CO5200848A1 - Derivados de 3(5)-ureido-pirazol, proceso para su prepa- racion y su utilizacion como agentes antitumorales - Google Patents
Derivados de 3(5)-ureido-pirazol, proceso para su prepa- racion y su utilizacion como agentes antitumoralesInfo
- Publication number
- CO5200848A1 CO5200848A1 CO00059913A CO00059913A CO5200848A1 CO 5200848 A1 CO5200848 A1 CO 5200848A1 CO 00059913 A CO00059913 A CO 00059913A CO 00059913 A CO00059913 A CO 00059913A CO 5200848 A1 CO5200848 A1 CO 5200848A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- cycloalkyl
- amino
- aminoalkyl
- aryl
- 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
- C07D231/40—Acylated on said nitrogen atom
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
Un derivado de 3-ureido-pirazol representado por la Fórmula (I): <EMI FILE="00059913_1" ID="1" IMF=JPEG >dondeR es un grupo alquilo C1-C6 arilo o arilalquilo, opcionalmente sustituido con uno o más sustituyentes hidroxi, halógeno, nitro, ciano, oxo, carboxi, amino, alquilamino, dialquilamino, alquilcarbonilamino, alcoxicarbonilamino, alcoxicarbonilalquilamino, aminocarbonilalquilamino, N-alquil-N-carbonilamino, N-cicloalquil-N-alquilaminoalquilo, aminoalquilo, aminocarbonilo, alquilo, cicloalquilo, alquiltio, alcoxi, alquilcarbonilo, alquilsulfonilo, alquilsulfonilamino, aminosulfonilo, alcoxicarbonilo, arilo, arilalquilo, ariloxi, ariltio, arilsulfonilo, arilamino, arilcarbonilo, N-alquil-piperazinilo, 4-morfolinilo, alquilo perfluorado C1-C4, alquenilo C2-C4, alquinilo C2-C4, aminoalquinilo C2-C4 o hidroxialquinilo C2-C4; R1 es -(CH2)n-R3;n es 0 o un entero entre 1 y 4;R3 es hidrógeno, hidroxi, amino, o se selecciona dentro del grupo consistente en cicloalquilo, arilo y heterociclilo, opcionalmente sustituido por uno o más sustituyentes hidroxi, halógeno, nitro, ciano, oxo, carboxi, amino, alquilamino, diaIquilamino, alquiI carboniIamino, alcoxicarbonilamino, alcoxicarbonilalquilamino, aminocarbonilalquilamino, N-alquil-N-carbonilamino, N- cicloalquil-alquilaminoalquilo, aminoalquilo, aminocarbonilo, alquilo, cicloalquilo, alquiltio, alcoxi, alquilcarbonilo, alquilsulfonilo, alquilsulfonilamino, aminosulfonilo, alcoxicarbonilo, arilo, arilalquilo, ariloxi, ariltio, arilsulfonilo, arilamino, arilcarbonilo, N-alquil-piperacinilo, 4-morfolinilo, alquilo(C1-C4 perfluorado, alquenilo C2-C4, alquinilo C2-C4, aminoalquilino C2-C4 o hidroxialquinilo C2-C4; R2 es hidrógeno, oR2 y R1, junto con el átomo de nitrógeno al que están ligados, forman un grupo heterociclilo o heteroarilo, opcionalmente sustituido con uno o más sustituyentes hidroxi, halógeno, nitro, ciano, oxo, carboxi, amino, alquilamino, dialquilamino, alquilcarbonilamino, alcoxicarbonilamino, alcoxicarbonilalquilamino, aminocarbonilalquilamino, N-alquil-N-carbonilamino, N-cicloalquil-N-alquilaminoalquilo, aminoalquilo, aminocarbonilo, alquilo, cicloalquilo, alquiltio, alcoxi, alquilcarbonilo, alquilsulfonilo, alquilsulfonilamino, aminosulfonilo, alcoxicarbonilo, arilo, arilalquilo, ariloxi, ariltio, arilsulfonilo, arilamino, arilcarbonilo, N-alquil-piperacinilo, 4-morfolinilo, alquilo C1-C4 perfluorado, alquenilo C2-C4, alquinilo C2-C4, aminoalquinilo C2-C4 o hidroxialquinilo C2-C4;o sales farmacéuticamente aceptables de los mismos;siempre que cuando n es 0 y R2 es hidrógeno, R es un grupo cicloalquilo C3-C6 opcionalmente sustituido por un grupo alquilo C1-C6 recto o ramificado.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US09/372,833 US6387900B1 (en) | 1999-08-12 | 1999-08-12 | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
Publications (1)
Publication Number | Publication Date |
---|---|
CO5200848A1 true CO5200848A1 (es) | 2002-09-27 |
Family
ID=23469810
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO00059913A CO5200848A1 (es) | 1999-08-12 | 2000-08-10 | Derivados de 3(5)-ureido-pirazol, proceso para su prepa- racion y su utilizacion como agentes antitumorales |
Country Status (25)
Country | Link |
---|---|
US (1) | US6387900B1 (es) |
EP (1) | EP1202734B1 (es) |
JP (1) | JP2003507328A (es) |
KR (1) | KR20020060158A (es) |
CN (1) | CN1379668A (es) |
AR (1) | AR035557A1 (es) |
AT (1) | ATE361070T1 (es) |
AU (1) | AU6747000A (es) |
BR (1) | BR0013277A (es) |
CA (1) | CA2380786A1 (es) |
CO (1) | CO5200848A1 (es) |
DE (1) | DE60034683T2 (es) |
EA (1) | EA200200249A1 (es) |
ES (1) | ES2284518T3 (es) |
HK (1) | HK1049790A1 (es) |
HU (1) | HUP0301857A2 (es) |
IL (1) | IL147925A0 (es) |
MX (1) | MXPA02001497A (es) |
NO (1) | NO20020687L (es) |
NZ (1) | NZ517238A (es) |
PE (1) | PE20010482A1 (es) |
PL (1) | PL354058A1 (es) |
SK (1) | SK2082002A3 (es) |
WO (1) | WO2001012188A1 (es) |
ZA (1) | ZA200201118B (es) |
Families Citing this family (75)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20070244120A1 (en) * | 2000-08-18 | 2007-10-18 | Jacques Dumas | Inhibition of raf kinase using substituted heterocyclic ureas |
CA2359244C (en) | 1999-01-13 | 2013-10-08 | Bayer Corporation | .omega.-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors |
US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
CN1615873A (zh) | 1999-12-24 | 2005-05-18 | 阿文蒂斯药物有限公司 | 氮杂吲哚类化合物 |
DK1268472T3 (da) | 2000-02-07 | 2004-12-06 | Bristol Myers Squibb Co | 3-aminopyrazolinhibitorer af cyclinafhængige kinaser |
EP1278749B1 (en) | 2000-04-25 | 2005-01-26 | Bristol-Myers Squibb Company | USE OF 5-THIO-, SULFINYL- AND SULFONYLPYRAZOLO 3,4-b]-PYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS |
OA12368A (en) * | 2000-08-31 | 2004-04-13 | Pfizer Prod Inc | Pyrazole derivatives and their use as protein kinase inhibitors. |
JP2004517840A (ja) * | 2000-11-27 | 2004-06-17 | フアルマシア・イタリア・エツセ・ピー・アー | フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用 |
GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
ATE345130T1 (de) * | 2001-12-03 | 2006-12-15 | Bayer Pharmaceuticals Corp | Arylharnstoff-verbindungen in kombination mit anderen zytostatisch oder zytotoxisch wirksamen stoffen zur behandlungen menschlicher krebserkrankungen |
US20050113283A1 (en) * | 2002-01-18 | 2005-05-26 | David Solow-Cordero | Methods of treating conditions associated with an EDG-4 receptor |
JP4636486B2 (ja) | 2002-02-11 | 2011-02-23 | バイエル、ファーマシューテイカルズ、コーポレイション | 脈管形成阻害活性を有するアリール尿素 |
KR20030071029A (ko) * | 2002-02-27 | 2003-09-03 | 주식회사 팜제니아 | 항암제 및 방사선 치료 증진제로서 유용한 조성물 |
US20030225089A1 (en) * | 2002-04-10 | 2003-12-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors |
DE10221052A1 (de) * | 2002-05-10 | 2003-12-04 | Transmit Technologietransfer | Wirkstoffe zu Therapie, Diagnostik und Prophylaxe von Erkrankungen, bei denen abnorme Proteinstrukturen auftreten |
CA2486101C (en) * | 2002-05-17 | 2009-07-07 | Pharmacia Italia S.P.A. | Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
ATE548354T1 (de) | 2002-07-24 | 2012-03-15 | Ptc Therapeutics Inc | Ureido-substituierte benzoesäureverbindungen und ihre verwendung für die nonsense-suppression und behandlung von erkrankungen |
CA2495284A1 (en) * | 2002-09-05 | 2004-03-18 | Neurosearch A/S | Diarylurea derivatives and their use as chloride channel blockers |
CA2501799C (en) * | 2002-10-09 | 2008-06-17 | Pfizer Products Inc. | Pyrazole compounds for treatment of neurodegenerative disorders |
UA81790C2 (uk) | 2002-12-19 | 2008-02-11 | Фармация Италия С.П.А. | Заміщені піролопіразольні похідні як інгібітори кінази |
UY28213A1 (es) | 2003-02-28 | 2004-09-30 | Bayer Pharmaceuticals Corp | Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos. |
GB0305426D0 (en) * | 2003-03-08 | 2003-04-16 | Glaxo Group Ltd | Novel compounds |
ATE366108T1 (de) | 2003-05-20 | 2007-07-15 | Bayer Pharmaceuticals Corp | Diaryl-harnstoffe für durch pdgfr vermittelte krankheiten |
ME00142B (me) | 2003-05-22 | 2010-10-10 | Nerviano Medical Sciences Srl | Derivati pirazolo-hinazolina, postupci za njihovo dobijanje i njihova upotreba kao inhibitora kinaze |
US7141568B2 (en) | 2003-07-09 | 2006-11-28 | Pfizer Italia S.R.L. | Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
PL1663978T3 (pl) | 2003-07-23 | 2008-04-30 | Bayer Healthcare Llc | Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów |
TW200526204A (en) | 2004-02-03 | 2005-08-16 | Pharmacia Italia Spa | 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors |
US7244757B2 (en) * | 2004-04-01 | 2007-07-17 | Pfizer Inc | Pyrazole-amine compounds for the treatment of neurodegenerative disorders |
EP1609789A1 (en) * | 2004-06-23 | 2005-12-28 | Eli Lilly And Company | Ureido-pyrazole derivatives and their use as kinase inhibitors |
PL1778686T3 (pl) * | 2004-08-12 | 2009-04-30 | Pfizer | Pochodne triazolopirydynylosulfanylowe jako inhibitory kinazy MAP P38 |
LT2937341T (lt) | 2004-12-30 | 2017-09-11 | Janssen Pharmaceutica N.V. | 4-(benzil)-piperazin-1-karboksilinės rūgšties fenilamido dariniai ir giminingi junginiai kaip riebalų rūgščių amido hidrolazės (rrah) moduliatoriai, skirti nerimo, skausmo ir kitų būklių gydymui |
US20060183758A1 (en) * | 2005-02-17 | 2006-08-17 | Cb Research And Development, Inc. | Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans |
US7429800B2 (en) * | 2005-06-30 | 2008-09-30 | Sabic Innovative Plastics Ip B.V. | Molding composition and method, and molded article |
WO2007009898A1 (en) | 2005-07-19 | 2007-01-25 | Nerviano Medical Sciences S.R.L. | 1h-thieno[2,3-c]pyrazole compounds useful as kinase inhibitors |
AR059826A1 (es) * | 2006-03-13 | 2008-04-30 | Univ California | Inhibidores de urea conformacionalmente restringidos de epoxido hidrolasa soluble |
JP2009535388A (ja) * | 2006-05-03 | 2009-10-01 | アストラゼネカ アクチボラグ | ピラゾール誘導体、及びそのpi3k阻害薬としての使用 |
ES2445791T3 (es) * | 2006-10-21 | 2014-03-05 | Abbvie Deutschland Gmbh & Co Kg | Compuestos hetererocíclicos y su uso como inhibidores de la glucógeno sintasa cinasa 3 |
CL2008000119A1 (es) | 2007-01-16 | 2008-05-16 | Wyeth Corp | Compuestos derivados de pirazol, antagonistas del receptor nicotinico de acetilcolina; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como demencia senil, alzheimer y esquizofrenia. |
US9512082B2 (en) | 2007-04-18 | 2016-12-06 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
US20090062294A1 (en) * | 2007-05-25 | 2009-03-05 | Richard Apodaca | Heteroaryl-substituted urea modulators of fatty acid amide hydrolase |
EP2163541A1 (en) * | 2008-09-12 | 2010-03-17 | Bayer Schering Pharma Aktiengesellschaft | Piperazine derivatives for binding and imaging amyloid plaques and their use |
CA2738909A1 (en) * | 2008-10-01 | 2010-05-06 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against ionizing radiation using selective cyclin-dependent kinase 4/6 inhibitors |
US8461159B2 (en) * | 2008-11-25 | 2013-06-11 | Jannsen Pharmaceutica BV | Heteroaryl-substituted urea modulators of fatty acid amide hydrolase |
WO2010068452A1 (en) * | 2008-11-25 | 2010-06-17 | Janssen Pharmaceutica Nv | Heteroaryl-substituted urea modulators of fatty acid amide hydrolase |
EP3406260B1 (en) | 2009-05-13 | 2020-09-23 | The University of North Carolina at Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
WO2010141817A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
US8901111B2 (en) | 2009-06-05 | 2014-12-02 | Janssen Pharmaceutica Nv | Aryl-substituted heterocyclic urea modulators of fatty acid amide hydrolase |
EP2528604B1 (en) | 2010-01-29 | 2017-11-22 | The Regents of the University of California | Acyl piperidine inhibitors of soluble epoxide hydrolase |
UA108233C2 (uk) | 2010-05-03 | 2015-04-10 | Модулятори активності гідролази амідів жирних кислот | |
US20130109019A1 (en) * | 2010-07-02 | 2013-05-02 | Adrian E. Murillo | Hapten conjugates for target detection |
BR112013003815A2 (pt) * | 2010-08-20 | 2019-09-24 | Gruenenthal Chemie | derivados de carboxamida cílicos substituódos e derivados de ureia como ligantes do receptor vaniloide |
JP5998142B2 (ja) | 2010-09-27 | 2016-09-28 | アボット ゲーエムベーハー ウント カンパニー カーゲー | 複素環化合物およびグリコーゲンシンターゼキナーゼ−3阻害薬としてのその使用 |
WO2012068381A2 (en) | 2010-11-17 | 2012-05-24 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from schema through inhibition of the proliferative kisses cdk4 and cdk6 |
RU2652638C2 (ru) | 2010-12-17 | 2018-04-28 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Замещенные пиразолхиназолиновые производные в качестве ингибиторов киназы |
US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
CN103649076B (zh) | 2011-05-13 | 2015-09-09 | 阵列生物制药公司 | 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物 |
AR087701A1 (es) * | 2011-08-31 | 2014-04-09 | Japan Tobacco Inc | Derivados de pirazol con actividad inhibidora de sglt1 |
WO2014078331A1 (en) * | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
SG11201503728XA (en) | 2012-11-13 | 2015-06-29 | Array Biopharma Inc | N-pyrrolidinyl, n'-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
AU2013344886B2 (en) | 2012-11-13 | 2017-06-29 | Array Biopharma Inc. | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain |
WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
US9546156B2 (en) | 2012-11-13 | 2017-01-17 | Array Biopharma Inc. | N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors |
US9828360B2 (en) | 2012-11-13 | 2017-11-28 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
PT2968290T (pt) | 2013-03-15 | 2019-11-27 | G1 Therapeutics Inc | Protecção transitória de células normais durante a quimioterapia |
CN105407723A (zh) | 2013-03-15 | 2016-03-16 | G1治疗公司 | 高效的抗赘生剂和抗增生剂 |
WO2015161287A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use in the protection of normal cells during chemotherapy |
NZ727418A (en) | 2014-05-15 | 2023-03-31 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor |
EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
WO2022135442A1 (zh) * | 2020-12-22 | 2022-06-30 | 上海拓界生物医药科技有限公司 | Cdk2抑制剂及其制备方法 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3754887A (en) * | 1969-05-05 | 1973-08-28 | Du Pont | Ureidopyrazoles defoliants |
US3646059A (en) * | 1969-05-05 | 1972-02-29 | Du Pont | Plant growth regulatory ureidopyrazoles |
DE69532817T2 (de) | 1994-11-10 | 2005-01-13 | Millenium Pharmaceuticals, Inc., Cambridge | Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose |
CA2273102A1 (en) * | 1996-12-03 | 1998-06-11 | Banyu Pharmaceutical Co., Ltd. | Urea derivatives |
JP2002502380A (ja) | 1997-05-22 | 2002-01-22 | ジー.ディー.サール アンド カンパニー | p38キナーゼ阻害剤としてのピラゾール誘導体 |
IL136738A0 (en) | 1997-12-22 | 2001-06-14 | Bayer Ag | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
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1999
- 1999-08-12 US US09/372,833 patent/US6387900B1/en not_active Expired - Fee Related
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2000
- 2000-08-03 PE PE2000000771A patent/PE20010482A1/es not_active Application Discontinuation
- 2000-08-10 CO CO00059913A patent/CO5200848A1/es not_active Application Discontinuation
- 2000-08-10 AR ARP000104118A patent/AR035557A1/es unknown
- 2000-08-11 AT AT00955241T patent/ATE361070T1/de not_active IP Right Cessation
- 2000-08-11 EP EP00955241A patent/EP1202734B1/en not_active Expired - Lifetime
- 2000-08-11 CN CN00812736A patent/CN1379668A/zh active Pending
- 2000-08-11 PL PL00354058A patent/PL354058A1/xx not_active Application Discontinuation
- 2000-08-11 ES ES00955241T patent/ES2284518T3/es not_active Expired - Lifetime
- 2000-08-11 KR KR1020027001815A patent/KR20020060158A/ko not_active Application Discontinuation
- 2000-08-11 WO PCT/US2000/017878 patent/WO2001012188A1/en active IP Right Grant
- 2000-08-11 HU HU0301857A patent/HUP0301857A2/hu unknown
- 2000-08-11 IL IL14792500A patent/IL147925A0/xx unknown
- 2000-08-11 AU AU67470/00A patent/AU6747000A/en not_active Abandoned
- 2000-08-11 MX MXPA02001497A patent/MXPA02001497A/es active IP Right Grant
- 2000-08-11 JP JP2001516534A patent/JP2003507328A/ja not_active Withdrawn
- 2000-08-11 SK SK208-2002A patent/SK2082002A3/sk unknown
- 2000-08-11 NZ NZ517238A patent/NZ517238A/en unknown
- 2000-08-11 DE DE60034683T patent/DE60034683T2/de not_active Expired - Fee Related
- 2000-08-11 CA CA002380786A patent/CA2380786A1/en not_active Abandoned
- 2000-08-11 EA EA200200249A patent/EA200200249A1/ru unknown
- 2000-08-11 BR BR0013277-2A patent/BR0013277A/pt not_active Application Discontinuation
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HUP0301857A2 (hu) | 2003-09-29 |
AR035557A1 (es) | 2004-06-16 |
MXPA02001497A (es) | 2003-07-21 |
CN1379668A (zh) | 2002-11-13 |
CA2380786A1 (en) | 2001-02-22 |
EP1202734B1 (en) | 2007-05-02 |
PE20010482A1 (es) | 2001-04-20 |
AU6747000A (en) | 2001-03-13 |
BR0013277A (pt) | 2002-06-18 |
HK1049790A1 (zh) | 2003-05-30 |
ATE361070T1 (de) | 2007-05-15 |
NO20020687L (no) | 2002-04-03 |
KR20020060158A (ko) | 2002-07-16 |
NO20020687D0 (no) | 2002-02-11 |
WO2001012188A1 (en) | 2001-02-22 |
SK2082002A3 (en) | 2002-09-10 |
IL147925A0 (en) | 2002-08-14 |
PL354058A1 (en) | 2003-12-15 |
EA200200249A1 (ru) | 2002-08-29 |
NZ517238A (en) | 2004-01-30 |
US6387900B1 (en) | 2002-05-14 |
ES2284518T3 (es) | 2007-11-16 |
JP2003507328A (ja) | 2003-02-25 |
EP1202734A1 (en) | 2002-05-08 |
DE60034683T2 (de) | 2008-01-17 |
DE60034683D1 (de) | 2007-06-14 |
EP1202734A4 (en) | 2004-09-01 |
ZA200201118B (en) | 2003-05-28 |
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