AR076666A1 - Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas) - Google Patents
Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas)Info
- Publication number
- AR076666A1 AR076666A1 ARP100101584A ARP100101584A AR076666A1 AR 076666 A1 AR076666 A1 AR 076666A1 AR P100101584 A ARP100101584 A AR P100101584A AR P100101584 A ARP100101584 A AR P100101584A AR 076666 A1 AR076666 A1 AR 076666A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- pyrimidylalkyl
- pyrazinyl
- cycloalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
utiles para tratamiento de diabetes, dislipidemia, aterosclerosis u obesidad. Reivindicacion 1: Compuesto de la formula (1)en la que m es el numero 1 o 2; n es el numero cero, 1 o 2, en el caso de que n sea cero, entonces m es 1; A es -S(O)2- o carbonilo; R1 es alquilo, aminoalquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalquilcicloalquilo, hidroxicicloalquilalquilo, (cicloalquil)(hidroxi)alquilo, (cicloalquil)(alcoxi)alquilo, alcoxicicloalquilalquilo, hidroxicicloalquilo, cicloalcoxialquilo, hidroxialquilo, alcoxialquilo, benciloxialquilo, feniloxialquilo, dihidro-furanilidenometilo, tetrahidro-furanilmetilo, dihidro-isoindolilo, dihidro quinolinilo, -NR4R5, azepanilo, morfolinilo, piperidinilo, pirrolidinilo, pirazolilo, imidazolilo, isoxazolilo, oxazolilo, tiofenilo, tiazolilo, piridinilo, piridinilalquilo, piridazinilo, piridazinilalquilo, pirazinilo, pirazinilalquilo, pirimidilo, pirimidilalquilo, fenilo, fenilalquilo, piperidinilo sustituido, pirrolidinilo sustituido, pirazolilo sustituido, imidazolilo sustituido, isoxazolilo sustituido, oxazolilo sustituido, tiofenilo sustituido, tiazolilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazinilo sustituido, pirazinilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, fenilo sustituido o fenilalquilo sustituido, dichos piperidinilo sustituido, pirrolidinilo sustituido, pirazolilo sustituido, imidazolilo sustituido, isoxazolilo sustituido, oxazolilo sustituido, tiofenilo sustituido, tiazolilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazinilo sustituido, pirazinilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, fenilo sustituido y fenilalquilo sustituido están sustituidos con uno a tres sustituyentes elegidos con independencia entre alquilo, haloalquilo, halogeno, hidroxi, alcoxi, haloalcoxi, feniloxi, alquilfeniloxi, alquilsulfonilo, oxopirrolidinilo, alcoxicarbonilo, benciloxi y -NR6R7; R2 es imidazolilo, imidazolilalquilo, fenilo, fenilalquilo, piridinilo, piridinilalquilo, piridazinilo, piridazinilalquilo, pirazolilo, pirazolilalquilo, alquilindazolilo, alquilbenzotiazolilo, difluorbenzo[1,3}dioxolilo, pirimidilo, pirimidilalquilo, pirazinilo, pirazinilalquilo, imidazolilo sustituido, imidazolilalquilo sustituido, fenilo sustituido, fenilalquilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazolilo sustituido, pirazolilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, pirazinilo sustituido o pirazinilalquilo sustituido, dichos imidazolilo sustituido, imidazolilalquilo sustituido, fenilo sustituido, fenilalquilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazolilo sustituido, pirazolilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, pirazinilo sustituido y pirazinilalquilo sustituido están sustituidos con uno a tres sustituyentes elegidos con independencia entre alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, halogeno, haloalcoxi, alcoxi, hidroxi, alcoxialquilo, hidroxialquilo, alquilsulfonilo, alquilsulfoniloxi, alquilsulfanilo, cicloalquilsulfoniloxi, cicloalcoxi, alquenilo, cicloalquilalcoxi, alcoxialcoxi, tetrahidrofuraniloxi, piridiniloxi, alcoxicarbonilalquilo, cianoalquilo, alquiloxazodiazolilalquilo, haloalquiloxazodiazolilalquilo, alcoxialquenilo, cicloalquilalquenilo, cicloalquilalcoxialquilo, alcoxicarbonilo, alquilcarbonilo, haloalquilhidroxialquilo, alquilaminocarbonilo, dialquilaminocarbonilo, hidroxioxetanilo, fluoroxetanilo e hidroxicicloalquilo; uno de R4 y R5 es hidrogeno o alquilo y el otro es hidrogeno, alquilo, hidroxialquilo, alcoxialquilo, cicloalquilo, fenilo, alquilfenilo, haloalcoxifenilo, fenilalquilo, halofenilo, halofenilalquilo, haloalquilfenilo o piridinilalquilo; uno de R6 y R7 es hidrogeno, alquilo, cicloalquilo o hidroxialquilo y el otro es hidrogeno, alquilo, cicloalquilo o hidroxialquilo; o sus sales farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09160026 | 2009-05-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076666A1 true AR076666A1 (es) | 2011-06-29 |
Family
ID=42269304
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101584A AR076666A1 (es) | 2009-05-12 | 2010-05-10 | Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas) |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8329904B2 (es) |
| EP (1) | EP2430023B1 (es) |
| JP (1) | JP5542916B2 (es) |
| KR (1) | KR101438263B1 (es) |
| CN (1) | CN102421777A (es) |
| AR (1) | AR076666A1 (es) |
| AU (1) | AU2010247472A1 (es) |
| BR (1) | BRPI1015038A2 (es) |
| CA (1) | CA2760340A1 (es) |
| ES (1) | ES2450119T3 (es) |
| IL (1) | IL214352A0 (es) |
| MX (1) | MX2011012017A (es) |
| SG (1) | SG175298A1 (es) |
| TW (1) | TW201043629A (es) |
| WO (1) | WO2010130665A1 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011009059A2 (en) * | 2009-07-17 | 2011-01-20 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Method of treating or preventing cancer |
| US8258158B2 (en) * | 2009-09-11 | 2012-09-04 | Hoffmann-La Roche Inc. | HSL inhibitors useful in the treatment of diabetes |
| US8097634B2 (en) | 2010-04-15 | 2012-01-17 | Hoffmann-La Roche Inc. | Azacyclic derivatives |
| GB201007789D0 (en) * | 2010-05-10 | 2010-06-23 | Glaxo Group Ltd | Novel Compound |
| GB201007791D0 (en) * | 2010-05-10 | 2010-06-23 | Glaxo Group Ltd | Novel compounds |
| US8552024B2 (en) * | 2010-08-13 | 2013-10-08 | Hoffman-La Roche Inc. | Azacyclic compounds |
| US8722721B2 (en) * | 2011-03-16 | 2014-05-13 | Hoffmann-La Roche Inc. | SEC-hydroxycyclohexyl derivatives |
| US8703807B2 (en) * | 2011-03-17 | 2014-04-22 | Hoffmann-La Roche Inc. | Azaspirodecanone compounds |
| US8809384B2 (en) * | 2011-03-25 | 2014-08-19 | Hoffmann-La Roche Inc. | Azaspirodecanone compounds |
| US8497288B2 (en) | 2011-05-09 | 2013-07-30 | Hoffmann-La Roche Inc. | Hexahydropyrroloimidazolone compounds |
| CN105073111A (zh) * | 2012-10-11 | 2015-11-18 | 默沙东公司 | 用作gpr120激动剂的取代的螺哌啶基化合物 |
| HRP20190613T1 (hr) | 2013-01-29 | 2019-06-28 | Aptinyx Inc. | Spiro-laktam modulatori nmda receptora i njihove uporabe |
| CN103408573B (zh) * | 2013-07-12 | 2015-12-23 | 上海工程技术大学 | 硼酸衍生物及其制备方法和应用 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| ES2886766T3 (es) | 2015-03-31 | 2021-12-20 | Enanta Pharm Inc | Derivados del ácido biliar como agonistas de FXR/TGR5 y métodos de uso de estos |
| WO2017189652A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| WO2017201152A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| PE20190503A1 (es) | 2016-08-01 | 2019-04-10 | Aptinyx Inc | Moduladores del receptor nmda espiro-lactam y uso de los mismos |
| BR112019001921A2 (pt) | 2016-08-01 | 2019-05-14 | Aptinyx Inc. | moduladores do receptor nmda de espiro-lactama e seus usos |
| MX388786B (es) | 2016-08-01 | 2025-03-20 | Aptinyx Inc | Moduladores nmda espiro-lactam y métodos de uso de los mismos. |
| JP2019537557A (ja) | 2016-10-04 | 2019-12-26 | エナンタ ファーマシューティカルズ インコーポレイテッド | Ｆｘｒアゴニストとしてのイソキサゾール類似体およびその使用方法 |
| WO2018081285A1 (en) * | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| KR102765806B1 (ko) * | 2017-09-05 | 2025-02-10 | 블랙손 테라퓨틱스, 인크. | 바소프레신 수용체 길항제 및 그와 관련된 제품 및 방법 |
| WO2019118571A1 (en) | 2017-12-12 | 2019-06-20 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| WO2019152687A1 (en) | 2018-01-31 | 2019-08-08 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| US10829486B2 (en) | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CN109503578A (zh) * | 2018-12-17 | 2019-03-22 | 上海合全药物研发有限公司 | 1-氧亚基-2,8-二氮杂螺[4.5]癸烷-4-甲酸乙酯-8-甲酸叔丁酯合成方法 |
| BR112021018864A2 (pt) | 2019-03-29 | 2021-11-30 | Sumitomo Chemical Co | Composto heterocíclico e composição de controle de praga artrópode nociva contendo o mesmo |
| US11555032B2 (en) | 2019-05-13 | 2023-01-17 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10247680B4 (de) | 2002-10-12 | 2005-09-01 | Aventis Pharma Deutschland Gmbh | Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase |
| WO2005084667A1 (en) | 2004-03-03 | 2005-09-15 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| EP1802623A1 (en) * | 2004-10-12 | 2007-07-04 | Novo Nordisk A/S | 11beta-hydroxysteroid dehydrogenase type 1 active spiro compounds |
| NZ554906A (en) * | 2004-11-10 | 2011-01-28 | Incyte Corp | Lactam compounds and their use as pharmaceuticals |
| TW200804382A (en) | 2005-12-05 | 2008-01-16 | Incyte Corp | Lactam compounds and methods of using the same |
| US20070208001A1 (en) * | 2006-03-03 | 2007-09-06 | Jincong Zhuo | Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
-
2010
- 2010-05-03 US US12/772,246 patent/US8329904B2/en not_active Expired - Fee Related
- 2010-05-10 MX MX2011012017A patent/MX2011012017A/es active IP Right Grant
- 2010-05-10 EP EP10718183.6A patent/EP2430023B1/en not_active Not-in-force
- 2010-05-10 SG SG2011077211A patent/SG175298A1/en unknown
- 2010-05-10 TW TW099114824A patent/TW201043629A/zh unknown
- 2010-05-10 ES ES10718183.6T patent/ES2450119T3/es active Active
- 2010-05-10 WO PCT/EP2010/056307 patent/WO2010130665A1/en not_active Ceased
- 2010-05-10 BR BRPI1015038A patent/BRPI1015038A2/pt not_active IP Right Cessation
- 2010-05-10 KR KR1020117029566A patent/KR101438263B1/ko not_active Expired - Fee Related
- 2010-05-10 JP JP2012510238A patent/JP5542916B2/ja not_active Expired - Fee Related
- 2010-05-10 AR ARP100101584A patent/AR076666A1/es unknown
- 2010-05-10 CN CN2010800205374A patent/CN102421777A/zh active Pending
- 2010-05-10 AU AU2010247472A patent/AU2010247472A1/en not_active Abandoned
- 2010-05-10 CA CA2760340A patent/CA2760340A1/en not_active Abandoned
-
2011
- 2011-07-28 IL IL214352A patent/IL214352A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102421777A (zh) | 2012-04-18 |
| US20100292212A1 (en) | 2010-11-18 |
| JP2012526154A (ja) | 2012-10-25 |
| IL214352A0 (en) | 2011-09-27 |
| TW201043629A (en) | 2010-12-16 |
| MX2011012017A (es) | 2011-12-06 |
| JP5542916B2 (ja) | 2014-07-09 |
| SG175298A1 (en) | 2011-11-28 |
| ES2450119T3 (es) | 2014-03-24 |
| AU2010247472A1 (en) | 2011-09-29 |
| EP2430023A1 (en) | 2012-03-21 |
| US8329904B2 (en) | 2012-12-11 |
| BRPI1015038A2 (pt) | 2016-04-12 |
| EP2430023B1 (en) | 2013-12-11 |
| WO2010130665A1 (en) | 2010-11-18 |
| CA2760340A1 (en) | 2010-11-18 |
| KR101438263B1 (ko) | 2014-09-05 |
| KR20120035160A (ko) | 2012-04-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |