CO5290256A1 - Derivados pirazol triciclicos - Google Patents

Derivados pirazol triciclicos

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Publication number
CO5290256A1
CO5290256A1 CO01039467A CO01039467A CO5290256A1 CO 5290256 A1 CO5290256 A1 CO 5290256A1 CO 01039467 A CO01039467 A CO 01039467A CO 01039467 A CO01039467 A CO 01039467A CO 5290256 A1 CO5290256 A1 CO 5290256A1
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Colombia
Prior art keywords
optionally substituted
group
formula
phenyl
heterocycloalkyl
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CO01039467A
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English (en)
Inventor
Kevin J Doyle
Paul Rafferty
Robert W Steele
David J Wilkins
D Arnold Lee
Michael Hockley
Anna M Ericsson
Iwasaki Nobuhiko
Ogawa Nobuo
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Knoll Gmbh
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Publication of CO5290256A1 publication Critical patent/CO5290256A1/es

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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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Abstract

Un compuesto caracterizado por que está representado por la fórmula:<EMI FILE="01039467_1" ID="1" IMF=JPEG >las mezclas racémicas, las mezclas racémico-diastereoméricas, tautómeros e isómeros ópticos de compuestos y las sales farmacéuticamente aceptables y las prodrogas de los mismos, en donde:m es un entero de 1 a 10;X representa a) un grupo opcionalmente sustituido de la fórmula -(CH2))n- en donde n es 1, 2 ó 3, b) carbonilo, c) oxígeno, d) un grupo de la fórmula -C=NOR10, en donde R10 es un grupo alquilo C1-4, e) un grupo de la fórmula NR11 én donde R11 es -H, un grupo alquilo C1-4 opcionalmente sustituido, o un fenilo opcionalmente sustituido, o f) un grupo de fórmula S(O)p en donde p es de valor 0, 1 ó 2;B representa un alquilo, un cicloalquilo, un arilo, un piridilo, un tienilo, un furilo o un pirrolilo; R1 es -H; un halo; hidroxilo; nitro; ciano; hidroxiamidino; aminometilo; formamidometilo; un alqueniloxilo opcionalmente sustituido; un alquenilo C2-4, opcionalmente sustituido; un alquinilo C2-4 opcionalmente sustituido; o un grupo representado por la fórmula -Y-W; con la condición que cuando R1 es - H, un alquilo C1-6 sin sustituir, un alcoxilo C1-6 sin sustituir, un halógeno, o trifluorometilo, el anillo A se sustituye con por lo menos un sustituyente que no es un halo, un alquilo C1-6 opcionalmente sustituido o un alcoxilo C1-6 opcionalmente sustituido;Y no está o es un alquilo C1-6, alcoxilo C1-6, -o-, -S- ó -C(O)-;W es -H, hidroxilo, fenilo opcionalmente sustituido, alcoxilo C1-6, o -NR2R3;con la condición que cuando el B es fenilo y R1 es -Y-W y W es -NR2R3, R2 y R3 son cada uno, independientemente, a) -H; b) un grupo alquilo C1-6 sustituido, con la condición que el sustituyente no es -NR6R7; - 2 -c) un cicloalquilo opcionalmente sustituido; d) un heterocicloalquilo opcionalmente sustituido; e) un cicloalquilalquilo opcionalmente sustituidos; f) un heterocicloalquilalquilo opcionalmente sustituido; g) un heteroarilo sustituido o un heteroaralquilo sustituido, con la condición que el heteroarilo o heteroaralquilo se sustituye con -NR9(CH2)1-6OR4, -NR9(CH2)1-6CO2R4, -NR9(CH2)1-6NR4R5, o un heterocicloalquilo opcionalmente sustituido; ocuando B es fenilo y R1, es -Y-W y W es -NR2R3, R2 y R3, junto con el átomo de nitrógeno a cual éstos están unidos, puede representar un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; cuando el B no es fenilo, R2 y R3, son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, -NH(CH2)1-6NR4R5, un cicloalquilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un heterocicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, o un heteroaralquilo opcionalmente sustituido; ocuando el B no es fenilo, R2 y R3, junto con el átomo de nitrógeno a cual los mismos están unidos representa un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido;R4, R5 y R9 son en cada caso, independientemente, -H o un alquilo C1-6 ; y el anillo A se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste de a) un halo; b) un grupo alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de el hidroxilo, halo, y NR6R7; c) un grupo alcoxilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionado del grupo que consiste de hidroxilo, halo, -NR6R7, un fenilo opcionalmente sustituido, y -NR17C(O)R19, con la condición que los sustituyentes no están unidos al carbono a que se une el oxígeno del grupo alcoxilo; d) un fenoxilo opcionalmente sustituido; e) hidroxilo; f) un grupo de la fórmula -C(O)R12 en donde R12 es un hidroxilo, un alcoxilo C1-6 o -NR13R14; g) un grupo de la fórmula NR17R18; h) un grupo de la fórmula -NR17C(O)R19; i) nitro; j) aralquilo opcionalmente sustituido; k) ciano; y l) un grupo alquenilo C2-4 o un grupo alquinilo C2-4 cada uno de los cuales es opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste de un grupo alquilo C1-6, un grupo alcoxilo C1-6 y un halo;R6 y R7, son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; oR6 y R7 junto con el átomo de nitrógeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R13, y R14 son cada uno, independientemente, -H, un grupo alquilo C1-6 opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituidos, un heteroarilo opcionalmente sustituido, un heterocicloalquilo opcionalmente sustituido, un cicloalquilalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, un heteroaralquilo opcionalmente sustituido, o un heterocicloalquilalquilo opcionalmente sustituido; oR13, y R14 junto con el átomo de nitrógeno al cual éstos están unidos representan un heterocicloalquilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido;R17 y R18 son cada uno, independientemente, seleccionado del grupo que consiste de -H, un grupo alquilo C1-2, un grupo cicloalquilo C3-12, y fenilo; yR19 es -H, un grupo alquilo C1-12 opcionalmente sustituido, un grupo cicloalquilo C3-12 opcionalmente sustituidos, un fenilo opcionalmente sustituido o un aralquilo opcionalmente sustituido.Teniendo en cuenta que B es un arilo, piridilo, tienilo, furilo o pirrolilo, entonces el anillo A es substituido con al menos un substituyente seleccionado del grupo que consiste de un grupo C1-6 alquil el cual es substituido con -NR6´R7´ un alcoxi C1-6 el cual es substituido con un grupo de fórmula -NR17C(O)R19 o un fenilo opcionalmente substituido, y un grupo de fórmula: - 3 -C (O) NR13' R14.R0' y R7 son cada uno independientes-H un cicloalquilo opcionalmente substituido un arilo opcionalmente substituido un heteroarilo opcionalmente substituido, un heterocicloalquilo opcionalmente substituido un cicloalquilalquilo opcionalmente substituido, un aralquilo opcionalmente substituido y un heteroaralquilo opcionalmente substituido un heterocicloalquilalquilo teniendo en cuenta que al menos uno de R9' o R7' no es H y queR13' y R14' son cada uno independientes de H, un cicloalquilo opcionalmente substituido, un naftilo opcionalmente substituido, un heteroarilo opcionalmente substituido, un heterocicloalquilo opcionalmente substituido, un cicloalquilalquilo opcionalmente substituido, un aralquilo opcionalmente substituido, un heteroaralquilo opcionalmente substituido, un heterocicloalquilalquilo opcionalmente substituido teniendo en cuenta que R13' o R14' no es H.
CO01039467A 2000-05-17 2001-05-17 Derivados pirazol triciclicos CO5290256A1 (es)

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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6297238B1 (en) * 1999-04-06 2001-10-02 Basf Aktiengesellschaft Therapeutic agents
GB0128160D0 (en) * 2001-11-23 2002-01-16 Merck Sharp & Dohme Novel compounds
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
EP1467730A4 (en) * 2002-01-22 2010-03-10 Univ California Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof
TWI264304B (en) * 2002-01-25 2006-10-21 Yung Shin Pharm Ind Co Ltd Methods of treating sepsis
US20040127492A1 (en) * 2002-02-19 2004-07-01 Pharmacia Corporation Cyclic pyrazoles for the inhibition of mitogen activated protein kinase-activated protein kinase-2
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
US20040254159A1 (en) * 2003-02-27 2004-12-16 Hasvold Lisa A. Heterocyclic kinase inhibitors
US7456169B2 (en) 2003-02-27 2008-11-25 Abbott Laboratories Inc. Heterocyclic kinase inhibitors
US7320986B2 (en) * 2003-03-07 2008-01-22 Abbott Labortories Fused tri and tetra-cyclic pyrazole kinase inhibitors
MXPA05009576A (es) * 2003-03-07 2005-12-12 Abbott Lab Inhibidores de pirazol-quinasa triciclicos y tetraciclicos, fundidos.
US8013156B2 (en) 2003-03-19 2011-09-06 Exelixis, Inc. Tie-2 modulators and methods of use
MY144339A (en) * 2003-09-08 2011-08-29 Aventis Pharma Inc Thienopyrazoles
US7037927B2 (en) * 2003-10-16 2006-05-02 Abbott Laboratories Amides that inhibit vanilloid receptor subtype 1 (VR1) receptor
MXPA06010904A (es) * 2004-03-24 2007-06-11 Abbott Lab Inhibidores de pirazol cinasa triciclicos.
US7378532B2 (en) * 2004-03-26 2008-05-27 Yung Shin Pharmaceutical Ind. Co., Ltd. Fused pyrazolyl compound
US7767657B2 (en) 2005-02-16 2010-08-03 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
CA2597982C (en) 2005-02-16 2014-07-08 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
JP2009506077A (ja) * 2005-08-26 2009-02-12 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 非ステロイド性抗アンドロゲン剤
ES2390135T3 (es) 2005-11-22 2012-11-06 Merck Sharp & Dohme Corp. Compuestos tricíclicos útiles como inhibidores de quinasas
SI2719388T1 (sl) 2006-02-16 2019-06-28 Anacor Pharmaceuticals, Inc. Majhne molekule, polnjene z borom, kot učinkovine proti vnetjem
CA2651732C (en) * 2006-05-18 2014-10-14 Mannkind Corporation Intracellular kinase inhibitors
MX2010009765A (es) 2008-03-06 2013-07-12 Anacor Pharmaceuticals Inc Moleculas pequeñas que contienen boro como agentes anti-inflamatorios.
EP2348863A4 (en) 2008-09-04 2012-03-07 Anacor Pharmaceuticals Inc BORN SMALL MOLECULES
WO2010028005A1 (en) 2008-09-04 2010-03-11 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
EP2395835A4 (en) * 2009-02-10 2013-04-17 Abbott Lab S1P5 RECEPTOR AGONISTS AND ANTAGONISTS, AND METHODS OF USE
AP4039A (en) 2009-08-14 2017-02-28 Daitao Chen Boron-containing small molecules as antiprotozoal agents
US8076395B2 (en) * 2009-09-11 2011-12-13 Air Products And Chemicals, Inc. Low temperature curable epoxy compositions containing urea curatives
WO2011049971A1 (en) 2009-10-20 2011-04-28 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as antiprotozoal agents
CN102686571B (zh) 2009-10-29 2015-11-25 百时美施贵宝公司 三环杂环化合物
TW201118073A (en) * 2009-10-30 2011-06-01 Merck Sharp & Dohme Hexahydrocyclopentyl [F] indazole pyridyl ethanols and derivatives thereof as selective glucocorticoid receptor modulators
US20110212918A1 (en) 2009-11-11 2011-09-01 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
WO2011094450A1 (en) 2010-01-27 2011-08-04 Anacor Pharmaceuticals, Inc Boron-containing small molecules
AP2012006482A0 (en) 2010-03-19 2012-10-31 Anacor Pharmacueticals Inc Boron-containing small molecules as anti-protozoalagent
JP5952280B2 (ja) 2010-09-07 2016-07-13 アナコール ファーマシューティカルズ，インコーポレーテッド 細菌感染治療用のベンゾオキサボロール誘導体
CN102603719B (zh) * 2011-01-25 2015-12-16 北京贵千金医药科技有限公司 化合物2-糠醇-(5’→11)-1,3-环戊二烯并[5,4-c]-1H-噌啉及其作为抗氧化剂在食品、化妆品或药品中的应用
US8853207B2 (en) 2012-04-12 2014-10-07 Development Center For Biotechnology Heterocyclic pyrazole compounds, method for preparing the same and use thereof
EP2909212B1 (en) 2012-09-07 2017-02-22 Takeda Pharmaceutical Company Limited Substituted 1,4-dihydropyrazolo[4,3-b]indoles
JP2016529234A (ja) * 2013-07-15 2016-09-23 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ 殺有害生物化合物
KR101712708B1 (ko) * 2014-10-08 2017-03-07 영남대학교 산학협력단 인데노 피리디니움 유도체 화합물을 유효성분으로 포함하는 염증성장질환 예방 또는 치료용 조성물
EP3623371A1 (en) 2014-12-16 2020-03-18 Axovant Sciences GmbH Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors
WO2016113261A1 (en) * 2015-01-13 2016-07-21 Basf Se Fused tricyclic compounds, compositions comprising these compounds and their use for con-trolling invertebrate pests
RU2017145964A (ru) 2015-06-10 2019-07-10 Аксовант Сайенсиз Гмбх Аминобензизоксазольные соединения в качестве агонистов α7-никотиновых ацетилхолиновых рецепторов
EP3334740A4 (en) 2015-08-12 2019-02-06 Axovant Sciences GmbH GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF ALPHA 7-NICOTINIC ACETYLCHOLINE RECEPTORS
EP3507278B1 (en) 2016-09-02 2021-01-27 Bristol-Myers Squibb Company Substituted tricyclic heterocyclic compounds
WO2019032631A1 (en) 2017-08-09 2019-02-14 Bristol-Myers Squibb Company OXIME ETHER COMPOUNDS
US11046646B2 (en) 2017-08-09 2021-06-29 Bristol-Myers Squibb Company Alkylphenyl compounds
JP2023533070A (ja) * 2020-07-08 2023-08-01 ユニヴェルシテ デクス－マルセイユ オーロン誘導体、並びに細菌及び／又は真菌を制御するためのそれらの使用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE789948A (fr) * 1971-10-13 1973-04-11 Sandoz Sa Nouveaux derives du pyrazole, leur preparation et leur application comme medicaments
US3957816A (en) * 1973-01-31 1976-05-18 Sandoz, Inc. Substituted naphtho pyrazoles
US3843664A (en) * 1973-02-20 1974-10-22 Sandoz Ag Substituted naphtho pyrazoles
US3959308A (en) * 1973-02-20 1976-05-25 Sandoz, Inc. Substituted naphtho pyrazoles
US3843665A (en) * 1973-04-11 1974-10-22 Sandoz Ag Process for preparing substituted indeno,naphtho and cyclohepta pyrazoles
US3843666A (en) * 1973-05-29 1974-10-22 Sandoz Ag Process for preparing substituted indeno,naphtho and cyclohepta pyrazoles
JPS60130521A (ja) 1983-12-19 1985-07-12 Morishita Seiyaku Kk 抗癌剤
US5670522A (en) * 1992-10-23 1997-09-23 Merck Sharp & Dohme Limited Dopamine receptor subtype ligands
GB9318691D0 (en) 1993-09-09 1993-10-27 Merck Sharp & Dohme Therapeutic agents
AU706262B2 (en) 1995-10-23 1999-06-10 Osteoscreen, Inc. Compositions and methods for treating bone deficit conditions
EP1021182A1 (en) 1997-10-06 2000-07-26 Basf Aktiengesellschaft Indeno[1,2-c] pyrazole derivatives for inhibiting tyrosine kinase activity
AU9691198A (en) 1997-10-06 1999-04-27 Basf Aktiengesellschaft Indeno{1,2-c}-, naphtho{1,2-c}- and benzo{6,7}cyclohepta{1,2-c}pyrazole derivatives
JP4665239B2 (ja) 1998-04-21 2011-04-06 アゲンニクス アーゲー 抗癌剤および抗増殖性薬剤としての５−アミノインデノ［１，２−ｃ］ピラゾール−４−オン
KR20010086005A (ko) 1998-11-06 2001-09-07 스타르크, 카르크 트리사이클릭 피라졸 유도체
SK14112001A3 (sk) 1999-04-06 2002-04-04 Knoll Gmbh Substituované 1,4-dihydroindeno [1,2-c] pyrazoly ako inhibítory tyrozínkinázy

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EP1289525A2 (en) 2003-03-12
AU2001263272A1 (en) 2001-11-26
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