ES2549926T3 - Derivados (aza)indolizínicos como inhibidores de la xantina-oxidasa - Google Patents
Derivados (aza)indolizínicos como inhibidores de la xantina-oxidasa Download PDFInfo
- Publication number
- ES2549926T3 ES2549926T3 ES11829191.3T ES11829191T ES2549926T3 ES 2549926 T3 ES2549926 T3 ES 2549926T3 ES 11829191 T ES11829191 T ES 11829191T ES 2549926 T3 ES2549926 T3 ES 2549926T3
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- ES
- Spain
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- mono
- cyano
- formula
- aza
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 125000003406 indolizinyl group Chemical class C=1(C=CN2C=CC=CC12)* 0.000 title 1
- 239000003064 xanthine oxidase inhibitor Substances 0.000 title 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000004755 (C2-C7) acylamino group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 1
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000004658 aryl carbonyl amino group Chemical group 0.000 abstract 1
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- -1 hydroxy, amino, carboxy, carbamoyl Chemical group 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/04—Drugs for disorders of the urinary system for urolithiasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- 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
- 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un derivado (aza)indolizínico representado por la fórmula (I):**Fórmula** en el que ninguno a dos de X1, X2, X3 y X4 son átomos de nitrógeno y los demás son CR1; uno de T1 y T2 representa ciano y el otro representa un grupo representado por la fórmula: **Fórmula** con la condición de que cuando T1 es ciano, al menos uno de X1 a X4 es un átomo de nitrógeno; R1 representa independientemente uno cualquiera de los siguientes (1) a (7): (1) un átomo de hidrógeno; (2) un átomo de halógeno; (3) un grupo hidroxi; (4) amino; (5) ciano; (6) carboxi; (7) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, mono(di)alquilamino C1-6, acilo C2-7, acilamino C2-7, mono(di)alquilcarbamoílo C1-6, alquilsulfonilo C1-6, alquilsulfonilamino C1-6, mono(di)alquilsulfamoílo C1-6, alquiltio C1-6, cicloalquilo C3-8, heterocicloalquilo de tres a ocho miembros, cicloalquenilo C5-8, heterocicloalquenilo de cinco a ocho miembros, cicloalquiloxi C3-8, cicloalquilamino C3-8, arilo C6, heteroarilo de cinco o seis miembros, ariloxi C6, arilamino C6, arilcarbonilo C6 o arilcarbonilamino C6, cada uno de los cuales puede tener cualquier grupo seleccionado del grupo de sustituyentes G; en que el grupo de sustituyentes G consta de un átomo de flúor, un átomo de cloro, un grupo hidroxi, amino, carboxi, carbamoílo, ciano, alquilo C1-6, alcoxi C1-6 y mono(di)alquilamino C1-6; el anillo U representa un anillo bencénico o un heteroarilo de cinco o seis miembros;
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010219600 | 2010-09-29 | ||
| JP2010219600 | 2010-09-29 | ||
| PCT/JP2011/072201 WO2012043638A1 (ja) | 2010-09-29 | 2011-09-28 | (アザ)インドリジン誘導体及びその医薬用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2549926T3 true ES2549926T3 (es) | 2015-11-03 |
Family
ID=45893077
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11829191.3T Active ES2549926T3 (es) | 2010-09-29 | 2011-09-28 | Derivados (aza)indolizínicos como inhibidores de la xantina-oxidasa |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9643969B2 (es) |
| EP (1) | EP2623505B1 (es) |
| JP (1) | JP5906191B2 (es) |
| KR (1) | KR20130099064A (es) |
| CN (2) | CN104592224B (es) |
| CA (1) | CA2811773A1 (es) |
| ES (1) | ES2549926T3 (es) |
| WO (1) | WO2012043638A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6386527B2 (ja) | 2013-03-11 | 2018-09-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | カリウムイオンチャネル阻害剤としてのピロロピリダジン |
| EP2970294B1 (en) | 2013-03-11 | 2016-12-28 | Bristol-Myers Squibb Company | Pyrrolotriazines as potassium ion channel inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| HUE052608T2 (hu) * | 2015-09-02 | 2021-05-28 | Sunshine Lake Pharma Co Ltd | Karboxi-szubsztituált (hetero) aromás gyûrûs származékok, elõállítási eljárásaik és alkalmazásaik |
| JP6898330B2 (ja) * | 2015-12-28 | 2021-07-07 | シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド | インドリジン誘導体、組成物、及び使用方法 |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| JP6999574B2 (ja) | 2016-04-22 | 2022-01-18 | インサイト・コーポレイション | Lsd1阻害剤の製剤 |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| CN111943957B (zh) * | 2019-05-17 | 2023-01-06 | 中国医学科学院药物研究所 | 喹啉甲酰胺类化合物及其制备方法和用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ193926A (en) | 1979-07-06 | 1984-05-31 | Labaz Sanofi Nv | 2-(alkyl or phenyl)-3(4-hydroxybenzoyl)indolizines |
| KR20080066938A (ko) * | 2005-10-07 | 2008-07-17 | 깃세이 야쿠힌 고교 가부시키가이샤 | 질소 함유 복소환 화합물 및 그것을 함유하는 의약 조성물 |
| CA2627839C (en) * | 2005-11-02 | 2014-08-19 | Bayer Healthcare Ag | Pyrrolo[2,1-f] [1,2,4] triazin-4-ylamines igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases |
| JP5330990B2 (ja) * | 2007-04-11 | 2013-10-30 | キッセイ薬品工業株式会社 | 含窒素複素環化合物およびそれを含有する医薬組成物 |
| US8003647B2 (en) | 2007-04-11 | 2011-08-23 | Kissei Pharmaceutical Co., Ltd. | (Aza)indole derivative and use thereof for medical purposes |
| SI2415771T1 (sl) * | 2009-03-31 | 2013-12-31 | Kissei Pharmaceutical Co., Ltd. | Derivat indolizina in njegova uporaba v medicinske namene |
-
2011
- 2011-09-28 ES ES11829191.3T patent/ES2549926T3/es active Active
- 2011-09-28 KR KR1020137006949A patent/KR20130099064A/ko not_active Ceased
- 2011-09-28 CN CN201510005098.4A patent/CN104592224B/zh not_active Expired - Fee Related
- 2011-09-28 EP EP11829191.3A patent/EP2623505B1/en not_active Not-in-force
- 2011-09-28 US US13/824,147 patent/US9643969B2/en not_active Expired - Fee Related
- 2011-09-28 JP JP2012536511A patent/JP5906191B2/ja not_active Expired - Fee Related
- 2011-09-28 WO PCT/JP2011/072201 patent/WO2012043638A1/ja not_active Ceased
- 2011-09-28 CN CN201180055764.5A patent/CN103221412B/zh not_active Expired - Fee Related
- 2011-09-28 CA CA2811773A patent/CA2811773A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US9643969B2 (en) | 2017-05-09 |
| JPWO2012043638A1 (ja) | 2014-02-24 |
| EP2623505A4 (en) | 2013-10-02 |
| JP5906191B2 (ja) | 2016-04-20 |
| CN104592224B (zh) | 2016-08-03 |
| EP2623505A1 (en) | 2013-08-07 |
| EP2623505B1 (en) | 2015-07-29 |
| WO2012043638A1 (ja) | 2012-04-05 |
| HK1206360A1 (en) | 2016-01-08 |
| CN103221412A (zh) | 2013-07-24 |
| HK1188442A1 (en) | 2014-05-02 |
| KR20130099064A (ko) | 2013-09-05 |
| CN104592224A (zh) | 2015-05-06 |
| CN103221412B (zh) | 2015-08-19 |
| US20130217878A1 (en) | 2013-08-22 |
| CA2811773A1 (en) | 2012-04-05 |
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