AR083700A1 - Derivados de pirrolidina - Google Patents
Derivados de pirrolidinaInfo
- Publication number
- AR083700A1 AR083700A1 ARP110104087A ARP110104087A AR083700A1 AR 083700 A1 AR083700 A1 AR 083700A1 AR P110104087 A ARP110104087 A AR P110104087A AR P110104087 A ARP110104087 A AR P110104087A AR 083700 A1 AR083700 A1 AR 083700A1
- Authority
- AR
- Argentina
- Prior art keywords
- pyridinyl
- pyrininyl
- oxo
- alkyl
- haloalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
- A61P3/08—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
- A61P35/00—Antineoplastic 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
-
- 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
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Proceso de obtención, composiciones farmacéuticas y usos.Reivindicación 1: Un compuesto de la fórmula (1), en la que: R1 es hidrógeno, alquilo, morfolinilo, haloalquilamino, alquiloxadiazolilo, hidroxilo, halopirrolidinilo, azetidinilo, alquilamino, amino, cianoalquilamino, halofenilalquilamino o cianocicloalquilamino; R2, R3, R4, R5 y R6 se eligen con independencia entre hidrógeno, alquilo, haloalquilo, hidroxialquilo, alcoxi, halo-alquiloxi, halógeno, hidroxilo, cianopiraziniloxi, pirazolilo, alquilpirazolilo, imidazolilo, benzoimidazolilo, 6-oxo-6H-piridazinilo, alquil-6-oxo-6H-piridazinilo, piperazinilo, N-alquilpiperazinilo, piperidinilo, difluoropirrolidinilo, fenilimidazolilo, oxo-pirrolidinilo, oxo-oxazolidinilo, morfolinilo, oxo-morfolinilo, oxo-piridinilo, 2-oxo-2H-pirazinilo, difluoropiperidinilo, haloalquilpiperidinilo, piperidinilalcoxi, oxetaniloxi, alquilpirazolilo, halopiridinilo, alquilpiridinilo, cicloalquilo, cicloalquilalquilo, halofenilo, alquilcarbonilaminocicloalquilalquilo, haloalquilpiperazinilo, alquilamino, alcoxialquilpiperazinilo, cicloalquilpiperazinilo, hexahidropirrolo[1,2-a]pirazinilo, 5,6-dihidro-8H-[1,2,4]triazolo[4,3-a]pirazin-7-ilo, alquilimidazolilo, azetidinilo, cicloalquilpiperazinilo, alquilimidazolilo, alcoxialcoxi, imidazo[4,5-c]piridinilo, alquilpiperazinilo, hexahidro-pirrolo[1,2-a]pirazinilo, haloazetidinilo, pirimidinilo y alqueniloxi; A1 es -CH2-, carbonilo, -C(O)O- o está ausente; A2 es nitrógeno o CR7; A3 es nitrógeno o CR8; A4 es nitrógeno o CR9; R7 es hidrógeno, alquilo, haloalquilo, halógeno, hidroxilo, haloalquilaminocarbonilo; halofenilalquilaminocarbonilo, fenilcicloalquilaminocarbonilo, haloalquilfenilalquilaminocarbonilo, halofenilcicloalquilaminocarbonilo o halofenilcicloalquilalquilaminocarbonilo; R8 es hidrógeno, alquilo, haloalquilo, halógeno o hidroxilo; o R7 y R8 junto con el átomo de carbono al que están unidos forman un cicloalquilo o pirrolidinilo sustituido, dicho pirrolidinilo sustituido es pirrolidinilo N-sustituido con haloalquilo o formilo; R9 es hidrógeno, alquilo, haloalquilo, halógeno o nitro; o R8 y R9 junto con el átomo de carbono al que están unidos forman un cicloalquilo; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10190239 | 2010-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083700A1 true AR083700A1 (es) | 2013-03-13 |
Family
ID=43645895
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110104087A AR083700A1 (es) | 2010-11-05 | 2011-11-03 | Derivados de pirrolidina |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8524710B2 (es) |
| EP (1) | EP2635562B1 (es) |
| JP (1) | JP5670580B2 (es) |
| KR (1) | KR101522119B1 (es) |
| CN (1) | CN103201274B (es) |
| AR (1) | AR083700A1 (es) |
| BR (1) | BR112013010699A2 (es) |
| CA (1) | CA2815611C (es) |
| ES (1) | ES2512445T3 (es) |
| MX (1) | MX346090B (es) |
| RU (1) | RU2548684C2 (es) |
| WO (1) | WO2012059507A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104114549A (zh) | 2012-02-17 | 2014-10-22 | 霍夫曼-拉罗奇有限公司 | 新型吡咯烷衍生物 |
| KR20140145171A (ko) * | 2012-04-17 | 2014-12-22 | 아스테라스 세이야쿠 가부시키가이샤 | 함질소 이환식 방향족 헤테로환 화합물 |
| US9458181B2 (en) * | 2013-10-08 | 2016-10-04 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| EP3174879B1 (en) * | 2014-08-01 | 2018-07-18 | Boehringer Ingelheim International GmbH | Substituted oxetanes and their use as inhibitors of cathepsin c |
| WO2018139438A1 (ja) | 2017-01-24 | 2018-08-02 | アステラス製薬株式会社 | フェニルジフルオロメチル置換プロリンアミド化合物 |
| WO2024099403A1 (zh) * | 2022-11-10 | 2024-05-16 | 北京普祺医药科技股份有限公司 | 一种具有软药性质的硫醚类化合物、药物组合物及其用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60030768T2 (de) | 1999-12-24 | 2007-11-08 | F. Hoffmann-La Roche Ag | Nitrilderivate als cathepsin k hemmer |
| AR036375A1 (es) * | 2001-08-30 | 2004-09-01 | Novartis Ag | Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos |
| SE0201976D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
| WO2008052934A1 (en) * | 2006-10-30 | 2008-05-08 | Glaxo Group Limited | Novel substituted pyrimidines as cysteine protease inhibitors |
| NZ595073A (en) | 2009-04-20 | 2012-11-30 | Hoffmann La Roche | Proline derivatives as cathepsin inhibitors |
-
2011
- 2011-10-24 US US13/279,364 patent/US8524710B2/en not_active Expired - Fee Related
- 2011-11-02 CN CN201180053448.4A patent/CN103201274B/zh not_active Expired - Fee Related
- 2011-11-02 ES ES11776459.7T patent/ES2512445T3/es active Active
- 2011-11-02 CA CA2815611A patent/CA2815611C/en not_active Expired - Fee Related
- 2011-11-02 EP EP11776459.7A patent/EP2635562B1/en not_active Not-in-force
- 2011-11-02 RU RU2013124993/04A patent/RU2548684C2/ru not_active IP Right Cessation
- 2011-11-02 JP JP2013537124A patent/JP5670580B2/ja not_active Expired - Fee Related
- 2011-11-02 KR KR1020137014194A patent/KR101522119B1/ko not_active IP Right Cessation
- 2011-11-02 WO PCT/EP2011/069219 patent/WO2012059507A1/en active Application Filing
- 2011-11-02 BR BR112013010699A patent/BR112013010699A2/pt not_active Application Discontinuation
- 2011-11-02 MX MX2013004667A patent/MX346090B/es active IP Right Grant
- 2011-11-03 AR ARP110104087A patent/AR083700A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| RU2548684C2 (ru) | 2015-04-20 |
| ES2512445T3 (es) | 2014-10-24 |
| MX346090B (es) | 2017-03-07 |
| EP2635562B1 (en) | 2014-09-03 |
| CA2815611A1 (en) | 2012-05-10 |
| MX2013004667A (es) | 2013-06-28 |
| CA2815611C (en) | 2015-12-29 |
| RU2013124993A (ru) | 2014-12-10 |
| BR112013010699A2 (pt) | 2016-08-09 |
| CN103201274B (zh) | 2014-08-20 |
| CN103201274A (zh) | 2013-07-10 |
| JP5670580B2 (ja) | 2015-02-18 |
| EP2635562A1 (en) | 2013-09-11 |
| JP2013541574A (ja) | 2013-11-14 |
| US20120115843A1 (en) | 2012-05-10 |
| KR20130089265A (ko) | 2013-08-09 |
| WO2012059507A1 (en) | 2012-05-10 |
| US8524710B2 (en) | 2013-09-03 |
| KR101522119B1 (ko) | 2015-05-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |