BR112013005141A2 - diazetidinil diamida como inibidores de monoacilglicerol lipase - Google Patents
diazetidinil diamida como inibidores de monoacilglicerol lipaseInfo
- Publication number
- BR112013005141A2 BR112013005141A2 BR112013005141A BR112013005141A BR112013005141A2 BR 112013005141 A2 BR112013005141 A2 BR 112013005141A2 BR 112013005141 A BR112013005141 A BR 112013005141A BR 112013005141 A BR112013005141 A BR 112013005141A BR 112013005141 A2 BR112013005141 A2 BR 112013005141A2
- Authority
- BR
- Brazil
- Prior art keywords
- diamide
- lipase inhibitors
- diazetidinyl
- monoacylglycerol lipase
- compounds
- Prior art date
Links
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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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
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- 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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- 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
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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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- 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
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
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- 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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- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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- Urology & Nephrology (AREA)
- Pulmonology (AREA)
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Abstract
di-azetidinil diamidea como inibidores de monoacilglicerol lipase. a presente invenção refere-se a compostos, composições e métodos para o tratamento de várias doenças , síndromes, condições e distúrbios incluindo dor. tais compostos são representados pela fórmula (i) a seguir: fórmula (i) em que q e z são aqui definidos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US37976410P | 2010-09-03 | 2010-09-03 | |
PCT/US2011/049885 WO2012030907A1 (en) | 2010-09-03 | 2011-08-31 | Di-azetidinyl diamide as monoacylglycerol lipase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112013005141A2 true BR112013005141A2 (pt) | 2016-05-10 |
Family
ID=44645814
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112013005141A BR112013005141A2 (pt) | 2010-09-03 | 2011-08-31 | diazetidinil diamida como inibidores de monoacilglicerol lipase |
Country Status (12)
Country | Link |
---|---|
US (3) | US20120058986A1 (pt) |
EP (1) | EP2611774B1 (pt) |
JP (1) | JP2013536852A (pt) |
KR (1) | KR20130101040A (pt) |
CN (1) | CN103068798A (pt) |
AR (1) | AR082891A1 (pt) |
AU (1) | AU2011296068B2 (pt) |
BR (1) | BR112013005141A2 (pt) |
CA (1) | CA2809991A1 (pt) |
RU (1) | RU2013114771A (pt) |
TW (1) | TW201305132A (pt) |
WO (1) | WO2012030907A1 (pt) |
Families Citing this family (40)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR112013005141A2 (pt) | 2010-09-03 | 2016-05-10 | Janssen Pharmaceutica Nv | diazetidinil diamida como inibidores de monoacilglicerol lipase |
UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
US9624170B2 (en) | 2013-12-26 | 2017-04-18 | 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 |
US10076517B2 (en) | 2014-09-22 | 2018-09-18 | Inserm (Institut National De La Santé Et De Ka Recherche Médicale | Methods and pharmaceutical compositions for the treatment of fibrosis |
US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
WO2016049565A1 (en) * | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
US10106556B2 (en) | 2015-03-30 | 2018-10-23 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
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 |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
US10730867B2 (en) | 2015-09-28 | 2020-08-04 | 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 |
US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
JP2018533939A (ja) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Rasの阻害剤をスクリーニングするための方法 |
MX2018005967A (es) | 2015-11-16 | 2018-08-29 | Araxes Pharma Llc | Compuestos de quinazolina 2-sustituida que comprenden un grupo heterociclico sustituido y metodos de uso de los mismos. |
US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
WO2017143283A1 (en) | 2016-02-19 | 2017-08-24 | Abide Therapeutics, Inc. | Radiolabeled monoacylglycerol lipase occupancy probe |
WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
US10610520B2 (en) | 2016-03-31 | 2020-04-07 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
WO2017171100A1 (en) | 2016-03-31 | 2017-10-05 | 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 |
JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Kras g12c変異体タンパク質の阻害剤 |
CN110312711A (zh) | 2016-10-07 | 2019-10-08 | 亚瑞克西斯制药公司 | 作为ras抑制剂的杂环化合物及其使用方法 |
US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic 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 |
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 |
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 |
US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
TW201900633A (zh) | 2017-05-25 | 2019-01-01 | 美商亞瑞克西斯製藥公司 | Kras之共價抑制劑 |
JP7189143B2 (ja) | 2017-09-29 | 2022-12-13 | 武田薬品工業株式会社 | 複素環化合物 |
CA3107168A1 (en) | 2018-08-01 | 2020-02-06 | Araxes Pharma Llc | Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer |
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WO1998037077A1 (en) | 1997-02-24 | 1998-08-27 | Zymogenetics, Inc. | Calcitonin mimetics |
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AU3565999A (en) | 1999-04-16 | 2000-11-02 | Coelacanth Chemical Corporation | Synthesis of azetidine derivatives |
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 |
US6995144B2 (en) | 2002-03-14 | 2006-02-07 | Eisai Co., Ltd. | Nitrogen containing heterocyclic compounds and medicines containing the same |
WO2004002531A1 (ja) | 2002-06-26 | 2004-01-08 | Ono Pharmaceutical Co., Ltd. | 血管の収縮または拡張による疾患治療剤 |
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EP1702916A1 (en) | 2005-03-18 | 2006-09-20 | Santhera Pharmaceuticals (Schweiz) GmbH | DPP-IV inhibitors |
CN101384553A (zh) | 2005-12-21 | 2009-03-11 | 先灵公司 | 可用作组胺h3拮抗剂的取代的苯胺衍生物 |
TW200813018A (en) * | 2006-06-09 | 2008-03-16 | Astrazeneca Ab | Novel compounds |
FR2915199B1 (fr) | 2007-04-18 | 2010-01-22 | Sanofi Aventis | Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique. |
FR2915197B1 (fr) * | 2007-04-18 | 2009-06-12 | Sanofi Aventis Sa | Derives de triazolopyridine-carboxamides, leur preparation et leur application therapeutique. |
JP5715945B2 (ja) * | 2008-04-25 | 2015-05-13 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | モノアシルグリセロールリパーゼ(mgll)の結晶構造 |
EP2180048B1 (en) | 2008-10-09 | 2014-12-17 | Janssen Pharmaceutica N.V. | Alternative crystal form of monoacylglycerol lipase (MGLL) |
JP2012524802A (ja) | 2009-04-22 | 2012-10-18 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | モノアシルグリセロールリパーゼ阻害剤としてのアゼチジニルジアミド |
US8435977B2 (en) | 2009-04-22 | 2013-05-07 | Janssen Pharmaceutica, Nv | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors |
KR20120014154A (ko) * | 2009-04-22 | 2012-02-16 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파제 억제제로서의 헤테로방향족 및 방향족 피페라지닐 아제티디닐 아미드 |
BR112013005141A2 (pt) | 2010-09-03 | 2016-05-10 | Janssen Pharmaceutica Nv | diazetidinil diamida como inibidores de monoacilglicerol lipase |
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- 2011-08-31 CA CA2809991A patent/CA2809991A1/en not_active Abandoned
- 2011-08-31 WO PCT/US2011/049885 patent/WO2012030907A1/en active Application Filing
- 2011-08-31 CN CN2011800423208A patent/CN103068798A/zh active Pending
- 2011-08-31 KR KR1020137007955A patent/KR20130101040A/ko not_active Application Discontinuation
- 2011-08-31 RU RU2013114771/04A patent/RU2013114771A/ru not_active Application Discontinuation
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- 2011-08-31 JP JP2013527247A patent/JP2013536852A/ja active Pending
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CN103068798A (zh) | 2013-04-24 |
US8759533B2 (en) | 2014-06-24 |
RU2013114771A (ru) | 2014-10-10 |
AU2011296068B2 (en) | 2015-07-09 |
US8759333B2 (en) | 2014-06-24 |
AU2011296068A1 (en) | 2013-03-14 |
US20120058986A1 (en) | 2012-03-08 |
US20130196969A1 (en) | 2013-08-01 |
JP2013536852A (ja) | 2013-09-26 |
CA2809991A1 (en) | 2012-03-08 |
TW201305132A (zh) | 2013-02-01 |
EP2611774A1 (en) | 2013-07-10 |
WO2012030907A1 (en) | 2012-03-08 |
US20130196968A1 (en) | 2013-08-01 |
EP2611774B1 (en) | 2015-03-18 |
KR20130101040A (ko) | 2013-09-12 |
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