HUP0102514A2 - Sejtburjánzás gátló hatású pirido-pirimidin és pirimido-pirimidin-származékok és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Sejtburjánzás gátló hatású pirido-pirimidin és pirimido-pirimidin-származékok és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0102514A2 HUP0102514A2 HU0102514A HUP0102514A HUP0102514A2 HU P0102514 A2 HUP0102514 A2 HU P0102514A2 HU 0102514 A HU0102514 A HU 0102514A HU P0102514 A HUP0102514 A HU P0102514A HU P0102514 A2 HUP0102514 A2 HU P0102514A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- alkyl
- pyrimidin
- atom
- double bond
- Prior art date
Links
- 230000004663 cell proliferation Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 title 1
- JOZPEVMCAKXSEY-UHFFFAOYSA-N pyrimido[5,4-d]pyrimidine Chemical class N1=CN=CC2=NC=NC=C21 JOZPEVMCAKXSEY-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 101100295741 Gallus gallus COR4 gene Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 1
- 125000005865 C2-C10alkynyl group Chemical group 0.000 abstract 1
- -1 C3-C-cycloalkyl Chemical group 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000002466 imines Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- SQDFHQJTAWCFIB-UHFFFAOYSA-N n-methylidenehydroxylamine Chemical class ON=C SQDFHQJTAWCFIB-UHFFFAOYSA-N 0.000 abstract 1
- 150000002923 oximes Chemical class 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 1
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 abstract 1
- 150000003573 thiols Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
A találmány tárgya (I) általános képletű vegyületek és gyógyászatilagalkalmazható sóik, ahol: a szaggatott vonal egy adott esetben jelenlévő kettős kötést jelent; Z jelentése N atom vagy CH csoport; Gjelentése N atom vagy CH csoport; W jelentése NH csoport, S atom, SO,vagy SO2 csoport; X jelentése O, S atom, vagy NR10 csoport; R1, R2, ésR10 jelentése egymástól függetlenül H atom, (CH2)nAr, COR4,(CH2)nheteroaril, (CH2)nheterociklil, C1-C10-alkil, C3-C-cikloalkil,C2-C10- alkenil- és C2-C10-alkinilcsoport, ahol n = 0, 1, 2, vagy 3,és a (CH2)nAr, (CH2)nheteroaril, alkil, cikloalkil, alkenil- ésalkinilcsoportok adott esetben legfeljebb 5 csoporttalszubsztituáltak, ahol kettős kötés van jelen, az R3 csoport hiányzik;másrészt R3 jelentése R2 jelentéseivel azonos, ahol R2 jelentése afentiekben megadott, valamint OH, NR4R5, COOR4, OR4, CONR4R5,SO2NR4R5, SO3R4, PO3R4 csoport, csoport, ahol T és Q jelentése afentiekben megadott; R6 jelentése alkilcsoport; R8 és R9 jelentéseegymástól függetlenül H atom, C1-C3-alkil, NR4R5, N(O)R4R5, NR4R5R6Y,hidroxil, alkoxi, tiol, tio-alkilcsoport, halogénatom, COR4, CO2R4,CONR4R5, SO2NR4R5, SO3R4, PO3R4, CHO, CN, vagy NO2 csoport; ha akettős kötés hiányzik, R9 jelentése még karbonil, tio-karbonil, iminés szubsztituált imincsoport, oxim és oxim-éter, és Y jelentése egyhalogén ellenion. A találmány szerinti vegyületek ciklin-függő kinázés tirozin kináz enzim gátló hatásúak és így proliferatív betegségekkezelésében alkalmazhatók. A találmány tárgyát képezik a fentivegyületeket tartalmazó gyógyszerkészítmények. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8670898P | 1998-05-26 | 1998-05-26 | |
US12615899P | 1999-03-25 | 1999-03-25 | |
PCT/US1999/010187 WO1999061444A2 (en) | 1998-05-26 | 1999-05-10 | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0102514A2 true HUP0102514A2 (hu) | 2001-11-28 |
HUP0102514A3 HUP0102514A3 (en) | 2002-03-28 |
Family
ID=26775058
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0102514A HUP0102514A3 (en) | 1998-05-26 | 1999-05-10 | Pyrido-pyrimidin and pyrimido-pyrimidin derivatives as inhibitors of cellular proliferation and pharmaceutical compositions thereof |
Country Status (29)
Country | Link |
---|---|
US (1) | US7501425B1 (hu) |
EP (1) | EP1080092B1 (hu) |
JP (1) | JP2002516327A (hu) |
KR (1) | KR20010043829A (hu) |
CN (1) | CN1138778C (hu) |
AP (1) | AP2000001964A0 (hu) |
AT (1) | ATE402177T1 (hu) |
AU (1) | AU763839B2 (hu) |
BG (1) | BG104960A (hu) |
BR (1) | BR9911590A (hu) |
CA (1) | CA2329703C (hu) |
DE (1) | DE69939168D1 (hu) |
EA (1) | EA003640B1 (hu) |
EE (1) | EE200000706A (hu) |
ES (1) | ES2310039T3 (hu) |
GE (1) | GEP20033093B (hu) |
HK (1) | HK1039483A1 (hu) |
HR (1) | HRP20000799A2 (hu) |
HU (1) | HUP0102514A3 (hu) |
ID (1) | ID27589A (hu) |
IL (1) | IL139599A0 (hu) |
IS (1) | IS5687A (hu) |
NO (1) | NO20005928D0 (hu) |
NZ (1) | NZ508268A (hu) |
PL (1) | PL344248A1 (hu) |
SK (1) | SK17532000A3 (hu) |
TR (1) | TR200003429T2 (hu) |
WO (1) | WO1999061444A2 (hu) |
YU (1) | YU73300A (hu) |
Families Citing this family (101)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2310039T3 (es) | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular. |
PL347432A1 (en) * | 1998-10-23 | 2002-04-08 | Hoffmann La Roche | Bicyclic nitrogen heterocycles |
DE60032623T2 (de) * | 1999-10-21 | 2007-10-11 | F. Hoffmann-La Roche Ag | Alkylamino-substituierte bicyclische heterocyclen als p38 protein-kinase-inhibitoren |
CN1171889C (zh) * | 1999-10-21 | 2004-10-20 | 霍夫曼-拉罗奇有限公司 | 作为p38蛋白激酶的抑制剂的杂烷基氨基-取代的双环氮杂环类化合物 |
AP2002002603A0 (en) * | 2000-01-24 | 2002-09-30 | Warner Lambert Co | 3-aminoquinazolin-2,4-dione antibacterial agents. |
MXPA02007221A (es) * | 2000-01-25 | 2002-11-29 | Warner Lambert Co | Inhibidores de pirido [2,3-d)pirimidin-2,7-diamina cinasa. |
US7053070B2 (en) | 2000-01-25 | 2006-05-30 | Warner-Lambert Company | Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors |
AR030053A1 (es) * | 2000-03-02 | 2003-08-13 | Smithkline Beecham Corp | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
US7235551B2 (en) * | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 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 |
DZ3308A1 (fr) * | 2000-03-06 | 2001-09-27 | Warner Lambert Co | Inhibiteurs de tyrosine kinase a base de 5-alkylpyrido [2,3-d] pyrimidines |
KR100571339B1 (ko) * | 2000-08-31 | 2006-04-17 | 에프. 호프만-라 로슈 아게 | 세포증식 억제제로서의 7-옥소 피리도피리미딘 |
US6506749B2 (en) | 2000-08-31 | 2003-01-14 | Syntex (U.S.A.) Llc | 7-oxo-pyridopyrimidines (I) |
JP4524072B2 (ja) | 2000-10-23 | 2010-08-11 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 新規化合物 |
GB0029015D0 (en) | 2000-11-28 | 2001-01-10 | Univ London | Medical device |
WO2002060382A2 (en) | 2001-01-19 | 2002-08-08 | Smithkline Beecham Corporation | Novel compounds and uses thereof |
CA2434834C (en) | 2001-02-12 | 2010-09-14 | F. Hoffmann-La Roche Ag | 6-substituted pyrido-pyrimidines |
US7105667B2 (en) | 2001-05-01 | 2006-09-12 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
BR0210099A (pt) | 2001-05-30 | 2004-04-13 | Warner Lambert Co | Agentes antibacterianos |
IL162721A0 (en) * | 2002-01-22 | 2005-11-20 | Warner Lambert Co | 2-(Pyridin-2-ylamino)-pyridoÄ2,3-dÜpyrimidin-7-ones |
US7176310B1 (en) | 2002-04-09 | 2007-02-13 | Ucb Sa | Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents |
US7629350B2 (en) | 2002-04-19 | 2009-12-08 | Smithkline Beecham Corporation | Compounds |
PA8577501A1 (es) | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
EP1539755B1 (en) | 2002-08-06 | 2007-09-26 | F. Hoffmann-La Roche Ag | 6-alkoxy-pyrido-pyrimidines as p-38 map kinase inhibitors |
US7084270B2 (en) * | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
TW200413381A (en) * | 2002-11-04 | 2004-08-01 | Hoffmann La Roche | Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents |
US7129351B2 (en) * | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
BRPI0406809A (pt) * | 2003-01-17 | 2005-12-27 | Warner Lambert Co | Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular |
RU2350617C2 (ru) * | 2003-04-10 | 2009-03-27 | Ф.Хоффманн-Ля Рош Аг | Пиримидиновые соединения, обладающие свойствами селективного ингибирования активности кдр и фрфр |
DE10325133A1 (de) * | 2003-06-04 | 2004-12-23 | Bayer Cropscience Ag | Triazolopyrimidine |
US7371750B2 (en) | 2003-07-29 | 2008-05-13 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
BRPI0416030A (pt) | 2003-11-13 | 2007-01-02 | Hoffmann La Roche | pirido-7-pirimidin-7-onas substituìdas com hidroxialquila |
EP1763514A2 (en) * | 2004-05-18 | 2007-03-21 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
DE602005013248D1 (de) | 2004-08-31 | 2009-04-23 | Hoffmann La Roche | Amidderivate von 3-phenyldihydropyrimidoä4,5-düpyrimidinonen, deren herstellung und verwendung als pharmazeutische mittel |
BRPI0514750A (pt) | 2004-08-31 | 2008-06-24 | Hoffmann La Roche | derivados amida de 7-amino-3-fenil-diidropirimido[4, 5-d]pirimidinonas, sua fabricação e uso como inibidores de proteìna cinase |
CA2590294A1 (en) | 2004-12-13 | 2006-06-22 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
AR053346A1 (es) | 2005-03-25 | 2007-05-02 | Glaxo Group Ltd | Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38 |
AR053450A1 (es) | 2005-03-25 | 2007-05-09 | Glaxo Group Ltd | Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38 |
EP1868612A4 (en) | 2005-03-25 | 2010-03-24 | Glaxo Group Ltd | NOVEL CONNECTIONS |
EA200702073A1 (ru) | 2005-03-25 | 2008-12-30 | Глэксо Груп Лимитед | Способ получения пиридо[2,3-d]пиримидин-7-оновых и 3,4-дигидропиримидо[4,5-d]пиримидин-2(1н)-оновых производных |
CA2636981A1 (en) | 2006-01-31 | 2007-08-09 | F. Hoffmann-La Roche Ag | 7h-pyrido[3,4-d]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors |
CN101784551A (zh) * | 2007-06-15 | 2010-07-21 | 万有制药株式会社 | 二环苯胺衍生物 |
JP5524084B2 (ja) | 2008-02-01 | 2014-06-18 | 武田薬品工業株式会社 | Hsp90阻害剤としてのオキシム誘導体 |
US8507505B2 (en) | 2008-12-12 | 2013-08-13 | Msd K.K. | Dihydropyrazolopyrimidinone derivative |
CA2745959A1 (en) * | 2008-12-12 | 2010-06-17 | Msd K.K. | Dihydropyrimidopyrimidine derivatives |
JP5908728B2 (ja) * | 2009-01-06 | 2016-04-26 | 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 | ピリミド−ジアゼピノンキナーゼ骨格化合物及び疾患を治療する方法 |
CA2750716A1 (en) * | 2009-02-25 | 2010-09-02 | Msd K.K. | Pyrimidopyrimidoindazole derivative |
SA111320200B1 (ar) * | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
CA2807498C (en) * | 2010-08-05 | 2017-02-07 | Temple University-Of The Commonwealth System Of Higher Education | 2-substituted-8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitriles and uses thereof |
US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
SG10201702654VA (en) | 2011-04-22 | 2017-06-29 | Signal Pharm Llc | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
EP3309148A1 (en) | 2011-10-14 | 2018-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
ES2572908T3 (es) | 2011-10-14 | 2016-06-03 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
JP6033318B2 (ja) | 2011-10-14 | 2016-11-30 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 第XIa因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
LT3176170T (lt) | 2012-06-13 | 2019-04-25 | Incyte Holdings Corporation | Pakeisti tricikliniai junginiai, kaip fgfr inhibitoriai |
DK2872491T3 (da) * | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
EP2906551B1 (en) | 2012-10-12 | 2018-02-28 | Bristol-Myers Squibb Company | Crystalline forms of a factor xia inhibitor |
WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
US9663524B2 (en) | 2013-03-15 | 2017-05-30 | Celgene Car Llc | Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors |
UA120248C2 (uk) | 2013-03-15 | 2019-11-11 | Селджен Кар Ллс | Гетероарильні сполуки та їх застосування |
EP2978751B1 (en) | 2013-03-25 | 2018-12-05 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
DK2986610T5 (en) * | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
EP3019491A4 (en) | 2013-07-09 | 2016-12-21 | Dana Farber Cancer Inst Inc | KINASE INHIBITORS FOR THE TREATMENT OF DISEASE |
SI3057943T1 (en) | 2013-10-18 | 2018-08-31 | Eisai R&D Management Co., Ltd. | Pyrimidine FGFR4 Inhibitors |
EP3060560A1 (en) | 2013-10-25 | 2016-08-31 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
SG11201604821YA (en) | 2013-12-20 | 2016-07-28 | Signal Pharm Llc | Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith |
LT3099687T (lt) | 2014-01-31 | 2018-09-10 | Bristol-Myers Squibb Company | Makrociklai su heterociklinėmis p2' grupėmis kaip faktoriaus xia inhibitoriai |
NO2760821T3 (hu) | 2014-01-31 | 2018-03-10 | ||
CN103880861B (zh) * | 2014-02-21 | 2016-02-03 | 温州医科大学 | 一种作用于FGF受体的4,6-二甲基-噁唑并[5,4-d]嘧啶-5,7(4H,6H)-二酮衍生物 |
JP6526796B2 (ja) | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Fxia阻害剤であるジアミドマクロ環 |
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
CN107438607B (zh) | 2015-02-20 | 2021-02-05 | 因赛特公司 | 作为fgfr抑制剂的双环杂环 |
WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
CA2982562C (en) | 2015-04-14 | 2023-06-13 | Eisai R&D Management Co., Ltd. | Crystalline fgfr4 inhibitor compound and uses thereof |
US11357769B2 (en) | 2016-05-10 | 2022-06-14 | Eisai R&D Management Co., Ltd. | Drug combinations for reducing cell viability and/or cell proliferation |
CN107459519A (zh) * | 2016-06-06 | 2017-12-12 | 上海艾力斯医药科技有限公司 | 稠合嘧啶哌啶环衍生物及其制备方法和应用 |
EP4047001A3 (en) * | 2016-07-05 | 2022-11-30 | The Broad Institute, Inc. | Bicyclic urea kinase inhibitors and uses thereof |
TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
WO2018160774A1 (en) | 2017-02-28 | 2018-09-07 | The General Hospital Corporation | Uses of pyrimidopyrimidinones as sik inhibitors |
AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
WO2019213506A1 (en) | 2018-05-04 | 2019-11-07 | Incyte Corporation | Salts of an fgfr inhibitor |
PE20210920A1 (es) | 2018-05-04 | 2021-05-19 | Incyte Corp | Formas solidas de un inhibidor de fgfr y procesos para prepararlas |
WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
KR20220100879A (ko) | 2019-10-14 | 2022-07-18 | 인사이트 코포레이션 | Fgfr 저해제로서의 이환식 헤테로사이클 |
WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
CA3188639A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
WO2022006456A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic pyridone compounds as jak2 v617f inhibitors |
WO2022046989A1 (en) | 2020-08-27 | 2022-03-03 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
US11919908B2 (en) | 2020-12-21 | 2024-03-05 | Incyte Corporation | Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors |
TW202302589A (zh) | 2021-02-25 | 2023-01-16 | 美商英塞特公司 | 作為jak2 v617f抑制劑之螺環內醯胺 |
US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
Family Cites Families (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2949466A (en) | 1958-03-04 | 1960-08-16 | Parke Davis & Co | Pyrimidine compounds and means of producing the same |
ES338687A1 (es) | 1966-04-06 | 1968-04-01 | Monsanto Co | Procedimiento para obtener composiciones de fluidos funcio-nales. |
US3912723A (en) | 1971-03-29 | 1975-10-14 | Pfizer | 2-Phenyl-as-triazine-3,5(2H,4H)diones |
IE49992B1 (en) | 1979-06-14 | 1986-01-22 | Wellcome Found | Alkoxybenzylpyridopyrimidines,methods for their preparation and pharmaceutical formulations thereof |
US4425346A (en) | 1980-08-01 | 1984-01-10 | Smith And Nephew Associated Companies Limited | Pharmaceutical compositions |
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 |
AU598093B2 (en) | 1987-02-07 | 1990-06-14 | Wellcome Foundation Limited, The | Pyridopyrimidines, methods for their preparation and pharmaceutical formulations thereof |
EP0584222B1 (en) * | 1991-05-10 | 1997-10-08 | Rhone-Poulenc Rorer International (Holdings) Inc. | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
US5679683A (en) | 1994-01-25 | 1997-10-21 | Warner-Lambert Company | Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
CA2200468A1 (en) | 1994-10-27 | 1996-05-09 | Wayne J. Thompson | Muscarine antagonists |
TJ342B (en) * | 1994-11-14 | 2002-10-06 | Warner Lambert Co | Derivatives of 6-aryl pyrido Ä2,3-dÜ pyrimidines and naphthyridines pharmaceutical composition possess inhibiting effect of cellular proliferation pr ovoking protein tyrosine kinase and method of inhibiting cellular proliferation |
IL117923A (en) * | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
CA2249446C (en) * | 1996-04-12 | 2008-06-17 | Warner-Lambert Company | Irreversible inhibitors of tyrosine kinases |
JP2001509805A (ja) | 1997-02-05 | 2001-07-24 | ワーナー−ランバート・コンパニー | 細胞増殖阻害剤としてのピリド〔2,3−d〕ピリミジンおよび4−アミノピリミジン |
ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
US6150359A (en) | 1997-08-20 | 2000-11-21 | Warner-Lambert Company | Naphthyridinones for inhibiting protein tyrosine kinase and cell cycle kinase mediated cellular proliferation |
JP4038624B2 (ja) | 1997-11-29 | 2008-01-30 | 日本農薬株式会社 | 縮合複素環誘導体及びその中間体並びに有害生物防除剤 |
ES2310039T3 (es) | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular. |
PL347432A1 (en) * | 1998-10-23 | 2002-04-08 | Hoffmann La Roche | Bicyclic nitrogen heterocycles |
CN1171889C (zh) | 1999-10-21 | 2004-10-20 | 霍夫曼-拉罗奇有限公司 | 作为p38蛋白激酶的抑制剂的杂烷基氨基-取代的双环氮杂环类化合物 |
DE60032623T2 (de) | 1999-10-21 | 2007-10-11 | F. Hoffmann-La Roche Ag | Alkylamino-substituierte bicyclische heterocyclen als p38 protein-kinase-inhibitoren |
AR030053A1 (es) | 2000-03-02 | 2003-08-13 | Smithkline Beecham Corp | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
-
1999
- 1999-05-10 ES ES99924165T patent/ES2310039T3/es not_active Expired - Lifetime
- 1999-05-10 YU YU73300A patent/YU73300A/sh unknown
- 1999-05-10 KR KR1020007013279A patent/KR20010043829A/ko not_active Application Discontinuation
- 1999-05-10 NZ NZ508268A patent/NZ508268A/xx unknown
- 1999-05-10 AT AT99924165T patent/ATE402177T1/de not_active IP Right Cessation
- 1999-05-10 ID IDW20002452A patent/ID27589A/id unknown
- 1999-05-10 JP JP2000550849A patent/JP2002516327A/ja not_active Abandoned
- 1999-05-10 AP APAP/P/2000/001964A patent/AP2000001964A0/en unknown
- 1999-05-10 HU HU0102514A patent/HUP0102514A3/hu unknown
- 1999-05-10 CN CNB998065587A patent/CN1138778C/zh not_active Expired - Fee Related
- 1999-05-10 EP EP99924165A patent/EP1080092B1/en not_active Expired - Lifetime
- 1999-05-10 BR BR9911590-5A patent/BR9911590A/pt not_active Application Discontinuation
- 1999-05-10 AU AU40734/99A patent/AU763839B2/en not_active Ceased
- 1999-05-10 TR TR2000/03429T patent/TR200003429T2/xx unknown
- 1999-05-10 WO PCT/US1999/010187 patent/WO1999061444A2/en not_active Application Discontinuation
- 1999-05-10 IL IL13959999A patent/IL139599A0/xx unknown
- 1999-05-10 DE DE69939168T patent/DE69939168D1/de not_active Expired - Fee Related
- 1999-05-10 PL PL99344248A patent/PL344248A1/xx not_active Application Discontinuation
- 1999-05-10 EA EA200001171A patent/EA003640B1/ru not_active IP Right Cessation
- 1999-05-10 GE GEAP19995700A patent/GEP20033093B/en unknown
- 1999-05-10 CA CA002329703A patent/CA2329703C/en not_active Expired - Fee Related
- 1999-05-10 US US09/623,737 patent/US7501425B1/en not_active Expired - Fee Related
- 1999-05-10 EE EEP200000706A patent/EE200000706A/xx unknown
- 1999-05-10 SK SK1753-2000A patent/SK17532000A3/sk unknown
-
2000
- 2000-10-27 IS IS5687A patent/IS5687A/is unknown
- 2000-11-17 BG BG104960A patent/BG104960A/xx unknown
- 2000-11-20 HR HR20000799A patent/HRP20000799A2/hr not_active Application Discontinuation
- 2000-11-23 NO NO20005928A patent/NO20005928D0/no not_active Application Discontinuation
-
2001
- 2001-11-08 HK HK01107828A patent/HK1039483A1/xx not_active IP Right Cessation
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HUP0102514A2 (hu) | Sejtburjánzás gátló hatású pirido-pirimidin és pirimido-pirimidin-származékok és ezeket tartalmazó gyógyszerkészítmények | |
IL129068A0 (en) | Sulfinic acid derivatives and their preparation and use | |
DE69809754D1 (en) | Substituierte 6-phenylphenanthridine | |
GEP20012413B (en) | Novel Substituted Cyclic Amino Acids as Pharmaceutical Agents | |
ES2180633T3 (es) | Uso de derivados de pteridina como inhibidores de la no-sintasa. | |
HUP0100757A1 (hu) | Foszfilopáz enzim inhibitor hatású indolszármazékok és ezeket a vegyületeket tartalmazó gyógyászati készítmények | |
NO971889D0 (no) | Forbindelser og sammensetninger for levering av aktive midler | |
HUP0401646A2 (hu) | Tumorellenes hatású kinazolinszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
HUP0100156A2 (hu) | Foszfolipáz-A2 inhibitor hatású indolszármazékok és alkalmazásuk gyógyászati készítmények előállítására | |
NO964058D0 (no) | Pyrimidinylderivater som interleukininhibitorer | |
HUP0103460A2 (hu) | Vírusellenes hatású indolszármazékok és a vegyületeket tartalmazó gyógyszerkészítmények | |
IL94433A0 (en) | Aminophenol derivatives,their preparation and pharmaceutical compositions containing them | |
HUP0202788A2 (hu) | Terápiásan hasznosítható tulajdonságokkal rendelkező indolil-3-glioxilsav-származékok és ezeket tartalmazó gyógyszerkészítmények | |
HUP0000664A2 (hu) | Azinil-oxi- és fenoxi-diaril-karbonsavszármazékok, eljárás előállításukra és alkalmazásuk gyógyszerkészítmények előállítására | |
DE69924292D1 (de) | Pyrazol verbindungen und ihre verwendung | |
HUP0301478A2 (hu) | Antibakteriális aktivitású pleuromutilinszármazékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
BR0209452A (pt) | Composto de cefem, processo para sua preparação, composição farmacêutica e uso do composto | |
DE69525740T2 (de) | Spezielle halofantrinhaltige Zusammensetzungen | |
HUP0402076A2 (hu) | Szubsztituált indolok, eljárás az előállításukra és fájdalomcsillapítókénti alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények | |
DE69834047D1 (de) | Verwendung einer Zubereitung und ein kosmetisches Verfahren zur Verminderung und Vorbeugung von beissender der Haut | |
IL102361A0 (en) | Benzomorphan derivatives,their preparation and pharmaceutical compositions containing them | |
HUP9702227A2 (hu) | Új benzopiránvegyületek, eljárás ezek előállítására és ezeket tartalmazó gyógyászati készítmények | |
NZ310385A (en) | Novel derivatives of swainsonine, processes for their preparation and their use as therapeutic agents | |
ES2104416T3 (es) | Glicosilamidas de 2-aminoacilamino-2-desoxi-azucares. | |
HUP9801451A2 (hu) | Tetrahidroimidazo[2,1-a]izokinolin-származékok és ezeket tartalmazó gyógyszerkészítmények, alkalmazásuk |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FD9A | Lapse of provisional protection due to non-payment of fees |