HUP0204431A1 - 1,5-Diszubsztituált-3,4-dihidro-1H-pirimido[4,5-d]pirimidin-2-on-vegyületek és falhasználásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
1,5-Diszubsztituált-3,4-dihidro-1H-pirimido[4,5-d]pirimidin-2-on-vegyületek és falhasználásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0204431A1 HUP0204431A1 HU0204431A HUP0204431A HUP0204431A1 HU P0204431 A1 HUP0204431 A1 HU P0204431A1 HU 0204431 A HU0204431 A HU 0204431A HU P0204431 A HUP0204431 A HU P0204431A HU P0204431 A1 HUP0204431 A1 HU P0204431A1
- Authority
- HU
- Hungary
- Prior art keywords
- optionally substituted
- group
- aryl
- aralkyl
- alkyl
- Prior art date
Links
- -1 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 102100023482 Mitogen-activated protein kinase 14 Human genes 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- 108010084680 Heterogeneous-Nuclear Ribonucleoprotein K Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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Abstract
A találmány (IV) vagy (IVa) általános képletű 1,5-diszubsztituált-3,4-dihidro-lH-pirimido[4,5-d]pirimidin-2-on-vegyületekre - amelyekképletében R1 adott esetben szubsztituált aril- vagyheteroarilcsoport; R2 hidrogénatom vagy adott esetbenszubsztituált alkil-, cikloalkil-, cikloalkil-alkil-, aril-, aralkil-,heteroaril-, heteroaril-alkil-, heterociklil- vagy heterociklil-alkilcsoport; R3 adott esetben szubsztituált alkil-, cikloalkil-,cikloalkil-alkil-, aril-, aralkil-, heteroaril-, heteroaril-alkil-,heterociklil- vagy heterociklil-alkil-csoport; Y kémiai kötés,CRb, karbonil-, N(Rd) csoport, oxigénatom vagy S(O)m csoport; Rbhidrogénatom, alkil-, =NRc, hidroxi-, merkapto-, alkoxi- vagy alkil-S(O)m- csoport; Rc és Rd hidrogénatom vagy alkilcsoport; X -R2, -OR2, -S(O)mR2, -(CH2)nNR4R14, -(CH2)nNR2R4 csoport; n 0,1, 2, 3, 4, 5, 6, 7, 8, 9 vagy 10; m 0, 1 vagy 2; R4 és R14hidrogénatom, adott esetben szubsztituált alkil-, aril- vagyaralkilcsoport, vagy R4 és Rl4 a nitrogénatommal együtt egy adottesetben az oxigén-, kénatom vagy NR9 általános képletű csoport közülkiválasztott további heteroatomot tartalmazó és adott esetbenszubsztituált heterociklusos gyűrűt képez; R6 hidrogénatomvagy adott esetben szubsztituált alkil-, cikloalkil-, heterociklil-,heterociklil-alkil-, aril-, aralkil-, heteroaril- vagy heteroaril-alkil-csoport; R9 hidrogénatom, -C(Z)R6, adott esetbenszubsztituált alkil-, aril- vagy aralkilcsoport; és Z oxigén-vagy kénatom - és gyógyászatilag elfogadható sóikra, a vegyületekelőállítási eljárásaira, valamint CSBP/p38 kipáz mediált betegségekkezelésére történő alkalmazására, továbbá az ilyen terápiában történőfelhasználásra szolgáló gyógyszerkészítményekre vonatkozik. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US18641900P | 2000-03-02 | 2000-03-02 | |
PCT/US2001/006688 WO2001064679A1 (en) | 2000-03-02 | 2001-03-02 | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0204431A1 true HUP0204431A1 (hu) | 2003-04-28 |
HUP0204431A3 HUP0204431A3 (en) | 2006-01-30 |
Family
ID=22684876
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0204431A HUP0204431A3 (en) | 2000-03-02 | 2001-03-02 | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use, process for their preparation and pharmaceutical compositions containing them |
Country Status (26)
Country | Link |
---|---|
EP (1) | EP1265900B1 (hu) |
JP (1) | JP2003525295A (hu) |
KR (1) | KR100806978B1 (hu) |
CN (1) | CN100482664C (hu) |
AR (2) | AR030053A1 (hu) |
AT (1) | ATE362473T1 (hu) |
AU (2) | AU2001239992B2 (hu) |
BR (1) | BR0108715A (hu) |
CA (1) | CA2402092C (hu) |
CY (1) | CY1106816T1 (hu) |
CZ (1) | CZ20022933A3 (hu) |
DE (1) | DE60128457T2 (hu) |
DK (1) | DK1265900T3 (hu) |
ES (1) | ES2287107T3 (hu) |
HK (1) | HK1052932A1 (hu) |
HU (1) | HUP0204431A3 (hu) |
IL (3) | IL151426A0 (hu) |
MX (1) | MXPA02008588A (hu) |
MY (1) | MY141144A (hu) |
NO (1) | NO326409B1 (hu) |
NZ (1) | NZ520914A (hu) |
PL (1) | PL358280A1 (hu) |
PT (1) | PT1265900E (hu) |
TW (1) | TWI290926B (hu) |
WO (1) | WO2001064679A1 (hu) |
ZA (1) | ZA200207017B (hu) |
Families Citing this family (32)
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ID27589A (id) | 1998-05-26 | 2001-04-12 | Warner Lambert Comapny | Pirimidina bisiklik dan dihidropirimidina bisiklik 3,4 sebagai penghambat proliferasi selular |
CZ20031125A3 (cs) * | 2000-10-23 | 2003-10-15 | Smithkline Beecham Corporation | Nové sloučeniny |
CA2431904A1 (en) * | 2000-12-20 | 2002-08-01 | Merck & Co., Inc. | (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents |
GB0124848D0 (en) | 2001-10-16 | 2001-12-05 | Celltech R&D Ltd | Chemical compounds |
MXPA04007838A (es) | 2002-02-12 | 2004-10-15 | Smithkline Beecham Corp | Derivados de nicotamida utiles como inhibidores p38. |
ES2345096T3 (es) * | 2002-02-13 | 2010-09-15 | F. Hoffmann-La Roche Ag | Nuevos derivados de piridina y pirimidina. |
PL373339A1 (en) * | 2002-04-19 | 2005-08-22 | Smithkline Beecham Corporation | Novel compounds |
GB0214268D0 (en) * | 2002-06-20 | 2002-07-31 | Celltech R&D Ltd | Chemical compounds |
US7196090B2 (en) | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
GB0218800D0 (en) * | 2002-08-13 | 2002-09-18 | Celltech R&D Ltd | Chemical compounds |
US7084270B2 (en) * | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
US7268139B2 (en) | 2002-08-29 | 2007-09-11 | Scios, Inc. | Methods of promoting osteogenesis |
US7112676B2 (en) | 2002-11-04 | 2006-09-26 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
US7384937B2 (en) | 2002-11-06 | 2008-06-10 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
EP1615928A1 (en) | 2003-04-10 | 2006-01-18 | F.Hoffmann-La Roche Ag | Pyrimido compounds |
US7244441B2 (en) | 2003-09-25 | 2007-07-17 | Scios, Inc. | Stents and intra-luminal prostheses containing map kinase inhibitors |
PT1699800E (pt) * | 2003-12-23 | 2010-04-12 | Novartis Ag | Inibidores de quinase p-38 heterocíclicos bicíclicos |
WO2006065703A1 (en) * | 2004-12-13 | 2006-06-22 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
EP1676574A3 (en) | 2004-12-30 | 2006-07-26 | Johnson & Johnson Vision Care, Inc. | Methods for promoting survival of transplanted tissues and cells |
JP5201817B2 (ja) * | 2005-10-28 | 2013-06-05 | 大塚製薬株式会社 | 医薬組成物 |
EP2031965A4 (en) * | 2006-06-16 | 2010-06-30 | Glaxo Group Ltd | NEW COMPOUNDS |
JP2009542818A (ja) * | 2006-06-16 | 2009-12-03 | グラクソ グループ リミテッド | 新規化合物 |
KR101040394B1 (ko) * | 2010-05-18 | 2011-06-09 | (주)이성산업 | 역화 방지 기능을 갖는 야외용 가스 히터 |
CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
CN111793068A (zh) | 2013-03-15 | 2020-10-20 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
WO2015055071A1 (zh) * | 2013-10-16 | 2015-04-23 | 上海璎黎药业有限公司 | 稠合杂环化合物、其制备方法、药物组合物和用途 |
US20190060286A1 (en) | 2016-02-29 | 2019-02-28 | University Of Florida Research Foundation, Incorpo | Chemotherapeutic Methods |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
CA3128468A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd |
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JPS60226882A (ja) * | 1984-04-24 | 1985-11-12 | Nippon Zoki Pharmaceut Co Ltd | 新規ピリミドピリミジン誘導体 |
KR20000029843A (ko) * | 1996-08-06 | 2000-05-25 | 디. 제이. 우드;스피겔 알렌 제이 | 치환된피리도-또는피리미도-함유6,6-또는6,7-비시클릭유도체 |
ID27589A (id) * | 1998-05-26 | 2001-04-12 | Warner Lambert Comapny | Pirimidina bisiklik dan dihidropirimidina bisiklik 3,4 sebagai penghambat proliferasi selular |
JP2002517486A (ja) * | 1998-06-12 | 2002-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | p38のインヒビター |
WO2000024744A1 (en) * | 1998-10-23 | 2000-05-04 | F. Hoffmann-La Roche Ag | Bicyclic nitrogen heterocycles |
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