KR940701264A - 안과질환에 대한 마크로라이드 화합물의 용도 - Google Patents
안과질환에 대한 마크로라이드 화합물의 용도Info
- Publication number
- KR940701264A KR940701264A KR1019930703221A KR930703221A KR940701264A KR 940701264 A KR940701264 A KR 940701264A KR 1019930703221 A KR1019930703221 A KR 1019930703221A KR 930703221 A KR930703221 A KR 930703221A KR 940701264 A KR940701264 A KR 940701264A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- independently represent
- compound
- allergic conjunctivitis
- represent
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 12
- 239000003120 macrolide antibiotic agent Substances 0.000 title claims abstract 6
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims abstract 7
- 208000002205 allergic conjunctivitis Diseases 0.000 claims abstract 7
- 208000024998 atopic conjunctivitis Diseases 0.000 claims abstract 7
- 239000000203 mixture Substances 0.000 claims abstract 2
- 238000011282 treatment Methods 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 230000000069 prophylactic effect Effects 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 238000000034 method Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000003700 epoxy group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- -1 methods Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 claims 1
- 230000002265 prevention 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61P27/14—Decongestants or antiallergics
-
- 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
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/01—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing oxygen
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
본 발명은 안과질환, 특히 알레르기성 결막염의 예방 또는 치료를 위한 FRZ-900506 및 그와 관련 화합물과 같은 마크로라이드 화합물에 관한 것이다. 또한 본 발명은 이 화합물을 함유하는 조성물에 관한 것이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- 알레르기성 결막염의 예방 또는 치료를 위한 하기 일반식(I)의 마크로라이드 화합물 또는 그의 약제학적으로 허용되는 염의 용도.상기식에서, 인접한 치환체쌍 [R1및 R2], [R3및 R4], [R5및 R6]은 각각 독립적으로 a) 두개의 인접한 수소원자를 나타내거나, b) 이들이 부착되어 있는 인접한 탄소원자 사이에서 제2의 결합을 형성하며, 상기 언급한 정의 이외에 R2는 또한 알킬 그룹을 나타낼 수도 있으며; R7은 H, OH, 보호된 하이드록시 또는 O-알킬을 나타내거나, R1과 함께 =0를 나타낼 수도 있고; R8및 R9는 각각 독립적으로 H 또는 OH를 나타내며; R10은 H, 알킬, 하나 또는 그 이상의 하이드록실 그룹에 의해 치환된 알킬, 알케닐, 하나 또는 그 이상의 하이드록실 그룹에 의해 치환된 알케닐, 또는 =0에 의해 치환된 알킬을 나타내고; X는 O, (H, OH), (H, H) 또는 -CH2O-를 나타내며; Y는 O, (H, OH), (H, H), N-NR11R12또는 N-OR13을 나타내고; R11및 R12는 각각 독립적으로 H, 알킬, 아릴 또는 토실을 나타내며; R13, R14, R15, R16, R17, R18, R19, R22및 R23은 각각 독립적으로 H 또는 알킬을 나타내고; R20및 R21은 각각 독립적으로 O를 나타내거나, 이들은 독립적으로 (Ra 20,H) 및 (Ra 21,H)를 각각 나타낼 수도 있으며; Ra 20및 Ra 21는 각각 독립적으로 OH, O-알킬 또는 OCH2OCH2CH2OCH3을 나타내거나, Ra 21은 보호된 하이드록시를 나타내고; Ra 20및 Ra 21은 또한 함께, 에폭사이드환중의 산소 원자를 나타낼 수 있으며; n은 1, 2 또는 3이고; 상기 언급한 정의 이외에도, Y, R10및 R23은 이들이 부착되어 있는 탄소원자와 함께 포화되거나 불포화될 수 있으며, 알킬, 하이드록시, 하나 또는 그 이상의 하이드록실 그룹에 의해 치환된 알킬, O-알킬, 벤질 및 -CH2Se(C6H5) 중에서 선택된 하나 또는 그 이상의 그룹에 의해치환될 수 있는 5- 또는 6-원 N-, S- 또는 O-함유 헤테로사이클릭환을 나타낼 수 있다.
- 제1항에서 정의된 마크로라이드 화합물(I)의 알레르기성 결막염의 예방 또는 치료제로서의 용도.
- 제1항에서 정의된 마크로라이드 화합물(I)을 함유하는 알레르기성 결막염에 대한 예방 또는 치료제.
- 제1항에서 정의된 마이크로라이드 화합물(I)을 포유동물에서 투여함을 특징으로 하는 알레르기성 결막염을 예방 또는 치료하는 방법.
- 알레르기성 결막염을 예방 또는 치료제를 제조하기 위한, 제1항에서 정의된 마이크로라이드 화합물(I)의 용도.
- 담체 또는 부형제와의 혼합물로서 제1항에 정의된 마이크로라이드 화합물(I)을 함유함을 특징으로 하는, 알레르기성 결막염에 대한 약제학적 조성물.
- 마크로라이드 화합물(I)을 담체 또는 부형제와 혼합시킴을 특징으로 하여 제6항에 따르는 약제학적 조성물을 제조하는 방법.
- 제1항 내지 7항에 사용된 마이크로라이드 화합물인 FK 506
- 실질적으로 본 명세서에 기술된 것으로, 본 발명에 따르는 용도, 예방 또는 치료제, 방법, 약제학적 조성물 또는 제조방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9109060.5 | 1991-04-26 | ||
GB919109060A GB9109060D0 (en) | 1991-04-26 | 1991-04-26 | New use |
GB9121661.4 | 1991-10-11 | ||
GB919121661A GB9121661D0 (en) | 1991-10-11 | 1991-10-11 | New use |
PCT/JP1992/000545 WO1992019278A1 (en) | 1991-04-26 | 1992-04-24 | Use of macrolide compounds for eye diseases |
Publications (2)
Publication Number | Publication Date |
---|---|
KR940701264A true KR940701264A (ko) | 1994-05-28 |
KR100237715B1 KR100237715B1 (ko) | 2000-02-01 |
Family
ID=26298796
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019930703221A KR100237715B1 (ko) | 1991-04-26 | 1992-04-24 | 안과질환에 대한 마크로라이드 화합물의 용도 |
Country Status (11)
Country | Link |
---|---|
US (1) | US5514686A (ko) |
EP (1) | EP0581959B1 (ko) |
JP (1) | JP3158437B2 (ko) |
KR (1) | KR100237715B1 (ko) |
AT (1) | ATE198708T1 (ko) |
CA (1) | CA2102241C (ko) |
DE (1) | DE69231644T2 (ko) |
DK (1) | DK0581959T3 (ko) |
ES (1) | ES2154262T3 (ko) |
GR (1) | GR3035269T3 (ko) |
WO (1) | WO1992019278A1 (ko) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BE1009856A5 (fr) * | 1995-07-14 | 1997-10-07 | Sandoz Sa | Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule. |
US6384073B1 (en) * | 1998-02-23 | 2002-05-07 | Fujisawa Pharmaceutical Co., Ltd. | Use of macrolide compounds for treating glaucoma |
US6376517B1 (en) * | 1998-08-14 | 2002-04-23 | Gpi Nil Holdings, Inc. | Pipecolic acid derivatives for vision and memory disorders |
US7338976B1 (en) | 1998-08-14 | 2008-03-04 | Gpi Nil Holdings, Inc. | Heterocyclic esters or amides for vision and memory disorders |
US6506788B1 (en) | 1998-08-14 | 2003-01-14 | Gpi Nil Holdings, Inc. | N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders |
US6337340B1 (en) | 1998-08-14 | 2002-01-08 | Gpi Nil Holdings, Inc. | Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders |
US7410995B1 (en) | 1998-08-14 | 2008-08-12 | Gpi Nil Holdings Inc. | N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders |
US6384056B1 (en) | 1998-08-14 | 2002-05-07 | Gpi Nil Holdings, Inc. | Heterocyclic thioesters or ketones for vision and memory disorders |
US6333340B1 (en) | 1998-08-14 | 2001-12-25 | Gpi Nil Holdings, Inc. | Small molecule sulfonamides for vision and memory disorders |
US6218423B1 (en) | 1998-08-14 | 2001-04-17 | Gpi Nil Holdings, Inc. | Pyrrolidine derivatives for vision and memory disorders |
US6339101B1 (en) | 1998-08-14 | 2002-01-15 | Gpi Nil Holdings, Inc. | N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders |
US6335348B1 (en) | 1998-08-14 | 2002-01-01 | Gpi Nil Holdings, Inc. | Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders |
US6399648B1 (en) | 1998-08-14 | 2002-06-04 | Gpi Nil Holdings, Inc. | N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders |
US7265150B1 (en) | 1998-08-14 | 2007-09-04 | Gpi Nil Holdings Inc. | Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders |
EP1173177B2 (en) * | 1999-04-30 | 2014-03-05 | Sucampo AG | Use of macrolide compounds for the treatment of dry eye |
AR033151A1 (es) * | 2001-04-12 | 2003-12-03 | Sucampo Pharmaceuticals Inc | Agente para el tratamiento oftalmico topico de las enfermedades inflamatorias oculares |
CN1259049C (zh) | 2001-07-06 | 2006-06-14 | 苏坎波公司 | 包含白介素-2抑制剂和抗菌剂的局部给药组合物 |
PL368642A1 (en) * | 2001-11-19 | 2005-04-04 | Novartis Ag | Use of an ascomycin for the treatment of blepharitis |
WO2003043650A1 (en) * | 2001-11-21 | 2003-05-30 | Sucampo Ag | Use of fk506 and analogues for treating allergic diseases |
CA2495103A1 (en) * | 2002-08-09 | 2004-02-19 | Sucampo Pharmaceuticals, Inc. | Pharmaceutical compositions comprising fk506 derivatives and their use for the treatment of allergic diseases |
PT1539157E (pt) * | 2002-09-18 | 2013-10-04 | Univ Pennsylvania | Rapamicina para utilização na inibição ou prevenção de neovascularização coroidal |
AR042890A1 (es) * | 2003-01-16 | 2005-07-06 | Sucampo Pharmaceuticals Inc | Metodo de tratamiento del ojo seco con una composicion oftalmica que contiene un compuesto macrolido |
CN1882338A (zh) * | 2003-09-18 | 2006-12-20 | 马库赛特公司 | 经巩膜递送 |
US8663639B2 (en) * | 2005-02-09 | 2014-03-04 | Santen Pharmaceutical Co., Ltd. | Formulations for treating ocular diseases and conditions |
ES2564194T3 (es) | 2005-02-09 | 2016-03-18 | Santen Pharmaceutical Co., Ltd. | Formulaciones líquidas para el tratamiento de enfermedades o dolencias |
BRPI0707612B8 (pt) | 2006-02-09 | 2021-05-25 | Macusight Inc | vaso lacrado e formulações líquidas contidas no mesmo |
US8222271B2 (en) | 2006-03-23 | 2012-07-17 | Santen Pharmaceutical Co., Ltd. | Formulations and methods for vascular permeability-related diseases or conditions |
ES2435197T3 (es) * | 2007-01-10 | 2013-12-16 | Board Of Regents, The University Of Texas System | Administración mejorada de composiciones de fármacos inmunosupresores para la administración por vía pulmonar |
US20080265343A1 (en) * | 2007-04-26 | 2008-10-30 | International Business Machines Corporation | Field effect transistor with inverted t shaped gate electrode and methods for fabrication thereof |
US11766421B2 (en) | 2017-09-25 | 2023-09-26 | Surface Ophthalmics, Inc. | Ophthalmic pharmaceutical compositions and methods for treating ocular surface disease |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4894366A (en) * | 1984-12-03 | 1990-01-16 | Fujisawa Pharmaceutical Company, Ltd. | Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same |
GB8616089D0 (en) * | 1986-07-02 | 1986-08-06 | Univ Manchester | Organic compounds |
AU630866B2 (en) * | 1987-12-09 | 1992-11-12 | Fisons Plc | Macrocyclic compounds |
EP0356399A3 (en) * | 1988-08-26 | 1991-03-20 | Sandoz Ag | Substituted 4-azatricyclo (22.3.1.04.9) octacos-18-ene derivatives, their preparation and pharmaceutical compositions containing them |
DE3906214A1 (de) * | 1989-02-28 | 1990-08-30 | Boehringer Mannheim Gmbh | Verwendung von macrolactone als antiallergica |
AU5187990A (en) * | 1989-03-02 | 1990-09-26 | Ensoniq Corporation | Apparatus and a method for fitting a hearing aid |
IE64214B1 (en) * | 1989-06-06 | 1995-07-26 | Fujisawa Pharmaceutical Co | Macrolides for the treatment of reversible obstructive airways diseases |
US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
KR920700212A (ko) * | 1989-06-14 | 1992-02-19 | 쟝 크라머·한스 루돌프 하우스 | 헤테로원자-함유 트리사이클릭 화합물 |
AU635286B2 (en) * | 1989-07-05 | 1993-03-18 | Astellas Pharma Inc. | Aqueous liquid composition for external use |
ZA924953B (en) * | 1991-07-25 | 1993-04-28 | Univ Louisville Res Found | Method of treating ocular inflammation |
-
1992
- 1992-04-24 DE DE69231644T patent/DE69231644T2/de not_active Expired - Lifetime
- 1992-04-24 US US08/133,194 patent/US5514686A/en not_active Expired - Lifetime
- 1992-04-24 EP EP92909558A patent/EP0581959B1/en not_active Expired - Lifetime
- 1992-04-24 CA CA002102241A patent/CA2102241C/en not_active Expired - Lifetime
- 1992-04-24 AT AT92909558T patent/ATE198708T1/de active
- 1992-04-24 KR KR1019930703221A patent/KR100237715B1/ko not_active IP Right Cessation
- 1992-04-24 WO PCT/JP1992/000545 patent/WO1992019278A1/en active IP Right Grant
- 1992-04-24 JP JP50869892A patent/JP3158437B2/ja not_active Expired - Lifetime
- 1992-04-24 DK DK92909558T patent/DK0581959T3/da active
- 1992-04-24 ES ES92909558T patent/ES2154262T3/es not_active Expired - Lifetime
-
2001
- 2001-01-18 GR GR20000402818T patent/GR3035269T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
ATE198708T1 (de) | 2001-02-15 |
DK0581959T3 (da) | 2001-01-29 |
EP0581959A1 (en) | 1994-02-09 |
JP3158437B2 (ja) | 2001-04-23 |
GR3035269T3 (en) | 2001-04-30 |
CA2102241A1 (en) | 1992-10-27 |
ES2154262T3 (es) | 2001-04-01 |
KR100237715B1 (ko) | 2000-02-01 |
DE69231644D1 (de) | 2001-02-22 |
WO1992019278A1 (en) | 1992-11-12 |
US5514686A (en) | 1996-05-07 |
JPH07500570A (ja) | 1995-01-19 |
EP0581959B1 (en) | 2001-01-17 |
DE69231644T2 (de) | 2001-05-23 |
CA2102241C (en) | 2003-12-30 |
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