EA200701582A1 - Замещённые 5-фенилпиримидины i в терапии - Google Patents
Замещённые 5-фенилпиримидины i в терапииInfo
- Publication number
- EA200701582A1 EA200701582A1 EA200701582A EA200701582A EA200701582A1 EA 200701582 A1 EA200701582 A1 EA 200701582A1 EA 200701582 A EA200701582 A EA 200701582A EA 200701582 A EA200701582 A EA 200701582A EA 200701582 A1 EA200701582 A1 EA 200701582A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- radical
- radicals
- carry
- alkyl
- ring
- Prior art date
Links
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 239000011593 sulfur Substances 0.000 abstract 2
- LVXOXXGCJHYEOS-UHFFFAOYSA-N 5-phenylpyrimidine Chemical class C1=CC=CC=C1C1=CN=CN=C1 LVXOXXGCJHYEOS-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- C07D239/48—Two nitrogen atoms
-
- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к замещенным 5-фенилпиримидинам формулы I, которые несут радикал Х в 4-й позиции пиримидинового кольца, радикал Y в 6-й позиции пиримидинового кольца, где Х означает одну из групп с формулой NRR, ORили SR, в которых R, R, независимо друг от друга, означают водород, C-С-алкил, С-С-алкенил, С-С-алкинил, C-С-галоалкил, С-С-циклоалкил, С-С-галоциклоалкил, фенил, или 5- или 6-членный гетероарил или 5- или 6-членный гетероциклил, содержащий 1, 2, 3 или 4 атома азота или 1, 2 или 3 атома азота и один атом серы или кислорода в качестве членов кольца, радикалы в котором могут быть незамещенными или могут нести 1, 2, 3 или 4 радикала R; или радикал NRRможет также формировать 5- или 6-членное, необязательно замещенное гетероциклическое кольцо, содержащее 1, 2, 3 или 4 атома азота или 1, 2 или 3 атома азота и один атом серы или кислорода в качестве членов кольца, которые не являются соседними с азотом из NRR, в котором два соседних атома углерода или один атом азота и один соседний атом углерода могут быть связаны С-С-алкиленовой цепью и где гетероциклическое кольцо может быть незамещенным или может нести 1,2,3 или 4 радикала R, как указано в п.1, Rимеет одно из значений, данных для R, кроме водорода; радикал Y выбирается из группы, состоящей из галогена, циано, С-С-алкила, С-С-алкенила, С-С-алкинила, С-С-циклоалкила, С-С-алкокси, С-С-алкенилокси, С-С-алкинилокси, C-С-алкилтио, ди(С-С-алкил)амино или C-С-алкиламино, где алкил, алкенил или алкинил радикалы Y могут быть замещены галогеном, циано, нитро, C-C-алкокси или С-С-алкоксикарбонилом; и где пиримидиновый радикал может также во 2-й позиции нести радикал, отличный от водорода, и где фенильное кольцо в 5-й позиции пиримидинового кольца может быть незамещенным или нести 1, 2, 3, 4 или 5 радикалов L, отличных от
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05001955 | 2005-01-31 | ||
| PCT/EP2006/000774 WO2006079556A2 (en) | 2005-01-31 | 2006-01-30 | Substituted 5-phenyl pyrimidines i in therapy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200701582A1 true EA200701582A1 (ru) | 2008-02-28 |
| EA014098B1 EA014098B1 (ru) | 2010-08-30 |
Family
ID=34933530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200701582A EA014098B1 (ru) | 2005-01-31 | 2006-01-30 | Замещённые 5-фенилпиримидины в терапии рака, фармацевтическая композиция на их основе и способ лечения рака у животных |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20080146593A1 (ru) |
| EP (1) | EP1845991A2 (ru) |
| JP (1) | JP2008528535A (ru) |
| KR (1) | KR20070104893A (ru) |
| CN (1) | CN101111250A (ru) |
| AR (1) | AR054220A1 (ru) |
| AU (1) | AU2006208621B2 (ru) |
| BR (1) | BRPI0607108A2 (ru) |
| CA (1) | CA2595958A1 (ru) |
| EA (1) | EA014098B1 (ru) |
| IL (1) | IL184375A0 (ru) |
| MX (1) | MX2007008397A (ru) |
| NZ (1) | NZ556448A (ru) |
| PE (1) | PE20061042A1 (ru) |
| TW (1) | TW200637556A (ru) |
| UA (1) | UA87895C2 (ru) |
| UY (1) | UY29352A1 (ru) |
| WO (1) | WO2006079556A2 (ru) |
| ZA (1) | ZA200707315B (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110144140A1 (en) * | 2006-09-07 | 2011-06-16 | Eriksen Birgitte L | Pyridinyl-pyrimidine derivatives useful as potassium channel modulating agents |
| TW200836741A (en) * | 2007-01-11 | 2008-09-16 | Basf Ag | 2-substituted pyrimidines I in therapy |
| KR100936278B1 (ko) * | 2007-12-14 | 2010-01-13 | 한국생명공학연구원 | 단백질 포스파타제의 활성을 억제하는 피리미딘 유도체또는 이의 약학적으로 허용가능한 염을 유효성분으로함유하는 암 예방 및 치료용 조성물 |
| AU2009282567B2 (en) * | 2008-08-20 | 2014-10-02 | Merck Sharp & Dohme Corp. | Substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| CZ305457B6 (cs) | 2011-02-28 | 2015-09-30 | Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. | Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití |
| CN111065635B (zh) * | 2018-01-04 | 2022-07-22 | 无锡安万生物科技有限公司 | 作为mth1抑制剂的新型嘧啶衍生物 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4006235A (en) * | 1973-03-23 | 1977-02-01 | Burroughs Wellcome Co. | Treating CNS lymphoma |
| GB8314643D0 (en) * | 1983-05-26 | 1983-06-29 | Wellcome Found | Pyrimidine derivatives |
| GB9012316D0 (en) * | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
| GB9700664D0 (en) * | 1997-01-14 | 1997-03-05 | British Tech Group | Anti-cancer agents |
| BR0207975A (pt) * | 2001-03-15 | 2004-06-15 | Basf Ag | Composto, processo para preparar 5 fenilpiridinas, produto intermediário, agente adequado para combater fungos nocivos fitopatogênicos, e, processo para combater fungos nocivos fitopatogênicos |
| US6887875B2 (en) * | 2001-06-12 | 2005-05-03 | Neurogen Corporation | 2,5-diarypyrimidine compounds |
| IL161893A0 (en) * | 2001-11-19 | 2005-11-20 | Basf Ag | 5-Phenylpyrimidines, agents comprising the same, method for production and use thereof |
| ATE428705T1 (de) * | 2002-02-21 | 2009-05-15 | Basf Se | 2-(2-pyridyl)-5-phenyl-6-aminopyrimidine, verfahren und zwischenprodukte zu ihrer herstellung und ihre verwendung zur bekämpfung von schadpilzen |
| AU2003249484A1 (en) * | 2002-07-22 | 2004-02-09 | Orchid Chemicals And Pharmaceuticals Ltd | Novel bio-active molecules |
| US7371758B2 (en) * | 2003-03-13 | 2008-05-13 | National Science & Technology Development Agency | Antimalarial pyrimidine derivatives and methods of making and using them |
| US20070054929A1 (en) | 2003-05-20 | 2007-03-08 | Basf Aktiengesellschaft | 2-Substituted pyrimidines |
| CA2532568A1 (en) * | 2003-07-24 | 2005-03-03 | Basf Aktiengesellschaft | 2-substituted pyrimidines |
| JP2007506746A (ja) * | 2003-09-24 | 2007-03-22 | ワイス・ホールディングズ・コーポレイション | 抗癌剤としての５−アリールピリミジン類 |
| US20050070712A1 (en) * | 2003-09-26 | 2005-03-31 | Christi Kosogof | Pyrimidine derivatives as ghrelin receptor modulators |
| DE102004003493A1 (de) * | 2004-01-23 | 2005-08-11 | Bayer Cropscience Ag | 5-Phenylpyrimidine |
| JP2008505957A (ja) * | 2004-07-14 | 2008-02-28 | ビーエーエスエフ アクチェンゲゼルシャフト | ２−置換ピリミジン、その調製方法および有害菌類を防除するためのその使用 |
-
2006
- 2006-01-27 TW TW095103598A patent/TW200637556A/zh unknown
- 2006-01-30 EA EA200701582A patent/EA014098B1/ru not_active IP Right Cessation
- 2006-01-30 AR AR20060100329A patent/AR054220A1/es unknown
- 2006-01-30 BR BRPI0607108-2A patent/BRPI0607108A2/pt not_active IP Right Cessation
- 2006-01-30 UA UAA200709766A patent/UA87895C2/ru unknown
- 2006-01-30 PE PE2006000121A patent/PE20061042A1/es not_active Application Discontinuation
- 2006-01-30 CN CNA2006800035983A patent/CN101111250A/zh active Pending
- 2006-01-30 AU AU2006208621A patent/AU2006208621B2/en not_active Ceased
- 2006-01-30 CA CA002595958A patent/CA2595958A1/en not_active Abandoned
- 2006-01-30 WO PCT/EP2006/000774 patent/WO2006079556A2/en active Application Filing
- 2006-01-30 US US11/815,042 patent/US20080146593A1/en not_active Abandoned
- 2006-01-30 JP JP2007552589A patent/JP2008528535A/ja active Pending
- 2006-01-30 EP EP06706482A patent/EP1845991A2/en not_active Withdrawn
- 2006-01-30 NZ NZ556448A patent/NZ556448A/en not_active IP Right Cessation
- 2006-01-30 MX MX2007008397A patent/MX2007008397A/es not_active Application Discontinuation
- 2006-01-30 KR KR1020077017631A patent/KR20070104893A/ko not_active Application Discontinuation
- 2006-01-31 UY UY29352A patent/UY29352A1/es unknown
-
2007
- 2007-07-03 IL IL184375A patent/IL184375A0/en unknown
- 2007-08-29 ZA ZA200707315A patent/ZA200707315B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1845991A2 (en) | 2007-10-24 |
| EA014098B1 (ru) | 2010-08-30 |
| BRPI0607108A2 (pt) | 2010-03-09 |
| KR20070104893A (ko) | 2007-10-29 |
| TW200637556A (en) | 2006-11-01 |
| WO2006079556A2 (en) | 2006-08-03 |
| WO2006079556A3 (en) | 2006-09-21 |
| JP2008528535A (ja) | 2008-07-31 |
| IL184375A0 (en) | 2007-10-31 |
| CA2595958A1 (en) | 2006-08-03 |
| AU2006208621B2 (en) | 2011-08-11 |
| ZA200707315B (en) | 2008-11-26 |
| UA87895C2 (en) | 2009-08-25 |
| CN101111250A (zh) | 2008-01-23 |
| MX2007008397A (es) | 2007-09-07 |
| AU2006208621A1 (en) | 2006-08-03 |
| UY29352A1 (es) | 2006-08-31 |
| US20080146593A1 (en) | 2008-06-19 |
| PE20061042A1 (es) | 2006-11-20 |
| NZ556448A (en) | 2010-12-24 |
| AR054220A1 (es) | 2007-06-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KZ KG TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): BY MD RU |