AR056207A1 - Compuestos de tetrahidro-pirrolizinona farmaceuticamente activos - Google Patents
Compuestos de tetrahidro-pirrolizinona farmaceuticamente activosInfo
- Publication number
- AR056207A1 AR056207A1 ARP060104371A ARP060104371A AR056207A1 AR 056207 A1 AR056207 A1 AR 056207A1 AR P060104371 A ARP060104371 A AR P060104371A AR P060104371 A ARP060104371 A AR P060104371A AR 056207 A1 AR056207 A1 AR 056207A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocyclyl
- alkyl
- alkenyl
- alkynyl
- aryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 14
- 125000003342 alkenyl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000000304 alkynyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004665 trialkylsilyl group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000004442 acylamino group Chemical group 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000005389 trialkylsiloxy group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004760 (C1-C4) alkylsulfonylamino group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- DYFILXZSBDRFBC-UHFFFAOYSA-N 2,3,5,6-tetrahydropyrrolizin-1-one Chemical class C1CC=C2C(=O)CCN21 DYFILXZSBDRFBC-UHFFFAOYSA-N 0.000 abstract 1
- 101100134927 Gallus gallus COR8 gene Proteins 0.000 abstract 1
- 102100022339 Integrin alpha-L Human genes 0.000 abstract 1
- 108010064548 Lymphocyte Function-Associated Antigen-1 Proteins 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 230000020411 cell activation Effects 0.000 abstract 1
- 230000021164 cell adhesion Effects 0.000 abstract 1
- 230000012292 cell migration Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 1
- -1 cyclohexylsulfonylamino Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 238000013508 migration Methods 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
- A61K31/40—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos de tetrahidro-pirrolizinona que median la actividad de LFA-1 con sus ligandos involucrados en la adhesion, migracion y activacion celular. Reivindicacion 1: Un compuesto de formula (1), en donde el anillo A es un grupo de las formulas A1 a A5; R1 es alquilo C1-18 alquenilo C2-18, alquinilo C2-18, o alquilo C1-18, alquenilo C2-18, alquinilo C2-18, substituidos por alcoxilo C1-4, un grupo sililo o sililoxilo, cicloalquilo C3-18, arilo C6-18, heterociclilo; R2 es cicloalquilo C3-18, arilo C3-18, o heterociclilo; R3 es hidrogeno o alquilo C1-8, alquenilo C2-8, alquinilo C2-8 insubstituidos, o alquilo C1-8, alquenilo C2-8, alquinilo C2-8, substituido por cicloalquilo C3-18, -arilo C3-18, o -heterociclilo; R4 es trialquilsililoxilo C1-6, N3, amino, alquilamino C1-8, dialquilamino C1-8, cicloalquilamino C3-8, acilamino C2-18, (acilo C2-18)alquilamino C1-4, alquisulfonilamino C1-4, arilsulfonilamino C6-12, ciclohexilsulfonilamino C3-8, o R4 es heterociclilo que comprende cuando menos un átomo de nitrogeno como un heteroátomo y que está enlazado por medio de ese átomo de nitrogeno a un compuesto de formula (1); R5 es hidrogeno, alquilo C1-18, alquenilo C2-18, alquinilo C2-18 insubstituidos, o alquilo C1- 18, alquenilo C2-18, alquinilo C2-18 substituidos por alcoxilo C1-4, trialquilsililo C1-6, trialquiI C1-6sililoxilo, cicloalquilo C3-18, arilo C6-18, tal como arilo C6-12, o heterociclilo; R6 es OR7 o SR7; R7 es hidrogeno, un grupo (SO)2-R9, en donde R9 es alquilo C1-4 o arilo C6-12, COR8, CSR8, alquilo C1-18, alquenilo C2-18 o alquinilo C2-18 insubstituidos, o alquilo C1-18, alquenilo C2-18,o alquinilo C2-18, substituidos por alcoxilo C1-4, trialquilsililo C1-6, trialquilsililoxilo C1-6, o heterociclilo; R8 es cicloalquilo C3-18, arilo C6-18, heterociclilo, alquilo C1-18, alquenilo C2-18 o alquinilo C2-18, o alquilo C1-18, alquenilo C2-18 o alquinilo C2-18 substituido por cicloalquilo C3-18, arilo C6-18, o heterociclilo, en donde cicloalquilo, arilo o heterociclilo están insubstituidos o substituidos por uno o más de alquilo C1-16, alquenilo C2-16, alquinilo C2-16, cicloalquilo C3-8, fenilo, bencilo, heterociclilo, haloalquilo C1-4, alcoxilo C1-8, fenoxilo, oxo, acilo C2-13, aciloxilo C2-13, amino, alquilamino C1-6, dialquilamino C1-6, acilamino C2-13, nitro, ciano, halogeno, alquilsulfonilo C1-4, tolilsulfonilo, trialquilsililo C1-6 o trisililoxilo C1-6; y en donde heterociclilo comprende heterociclilo alifático y aromático, de 3 a 8 miembros del anillo, de 1 a 4 heteroátomos seleccionados a partir de N, O, S, heterociclilo fusionado, tal como heterociclilo fusionado con otro anillo (sistema), con la condicion de que, si R4 es heterociclilo, este heterociclilo comprende cuando menos un átomo de nitrogeno como un heteroátomo y está enlazado por medio de ese átomo de nitrogeno a un compuesto de formula (1).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0520379A GB0520379D0 (en) | 2005-10-06 | 2005-10-06 | Organic compounds |
| GBGB0520376.5A GB0520376D0 (en) | 2005-10-06 | 2005-10-06 | Organic compounds |
| GB0520377A GB0520377D0 (en) | 2005-10-06 | 2005-10-06 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056207A1 true AR056207A1 (es) | 2007-09-26 |
Family
ID=37507534
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104371A AR056207A1 (es) | 2005-10-06 | 2006-10-04 | Compuestos de tetrahidro-pirrolizinona farmaceuticamente activos |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20080262070A1 (es) |
| EP (1) | EP1937685A1 (es) |
| JP (1) | JP2009510150A (es) |
| KR (1) | KR20080050605A (es) |
| AR (1) | AR056207A1 (es) |
| AU (1) | AU2006299017B2 (es) |
| BR (1) | BRPI0616870A2 (es) |
| CA (1) | CA2624488A1 (es) |
| GT (1) | GT200600449A (es) |
| PE (1) | PE20070707A1 (es) |
| TW (1) | TW200800169A (es) |
| WO (1) | WO2007039286A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3797775A1 (en) * | 2007-10-19 | 2021-03-31 | Novartis AG | Compositions and methods for treatment of diabetic retinopathy |
| DE102010008644A1 (de) | 2010-02-15 | 2011-08-18 | Bayer Schering Pharma Aktiengesellschaft, 13353 | Zyklische Ketoenole zur Therapie |
| CN103492367B (zh) | 2011-02-17 | 2015-04-01 | 拜耳知识产权有限责任公司 | 用于治疗的取代的3-(联苯-3-基)-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮 |
| DE102011080405A1 (de) | 2011-08-04 | 2013-02-07 | Bayer Pharma AG | Substituierte 3-(Biphenyl-3-yl)-8,8-difluor-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-one zur Therapie |
| DE102011080406A1 (de) | 2011-08-04 | 2013-02-07 | Bayer Pharma AG | Substituierte 3-(Biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro8[4.5]dec-3-en-2-one |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4581462A (en) * | 1983-08-25 | 1986-04-08 | The Upjohn Company | Pyrrolizidine-3-ones |
| MXPA02003977A (es) * | 1999-10-20 | 2003-09-25 | Tanabe Seiyaku Co | Inhibidores de adhesion de celula mediada por al°2. |
| WO2002050080A1 (en) * | 2000-12-19 | 2002-06-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| TW200303200A (en) * | 2002-02-07 | 2003-09-01 | Tanabe Seiyaku Co | Inhibitors of α L β 2 integrin mediated cell adhesion |
| US20030232817A1 (en) * | 2002-05-29 | 2003-12-18 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful for the treatment of inflammatory disease |
| US7375237B2 (en) * | 2004-08-18 | 2008-05-20 | Bristol-Myers Squibb Company | Pyrrolizine compounds useful as anti-inflammatory agents |
-
2006
- 2006-10-04 AU AU2006299017A patent/AU2006299017B2/en not_active Expired - Fee Related
- 2006-10-04 BR BRPI0616870-1A patent/BRPI0616870A2/pt not_active IP Right Cessation
- 2006-10-04 JP JP2008533928A patent/JP2009510150A/ja active Pending
- 2006-10-04 US US12/089,254 patent/US20080262070A1/en not_active Abandoned
- 2006-10-04 PE PE2006001210A patent/PE20070707A1/es not_active Application Discontinuation
- 2006-10-04 WO PCT/EP2006/009598 patent/WO2007039286A1/en active Application Filing
- 2006-10-04 CA CA002624488A patent/CA2624488A1/en not_active Abandoned
- 2006-10-04 EP EP06806035A patent/EP1937685A1/en not_active Withdrawn
- 2006-10-04 KR KR1020087008230A patent/KR20080050605A/ko active IP Right Grant
- 2006-10-04 AR ARP060104371A patent/AR056207A1/es unknown
- 2006-10-05 TW TW095137242A patent/TW200800169A/zh unknown
- 2006-10-05 GT GT200600449A patent/GT200600449A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006299017A1 (en) | 2007-04-12 |
| KR20080050605A (ko) | 2008-06-09 |
| JP2009510150A (ja) | 2009-03-12 |
| BRPI0616870A2 (pt) | 2011-07-05 |
| TW200800169A (en) | 2008-01-01 |
| AU2006299017B2 (en) | 2010-11-04 |
| GT200600449A (es) | 2007-06-11 |
| US20080262070A1 (en) | 2008-10-23 |
| PE20070707A1 (es) | 2007-08-20 |
| WO2007039286A1 (en) | 2007-04-12 |
| CA2624488A1 (en) | 2007-04-12 |
| EP1937685A1 (en) | 2008-07-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |