MA26946A1 - Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases. - Google Patents
Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases.Info
- Publication number
- MA26946A1 MA26946A1 MA27050A MA27050A MA26946A1 MA 26946 A1 MA26946 A1 MA 26946A1 MA 27050 A MA27050 A MA 27050A MA 27050 A MA27050 A MA 27050A MA 26946 A1 MA26946 A1 MA 26946A1
- Authority
- MA
- Morocco
- Prior art keywords
- formula
- compounds
- syndrome
- kinase inhibitors
- pyrazole derivatives
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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- 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
- C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
Abstract
DEPOSANT Société dite : PFIZER PRODUCTS INC. REVENDICATION DE PRIORITES US 31 Aoét 2000 60/229,415 Voir en annexe le titre de l'invention et le texte de l'abrégé Dérivés de pyrazole nouveaux et leur utilisation comme inhibiteurs de protéine-kinases L'invention propose des composés de formule (1) dans laquelle R1, R2, R3 et R4 répondent aux définitions, et leurs sels pharmaceutiquement acceptables. Les composés de formule (1) sont indiqués en tant qu'agents ayant une activité inhibitrice de cdk2, et GSK-3. Des compositions pharmaceutiques et méthodes comprenant des composés de formule (1) pour le traitement et la prévention de maladies et d'affections comprenant une croissance cellulaire anormale, telle qu'un cancer, et des maladies et affections neuro-dégénératives ainsi que celles affectées par la neurotransmission de la dopamine. Il est décrit également des compositions et méthodes pharmaceutiques, comprenant des composés de formule (1) pour le traitement de la stérilité masculine et de la motilité du sperme ; du diabète sucré ; d'une tolérance entravée au glucose ; du syndrome métabolique ou syndrome X ; du syndrome d'ovaire polykystique ; de 1'adipogénèse et de l'obésité ; de la myogénèse et de la fragilité, par exemple du déclin des performances physiques dé à l'??ge ; de la sarcopénie aigue, par exemple de l'atrophie musculaire et/ou de la cachexie associées aux brélures, à l'état alité, à une immobilisation des membres ou à une intervention chirurgicale thoracique, abdominale et/ou orthopédique importante ; de la septicémie ; de la perte des cheveux, de l'éclaircissement capillaire et de la calvitie ; et d'une immunodéficience.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22941500P | 2000-08-31 | 2000-08-31 |
Publications (1)
Publication Number | Publication Date |
---|---|
MA26946A1 true MA26946A1 (fr) | 2004-12-20 |
Family
ID=22861151
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MA27050A MA26946A1 (fr) | 2000-08-31 | 2003-02-21 | Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases. |
Country Status (38)
Country | Link |
---|---|
EP (1) | EP1313710A1 (fr) |
JP (1) | JP2004507526A (fr) |
KR (1) | KR20030027093A (fr) |
CN (1) | CN1518543A (fr) |
AP (1) | AP2001002266A0 (fr) |
AR (1) | AR035345A1 (fr) |
AU (1) | AU2001280009A1 (fr) |
BG (1) | BG107455A (fr) |
BR (1) | BR0113574A (fr) |
CA (1) | CA2420363A1 (fr) |
CR (1) | CR6881A (fr) |
CZ (1) | CZ2003468A3 (fr) |
DO (1) | DOP2001000243A (fr) |
DZ (1) | DZ3398A1 (fr) |
EA (1) | EA200300205A1 (fr) |
EC (1) | ECSP034480A (fr) |
EE (1) | EE200300085A (fr) |
GT (1) | GT200100179A (fr) |
HN (1) | HN2001000192A (fr) |
HR (1) | HRP20030140A2 (fr) |
HU (1) | HUP0302669A3 (fr) |
IL (1) | IL154016A0 (fr) |
IS (1) | IS6687A (fr) |
MA (1) | MA26946A1 (fr) |
MX (1) | MXPA03001785A (fr) |
NO (1) | NO20030958L (fr) |
NZ (1) | NZ523656A (fr) |
OA (1) | OA12368A (fr) |
PA (1) | PA8528101A1 (fr) |
PE (1) | PE20020470A1 (fr) |
PL (1) | PL360742A1 (fr) |
SK (1) | SK2002003A3 (fr) |
SV (1) | SV2002000618A (fr) |
TN (1) | TNSN01132A1 (fr) |
UY (1) | UY26909A1 (fr) |
WO (1) | WO2002018346A1 (fr) |
YU (1) | YU14703A (fr) |
ZA (1) | ZA200301064B (fr) |
Families Citing this family (73)
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US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
EP2298311B1 (fr) | 1999-01-13 | 2012-05-09 | Bayer HealthCare LLC | Urées de diphényle à substitution omega-carboxyaryle en tant qu'inhibiteurs de la p38 kinase |
AU2001292670A1 (en) | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
BR0116411A (pt) | 2000-12-21 | 2003-11-11 | Vertex Pharma | Compostos de pirazol úteis como inibidores de proteìna cinase |
WO2003026649A1 (fr) * | 2001-09-27 | 2003-04-03 | Applied Research Systems Ars Holding N.V. | Methodes pouvant augmenter des concentrations en testosterone endogene |
US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
MXPA04007832A (es) | 2002-02-11 | 2005-09-08 | Bayer Pharmaceuticals Corp | Aril-ureas con actividad inhibitoria de angiogenesis. |
JP2006501191A (ja) * | 2002-07-17 | 2006-01-12 | ファルマシア・イタリア・エス・ピー・エー | キナーゼ阻害剤としてのヘテロ二環式ピラゾール誘導体 |
BR0315158A (pt) | 2002-10-09 | 2005-08-16 | Pfizer Prod Inc | Compostos de pirazol para o tratamento de distúrbios neurodegenarativos |
AU2003301302A1 (en) * | 2002-10-15 | 2004-05-04 | Smithkline Beecham Corporation | Pyradazine compounds as gsk-3 inhibitors |
ATE410415T1 (de) * | 2003-02-27 | 2008-10-15 | Smithkline Beecham Corp | Neue verbindungen |
CA2526617C (fr) | 2003-05-20 | 2015-04-28 | Bayer Pharmaceuticals Corporation | Diaryl-urees presentant une activite d'inhibition des kinases |
JP4220548B2 (ja) * | 2003-06-05 | 2009-02-04 | エラン ファーマシューティカルズ,インコーポレイテッド | アシル化されたアミノ酸・アミジルピラゾール、および関連化合物 |
PL1651612T3 (pl) * | 2003-07-22 | 2012-09-28 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
UA84156C2 (ru) | 2003-07-23 | 2008-09-25 | Байер Фармасьютикалс Корпорейшн | Фторозамещённая омега-карбоксиарилдифенилмочевина для лечения и профилактики болезней и состояний |
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US7244757B2 (en) * | 2004-04-01 | 2007-07-17 | Pfizer Inc | Pyrazole-amine compounds for the treatment of neurodegenerative disorders |
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EP1751139B1 (fr) | 2004-04-30 | 2011-07-27 | Bayer HealthCare LLC | Derives de pyrazolyl uree substitues utiles dans le traitement du cancer |
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NZ599866A (en) | 2009-11-06 | 2014-09-26 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
US9266855B2 (en) | 2010-09-27 | 2016-02-23 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
MA34948B1 (fr) | 2011-02-07 | 2014-03-01 | Plexxikon Inc | Composes et procedes de modulation de kinase, et leurs indications |
TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
JP6545681B2 (ja) | 2013-08-16 | 2019-07-17 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 3−置換シクロペンチルアミン誘導体 |
CN106580986B (zh) * | 2016-11-28 | 2017-09-15 | 王保亮 | 一种治疗少弱精子症的药物组合物 |
MX2021007925A (es) | 2018-12-31 | 2021-10-26 | Biomea Fusion Llc | Inhibidores irreversibles de la interaccion menina-mll. |
EP3906029A4 (fr) | 2018-12-31 | 2022-09-21 | Biomea Fusion, LLC | Inhibiteurs de l'interaction ménine-mll |
JP7094456B2 (ja) * | 2019-01-31 | 2022-07-01 | ファイザー・インク | Cdk2阻害剤 |
TW202229268A (zh) * | 2020-12-22 | 2022-08-01 | 大陸商上海拓界生物醫藥科技有限公司 | Cdk2抑制劑及其製備方法 |
UY39832A (es) | 2021-06-28 | 2023-01-31 | Blueprint Medicines Corp | Inhibidores de cdk2 |
TW202317564A (zh) * | 2021-07-01 | 2023-05-01 | 大陸商上海拓界生物醫藥科技有限公司 | Cdk2抑制劑及其製備方法和用途 |
TW202325280A (zh) * | 2021-11-09 | 2023-07-01 | 大陸商上海拓界生物醫藥科技有限公司 | 一種胺基吡唑衍生物及其製備方法和用途 |
WO2023092088A1 (fr) * | 2021-11-19 | 2023-05-25 | Blueprint Medicines Corporation | Inhibiteurs de cdk2 et leurs procédés de fabrication et d'utilisation |
WO2023239629A1 (fr) * | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Composés et compositions pharmaceutiques qui dégradent cdk2 |
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Publication number | Priority date | Publication date | Assignee | Title |
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NZ505844A (en) * | 1997-12-22 | 2003-10-31 | Bayer Ag | Inhibition of raf kinase using substituted heterocyclic ureas |
KR100579792B1 (ko) * | 1998-05-13 | 2006-05-12 | 동화약품공업주식회사 | 신규 2,5-피리딘디카복실산 유도체 |
GB9811427D0 (en) * | 1998-05-29 | 1998-07-22 | Zeneca Ltd | Chemical compounds |
AU6314900A (en) * | 1999-07-26 | 2001-02-13 | Banyu Pharmaceutical Co., Ltd. | Biarylurea derivatives |
US6387900B1 (en) * | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
BR0013143A (pt) * | 1999-08-12 | 2002-06-11 | Pharmacia Italia Spa | Derivados de 3 (5) amino pirazol, processo para sua preparação e uso dos mesmos como agentes antitumorais |
CZ20021703A3 (cs) * | 1999-11-30 | 2003-06-18 | Pfizer Products Inc. | 2,4-Diaminopyrimidinové sloučeniny užitečné jako imunosupresiva |
EP1274706A1 (fr) * | 2000-04-18 | 2003-01-15 | Agouron Pharmaceuticals, Inc. | Pyrazoles permettant d'inhiber des proteines kinases |
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2001
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- 2001-08-24 WO PCT/IB2001/001540 patent/WO2002018346A1/fr not_active Application Discontinuation
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- 2001-08-24 EP EP01958287A patent/EP1313710A1/fr not_active Withdrawn
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