KR920019348A - 탄산탈수효소 억제제 및 β-아드레날린 길항제의 배합물을 포함하는 안과용 조성물 - Google Patents

탄산탈수효소 억제제 및 β-아드레날린 길항제의 배합물을 포함하는 안과용 조성물 Download PDF

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KR920019348A
KR920019348A KR1019920006335A KR920006335A KR920019348A KR 920019348 A KR920019348 A KR 920019348A KR 1019920006335 A KR1019920006335 A KR 1019920006335A KR 920006335 A KR920006335 A KR 920006335A KR 920019348 A KR920019348 A KR 920019348A
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carbonic anhydrase
formulation
anhydrase inhibitor
ophthalmologically acceptable
adrenergic antagonist
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KR1019920006335A
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English (en)
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제이. 볼드윈 존
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제임스 에프. 노턴
머크 앤드 캄파니, 인코포레이티드
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Application filed by 제임스 에프. 노턴, 머크 앤드 캄파니, 인코포레이티드 filed Critical 제임스 에프. 노턴
Publication of KR920019348A publication Critical patent/KR920019348A/ko

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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

탄산탈수효소 억제제 및 β-아드레날린 길항제의 배합물을 포함하는 안과용 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 예비연구로부터 IOP의 평균 변화율(%)을 도시한 것이다.

Claims (10)

  1. 안과학적으로 허용되는 담체, 탄산탈수효소 억제제 또는 안과학적으로 허용되는 이의 염 0.5 내지 5%(w/w) 및 β-아드레날린 길항제 또는 안과학적으로 허용되는 이의 염 0.01 내지 1.0%를 포함하는 안내압이 높은 환자를 치료하기 위한 안과용 제제.
  2. 제1항에 있어서, 탄산탈수효소 억제제 농도가 0.5 내지 3%이며 β-아드레날린 길항제 농도가 0.1 내지 0.5%인 제제.
  3. 제1항 또는 제2항에 있어서, 안과학적으로 허용되는 담체, 일반식(I)의 탄산탈수효소 억제제, 개별적인 부분입체 이성체, 에난티오머, 이의 혼합물 또는 안과학적으로 허용되는 이의 염 0.05 내지 5% 베탁솔올, 부페놀올, 카르테올올, 레보부놀올, 메티프란올올 및 티몰올 또한 안과학적으로 허용되는 이의 염으로부터 선택된 β-아드레날린 길항제 0.01 내지 1.0%를 포함하는, 높은 안내압의 치료를 위한 안과용 제제.
    상기 식에서, A는 탄소 또는 질소이고, Z는 -NHR 또는 -OR이고, R은 직쇄 또는 측쇄의 C1-6알킬이고, R1은 수소, C1-3알킬, 또는 C1-4알콕시, -C1-4알킬이고, X는 -S(O)2- 또는 -C(O)-이다.
  4. 제3항에 있어서, A가 탄소이고, Z는 -NHR이고 X는 -SO2-인 제제.
  5. 제3항 또는 제4항에 있어서, R이 -CH2CH3, -CH2CH2CH3또는 CH2CH(CH3)2이고, R1은 수소, -CH3, -CH2CH|2CH3, -CH2CH2CH2CH3또는 -CH2OCH2CH3인 제제.
  6. 제1항 내지 제5항 중 어느 한 항에 있어서, β-아드레날린 길항제가 티몰올 또는 안과학적으로 허용되는 이의 염인 제제.
  7. 제3 내지 제6항 중 어느 한 항에 있어서, A는 탄소이고, R은 -CH2CH3이고 R1은 -CH2CH2CH3이고, R1은 V-CH3dlrjsk, R은 -CH2CH2CH|2OCH3이거나, R은 -CH2CH3이고 R1은 -CH2CH2CH3이거나, R은 CH2CH2(CH3)2이고 R1은 수소이거나, R은 -CH2CH3이고 R1은 -CH2OCH2CH3이고 탄산탈수 효소 억제제의 탄소 4 및 6은 둘 모두 S 절대 입체화학배열인 제제.
  8. 제7항에 있어서, 탄산탈수효소 억제제의 농도는 0.7 또는 2.0%이고 티몰올의 농도는 0.5%인 제제.
  9. 제1항 내지 제8항 중 어느 한 항에 있어서, 겔란 고무 0.1 내지 2%를 추가로 포함하는 제제.
  10. 제1항 내지 제9항 중 어느 한 항의 제제의 단위 투여량을 치료를 필요로 하는 환자에게 국소 안내 투여함을 포함하여 높은 안내압을 치료하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920006335A 1991-04-17 1992-04-16 탄산탈수효소 억제제 및 β-아드레날린 길항제의 배합물을 포함하는 안과용 조성물 KR920019348A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US68671891A 1991-04-17 1991-04-17
US07/686,718 1991-04-17
US83491392A 1992-02-13 1992-02-13
US07/834,913 1992-02-13

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KR920019348A true KR920019348A (ko) 1992-11-19

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EP (1) EP0509752B1 (ko)
JP (1) JP2527513B2 (ko)
KR (1) KR920019348A (ko)
CN (1) CN1073421C (ko)
AT (1) ATE182787T1 (ko)
AU (1) AU648659C (ko)
CA (1) CA2065965C (ko)
CH (1) CH0509752H1 (ko)
CY (1) CY2146B1 (ko)
CZ (1) CZ285129B6 (ko)
DE (3) DE69229688T4 (ko)
DK (1) DK0509752T3 (ko)
ES (1) ES2133304T3 (ko)
GR (1) GR3031467T3 (ko)
HK (1) HK1009251A1 (ko)
IE (1) IE921240A1 (ko)
IL (1) IL101537A (ko)
LU (1) LU90506I2 (ko)
MX (1) MX9201785A (ko)
NL (1) NL990041I2 (ko)
NO (1) NO306196B1 (ko)
RO (1) RO113612B1 (ko)
SK (1) SK282039B6 (ko)
WO (1) WO1992018124A1 (ko)
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Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993016701A2 (en) * 1992-02-21 1993-09-02 Alcon Laboratories, Inc. Topical antiglaucoma compositions comprising carbonic anhydrase inhibitors and beta-blockers
US5932572A (en) * 1992-02-21 1999-08-03 Alcon Laboratories, Inc. Topical anti-glaucoma compositions
US6071904A (en) * 1996-12-11 2000-06-06 Alcon Laboratories, Inc. Process for manufacturing ophthalmic suspensions
FI981473A (fi) * 1998-06-25 1999-12-26 Orion Yhtymae Oyj Menetelmä pulmonaalihypertension hoitamiseksi
TWI298257B (en) 2001-05-31 2008-07-01 Allergan Inc Hypotensive lipid and timolol compositions and methods of using same
CN100345594C (zh) * 2004-01-19 2007-10-31 无锡杰西医药科技有限公司 乙酰唑胺滴眼液
US8211450B2 (en) * 2010-05-05 2012-07-03 Senju Usa, Inc. Ophthalmic composition
SI3431074T1 (sl) 2010-07-29 2022-07-29 Allergan, Inc. Raztopine bimatoprosta in timolola brez konzervansov
US9061034B2 (en) 2010-07-29 2015-06-23 Allergan, Inc. Preservative free bimatoprost and timolol solutions
JP5893204B1 (ja) * 2015-02-23 2016-03-23 参天製薬株式会社 防腐効果のある医薬の組合せ
JP6132968B1 (ja) * 2016-01-29 2017-05-24 参天製薬株式会社 ドルゾラミド、高分子およびホウ酸を含有する医薬組成物

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4863922A (en) * 1984-12-12 1989-09-05 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use

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ES2133304T3 (es) 1999-09-16
DE69229688D1 (de) 1999-09-09
AU648659C (en) 2008-02-14
YU39392A (sh) 1995-12-04
DE10075002I1 (de) 2000-03-30
IL101537A0 (en) 1992-12-30
RO113612B1 (ro) 1998-09-30
GR3031467T3 (en) 2000-01-31
CN1073421C (zh) 2001-10-24
DK0509752T3 (da) 1999-12-06
NO933714L (no) 1993-10-15
CH0509752H1 (ko) 2012-11-30
AU648659B2 (en) 1994-04-28
SK282039B6 (sk) 2001-10-08
CZ209893A3 (en) 1994-06-15
NO306196B1 (no) 1999-10-04
CN1066781A (zh) 1992-12-09
NO933714D0 (no) 1993-10-15
CZ285129B6 (cs) 1999-05-12
LU90506I2 (fr) 2000-03-28
WO1992018124A1 (en) 1992-10-29
CY2146B1 (en) 2002-06-21
DE69229688C5 (de) 2010-10-21
EP0509752B1 (en) 1999-08-04
CA2065965A1 (en) 1992-10-18
JP2527513B2 (ja) 1996-08-28
DE69229688T4 (de) 2010-08-19
IL101537A (en) 1997-11-20
IE921240A1 (en) 1992-10-21
HK1009251A1 (en) 1999-05-28
DE10075002I2 (de) 2004-07-01
EP0509752A2 (en) 1992-10-21
EP0509752A3 (en) 1993-03-03
MX9201785A (es) 1992-10-01
JPH05117167A (ja) 1993-05-14
DE69229688T2 (de) 2000-02-24
AU1497992A (en) 1992-10-22
NL990041I1 (nl) 2000-02-01
ATE182787T1 (de) 1999-08-15
NL990041I2 (nl) 2000-04-03
SK110393A3 (en) 1994-02-02
CA2065965C (en) 1998-06-16

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