MXPA04010860A - Composiciones terapeuticas de 1,2,3,6-tetrahidropirimidin-2-ona y metodos para usarla. - Google Patents
Composiciones terapeuticas de 1,2,3,6-tetrahidropirimidin-2-ona y metodos para usarla.Info
- Publication number
- MXPA04010860A MXPA04010860A MXPA04010860A MXPA04010860A MXPA04010860A MX PA04010860 A MXPA04010860 A MX PA04010860A MX PA04010860 A MXPA04010860 A MX PA04010860A MX PA04010860 A MXPA04010860 A MX PA04010860A MX PA04010860 A MXPA04010860 A MX PA04010860A
- Authority
- MX
- Mexico
- Prior art keywords
- phenyl
- tetrahydropyrimidine
- therapeutic
- trifluoromethyl
- fluoro
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 5
- 230000001225 therapeutic effect Effects 0.000 title abstract 3
- QGKGASXQTBQINX-UHFFFAOYSA-N 3,4-dihydro-1h-pyrimidin-2-one Chemical compound O=C1NCC=CN1 QGKGASXQTBQINX-UHFFFAOYSA-N 0.000 title abstract 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 abstract 2
- 239000000018 receptor agonist Substances 0.000 abstract 2
- 229940044601 receptor agonist Drugs 0.000 abstract 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 abstract 1
- 208000003251 Pruritus Diseases 0.000 abstract 1
- 239000000150 Sympathomimetic Substances 0.000 abstract 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 230000001387 anti-histamine Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 239000000739 antihistaminic agent Substances 0.000 abstract 1
- 238000001816 cooling Methods 0.000 abstract 1
- 239000000850 decongestant Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 210000000744 eyelid Anatomy 0.000 abstract 1
- 239000003862 glucocorticoid Substances 0.000 abstract 1
- 229960003444 immunosuppressant agent Drugs 0.000 abstract 1
- 230000001861 immunosuppressant effect Effects 0.000 abstract 1
- 239000003018 immunosuppressive agent Substances 0.000 abstract 1
- 239000003589 local anesthetic agent Substances 0.000 abstract 1
- 230000005923 long-lasting effect Effects 0.000 abstract 1
- 229940041616 menthol Drugs 0.000 abstract 1
- 210000004877 mucosa Anatomy 0.000 abstract 1
- 210000004400 mucous membrane Anatomy 0.000 abstract 1
- 230000035807 sensation Effects 0.000 abstract 1
- 230000001975 sympathomimetic effect Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P17/04—Antipruritics
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0031—Rectum, anus
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
- A61K9/025—Suppositories; Bougies; Bases therefor; Ovules characterised by shape or structure, e.g. hollow layered, coated
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/08—Inhaling devices inserted into the nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M2202/00—Special media to be introduced, removed or treated
- A61M2202/06—Solids
- A61M2202/064—Powder
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se proporciona una composicion terapeutica que comprende un agonista de receptor de frio de 1,2,3,6-tetrahidropirimidina-2-ona substituido con 1-R1-fenilo, 4-R2-fenilo en una cantidad efectiva terapeuticamente. La composicion ademas comprende preferentemente uno o mas farmacos activos farmaceuticamente tales como un glucocorticosteroide antiinflamatorio, un descongestionante de amina simpatomimetico, una antihistamina, un anestesico local, mentol o un analogo de mentol, un inmunosupresante, y mezclas de los mismos. El agonista de receptor de frio puede estar representado por la formula general (1) -[R1-fenil]-4-[R2-fenil]-1,2,3,6-tetrahidropirimidina-2-ona en donde: R1 es-hidroxi, --cloro, -fluoro, -alquilo, -acetoxi, -trifluorometilo; y R2 es -nitro, -cloro, -fluoro, -alquilo, - trifluurometilo. Las composiciones terapeuticas de la invencion producen enfriamiento y relajamiento de larga duracion, particularmente cuando se formula para suministro para suprimir las sensaciones de picor y dolor, tal como para suministro a piel inflamada, a las membranas mucosas de los parpados, de las areas anogenitales y de las vias respiratorias y a la mucosa enterica.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/139,193 US6919348B2 (en) | 2002-05-02 | 2002-05-02 | Therapeutic 1,2,3,6-tetrahydropyrimidine-2-one compositions and methods therewith |
| US10/191,481 US20030207903A1 (en) | 2002-05-02 | 2002-07-08 | 1,2,3,6-tetrahydropyrimidine-2-one compositions and therapeutic methods therewith for sexual disfunction |
| US10/233,126 US20030206873A1 (en) | 2002-05-02 | 2002-08-29 | 1,2,3,6-tetrahydropyrimidine-2-one compositions and therapeutic methods therewith for gastrointestinal dysfunction |
| US10/232,798 US6743801B2 (en) | 2002-05-02 | 2002-08-29 | 1,2,3,6-tetrahydropyrimidine-2-one compositions and therapeutic methods therewith for pain and inflammation |
| US10/267,896 US6933301B2 (en) | 2002-05-02 | 2002-10-08 | 1,2,3,6-tetrahydropyrimidine-2-one compositions, articles and therapeutic methods for upper airway breathing disorders |
| PCT/GB2003/001811 WO2003092697A1 (en) | 2002-05-02 | 2003-04-28 | Therapeutic 1,2,3,6-tetrahydropyrimidine-2-one compositions and methods therewith |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA04010860A true MXPA04010860A (es) | 2005-11-17 |
Family
ID=29408146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA04010860A MXPA04010860A (es) | 2002-05-02 | 2003-04-28 | Composiciones terapeuticas de 1,2,3,6-tetrahidropirimidin-2-ona y metodos para usarla. |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1503763B1 (es) |
| JP (1) | JP4558479B2 (es) |
| CN (1) | CN1665507B (es) |
| AU (1) | AU2003222990B2 (es) |
| CA (1) | CA2483090C (es) |
| IL (1) | IL164887A0 (es) |
| MX (1) | MXPA04010860A (es) |
| WO (1) | WO2003092697A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0221697D0 (en) * | 2002-09-18 | 2002-10-30 | Unilever Plc | Novel compouds and their uses |
| ES2476902T5 (es) * | 2003-07-02 | 2018-04-03 | Genentech, Inc. | Compuestos activadores de TRP-P8 y métodos de tratamiento terapéuticos |
| WO2006131203A1 (en) * | 2005-06-10 | 2006-12-14 | Unilever N.V. | Oral care composition comprising a 1 , 2 , 3 , 6-tetrahydropyrimidine-2-one cooling agent |
| FR2895260B1 (fr) * | 2005-12-23 | 2009-02-20 | Servier Lab | Nouvelle composition pharmaceutique a base d'huile essentielle pour pulverisation nasale et/ou buccale |
| US7727516B2 (en) * | 2006-02-28 | 2010-06-01 | The Procter & Gamble Company | Reduction of hair growth |
| GB0615136D0 (en) * | 2006-07-29 | 2006-09-06 | Univ Edinburgh | Induction of analgesia in neuropathic pain |
| WO2008038126A2 (en) * | 2006-09-29 | 2008-04-03 | Infa S.A. | Packaging system for pharmaceutical compositions and kit for intravenous administration |
| KR101049788B1 (ko) * | 2011-01-28 | 2011-07-19 | 주식회사 에코덤 | 다양한 피부질환에서 소양증의 치유 또는 개선용 경피흡수제제 |
| RU2590979C2 (ru) * | 2011-02-11 | 2016-07-10 | ЗедЭкс ФАРМА, ЭлЭлСи | Составы l-ментола, состоящие из множества частиц, и связанные с ними способы |
| EP2497458A1 (en) | 2011-03-08 | 2012-09-12 | B.R.A.I.N. Biotechnology Research And Information Network AG | Small molecule modulators of the cold and menthol receptor TRPM8 |
| CN102178676B (zh) * | 2011-04-29 | 2012-07-25 | 山东大学 | 一种治疗脑胶质瘤的药物组合物 |
| DE102012218733A1 (de) * | 2012-10-15 | 2014-04-17 | Beiersdorf Ag | Kosmetische oder dermatologische Zubereitung zur Prophylaxe und/oder Behandlung atopischer Dermatitis |
| JP7655568B2 (ja) * | 2019-10-25 | 2025-04-02 | ムココルト アクチエボラグ | 粘膜又は皮膚における炎症状態の治療 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3821221A (en) * | 1970-08-25 | 1974-06-28 | Delmar Chem | 1,2,3,6-tetrahydropyrimidine-2-one compounds and processes for makingthem |
| GB1476351A (en) * | 1974-04-17 | 1977-06-10 | Wilkinson Sword Ltd | Compounds having a physiological cooling effect and compo sitions containing them |
| JPS5310597A (en) * | 1976-07-15 | 1978-01-31 | Shiyoujirou Narumiya | Slowly vertically dropping device |
| CA1306192C (en) * | 1986-12-17 | 1992-08-11 | Andrew Hamilton Ward | Medicament containing a silicon derivative of menthol |
| JPH01185267A (ja) * | 1988-01-19 | 1989-07-24 | Geran Kaihatsu Kenkyusho:Kk | 新吸入器 |
| FR2777187B1 (fr) * | 1998-04-14 | 2000-05-19 | Yves Theodore Stephane Tillet | Composition pour faciliter l'action du levomenthol sur les thermorecepteurs de la muqueuse congestionnee du vestibule nasal et la regeneration naturelle de cette muqueuse |
| US20020009478A1 (en) * | 1998-08-24 | 2002-01-24 | Douglas Joseph Dobrozsi | Oral liquid mucoadhesive compositions |
| JP2002536069A (ja) * | 1999-02-02 | 2002-10-29 | エイボン プロダクツ インコーポレーテッド | のぼせの不快感を軽減する方法およびそのための組成物 |
-
2003
- 2003-04-28 CN CN038158841A patent/CN1665507B/zh not_active Expired - Fee Related
- 2003-04-28 WO PCT/GB2003/001811 patent/WO2003092697A1/en not_active Ceased
- 2003-04-28 AU AU2003222990A patent/AU2003222990B2/en not_active Ceased
- 2003-04-28 MX MXPA04010860A patent/MXPA04010860A/es active IP Right Grant
- 2003-04-28 EP EP03718956A patent/EP1503763B1/en not_active Expired - Lifetime
- 2003-04-28 JP JP2004500881A patent/JP4558479B2/ja not_active Expired - Fee Related
- 2003-04-28 CA CA2483090A patent/CA2483090C/en not_active Expired - Lifetime
-
2004
- 2004-10-27 IL IL16488704A patent/IL164887A0/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1665507B (zh) | 2010-05-26 |
| EP1503763B1 (en) | 2009-12-02 |
| JP4558479B2 (ja) | 2010-10-06 |
| AU2003222990A1 (en) | 2003-11-17 |
| CA2483090C (en) | 2011-01-25 |
| CA2483090A1 (en) | 2003-11-13 |
| CN1665507A (zh) | 2005-09-07 |
| JP2005526841A (ja) | 2005-09-08 |
| WO2003092697A1 (en) | 2003-11-13 |
| AU2003222990B2 (en) | 2009-11-12 |
| EP1503763A1 (en) | 2005-02-09 |
| IL164887A0 (en) | 2005-12-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |