JP2014530846A5 - - Google Patents
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- Publication number
- JP2014530846A5 JP2014530846A5 JP2014536349A JP2014536349A JP2014530846A5 JP 2014530846 A5 JP2014530846 A5 JP 2014530846A5 JP 2014536349 A JP2014536349 A JP 2014536349A JP 2014536349 A JP2014536349 A JP 2014536349A JP 2014530846 A5 JP2014530846 A5 JP 2014530846A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- pharmaceutical composition
- oxymetazoline
- brimonidine
- 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.)
- Pending
Links
- 150000003839 salts Chemical class 0.000 claims 17
- 239000011780 sodium chloride Substances 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- WYWIFABBXFUGLM-UHFFFAOYSA-N Oxymetazoline Chemical group CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 WYWIFABBXFUGLM-UHFFFAOYSA-N 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 7
- 229960001528 oxymetazoline Drugs 0.000 claims 7
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 claims 6
- 229960003679 brimonidine Drugs 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 239000000695 adrenergic alpha-agonist Substances 0.000 claims 5
- 210000003491 Skin Anatomy 0.000 claims 3
- 230000001815 facial Effects 0.000 claims 3
- 238000011010 flushing procedure Methods 0.000 claims 3
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 claims 2
- OFHCOWSQAMBJIW-AVJTYSNKSA-N Alfacalcidol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C OFHCOWSQAMBJIW-AVJTYSNKSA-N 0.000 claims 2
- 229960002342 Mephentermine Drugs 0.000 claims 2
- RXQCGGRTAILOIN-UHFFFAOYSA-N Mephentermine Chemical compound CNC(C)(C)CC1=CC=CC=C1 RXQCGGRTAILOIN-UHFFFAOYSA-N 0.000 claims 2
- 229960005192 Methoxamine Drugs 0.000 claims 2
- WJAJPNHVVFWKKL-UHFFFAOYSA-N Methoxamine hydrochloride Chemical compound COC1=CC=C(OC)C(C(O)C(C)N)=C1 WJAJPNHVVFWKKL-UHFFFAOYSA-N 0.000 claims 2
- 229960001802 Phenylephrine Drugs 0.000 claims 2
- SONNWYBIRXJNDC-VIFPVBQESA-N Phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 claims 2
- BYJAVTDNIXVSPW-UHFFFAOYSA-N Tetrahydrozoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 claims 2
- HUCJFAOMUPXHDK-UHFFFAOYSA-N Xylometazoline Chemical compound CC1=CC(C(C)(C)C)=CC(C)=C1CC1=NCCN1 HUCJFAOMUPXHDK-UHFFFAOYSA-N 0.000 claims 2
- 229960005016 naphazoline Drugs 0.000 claims 2
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 2
- 229940016284 tetrahydrozoline Drugs 0.000 claims 2
- 229960000337 tetryzoline Drugs 0.000 claims 2
- 229960000833 xylometazoline Drugs 0.000 claims 2
- 229960001724 Brimonidine tartrate Drugs 0.000 claims 1
- 229960001094 Midodrine Drugs 0.000 claims 1
- PTKSEFOSCHHMPD-UHFFFAOYSA-N Midodrine Chemical compound COC1=CC=C(OC)C(C(O)CNC(=O)CN)=C1 PTKSEFOSCHHMPD-UHFFFAOYSA-N 0.000 claims 1
- 229960005162 Oxymetazoline hydrochloride Drugs 0.000 claims 1
- 239000000533 adrenergic alpha-1 receptor agonist Substances 0.000 claims 1
- 239000000384 adrenergic alpha-2 receptor agonist Substances 0.000 claims 1
- QZHBYNSSDLTCRG-WUUYCOTASA-N brimonidine tartrate Chemical compound [H+].[H+].[O-]C(=O)[C@@H](O)[C@H](O)C([O-])=O.C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 QZHBYNSSDLTCRG-WUUYCOTASA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- BEEDODBODQVSIM-UHFFFAOYSA-N oxymetazoline hydrochloride Chemical group Cl.CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 BEEDODBODQVSIM-UHFFFAOYSA-N 0.000 claims 1
Claims (11)
- 少なくとも1種のαアドレナリン作動性受容体アゴニストを含む少なくとも1種の医薬的に活性な化合物および局所的に許容できる担体を含む、ヒトにおけるホスホジエステラーゼ5型阻害薬の全身使用に伴う顔面皮膚潮紅の軽減のための医薬組成物。
- 少なくとも1種のα1アドレナリン作動性受容体アゴニストを含む、請求項１の医薬組成物。
- 少なくとも1種のα2アドレナリン作動性受容体アゴニストを含む、請求項１の医薬組成物。
- αアドレナリン作動性受容体アゴニストが、オキシメタゾリン、テトラヒドロゾリン、ナファゾリン、キシロメタゾリン、フェニレフリン、メトキサミン、メフェンテルミン、メタラミノール、デスグリミドドリン、ミドドリン、ブリモニジン、及びその医薬的に許容できる塩、及び該化合物又は塩の任意の組合せから成る群より選択される、請求項１の医薬組成物。
- αアドレナリン作動性受容体アゴニストが、オキシメタゾリン、テトラヒドロゾリン、ナファゾリン、キシロメタゾリン、フェニレフリン、メトキサミン、メフェンテルミン、メタラミノール、デスグリミドドリン、ミドドリン、及びその医薬的に許容できる塩、及び該化合物又は塩の任意の組合せから成る群より選択される、請求項１の医薬組成物。
- 少なくとも1種のαアドレナリン作動性受容体アゴニスト又はその医薬的に許容できる塩が、ブリモニジン、オキシメタゾリン、又はその医薬的に許容できる塩、又はいずれかの該化合物若しくは塩の組合せから成る群より選択される、請求項１に記載の医薬組成物。
- ホスホジエステラーゼ5型阻害薬の全身使用に伴う顔面皮膚潮紅を軽減するための唯一の医薬的に活性な化合物が、ブリモニジン若しくはその医薬的に許容できる塩又はオキシメタゾリン若しくはその医薬的に許容できる塩；又はブリモニジン若しくはその医薬的に許容できる塩とオキシメタゾリン若しくはその医薬的に許容できる塩との組合せである、請求項１に記載の医薬組成物。
- 組成物中のいかなる種類にせよ唯一の医薬的に活性な化合物が、ブリモニジン若しくはその医薬的に許容できる塩又はオキシメタゾリン若しくはその医薬的に許容できる塩；又はブリモニジン若しくはその医薬的に許容できる塩とオキシメタゾリン若しくはその医薬的に許容できる塩との組合せである、請求項１に記載の医薬組成物。
- 医薬的に許容できる塩がオキシメタゾリン塩酸塩である、請求項１に記載の医薬組成物。
- 医薬的に許容できる塩がブリモニジン酒石酸塩である、請求項１に記載の医薬組成物。
- αアドレナリン作動性受容体アゴニストが、ヒトの顔面皮膚潮紅を軽減する唯一の化合物である、請求項１に記載の医薬組成物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161548844P | 2011-10-19 | 2011-10-19 | |
| US61/548,844 | 2011-10-19 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014530846A JP2014530846A (ja) | 2014-11-20 |
| JP2014530846A5 true JP2014530846A5 (ja) | 2015-11-26 |
Family
ID=47631462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014536349A Pending JP2014530846A (ja) | 2011-10-19 | 2012-10-12 | ホスホジエステラーゼ５型阻害薬の全身使用に伴う顔面潮紅の軽減方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9744168B2 (ja) |
| EP (1) | EP2768502A2 (ja) |
| JP (1) | JP2014530846A (ja) |
| KR (1) | KR20140091543A (ja) |
| CN (1) | CN103889417A (ja) |
| AU (1) | AU2012324543B2 (ja) |
| BR (1) | BR112014009210A2 (ja) |
| CA (1) | CA2850273A1 (ja) |
| IL (1) | IL231820A0 (ja) |
| MX (1) | MX2014004383A (ja) |
| RU (1) | RU2014119879A (ja) |
| WO (1) | WO2013057579A2 (ja) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120076738A1 (en) * | 2010-09-28 | 2012-03-29 | Michael Graeber | Combination treatment for dermatological conditions |
| MX2016016400A (es) * | 2014-06-11 | 2017-06-12 | Allergan Inc | Formulaciones de oximetazolina estabilizadas y sus usos. |
| CA3039561A1 (en) * | 2016-10-07 | 2018-04-12 | Micreos Human Health B.V. | Vasoconstrictive and antibacterial combination treatment for rosacea |
| KR102122980B1 (ko) * | 2018-12-28 | 2020-06-18 | 한국프라임제약주식회사 | 들깨 잎 추출물을 유효성분으로 함유하는 갱년기 관련 안면홍조 완화용 조성물 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3278447A (en) | 1963-12-02 | 1966-10-11 | Cloro Bac Products Inc | Process for stabilizing chlorine dioxide solution |
| DE2436883C2 (de) | 1974-07-29 | 1985-08-22 | Schering AG, 1000 Berlin und 4709 Bergkamen | Benzimidazol-Derivate, Verfahren zu ihrer Herstellung und diese enthaltende Arzneimittel |
| DE2436882A1 (de) | 1974-07-29 | 1976-02-19 | Schering Ag | Neue oxyphenylbutazon-derivate und ihre herstellung |
| DE2632678C2 (de) | 1976-07-16 | 1986-02-27 | Schering AG, 1000 Berlin und 4709 Bergkamen | 6α-Fluor-12α-Halogen-Kortikoide und Verfahren zu ihrer Herstellung |
| NZ185295A (en) | 1976-10-04 | 1980-04-28 | Schering Ag | 9-chloroprednisolone derivatives and pharmaceutical compositions |
| US4285967A (en) | 1978-06-30 | 1981-08-25 | Estee Lauder Inc. | Cosmetic preparation for reducing redness of blemishes |
| US4908387A (en) | 1988-06-06 | 1990-03-13 | The Regents Of The University Of California | Use of beta2 antagonists in the treatment of inflammatory diseases, in particular, rheumatoid arthritis |
| CA2003198C (en) | 1988-11-29 | 1995-03-21 | Anthony J. Dziabo, Jr. | Aqueous ophthalmic solutions and method for preserving same |
| US5736165A (en) | 1993-05-25 | 1998-04-07 | Allergan | In-the-eye use of chlorine dioxide-containing compositions |
| ES2187533T3 (es) | 1993-10-13 | 2003-06-16 | Allergan Inc | Usdo de derivados de (2-imidazolin-2-ilamino)quinoxalina. |
| US6117871A (en) | 1993-12-17 | 2000-09-12 | The Procter & Gamble Company | 6-(2-imidazolinylamino)quinoxaline compounds useful as alpha-2 adrenoceptor agonists |
| US6194415B1 (en) | 1995-06-28 | 2001-02-27 | Allergan Sales, Inc. | Method of using (2-imidazolin-2-ylamino) quinoxoalines in treating neural injury |
| CA2154979A1 (en) | 1995-07-28 | 1997-01-29 | Kenneth T. Armstrong | Topical phenylephrine preparation |
| US5910312A (en) | 1996-10-09 | 1999-06-08 | Ideal Ideas, Inc. | Acne treatment composition with vasoconstrictor |
| ES2239466T3 (es) | 1998-10-20 | 2005-09-16 | Omeros Corporation | Solucion de irrigacion y metodo de inhibicion del dolor y de la inflamacion. |
| SE9901295D0 (sv) | 1999-04-13 | 1999-04-13 | Jan Hedner | Sätt och medel för att förebygga, behandla och diagnostisera kardiovaskulära komplikationer hos patienter med obstruktiv sömnapné |
| EP1206282A1 (en) | 1999-08-19 | 2002-05-22 | Lavipharm S.A. | Film forming polymers, methods of use, and devices and applications thereof |
| US6468989B1 (en) | 2000-07-13 | 2002-10-22 | Dow Pharmaceutical Sciences | Gel compositions containing metronidazole |
| CN101897704B (zh) | 2000-07-14 | 2014-10-29 | 阿勒根公司 | 含有α-2肾上腺素能激动剂的组合物 |
| US6387383B1 (en) | 2000-08-03 | 2002-05-14 | Dow Pharmaceutical Sciences | Topical low-viscosity gel composition |
| US6680062B2 (en) | 2001-10-05 | 2004-01-20 | Color Access, Inc. | Anti-irritating rosacea treatment |
| US7345065B2 (en) | 2002-05-21 | 2008-03-18 | Allergan, Inc. | Methods and compositions for alleviating pain |
| US7439241B2 (en) | 2003-05-27 | 2008-10-21 | Galderma Laboratories, Inc. | Compounds, formulations, and methods for treating or preventing rosacea |
| US8410102B2 (en) | 2003-05-27 | 2013-04-02 | Galderma Laboratories Inc. | Methods and compositions for treating or preventing erythema |
| US20050020600A1 (en) * | 2003-07-23 | 2005-01-27 | Scherer Warren J. | Methods of treating cutaneous flushing using selective alpha-2-adrenergic receptor agonists |
| US7812049B2 (en) * | 2004-01-22 | 2010-10-12 | Vicept Therapeutics, Inc. | Method and therapeutic/cosmetic topical compositions for the treatment of rosacea and skin erythema using α1-adrenoceptor agonists |
| MXPA06013649A (es) * | 2004-05-25 | 2007-07-09 | Sansrosa Pharmaceutical Dev In | Compuestos, formulaciones, y metodos para tratar o prevenir desordenes inflamatorios de la piel. |
| US20090061020A1 (en) | 2007-08-31 | 2009-03-05 | Theobald Klaus P | Brimonidine Compositions for Treating Erythema |
| EP2230910A4 (en) | 2007-12-21 | 2011-04-13 | Galderma Lab Inc | PRE-SURGICAL TREATMENT |
| WO2009158144A1 (en) | 2008-05-30 | 2009-12-30 | Fairfield Clinical Trials Llc | Method and composition for dermatoses |
| US20100104624A1 (en) * | 2008-06-11 | 2010-04-29 | Peter Langecker | Combination therapy using phosphodiesterase inhibitors |
| EP3569223A1 (en) | 2009-10-30 | 2019-11-20 | Intratus, Inc. | Methods and compositions for sustained delivery of drugs |
| AU2011231543B2 (en) | 2010-03-26 | 2015-01-15 | Galderma Research & Development | Improved methods and compositions for safe and effective treatment of erythema |
-
2012
- 2012-10-12 US US14/344,099 patent/US9744168B2/en not_active Expired - Fee Related
- 2012-10-12 EP EP12821025.9A patent/EP2768502A2/en not_active Withdrawn
- 2012-10-12 BR BR112014009210A patent/BR112014009210A2/pt not_active IP Right Cessation
- 2012-10-12 CN CN201280051534.6A patent/CN103889417A/zh active Pending
- 2012-10-12 KR KR1020147011912A patent/KR20140091543A/ko not_active Application Discontinuation
- 2012-10-12 CA CA2850273A patent/CA2850273A1/en not_active Abandoned
- 2012-10-12 RU RU2014119879/15A patent/RU2014119879A/ru not_active Application Discontinuation
- 2012-10-12 AU AU2012324543A patent/AU2012324543B2/en not_active Expired - Fee Related
- 2012-10-12 JP JP2014536349A patent/JP2014530846A/ja active Pending
- 2012-10-12 WO PCT/IB2012/002500 patent/WO2013057579A2/en active Application Filing
- 2012-10-12 MX MX2014004383A patent/MX2014004383A/es unknown
-
2014
- 2014-03-31 IL IL231820A patent/IL231820A0/en unknown
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