AR086686A1 - Composiciones y metodos para tratar, controlar, reducir, o aliviar el dolor inflamatorio - Google Patents
Composiciones y metodos para tratar, controlar, reducir, o aliviar el dolor inflamatorioInfo
- Publication number
- AR086686A1 AR086686A1 ARP120101996A ARP120101996A AR086686A1 AR 086686 A1 AR086686 A1 AR 086686A1 AR P120101996 A ARP120101996 A AR P120101996A AR P120101996 A ARP120101996 A AR P120101996A AR 086686 A1 AR086686 A1 AR 086686A1
- Authority
- AR
- Argentina
- Prior art keywords
- groups
- unsubstituted
- substituted
- alkyl groups
- group
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 7
- 206010065390 Inflammatory pain Diseases 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 abstract 5
- 125000004122 cyclic group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- -1 cyano, hydroxy Chemical group 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000004215 Carbon black (E152) Substances 0.000 abstract 1
- 206010015958 Eye pain Diseases 0.000 abstract 1
- 230000002411 adverse Effects 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 229940121363 anti-inflammatory agent Drugs 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 1
- 229930195733 hydrocarbon Natural products 0.000 abstract 1
- 150000002430 hydrocarbons Chemical class 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 239000007943 implant Substances 0.000 abstract 1
- 238000002347 injection Methods 0.000 abstract 1
- 239000007924 injection Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 230000000699 topical effect Effects 0.000 abstract 1
Classifications
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Una composición para tratar, controlar, reducir o aliviar el dolor inflamatorio comprende un agonista de los receptores glucocorticoides disociado (“DIGRA”), un profármaco del mismo, una sal farmacéuticamente aceptable del mismo, o un éster farmacéuticamente aceptable del mismo. La composición puede comprender un agente antiinflamatorio adicional y puede ser formulado como aplicación tópica, inyección o implante. Puede ser utilizada en un método de control del dolor ocular postquirúrgico en una forma en que se reduce el riesgo de generar efectos secundarios adversos que sí aparecen con otros agentes terapéuticos.Reivindicación 1: Una composición que comprende: (a) portador farmacéuticamente aceptable; y (b) un agonista de los receptores glucocorticoides disociado (“DIGRA”), un profármaco del mismo, una sal farmacéuticamente aceptable del mismo, o un éster farmacéuticamente aceptable del mismo, en una cantidad eficaz para tratar, controlar, reducir o aliviar el dolor inflamatorio en un sujeto, donde el DIGRA comprende un compuesto que tiene la fórmula (1) donde A y Q se seleccionan independientemente del grupo constituido por grupos arilo y heteroarilo no sustituidos y sustituidos, grupos cicloalquilo y heterocicloalquilo no sustituidos y sustituidos, grupos cicloalquenilo y heterocicloalquenilo no sustituidos y sustituidos, grupos cicloalquinilo y heterocicloalquinilo no sustituidos y sustituidos, y grupos heterocíclicos no sustituidos y sustituidos; R1 y R2 se seleccionan independientemente del grupo constituido por hidrógeno, grupos alquilo C1-15 lineal o ramificado no sustituidos, grupos alquilo C1-15 lineal o ramificado sustituidos, grupos cicloalquilo C3-15 no sustituidos, y grupos cicloalquilo C3-15 sustituidos; R3 es uno del grupo integrado por hidrógeno, grupos alquilo C1-15 lineal o ramificado no sustituidos, grupos alquilo C1-15 lineal o ramificado sustituidos, grupos cicloalquilo y heterocicloalquilo C3-15 no sustituidos, grupos cicloalquilo y heterocicloalquilo C3-15 sustituidos, grupos arilo, grupos heteroarilo, y grupos heterociclílicos; B comprende un grupo carbonilo, amino, hidrocarbono divalente, o heterohidrocarbono; E es grupo hidroxi o amino; y D está ausente o comprende un grupo carbonilo, -NH-, o -NR’-, donde R’ comprende un grupo alquilo C1-15 lineal o ramificado, no sustituido o sustituido; y donde R1 y R2 pueden formar juntos un grupo cicloalquilo C3-15 no sustituido o sustituido. Reivindicación 10: La composición de acuerdo con la reivindicación 2, donde el DIGRA tiene la fórmula (2) donde R4 y R5 se seleccionan independientemente del grupo constituido por hidrógeno, halógeno, ciano, hidroxi, grupos alcoxi C1-5, grupos alquilo C1-5 lineales o ramificados no sustituidos, grupos alquilo C1-5 lineales o ramificados sustituidos, grupos alquilo C3-10 cíclicos no sustituidos, y grupos alquilo C3-10 cíclicos sustituidos. Reivindicación 11: La composición de acuerdo con la reivindicación 2, donde el DIGRA tiene la fórmula (3) donde R4 y R5 se seleccionan independientemente del grupo constituido por hidrógeno, halógeno, ciano, hidroxi, grupos alcoxi C1-5, grupos alquilo C1-5 lineales o ramificados no sustituidos, grupos alquilo C1-5 lineales o ramificados sustituidos, grupos alquilo C3-10 cíclicos no sustituidos, y grupos alquilo C3-10 cíclicos sustituidos. Reivindicación 12: La composición de acuerdo con la reivindicación 2, donde el DIGRA tiene la fórmula (4).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161494137P | 2011-06-07 | 2011-06-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086686A1 true AR086686A1 (es) | 2014-01-15 |
Family
ID=47293674
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101996A AR086686A1 (es) | 2011-06-07 | 2012-06-06 | Composiciones y metodos para tratar, controlar, reducir, o aliviar el dolor inflamatorio |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20120316199A1 (es) |
| KR (1) | KR20140035481A (es) |
| AR (1) | AR086686A1 (es) |
| AU (1) | AU2012268692A1 (es) |
| CA (1) | CA2838876A1 (es) |
| MX (1) | MX2013014518A (es) |
| TW (1) | TW201300378A (es) |
| WO (1) | WO2012170175A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201505527D0 (en) | 2015-03-31 | 2015-05-13 | Jmedtech Pte Ltd | Composition |
| JP2020536955A (ja) | 2017-10-06 | 2020-12-17 | ファウンドリー セラピューティクス， インコーポレイテッド | 治療剤の制御放出のための埋込み可能なデポー |
| US12364792B2 (en) | 2018-01-08 | 2025-07-22 | Foundry Therapeutics, Inc. | Devices, systems, and methods for treating intraluminal cancer via controlled delivery of therapeutic agents |
| US12458589B2 (en) | 2018-05-12 | 2025-11-04 | Foundry Therapeutics, Inc. | Implantable polymer depots for the controlled release of therapeutic agents |
| EP3843710A1 (en) | 2018-08-28 | 2021-07-07 | Foundry Therapeutics, Inc. | Polymer implants |
| KR20210119980A (ko) | 2019-01-22 | 2021-10-06 | 아크리베스 바이오메디컬 게엠베하 | 손상된 피부 상처를 치료하기 위한 선택적 글루코코르티코이드 수용체 개질제 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5378475A (en) | 1991-02-21 | 1995-01-03 | University Of Kentucky Research Foundation | Sustained release drug delivery devices |
| US6051576A (en) | 1994-01-28 | 2000-04-18 | University Of Kentucky Research Foundation | Means to achieve sustained release of synergistic drugs by conjugation |
| US5773019A (en) | 1995-09-27 | 1998-06-30 | The University Of Kentucky Research Foundation | Implantable controlled release device to deliver drugs directly to an internal portion of the body |
| US5902598A (en) | 1997-08-28 | 1999-05-11 | Control Delivery Systems, Inc. | Sustained release drug delivery devices |
| US6242196B1 (en) | 1997-12-11 | 2001-06-05 | Dana-Farber Cancer Institute | Methods and pharmaceutical compositions for inhibiting tumor cell growth |
| WO2000000194A1 (en) | 1998-06-27 | 2000-01-06 | Photogenesis, Inc. | Ophthalmic uses of ppargamma agonists and ppargamma antagonists |
| US6726918B1 (en) | 2000-07-05 | 2004-04-27 | Oculex Pharmaceuticals, Inc. | Methods for treating inflammation-mediated conditions of the eye |
| DE60309829T2 (de) * | 2002-01-14 | 2007-09-13 | Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield | Glucocorticoidmimetika, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische formulierungen und ihre verwendungen |
| JP2005521717A (ja) | 2002-03-26 | 2005-07-21 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用 |
| KR101022977B1 (ko) | 2002-03-26 | 2011-03-18 | 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 | 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도 |
| US6897224B2 (en) | 2002-04-02 | 2005-05-24 | Schering Ag | Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors |
| US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| MXPA05006872A (es) | 2003-01-03 | 2005-08-16 | Boehringer Ingelheim Pharma | Derivados de 1-propanol y 1-propilamina y su uso como ligandos glucocorticoides. |
| US20040224992A1 (en) | 2003-02-27 | 2004-11-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| WO2004097410A1 (en) | 2003-04-30 | 2004-11-11 | Pfizer Products Inc. | Screening methods for cataractogenic risk |
| UY28526A1 (es) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos |
| US7795272B2 (en) | 2004-03-13 | 2010-09-14 | Boehringer Ingelheim Pharmaceutical, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof |
| CA2558019A1 (en) | 2004-03-22 | 2005-10-13 | Boehringer Ingelheim Pharmaceuticals, Inc. | Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics |
| DE102004055633A1 (de) | 2004-11-12 | 2006-05-18 | Schering Ag | 5-substituierte Chinolin- und Isochinolin-Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer |
| US7417056B2 (en) | 2004-11-12 | 2008-08-26 | Schering Ag | 5-substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents |
| CN102304124B (zh) | 2005-09-14 | 2014-10-22 | 参天制药株式会社 | 具有糖皮质激素受体结合活性的1,2-二氢喹啉衍生物 |
| WO2008146871A1 (ja) | 2007-05-29 | 2008-12-04 | Santen Pharmaceutical Co., Ltd. | グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド構造を導入したフェニル基を置換基として有する新規１，２，３，４－テトラヒドロキノキサリン誘導体 |
| US20120065228A1 (en) * | 2007-08-10 | 2012-03-15 | Jinzhong Zhang | Compositions and methods for treating, controlling, reducing, or ameliorating ocular inflammatory with lower risk of increased intraocular pressure |
| US20090042936A1 (en) * | 2007-08-10 | 2009-02-12 | Ward Keith W | Compositions and Methods for Treating or Controlling Anterior-Segment Inflammation |
| US20110281882A1 (en) * | 2007-08-10 | 2011-11-17 | Jinzhong Zhang | Compositions and Methods for Treating, Controlling, Reducing, or Ameliorating Inflammatory Pain |
-
2012
- 2012-05-09 US US13/467,080 patent/US20120316199A1/en not_active Abandoned
- 2012-05-17 MX MX2013014518A patent/MX2013014518A/es unknown
- 2012-05-17 CA CA2838876A patent/CA2838876A1/en not_active Abandoned
- 2012-05-17 WO PCT/US2012/038368 patent/WO2012170175A1/en not_active Ceased
- 2012-05-17 KR KR1020147000259A patent/KR20140035481A/ko not_active Withdrawn
- 2012-05-17 AU AU2012268692A patent/AU2012268692A1/en not_active Abandoned
- 2012-05-28 TW TW101119019A patent/TW201300378A/zh unknown
- 2012-06-06 AR ARP120101996A patent/AR086686A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| MX2013014518A (es) | 2014-01-31 |
| KR20140035481A (ko) | 2014-03-21 |
| AU2012268692A1 (en) | 2014-01-16 |
| TW201300378A (zh) | 2013-01-01 |
| WO2012170175A1 (en) | 2012-12-13 |
| CA2838876A1 (en) | 2012-12-13 |
| US20120316199A1 (en) | 2012-12-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |