигидро-6-оксо-2-пиримидинил)амино-бензонитрила |
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| CA2628863A1 (en) * | 2005-10-06 | 2007-04-19 | University Of Massachusetts | Composition and synthesis of new reagents for inhibition of hiv replication |
| WO2007049041A1 (en) | 2005-10-28 | 2007-05-03 | Astrazeneca Ab | 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer |
| JP5225104B2 (ja) | 2006-01-19 | 2013-07-03 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 新しい、ヒストンデアセチラーゼのインヒビターとしてのアミノフェニル誘導体 |
| CA2630717C (en) | 2006-01-19 | 2015-02-24 | Janssen Pharmaceutica N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
| DK1981875T3 (da) | 2006-01-19 | 2014-07-14 | Janssen Pharmaceutica Nv | Substituerede indolylalkylaminoderivater som inhibitorer af histondeacetylase |
| US8962643B2 (en) | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| JP5078986B2 (ja) | 2006-03-30 | 2012-11-21 | テイボテク・フアーマシユーチカルズ | Ｈｉｖを阻害する５−アミド置換されたピリミジン |
| JP5070278B2 (ja) | 2006-03-30 | 2012-11-07 | テイボテク・フアーマシユーチカルズ | Ｈｉｖを阻害する５−（ヒドロキシメチレンおよびアミノメチレン）置換されたピリミジン |
| PE20120006A1 (es) | 2006-05-15 | 2012-02-02 | Boehringer Ingelheim Int | Compuestos derivados de pirimidina como inhibidores de la quinasa aurora |
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| DK2484346T3 (en) | 2006-06-19 | 2017-04-24 | Alpharma Pharmaceuticals Llc | Pharmaceutical compositions |
| JP2010506833A (ja) * | 2006-10-11 | 2010-03-04 | アルファーマ，インコーポレイテッド | 医薬組成物 |
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| US9006243B2 (en) | 2006-12-29 | 2015-04-14 | Janssen R&D Ireland | HIV inhibiting 6-substituted pyrimidines |
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