AR064877A1 - Derivados de glicina n-sustituidos: inhibidores de prolil hidroxilasa - Google Patents
Derivados de glicina n-sustituidos: inhibidores de prolil hidroxilasaInfo
- Publication number
- AR064877A1 AR064877A1 ARP080100142A ARP080100142A AR064877A1 AR 064877 A1 AR064877 A1 AR 064877A1 AR P080100142 A ARP080100142 A AR P080100142A AR P080100142 A ARP080100142 A AR P080100142A AR 064877 A1 AR064877 A1 AR 064877A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- heterocycloalkyl
- cycloalkyl
- Prior art date
Links
- 102000008109 Mixed Function Oxygenases Human genes 0.000 title 1
- 108010074633 Mixed Function Oxygenases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 9
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000304 alkynyl group Chemical group 0.000 abstract 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 3
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 abstract 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- -1 -NR5R6 Chemical group 0.000 abstract 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001768 cations Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur 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
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
- C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un compuesto de formula 1 en la que :R1 es hidrogeno -NR5R6, alquilo C1-10, alquelino C2-10, cicloalquelino C3-8, alquil C1-10-cicloalquilo C3-8, cicloalquenilo C5-8, alquil C1-10-cicloalquenilo C5-8, heterocicloalquilo C3-8, alquil C1-10- heterocicloalquilo C3-8, arilo, alquil C1-10-heteroarilo; R2 es -NR7R8 o -OR9; R3es H o alquilo C1-4; R4 es hidrogeno, -NR5R6, alquiloC1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-8, alquil C1-10-cicloalquilo C3-8, cicloalquenilo C5-8, alquil C1-10-cicloalquenilo C5-8, heterocicloalquilo C3-8, alquil C1-10-heterocicloalquilo C3-8,arilo, alquil C1-10-arilo, heteroarilo o alquil C1-10-heteroarilo; cada uno de R5 y R6 se selecciona independientemente entre el grupo que consiste en hidrogeno, alquilo C1-10, cicloalquilo C3-8, alquil C1-10-cicloalquilo C3-8, heterocicloalquilo C3-8, alquil C1-10-heterocicloalquilo C3-8, arilo, alquil C1-10-arilo, heteroarilo, alquil C1-10-heteroarilo, -CO(alquilo C1-4), -CO(cicloalquilo C3-6), - CO(heterocicloalquilo C3-6), -CO(arilo), -CO(heteroarilo) y -SO2(alquilo C1-4); o R5 y R6 tomados juntos con el nitrogeno al que estan unidos forman un anillo saturado de 5, 6 o 7 miembros que contiene opcionalmente otro heteroatomo seleccionado entre el grupo que consiste en oxigeno, nitrogeno y azufre; cada uno de R7 y R8 se selecciona independientemente entre el grupo que consiste en hidrogeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-8, heterocicloalquilo C3-8, arilo y heteroarilo; R9 es H o un cation, o alquilo C1-10 que esta sin sustituir o sustituido con uno o mas sustituyentes seleccionados independientemente entre el grupo que consiste en cicloalquilo C3-6, heterocicloalquilo, arilo y heteroarilo, donde cualquier carbonoo heteroatomo de R1,R2,R3, R4, R5, R6, R7, R8 y R9 esta sin sustituir o cuando sea posible, esta sustituido con uno o mas sustituyentes seleccionados independientemente entre el grupo que consiste en un grupo alquilo C1-6, arilo, heteroarilo, halogeno, -OR10, -NR5R6, ciano, nitro, -C(O)R10, -C(O)OR10, -SR10, -S(O)R10, -S(O)2R10, -NR5R6, -CONR5R6, -N(R5)C(O)R10, -N(R5)C(O)OR10, -OC(O)NR5R6, -N(R5)C(O)NR5R6, -SO2NR5R6, -N(R5)SO2R10, alquenilo C1-10, alquinilo C1- 10,cicloalquilo C3-6, heterocicloalquilo C3-6, arilo o heteroarilo, donde R5 y R6 son como se ha definido anteriormente y R10 es hidrogeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, -CO(alquilo C1-4), -CO(arilo), CO(heteroarilo), - CO(cicloalquilo C3-6), -CO(heterocicloalquilo C3-6), -SO2(alquilo C1-4), cicloalquilo C3-8, heterocicloalquilo C3-8, arilo C6-14, alquil C1-10-arilo, heteroarilo y alquil C1-10-heteroarilo; o una sal farmacéuticamente aceptable o solvato del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88470607P | 2007-01-12 | 2007-01-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR064877A1 true AR064877A1 (es) | 2009-04-29 |
Family
ID=39618260
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100142A AR064877A1 (es) | 2007-01-12 | 2008-01-11 | Derivados de glicina n-sustituidos: inhibidores de prolil hidroxilasa |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20080171756A1 (es) |
| AR (1) | AR064877A1 (es) |
| CL (1) | CL2008000065A1 (es) |
| PE (1) | PE20090048A1 (es) |
| TW (1) | TW200845994A (es) |
| WO (1) | WO2008089051A1 (es) |
Families Citing this family (49)
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| US7588924B2 (en) | 2006-03-07 | 2009-09-15 | Procter & Gamble Company | Crystal of hypoxia inducible factor 1 alpha prolyl hydroxylase |
| TWI394747B (zh) | 2006-06-23 | 2013-05-01 | Smithkline Beecham Corp | 脯胺醯基羥化酶抑制劑 |
| PT3357911T (pt) | 2006-06-26 | 2022-07-11 | Akebia Therapeutics Inc | Inibidores da prolil-hidroxilase e métodos de utilização |
| US8048892B2 (en) | 2006-12-18 | 2011-11-01 | Amgen Inc. | Azaquinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof |
| WO2008076427A2 (en) * | 2006-12-18 | 2008-06-26 | Amgen Inc. | Naphthalenone compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof |
| US7569726B2 (en) * | 2007-04-18 | 2009-08-04 | Amgen Inc. | Indanone derivatives that inhibit prolyl hydroxylase |
| ES2442847T3 (es) * | 2007-04-18 | 2014-02-13 | Amgen, Inc | Quinolonas y azaquinolonas que inhiben la prolil hidroxilasa |
| AU2008248165B2 (en) * | 2007-05-04 | 2011-12-08 | Amgen Inc. | Diazaquinolones that inhibit prolyl hydroxylase activity |
| EP2150251B9 (en) * | 2007-05-04 | 2013-02-27 | Amgen, Inc | Thienopyridine and thiazolopyridine derivatives that inhibit prolyl hydroxylase activity |
| EP2252619B1 (en) | 2008-01-11 | 2013-10-09 | Fibrogen, Inc. | Isothiazole-pyridine derivatives as modulators of hif (hypoxia inducible factor) activity |
| WO2009100250A1 (en) | 2008-02-05 | 2009-08-13 | Fibrogen, Inc. | Chromene derivatives and use thereof as hif hydroxylase activity inhibitors |
| SI2294066T1 (sl) | 2008-04-28 | 2014-12-31 | Janssen Pharmaceutica N.V. | Benzoimidazoli kot inhibitorji prolil-hidroksilaze |
| CN102264740B (zh) | 2008-08-20 | 2014-10-15 | 菲布罗根有限公司 | 一种吡咯[1,2-b]哒嗪衍生物及其作为hif调节剂的用途 |
| EP2326178A4 (en) * | 2008-08-21 | 2012-10-24 | Glaxosmithkline Llc | INHIBITORS OF PROLYL-HYDROXYLASE |
| US20110144167A1 (en) * | 2008-08-25 | 2011-06-16 | Smithkline Beecham Corporation | Prolyl Hydroxylase Inhibitors |
| AU2009314155B2 (en) | 2008-11-14 | 2015-10-08 | Fibrogen, Inc. | Thiochromene derivatives as HIF hydroxylase inhibitors |
| EP2399910B1 (en) | 2009-02-13 | 2014-04-02 | Shionogi&Co., Ltd. | Triazine derivatives as p2x3 and/or p2x2/3 receptor antagonists and pharmaceutical composition containing them |
| AU2010266559A1 (en) * | 2009-06-30 | 2011-12-15 | Merck Sharp & Dohme Corp. | Substituted 4-hydroxypyrimidine-5-carboxamides |
| US8815865B2 (en) | 2009-06-30 | 2014-08-26 | Merck Sharp & Dohme Corp. | Substituted 4-hydroxypyrimidine-5-carboxamides |
| MY163022A (en) * | 2009-10-21 | 2017-07-31 | Daiichi Sankyo Co Ltd | 5-hydroxypyrimidine-4-carboxamide derivative |
| BR112012010766A2 (pt) | 2009-11-06 | 2015-10-06 | Aerpio Therapeutics Inc | composições e métodos de tratamento da colite e de outras doenças instestinais |
| EP2604260B1 (en) * | 2010-08-10 | 2017-05-10 | Shionogi&Co., Ltd. | Novel heterocyclic derivatives and pharmaceutical composition containing same |
| JP5594706B2 (ja) | 2010-08-10 | 2014-09-24 | 塩野義製薬株式会社 | トリアジン誘導体およびそれを含有する鎮痛作用を有する医薬組成物 |
| WO2012106472A1 (en) | 2011-02-02 | 2012-08-09 | Fibrogen, Inc. | Naphthyridine derivatives as inhibitors of hypoxia inducible factor (hif) hydroxylase |
| GB201102659D0 (en) | 2011-02-15 | 2011-03-30 | Isis Innovation | Assay |
| NO2686520T3 (es) | 2011-06-06 | 2018-03-17 | ||
| WO2012170442A1 (en) | 2011-06-06 | 2012-12-13 | Akebia Therapeutics Inc. | Compounds and compositions for stabilizing hypoxia inducible factor-2 alpha as a method for treating cancer |
| GB201113101D0 (en) | 2011-07-28 | 2011-09-14 | Isis Innovation | Assay |
| AU2012328763A1 (en) | 2011-10-25 | 2014-05-01 | Janssen Pharmaceutica Nv | Meglumine salt formulations of 1-(5,6-dichloro-1H-benzo(d)imidazol-2-yl)-1H-pyrazole-4-carboxylic acid |
| JP6124351B2 (ja) | 2012-02-09 | 2017-05-10 | 塩野義製薬株式会社 | 複素環および炭素環誘導体 |
| RU2503665C1 (ru) * | 2012-05-03 | 2014-01-10 | Открытое акционерное общество "Государственный научно-исследовательский институт "Кристалл" (ОАО "ГосНИИ "Кристалл") | Способ получения 2-метилпиримидин-4,6-(3н,5н)-диона |
| RU2503666C1 (ru) * | 2012-06-25 | 2014-01-10 | Открытое акционерное общество "Государственный научно-исследовательский институт "Кристалл" (ОАО "ГосНИИ "Кристалл") | Способ получения 2-метилпиримидин-4,6-(3н, 5н)-диона |
| EP2881384B1 (en) | 2012-07-30 | 2018-05-30 | Taisho Pharmaceutical Co., Ltd. | Partially saturated nitrogen-containing heterocyclic compound |
| EP3007695B1 (en) | 2013-06-13 | 2024-02-07 | Akebia Therapeutics, Inc. | Compositions and methods for treating anemia |
| TWI637949B (zh) | 2013-06-14 | 2018-10-11 | 塩野義製藥股份有限公司 | 胺基三衍生物及含有其等之醫藥組合物 |
| CR20160222U (es) | 2013-11-15 | 2016-08-26 | Akebia Therapeutics Inc | Formas solidas de acido { [ -(3- clorofenil) -3- hidroxipiridin -2-carbonil] amino} acetico, composiciones, y usos de las mismas |
| JP5975122B2 (ja) * | 2014-01-29 | 2016-08-23 | 大正製薬株式会社 | ［（４−ヒドロキシ−２−オキソ−１，２，５，６−テトラヒドロ−３−ピリジニル）カルボニル］グリシン化合物の結晶形及びそれらの製造方法 |
| WO2016034108A1 (zh) | 2014-09-02 | 2016-03-10 | 广东东阳光药业有限公司 | 喹啉酮类化合物及其应用 |
| CA2974691A1 (en) | 2015-01-23 | 2016-07-28 | Akebia Therapeutics, Inc. | Solid forms of 2-(5-(3-fluorophenyl)-3-hydroxypicolinamido)acetic acid, compositions, and uses thereof |
| UA123308C2 (uk) | 2015-04-01 | 2021-03-17 | Екебіа Терапьютікс, Інк. | Композиції і способи для лікування анемії |
| UY36949A (es) | 2015-10-14 | 2017-04-28 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | 2,4-dihidroxi-nicotinamidas como agonistas de apj |
| MX391259B (es) | 2015-10-14 | 2025-03-21 | X Therma Inc | Composiciones y métodos para reducir la formación de cristales de hielo. |
| AU2017238504B2 (en) * | 2016-03-24 | 2021-05-27 | Bristol-Myers Squibb Company | 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides as APJ agonists |
| JP7440989B2 (ja) | 2018-05-09 | 2024-02-29 | アケビア セラピューティクス インコーポレイテッド | ２－［５－（３－クロロフェニル）－３－ヒドロキシピリジン－２－カルボニル］アミノ］酢酸を調製するための方法 |
| US11524939B2 (en) | 2019-11-13 | 2022-12-13 | Akebia Therapeutics, Inc. | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} acetic acid |
| RU2738605C1 (ru) * | 2020-03-06 | 2020-12-14 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургский государственный химико-фармацевтический университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО СПХФУ Минздрава России) | 5-Замещённые-6-гидрокси-2,3-дифенилпиримидин-4-(3Н)-оны и способ их получения |
| RU2738107C1 (ru) * | 2020-03-06 | 2020-12-08 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургский государственный химико-фармацевтический университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО СПХФУ Минздрава России) | Способ получения 5-замещённых-6-гидрокси-2,3-дифенилпиримидин-4(3Н)-онов |
| RU2757391C1 (ru) * | 2021-02-24 | 2021-10-14 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургский государственный химико-фармацевтический университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО СПХФУ Минздрава России) | 1,2-Дифенил-5-бутил-6-оксо-1,6-дигидропиримидин-4-олят натрия и способ его получения |
| CN118005535B (zh) * | 2024-04-10 | 2024-12-27 | 天津市长芦化工新材料有限公司 | 全氟异丁腈的合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5912261A (en) * | 1994-12-20 | 1999-06-15 | Nippon Zoki Pharmaceutical Co., Ltd. | Carboxyalkyl heterocyclic derivatives |
| CN102552261A (zh) * | 2001-12-06 | 2012-07-11 | 法布罗根股份有限公司 | 提高内源性红细胞生成素(epo)的方法 |
| WO2003106434A1 (ja) * | 2002-06-14 | 2003-12-24 | 味の素株式会社 | ピリミジン化合物の製造方法 |
| US7183287B2 (en) * | 2003-04-03 | 2007-02-27 | Pharmacia Corporation | Substituted pyrimidinones |
-
2008
- 2008-01-10 TW TW097100935A patent/TW200845994A/zh unknown
- 2008-01-10 CL CL200800065A patent/CL2008000065A1/es unknown
- 2008-01-11 AR ARP080100142A patent/AR064877A1/es not_active Application Discontinuation
- 2008-01-11 PE PE2008000123A patent/PE20090048A1/es not_active Application Discontinuation
- 2008-01-11 WO PCT/US2008/050831 patent/WO2008089051A1/en not_active Ceased
- 2008-01-11 US US11/972,707 patent/US20080171756A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| PE20090048A1 (es) | 2009-03-28 |
| TW200845994A (en) | 2008-12-01 |
| CL2008000065A1 (es) | 2008-09-22 |
| WO2008089051A1 (en) | 2008-07-24 |
| US20080171756A1 (en) | 2008-07-17 |
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