PE20081169A1 - Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp - Google Patents

Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp

Info

Publication number
PE20081169A1
PE20081169A1 PE2007001561A PE2007001561A PE20081169A1 PE 20081169 A1 PE20081169 A1 PE 20081169A1 PE 2007001561 A PE2007001561 A PE 2007001561A PE 2007001561 A PE2007001561 A PE 2007001561A PE 20081169 A1 PE20081169 A1 PE 20081169A1
Authority
PE
Peru
Prior art keywords
alkyl
optionally substituted
fluorobutil
dimethylpropyl
difluorophenyl
Prior art date
Application number
PE2007001561A
Other languages
English (en)
Inventor
Yi Xia
Kris G Mendenhall
Paul A Bersanti
Annette O Walter
David Duhl
Paul A Renhowe
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20081169A1 publication Critical patent/PE20081169A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRAZOL Y TRIAZOL DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO; R2 ES H O ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO; R3 ES L1-A1, EN DONDE L1 ES -C(O)-, -C(S)-, -S(O)- O -S(O)2-; A1 ES ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO, ALCOXI(C1-C6) OPCIONALMENTE SUSTITUIDO, ARILO(C6-C14), ENTRE OTROS; R4 ES H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO, ALQUENILO(C2-C6), ENTRE OTROS; X ES CR5 O N, EN DONDE R5 ES H, HALO O ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO; R6 ES CICLOALQUILO(C3-C10), ARILO(C6-C14), HETEROARILO, ENTRE OTROS; R7 ES -L2-A2, EN DONDE L2 ES ALQUILENO(C1-C5) Y A2 ES ARILO(C6-C14), HETEROARILO, CICLOALQUILO(C3-C10), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-((S)-3-AMINO-4-FLUOROBUTIL)-N-((R)-1-(1-BENCIL-3-(2,5-DIFLUOROFENIL)-1H-1,2,4-TRIAZOL-5-IL)-2,2-DIMETILPROPIL)NICOTINAMIDA, N-((S)-3-AMINO-4-FLUOROBUTIL)-N-((R)-1-(1-BENCIL-3-(2,5-DIFLUOROFENIL)-1H-1,2,4-TRIAZOL-5-IL)-2,2-DIMETILPROPIL)MORFOLINO-4-CARBOXAMIDA, N-((S)-3-AMINO-4-FLUOROBUTIL)-N-((R)-1-(1-BENCIL-3-(2,5-DIFLUOROFENIL)-1H-1,2,4-TRIAZOL-5-IL)-2,2-DIMETILPROPIL)-2-METOXIACETAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA KINESINA DEL HUSO (KSP) SIENDO UTILES EN EL TRATAMIENTO DE CANCER, HIPERPLASIAS, RESTENOSIS
PE2007001561A 2006-11-13 2007-11-13 Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp PE20081169A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US85896406P 2006-11-13 2006-11-13

Publications (1)

Publication Number Publication Date
PE20081169A1 true PE20081169A1 (es) 2008-09-24

Family

ID=39144618

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001561A PE20081169A1 (es) 2006-11-13 2007-11-13 Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp

Country Status (32)

Country Link
US (2) US8129358B2 (es)
EP (1) EP2091926B1 (es)
JP (1) JP5264755B2 (es)
KR (1) KR20090081020A (es)
CN (1) CN101558049B (es)
AR (1) AR063805A1 (es)
AU (1) AU2007323998B2 (es)
BR (1) BRPI0719002A2 (es)
CA (1) CA2668661A1 (es)
CL (1) CL2007003272A1 (es)
CO (1) CO6382171A2 (es)
CR (1) CR10787A (es)
DO (1) DOP2009000106A (es)
EA (1) EA017748B1 (es)
EC (1) ECSP099326A (es)
ES (1) ES2557478T3 (es)
GE (1) GEP20125389B (es)
GT (1) GT200900122A (es)
HN (1) HN2009000968A (es)
IL (1) IL198471A0 (es)
MA (1) MA30959B1 (es)
MX (1) MX2009005071A (es)
NI (1) NI200900084A (es)
NO (1) NO20092226L (es)
NZ (1) NZ576640A (es)
PE (1) PE20081169A1 (es)
SM (1) SMP200900045B (es)
TN (1) TN2009000178A1 (es)
TW (1) TW200831480A (es)
UA (1) UA97256C2 (es)
WO (1) WO2008063912A1 (es)
ZA (1) ZA200902940B (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2091926B1 (en) * 2006-11-13 2015-10-21 Novartis AG Substituted pyrazole and triazole compounds as ksp inhibitors
JP2010515687A (ja) * 2007-01-05 2010-05-13 ノバルティス アーゲー キネシンスピンドルタンパク質阻害剤（ｅｇ−５）としてのイミダゾール誘導体
CA2794406A1 (en) * 2010-04-15 2011-10-20 Novartis Ag Triazole compounds as ksp inhibitors
JP2013525290A (ja) * 2010-04-15 2013-06-20 ノバルティス アーゲー Ｋｓｐ阻害剤としてのオキサゾールおよびチアゾール化合物
WO2014089140A1 (en) * 2012-12-05 2014-06-12 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
CN105451773A (zh) * 2013-03-15 2016-03-30 诺华股份有限公司 细胞增殖抑制剂及其缀合物
US9498540B2 (en) 2013-03-15 2016-11-22 Novartis Ag Cell proliferation inhibitors and conjugates thereof
KR101803671B1 (ko) 2013-12-04 2017-11-30 머크 샤프 앤드 돔 코포레이션 역전사효소 억제제의 제조 방법
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
US20190161499A1 (en) * 2015-12-11 2019-05-30 Syngenta Participations Ag Pesticidally active 1,2,4-triazole derivatives
CA3166630A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4235871A (en) * 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) * 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5023252A (en) * 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4837028A (en) * 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US5011472A (en) * 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
US5185450A (en) * 1991-02-19 1993-02-09 University Of South Florida Tetrazolium compounds for cell viability assays
AUPP042397A0 (en) * 1997-11-18 1997-12-11 Fujisawa Pharmaceutical Co., Ltd. 5-arylpyrazole compounds
EP1165519A1 (en) 1999-04-02 2002-01-02 Neurogen Corporation Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics
US6545004B1 (en) * 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
MXPA02004162A (es) 1999-10-27 2003-08-20 Cytokinetics Inc Metodo y composiciones que utilizan quinazolinonas.
KR20030060904A (ko) 2000-10-06 2003-07-16 뉴로젠 코포레이션 Ｃｒｆ 수용체 조절자로서 벤즈이미다졸 및 인돌 유도체
US6992082B2 (en) 2001-01-19 2006-01-31 Cytokinetics, Inc. Phenothiazine kinesin inhibitors
US20040132830A1 (en) 2001-01-19 2004-07-08 Finer Jeffrey T Triphenylmethane kinesin inhibitors
AU2002363429B2 (en) 2001-11-07 2008-05-08 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1450816A4 (en) 2001-11-08 2008-02-13 Univ Chicago METHOD FOR TREATING DISORDER IN CONNECTION WITH INCREASED CHOLESTERITE CONCENTRATION
AU2002346471A1 (en) 2001-11-20 2003-06-10 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
WO2003050122A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1458726B1 (en) 2001-12-06 2009-07-15 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003049678A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003049679A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
US7378411B2 (en) 2001-12-06 2008-05-27 Merck & Co., Inc. Substituted thienopyrimidinones as a mitotic kinesin inhibitor
JP2005516004A (ja) * 2001-12-07 2005-06-02 ヴァージニア コモンウェルス ユニバーシティ 新形成の治療
JP2005526709A (ja) 2002-01-10 2005-09-08 ニューロジェン・コーポレーション メラニン凝集ホルモン受容体リガンド：置換ベンゾイミダゾールアナログ
AU2003213092A1 (en) 2002-02-15 2003-09-09 Smithkline Beecham Corporation Syntheses of quinazolinones
AU2003249597B2 (en) 2002-03-08 2007-06-28 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
US7214800B2 (en) 2002-05-09 2007-05-08 Cytokinetics, Inc. Compounds, compositions, and methods
RU2004135554A (ru) 2002-05-09 2006-01-20 Цитокинетикс, Инк. (Us) Пиримидиноны, композиции на их основе и способы их использования
AU2003290507A1 (en) 2002-05-10 2004-04-08 Cytokinetics, Inc. Compounds, compositions and methods
AU2003265242A1 (en) 2002-05-23 2003-12-22 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003231799A1 (en) 2002-05-23 2003-12-12 Merck & Co., Inc. Mitotic kinesin inhibitors
ES2282647T3 (es) 2002-06-14 2007-10-16 MERCK & CO., INC. Inhibidores de cinesina mitotica.
ATE446094T1 (de) 2002-06-14 2009-11-15 Merck & Co Inc Mitotische kinesin-hemmer
GB0214139D0 (en) * 2002-06-19 2002-07-31 Glaxo Group Ltd Chemical compounds
CA2489562A1 (en) 2002-07-08 2004-01-15 Merck & Co., Inc. Mitotic kinesin binding site
ATE423110T1 (de) 2002-07-17 2009-03-15 Cytokinetics Inc Verbindungen, zusammensetzungen und verfahren zur behandlung von zellulären proliferativen erkrankungen
WO2004009036A2 (en) 2002-07-23 2004-01-29 Cytokinetics, Inc. Compounds compositions and methods
JP2005536553A (ja) 2002-08-21 2005-12-02 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
EP1554265A4 (en) 2002-09-13 2008-05-07 Cytokinetics Inc COMPOSITIONS, COMPOSITIONS AND M THODES
WO2004100873A2 (en) 2003-05-07 2004-11-25 Cytokinetics, Inc. Compounds, compositions, and methods
EP1622878A4 (en) 2003-05-15 2008-04-09 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
JP4895220B2 (ja) * 2004-04-06 2012-03-14 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド キネシン有糸分裂インヒビター
DE602005008953D1 (de) * 2004-05-21 2008-09-25 Novartis Vaccines & Diagnostic Substituierte chinolinderivate als inhibitoren von mitotischem kinesin
KR101170925B1 (ko) * 2004-06-18 2012-08-07 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 암 치료용 키네신 방추 단백질 (ｋｓｐ) 억제제로서의ｎ-(1-(1-벤질-4-페닐-1ｈ-이미다졸-2-일)-2,2-디메틸프로필)벤자미드 유도체 및 관련 화합물
CN101233115A (zh) * 2004-10-19 2008-07-30 诺华疫苗和诊断公司 吲哚和苯并咪唑衍生物
US7829589B2 (en) * 2005-06-10 2010-11-09 Elixir Pharmaceuticals, Inc. Sulfonamide compounds and uses thereof
TW200800951A (en) * 2005-08-09 2008-01-01 Novartis Ag Substituted imidazole compounds as KSP inhibitors
EP2091926B1 (en) * 2006-11-13 2015-10-21 Novartis AG Substituted pyrazole and triazole compounds as ksp inhibitors

Also Published As

Publication number Publication date
NI200900084A (es) 2010-01-29
CL2007003272A1 (es) 2008-03-24
US8129358B2 (en) 2012-03-06
CN101558049B (zh) 2012-08-15
UA97256C2 (ru) 2012-01-25
CA2668661A1 (en) 2008-05-29
EP2091926B1 (en) 2015-10-21
GT200900122A (es) 2011-09-14
EA017748B1 (ru) 2013-02-28
CN101558049A (zh) 2009-10-14
ECSP099326A (es) 2009-06-30
EA200900631A1 (ru) 2009-12-30
US20100034813A1 (en) 2010-02-11
NZ576640A (en) 2011-10-28
US7902240B2 (en) 2011-03-08
KR20090081020A (ko) 2009-07-27
ZA200902940B (en) 2010-05-26
SMAP200900045A (it) 2009-07-14
BRPI0719002A2 (pt) 2013-12-17
ES2557478T3 (es) 2016-01-26
MX2009005071A (es) 2009-05-25
EP2091926A1 (en) 2009-08-26
WO2008063912A1 (en) 2008-05-29
AU2007323998A1 (en) 2008-05-29
CO6382171A2 (es) 2012-02-15
DOP2009000106A (es) 2009-05-31
JP2010509365A (ja) 2010-03-25
IL198471A0 (en) 2010-02-17
TW200831480A (en) 2008-08-01
CR10787A (es) 2009-07-02
NO20092226L (no) 2009-08-12
JP5264755B2 (ja) 2013-08-14
GEP20125389B (en) 2012-01-25
HN2009000968A (es) 2011-10-25
US20080200462A1 (en) 2008-08-21
TN2009000178A1 (en) 2010-10-18
AR063805A1 (es) 2009-02-18
MA30959B1 (fr) 2009-12-01
SMP200900045B (it) 2010-03-01
AU2007323998B2 (en) 2011-09-22

Similar Documents

Publication Publication Date Title
PE20081169A1 (es) Compuestos tipo pirazol y triazol sustituidos como inhibidores de ksp
PE20110367A1 (es) DERIVADOS DE 4-CIANO-4-FENIL-PIRROLIDIN-2-CARBOXAMIDAS SUSTITUIDAS COMO INHIBIDORES DE LA INTERACCION p53-MDM2
PE20090895A1 (es) Derivados de triazol como inhibidores de la jak quinasa
PE20091573A1 (es) Derivados heterociclicos de urea como inhibidores de adn girasa y/o topoisomerasa
TW200716531A (en) Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia
PE20090816A1 (es) Derivados de pirrolopirimidinona como agentes ligandos de los receptores p2x3
MX2007007428A (es) Compuestos heterociclicos, antagonistas de ccr2b.
NO20071719L (no) Pyridylinhibitorer for "hedgehog"-signalisering
PE20090773A1 (es) Derivados de morfolina pirimidina
PE20141681A1 (es) Inhibidores de btk
CY1106679T1 (el) Αζαδικυκλικες ετεροκυκλικες ενωσεις ως τροποποιητες κανναβινοειδους υποδοχεα
NO20083207L (no) Inhibitorer av IAP
PE20070352A1 (es) Compuestos de imidazol sustituidos como inhibidores de ksp
CR8744A (es) Compuestos terapeuticos
TW200740775A (en) Macrocylic inhibitors of hepatitis C virus
GEP20125456B (en) Azetidines as mek inhibitors for the treatment of proliferative diseases
PE20091201A1 (es) AMIDAS SUSTITUIDAS COMO INHIBIDORES DE LA TIROSINA QUINASA DE BRUTON (Btk)
NO20060664L (no) N-substituerte benzimidazolyl C-kit inhibitorer
NO20060665L (no) N-substituerte pyrazolyl-amidyl-benzimidazolyl C-kit inhibitorer
AR047076A1 (es) Compuestos de pirrolotriazina como inhibidores de tirosina quinasas, composiciones farmaceuticas
DK1888063T3 (da) Antimykotiske midler
TW200526658A (en) Heterocyclic inhibitors of MEK and methods of use thereof
PE20110062A1 (es) N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
GEP20074148B (en) Pyrrolo-triazine aniline compounds useful as kinase inhibitors
PE20090601A1 (es) Derivados de piridin-il-oxi-piridinas como inhibidores de alk5

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed