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AR076378A1 - Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor. - Google Patents

Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.

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Publication number
AR076378A1
AR076378A1 ARP100101339A ARP100101339A AR076378A1 AR 076378 A1 AR076378 A1 AR 076378A1 AR P100101339 A ARP100101339 A AR P100101339A AR P100101339 A ARP100101339 A AR P100101339A AR 076378 A1 AR076378 A1 AR 076378A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
compound
aryl
phenyl
Prior art date
Application number
ARP100101339A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR076378A1 publication Critical patent/AR076378A1/es

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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicacion 1: Un compuesto de Formula (1) en la cual Y y Z son independientemente seleccionados entre a) y b) de tal manera que uno de Y y Z sea seleccionado del grupo a) y el otro sea seleccionado del grupo b); El Grupo a) es: i) arilo C6-10 sustituido, ii) cicloalquilo C3-8 opcionalmente sustituido con uno a dos sustituyentes fluor, iii) trifluorometilo o iv) heteroarilo seleccionado del grupo que consiste en tienilo, furanilo, tiazolilo, isotiazolilo, oxazolilo, pirrolilo, pirimidinilo, isoxazolilo, benzotienilo, tieno[3,2-b]tiofen-2-ilo, pirazolilo, triazolilo, tetrazolilo y [1,2,3]tiadiazolilo; donde arilo C6-10 está sustituido con; y el heteroarilo está opcionalmente sustituido con; un sustituyente seleccionado del grupo que consiste en fluor, cloro, bromo, alquilo C1-4, alcoxi C1-4, ciano, alquilcarbonilamino C1-4 y trifluorometilo; El Grupo b) es i) arilo C6-10 ii) heteroarilo seleccionado del grupo que consiste en tiazolilo, piridinilo, indolilo, indazolilo, benzoxazolilo, benzotiazolilo, benzofuranilo, benzotienilo, 1H-pirrolo[3,2-b]piridin-5-ilo, 1H-tieno[2,3-c]pirazol-5-ilo, 1H-pirrolo[2,3-b]piridin-5-ilo, 1H-pirazolo[3,4-b]piridin-5-ilo, furo[2,3-b]piridin-2-ilo, quinolinilo, quinazolinilo, furanilo, [1,2,3]triazolilo, tienilo, oxazolilo, [1,3,4]oxadiazol-2-ilo, pirrolilo, pirazolilo y bencimidazolilo; iii) 2,3-dihidro-1H-indolilo; iv) 2,3 difenil-indolilo; v) difenil-imidazolilo; vi) 1-(2,4-diclorofenil)-4,5,6,7-tetrahidro-1H-indazol-3-ilo; vii) 3-(4-clorofenil)-4,5,6,7-tetrahidro-indazol-2-ilo; viii) 1-(4-fluorofenil)-1H-pirrolo[3,2-b]piridin-6-ilo o ix) difenil-1H-pirazol-3-ilo: donde cada fenilo esta opcionalmente sustituido con uno a dos sustituyentes cloro y donde dicho pirazolilo esta opcionalmente sustituido con un sustituyente metilo; donde arilo C6-10, 2,3-dihidro-1H-indolilo y heteroarilo del Grupo b) están opcional e independientemente sustituidos con uno a dos sustituyentes seleccionados del grupo que consiste en bromo, cloro, fluor, yodo, alquilo C1-4, alcoxi C1-4 y trifluorometilo; y están sustituidos con un sustituyente adicional seleccionado del grupo que consiste en i) arilo C6-10 ii) heteroarilo seleccionado del grupo que consiste en pirimidinilo tienilo, quinolinilo piridinilo, isoxazolilo, tiazolilo, bencimidazolilo, pirrolilo, furanilo, pirimidinilo y pirazolilo; o iii) 5,6-dihidro-4H-ciclopentapirazol-2-ilo donde dicho heteroarilo y 5,6-dihidro-4H-ciclopentapirazol-2-ilo están opcionalmente sustituidos con un sustituyente fenilo, dicho fenilo está opcionalmente sustituido con uno a dos sustituyentes cloro o trifluorometilo; y donde el fenilo del arilo C6-10 y heteroarilo está opcional e independientemente sustituido con uno a dos sustituyentes seleccionados del grupo que consiste en alcoxicarbonilamino C1-4 alquilo C1-4 cianometilo; alcoxi C1-4 uno a tres sustituyentes fluor o cloro; trifluorometilo; trifluorometoxi; trifluorometiltio; alquilcarbonilo C1-4; alcoxicarbonilo C1-4; alcoxicarbonil(C1-4)alquenilo C2-4; cianoalquenilo C2-4; (2-ciano)etilaminocarbonilo; ciano; carboxi; aminocárbonilo; alquilaminocarbonilo C1-4 di(alquil C1-4)aminocarbonilo; formilo; nitro; bromo; hidroxi; di(alquil C1-4)aminosulfonilo; alquilsulfonilo C1-4; di(alquil C1-4)aminosulfonilo; morfolin-4-ilsulfonilo; -OCH2O- acoplado en átomos de carbono adyacentes y NRcRd; donde Rc es hidrogeno o alquilo C1-6 y donde Rd es hidrogeno, alquilo C1-6, cianoalquilo C1-4, cicloalquilo C3-8, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, cicloalquilcarbonilo C3-8, cicloalquil(C3-8)alquilo C1-4, aminocarbonilo, di(alquil C1-4)aminocarbonilo, arilcarbonilo C6-10; di(alquil C1-4)aminosulfonilo y alquilsulfonilo C1-4; s es 0, 1 o 2; siempre que, cuando s es 2, R1 sea independientemente seleccionado del grupo que consiste en fenilo, alquilo C1-3 y aril(C6-10)alquilo C1-3 R1 es arilo C6-10, alquilo C1-3, benciloximetilo, hidroxialquilo C1-3, aminocarbonilo, carboxi, trifluorometilo, ciclopropilo espirofusionado, 3-oxo o arilalquilo C1-3 o, cuando s es 2 y R1 es, los sustituyentes alquilo C1-3 se toman con el anillo de piperazinilo para formar un sistema de anillos de 3,8-diaza-biciclo[3.2.1]octanil o 2,5-diaza-biciclo[2.2.2]]octanilo; y con la condicion de que un compuesto de la formula (1) no sea un compuesto en el cual Y es 3-clorobenzotien-2-ilo, Z es 4-bifenilo y s es 0; un compuesto en el cual Y es 3-clorotien-2-ilo, Z es 4-bifenilo y s es 0; un compuesto en el cual Y es 2-cianofenilo, Z es 4-bifenilo y s es 0; un compuesto en el cual Y es 5-metil-isoxazol-3-ilo, Z es 4-bifenilo y s es 0; un compuesto en el cual Y es tiazol-2-ilo, Z es 5-(4-clorofenil)oxazol-4-ilo y s es 0; un compuesto en el cual Y es tiazol-2-ilo, Z es 3-fenil-1H-pirazol-4-ilo y s es 0; un compuesto en el cual Y es tiazol-2-ilo, Z es 5-(2-fluoropiridin-3-il)-1H-bencimidazol-2-ilo y s es 0; un compuesto en el cual Y es tiazol-4-ilo, Z es 1-fenil-5-trifluorometil-pirazol-4-ilo y s es 0; un compuesto en el cual Y es pirimidin-2-ilo, Z es 4-bifenilo y s es 0; un compuesto en el cual Y es tiazol-4-ilo, Z es 4-bifenilo, s es 1 y R1 es 3-fenilo; y los enantiomeros, diastereomeros, solvatos y sales farmacéuticamente aceptables del mismo.
ARP100101339A 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor. AR076378A1 (es)

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ARP100101343A AR076382A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.
ARP100101340A AR076379A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc.
ARP100101341A AR076380A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasa(mgl), composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades y patologias que incluyen dolor inflamatorio.
ARP100101335A AR076374A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de lipasas de monoacil glicerol
ARP100101338A AR076377A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
ARP100101339A AR076378A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.

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ARP100101343A AR076382A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.
ARP100101340A AR076379A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc.
ARP100101341A AR076380A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasa(mgl), composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades y patologias que incluyen dolor inflamatorio.
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Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2730506A1 (en) 2008-07-21 2010-01-28 Novartis Ag Silicone-containing polymeric materials with hydrolyzable groups
AR076381A1 (es) * 2009-04-22 2011-06-08 Janssen Pharmaceutica Nv Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
US9082128B2 (en) * 2009-10-19 2015-07-14 Uniloc Luxembourg S.A. System and method for tracking and scoring user activities
US9051296B2 (en) 2009-11-16 2015-06-09 Raqualia Pharma Inc. Aryl carboxamide derivatives as TTX-S blockers
ES2703176T3 (es) 2010-03-11 2019-03-07 Univ New York Compuestos amido como moduladores de RORgammat y usos de los mismos
WO2012030907A1 (en) 2010-09-03 2012-03-08 Janssen Pharmaceutica Nv Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
KR20140001206A (ko) * 2010-09-27 2014-01-06 얀센 파마슈티카 엔.브이. 모노아실글리세롤 리파아제 억제제로서의 옥소피페라진-아제티딘 아미드 및 옥소다이아제핀-아제티딘 아미드
CN102417483A (zh) * 2010-09-27 2012-04-18 中国药科大学 作为parp抑制剂的2-苯基-1h-苯并咪唑-4-甲酸酯衍生物
US8513423B2 (en) 2010-10-22 2013-08-20 Janssen Pharmaceutica, Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
CA2815350A1 (en) * 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
RU2013123274A (ru) 2010-10-22 2014-11-27 Янссен Фармацевтика Нв Аминопирролидиназетидиндиамиды как ингибиторы моноацилглицеринлипазы
RU2598842C2 (ru) * 2011-01-20 2016-09-27 Мерк Шарп Энд Домэ Корп. Антагонисты рецептора минералокортикоидов
US9388164B2 (en) 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
MX2014003883A (es) * 2011-09-30 2014-08-27 Janssen Pharmaceutica Nv Inhibidores de monoacilglicerol lipasa para el tratamiento de enfermedades metabolicas y transtornos relacionados.
CN103957916A (zh) * 2011-09-30 2014-07-30 詹森药业有限公司 用于治疗代谢疾病和相关失调的单酰甘油脂肪酶抑制剂
KR20140072897A (ko) * 2011-09-30 2014-06-13 얀센 파마슈티카 엔.브이. （１－（４－플루오로페닐）－１ｈ－인돌－５－일）－（３－（４－（티아졸－2－카르보닐）피페라진－１－일）아제티딘－１－일）메탄온의 결정성 하이드로클로라이드 염，및 통증 및 대사 장애의 치료에 있어서의 이의 용도
EA028085B1 (ru) 2012-01-06 2017-10-31 Эбайд Терапьютикс, Инк. Карбаматные соединения и их применение
CN102603485A (zh) * 2012-02-07 2012-07-25 北京颖新泰康国际贸易有限公司 制备2-甲基-3-苯基苯甲醇的方法
TWI562295B (en) 2012-07-31 2016-12-11 Mediatek Inc Semiconductor package and method for fabricating base for semiconductor package
WO2014074848A1 (en) 2012-11-08 2014-05-15 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions and their use as pkm2 modulators
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
MX364438B (es) * 2013-03-15 2019-04-26 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
UY35464A (es) * 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
EP2999469A1 (de) 2013-05-23 2016-03-30 Bayer Pharma Aktiengesellschaft Pharmazeutische zusammensetzung und deren verwendung sowie anwendungsregime dieser pharmazeutischen zusammensetzung zur bedarfsweisen ( on-demand") kontrazeption
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
CN105764901B (zh) * 2013-11-12 2018-06-22 豪夫迈·罗氏有限公司 作为用于治疗神经变性疾病的神经源性药的吡啶并[4，3-b]吡嗪-2-甲酰胺
EP3087067B1 (en) 2013-12-26 2018-10-24 Takeda Pharmaceutical Company Limited 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (magl) inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
JP6640840B2 (ja) 2014-09-22 2020-02-05 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 線維症を処置するための方法及び医薬組成物
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
WO2016158956A1 (ja) * 2015-03-30 2016-10-06 武田薬品工業株式会社 複素環化合物
KR20180005178A (ko) 2015-04-10 2018-01-15 아락세스 파마 엘엘씨 치환된 퀴나졸린 화합물 및 이의 사용방법
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法
IL305843B2 (en) 2015-07-20 2025-01-01 Genzyme Corp CSF-1R receptor antibodies
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
TN2017000544A1 (en) 2015-07-31 2019-04-12 Pfizer 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
AU2016355433C1 (en) 2015-11-16 2021-12-16 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
KR102482200B1 (ko) 2016-01-27 2022-12-27 우니페르지타에트 취리히 가려움증 치료를 위한 ｇａｂａａ 수용체 조절인자의 용도
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
EP3436444B1 (en) 2016-03-31 2020-05-13 Takeda Pharmaceutical Company Limited Heterocyclic compound
US10610520B2 (en) 2016-03-31 2020-04-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2018068017A1 (en) 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
JOP20190106A1 (ar) * 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
SG11201906417RA (en) 2017-01-20 2019-08-27 Pfizer 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors
JP2020506903A (ja) 2017-01-23 2020-03-05 ファイザー・インク Ｍａｇｌ阻害薬としての複素環式スピロ化合物
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
SMT202300071T1 (it) 2017-05-23 2023-05-12 H Lundbeck As Inibitori del pirazolo magl
US10927105B1 (en) 2017-05-23 2021-02-23 Lundbeck La Jolla Research Center, Inc. Pyrazole MAGL inhibitors
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
EP3630746A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Compounds and methods of use thereof for treatment of cancer
EP3689879B1 (en) 2017-09-29 2025-02-12 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3765459A1 (en) 2018-03-13 2021-01-20 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
MX2020012158A (es) 2018-05-15 2021-01-29 H Lundbeck As Inhibidores de magl.
AU2019312670B2 (en) 2018-08-01 2025-01-02 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
AU2019338207B2 (en) 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
MX2021002805A (es) 2018-09-10 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
JP2022500388A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
CN109020890B (zh) * 2018-09-12 2022-02-08 南京大学 一类饱和脂肪环骈吡唑衍生物的制备及其应用
CA3118752A1 (en) * 2018-11-09 2020-05-14 Vivace Therapeutics, Inc. Bicyclic compounds
US20220031676A1 (en) * 2018-11-28 2022-02-03 H. Lundbeck A/S Methods of treating disease with magl inhibitors
WO2020118066A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3917911A1 (en) * 2019-01-31 2021-12-08 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
EP3936192B1 (en) 2019-03-06 2025-04-09 Daiichi Sankyo Company, Limited Pyrrolopyrazole derivative
JP7653362B2 (ja) 2019-04-16 2025-03-28 ビバーチェ セラピューティクス，インク． 二環式化合物
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
US11787796B2 (en) 2019-09-18 2023-10-17 Takeda Pharmaceutical Company Limited Plasma Kallikrein inhibitors and uses thereof
JP7695232B2 (ja) 2019-09-18 2025-06-18 武田薬品工業株式会社 ヘテロアリール血漿カリクレインインヒビター
EP4034123A4 (en) 2019-09-24 2023-11-01 Mirati Therapeutics, Inc. COMBINATION THERAPIES
JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ．ベー． 放射線標識されたｍｇｌ ｐｅｔリガンド
JP2023507571A (ja) 2019-12-20 2023-02-24 ミラティ セラピューティクス， インコーポレイテッド Ｓｏｓ１阻害剤
KR20220146458A (ko) * 2020-01-23 2022-11-01 마이오포르테 테라퓨틱스 인코포레이티드 Pgdh 억제제 및 그의 제조 및 사용 방법
EP3875452A1 (en) * 2020-03-04 2021-09-08 Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis Monoacylglycerol lipase inhibitors
JP7729831B2 (ja) * 2020-03-26 2025-08-26 ヤンセン ファーマシューティカ エヌ．ベー． モノアシルグリセロールリパーゼ調節因子としてのアミノシクロブタン
MX2023002942A (es) 2020-09-11 2023-05-22 Mirati Therapeutics Inc Formas cristalinas de un inhibidor de kras g12c.
EP4228650A4 (en) * 2020-10-15 2024-12-18 Myoforte Therapeutics Inc. INHALATED FORMULATIONS OF PGDH INHIBITORS AND METHODS OF USE THEREOF
AU2021401232A1 (en) 2020-12-15 2023-06-22 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
KR102682408B1 (ko) * 2021-05-12 2024-07-05 에이치케이이노엔 주식회사 신규한 벤조티아졸 유도체, 이의 제조방법 및 이의 간질환 예방 또는 치료 용도
EP4377314A4 (en) * 2021-07-28 2025-06-18 Epirium Bio Inc. BICYCLIC PGDH INHIBITORS AND METHODS OF PREPARATION AND USE
WO2023130023A1 (en) 2021-12-29 2023-07-06 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9600235D0 (en) * 1996-01-05 1996-03-06 Pfizer Ltd Therapeutic agents
AU6179998A (en) 1997-02-24 1998-09-09 Zymogenetics Inc. Calcitonin mimetics
AU1089599A (en) 1997-10-15 1999-05-03 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6566356B2 (en) 2000-03-03 2003-05-20 Aventis Pharma S.A. Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation
AR033517A1 (es) 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
FR2829028B1 (fr) 2001-08-29 2004-12-17 Aventis Pharma Sa Association d'un antagoniste du recepteur cb1 et d'un produit qui active la neurotransmission dopaminergique dans le cerveau, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de
AR037364A1 (es) * 2001-11-16 2004-11-03 Schering Corp Azetidinil diaminas utiles como ligandos del receptor de nociceptina orl-1
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
EP1522314B1 (en) 2002-06-26 2014-03-05 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
WO2004056800A1 (en) * 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
FR2854633B1 (fr) * 2003-05-07 2005-06-24 Sanofi Synthelabo Derives de piperidinyl-et piperazinyl-alkylcarbamates, leur preparation et leur application en therapeutique
ES2307025T3 (es) * 2003-06-10 2008-11-16 Janssen Pharmaceutica Nv Combinacion de opioides y un derivado de la piperazina para el tratamiento del dolor.
EP1702916A1 (en) 2005-03-18 2006-09-20 Santhera Pharmaceuticals (Schweiz) GmbH DPP-IV inhibitors
MX2007015606A (es) * 2005-06-23 2008-02-25 Astrazeneca Ab Nuevos derivados de azetidina como antagonistas del receptor de neuroquinina para el tratamiento de enfermedades gastrointestinales.
KR20080080201A (ko) * 2005-12-21 2008-09-02 쉐링 코포레이션 히스타민 ｈ3 길항제로서 유용한 치환된 아닐린 유도체
DE102006016023A1 (de) * 2006-04-05 2007-10-11 Basf Ag Funktionale Expression von Triacylglycerol-Lipasen
TWI403508B (zh) 2006-08-26 2013-08-01 Abbott Gmbh & Co Kg 經取代苯并咪唑酮衍生物、包含其之醫藥品及其用途
FR2915197B1 (fr) * 2007-04-18 2009-06-12 Sanofi Aventis Sa Derives de triazolopyridine-carboxamides, leur preparation et leur application therapeutique.
FR2915198B1 (fr) 2007-04-18 2009-12-18 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique.
FR2915199B1 (fr) * 2007-04-18 2010-01-22 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique.
WO2009117444A1 (en) 2008-03-17 2009-09-24 Northeastern University Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors
WO2009132267A1 (en) 2008-04-25 2009-10-29 Janssen Pharmaceutica Nv Crystal structure of monoacylglycerol lipase (mgll)
EP2180048B1 (en) 2008-10-09 2014-12-17 Janssen Pharmaceutica N.V. Alternative crystal form of monoacylglycerol lipase (MGLL)
US8415341B2 (en) 2009-04-22 2013-04-09 Janssen Pharmaceutica, Nv Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
TWI495637B (zh) 2009-04-22 2015-08-11 Janssen Pharmaceutica Nv 用作單醯基甘油脂肪酶抑制劑之雜芳族及芳族六氫吡基吖丁啶基醯胺（一）
AR076381A1 (es) * 2009-04-22 2011-06-08 Janssen Pharmaceutica Nv Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
DE102012109699A1 (de) 2012-10-11 2014-04-17 Pavel Abdulkin Verfahren zum Bereitstellen einer Gold-Nano-Hülle um kleine, magnetische Partikel im Submikrometerbereich und so erhaltene Partikel

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