KR960700743A - Combination of Retroviral Inhibitors - Google Patents

Combination of Retroviral Inhibitors Download PDF

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Publication number
KR960700743A
KR960700743A KR1019950703531A KR19950703531A KR960700743A KR 960700743 A KR960700743 A KR 960700743A KR 1019950703531 A KR1019950703531 A KR 1019950703531A KR 19950703531 A KR19950703531 A KR 19950703531A KR 960700743 A KR960700743 A KR 960700743A
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KR
South Korea
Prior art keywords
benzyl
formula
benzyloxy
compound
pharmaceutical composition
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KR1019950703531A
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Korean (ko)
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KR100293299B1 (en
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에이. 스탠리 탐스
데브라 엘 테일러
Original Assignee
게리 디. 스트리트
메렐 다우 파마슈티칼스 인크
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Publication of KR100293299B1 publication Critical patent/KR100293299B1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

카스타노스피민 에스테르 및 짧은 펩티드 유사물의 조합은 레트로비루스 감염의 치료에 사용할 수 있다. 그 조합은 AIDS 및 ARC와 기타 레트로비루스 HIV 또는 다른 연관된 비루스에 의한 질병의 치료를 위해 사용될 수 있다.Combinations of castanospirin esters and short peptide analogs can be used for the treatment of retrovirus infection. The combination can be used for the treatment of diseases caused by AIDS and ARC and other retrovirus HIV or other related viruses.

Description

레트로비루스 억제제의 조합(Combination of Retroviral inhibitors)Combination of Retroviral Inhibitors

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (9)

식 (Ⅰ)Formula (Ⅰ) (상기 식에서, R1은 C1-8알카노일, C1-10알케노일, C1-8알콕시아세틸, 또는 알킬 또는 할로겐 기로 임의로 치환된 벤조일이다)의 화합물 또는 그의 약제학적으로 허용가능한 염 및 식(Ⅱ)Wherein R 1 is C 1-8 alkanoyl, C 1-10 alkenoyl, C 1-8 alkoxyacetyl, or benzoyl optionally substituted with an alkyl or halogen group, or a pharmaceutically acceptable salt thereof Formula (Ⅱ) (상기 식에서, R1은 벤질록시,(3-피리딜)에틸, 이소퀴놀일, 4-알콕시-벤질록시, 또는 모르폴릴이고, P2는 이소프로필, 시클로펜틸, 2-(4, 4-디플루오로)-피롤리딜, 2-히드록시-2-프로필, t-부틸이며,P1은 피페로닐, 4-(벤질록시)벤질, 3-(벤질록시)벤질, (4-벤질록시-3메톡시)벤질이고, R5가 H일 때, R6은 벤질, 피페로닐, CH2-피리딜, 4-(벤질록시)벤질, 모르폴리노, 테트라히드로이소쿠놀일, 4-(3-히드록시프로필)벤질, 2-(3-히드록시프로필)벤질, 및또는 Y 및 Z는 둘다 일반적으로 정의되나 특히(특히 D형태의)Y가 이소프로필, 또는 페닐이고, Z가 벤질록시메틸렌, CHO, COOH, 알콕시 또는 COOR4인 -CH(Y)(Z)이고, R5가 H가 아닐 때, R5는 메틸, 4-히드록시부틸 또는 3-히드록시프로필이고 R6는 벤족시 또는 벤질이며, R5및 R6가 질소가 붙는 헤테로환 부를 형성할 때및 모르폴리노가 헤테로환 부인 것이 바람직하다)의 화합물 및 그의 수화물, 동배체 및 약제학적으로 허용가능한 염을 포함하는 약제학적 조성물.Wherein R 1 is benzyloxy, (3-pyridyl) ethyl, isoquinolyl, 4-alkoxy-benzyloxy, or morpholinyl, P 2 is isopropyl, cyclopentyl, 2- (4, 4-difluoro) -pyrrolidyl, 2 -Hydroxy-2-propyl, t-butyl, P 1 is piperonyl, 4- (benzyloxy) benzyl, 3- (benzyloxy) benzyl, (4-benzyloxy-3methoxy) benzyl, R When 5 is H, R 6 is benzyl, piperonyl, CH 2 -pyridyl, 4- (benzyloxy) benzyl, morpholino, tetrahydroisokunolyl, 4- (3-hydroxypropyl) benzyl, 2- (3-hydroxypropyl) benzyl, and Or both Y and Z are generally defined but in particular (especially in the form of D) -CH (Y) (Z) wherein Y is isopropyl, or phenyl, Z is benzyloxymethylene, CHO, COOH, alkoxy or COOR 4 When R 5 is not H, R 5 is methyl, 4-hydroxybutyl or 3-hydroxypropyl and R 6 is benzox or benzyl, and R 5 and R 6 form a heterocyclic moiety with nitrogen; And morpholino is preferably heterocyclic denaturation) and a hydrate, isotope and pharmaceutically acceptable salt thereof. 제1항에 있어서, 식(Ⅱ)의 화합물이, N-3차 부틸-데카히드로-2[R(R)-히드록시-4-페닐-3(S)-[[N(2-퀴놀일카르보닐)-L-아스파라기닐]아미노]-부틸]-(4aS, 8aS)-이소퀴놀린-3(S)-카르복사미드, [1(S)-[[3,3-디플루오로-2,4-디옥소-1-[[4-(페닐메틸)아미노]부틸]아미노카르보닐]-2-메틸프로필]카르보아민산, 페닐메틸 에스테르, 또는 N-[4-(N-벤질록시카르보닐-L-발릴)아미노--2,2-디플루오로-1,3,-디옥소-5-(e-벤질록시)페닐-펜틸]-(0-벤질)-D-발리놀인 약제학적 조성물The compound of formula (II) according to claim 1, wherein the compound of formula (II) is N-tert-butyl-decahydro-2 [R (R) -hydroxy-4-phenyl-3 (S)-[[N (2-quinolyl). Carbonyl) -L-asparaginyl] amino] -butyl]-(4aS, 8aS) -isoquinoline-3 (S) -carboxamide, [1 (S)-[[3,3-difluoro- 2,4-dioxo-1-[[4- (phenylmethyl) amino] butyl] aminocarbonyl] -2-methylpropyl] carboamine acid, phenylmethyl ester, or N- [4- (N-benzyloxy Carbonyl-L-valyl) amino--2,2-difluoro-1,3, -dioxo-5- (e-benzyloxy) phenyl-pentyl]-(0-benzyl) -D-valinolyn Pharmaceutical composition 제1항에 있어서, 제2항의 화합물이 10%이상의 양인 약제학적 조성물The pharmaceutical composition of claim 1, wherein the compound of claim 2 is in an amount of at least 10%. 제1항에 있어서, 식(Ⅰ)의 화합물이 [1S-(1a,6b,7a,8b,8ab]-옥타히드로-1,6,7,8-인돌리진테트롤 6-부타노에이트인 약제학적 조성물The agent according to claim 1, wherein the compound of formula (I) is [1S- (1a, 6b, 7a, 8b, 8ab] -octahydro-1,6,7,8-indolizintetrol 6-butanoate Pharmaceutical composition 제4항에 있어서, 10% 이상의 식(Ⅰ)의 화합물을 포함하는 약제학적 조성물The pharmaceutical composition of claim 4 comprising at least 10% of a compound of formula (I). 상기 임의의 항에 있어서, 비경구 투여용 약제학적 조성물The pharmaceutical composition according to any of the above, for parenteral administration. 상기 임의의 항에 있어서, 허용가능한 약제학적 담체에서의 생리적으로 기증적인 염 또는 그의 기타 유도체로서의 식(Ⅰ)의 화합물 및 식(Ⅱ)의 화합물을 포함하는 약제학적 조성물A pharmaceutical composition according to any of the above, comprising a compound of formula (I) and a compound of formula (II) as physiologically donating salts or other derivatives thereof in an acceptable pharmaceutical carrier. 제1항에 따른 조성물의 항비루스 유효량을 환자에게 투여함을 포함하는 이를 필요로 하는 환자의 HIV 감염 치료방법A method for treating HIV infection in a patient in need thereof comprising administering to the patient an antiviral effective amount of the composition of claim 1 HIV 감염을 치료하기 위하여 동시에 분리하여 또는 연속적으로 사용하기 위한 조합 제조물로서 제1항 또는 2항에 정의된 식(Ⅱ)의 화합물을 함유하는 제품A product containing a compound of formula (II) as defined in claim 1 or 2 as a combination preparation for simultaneous or separate use for the treatment of HIV infection. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019950703531A 1993-02-22 1994-01-18 Retrovirus inhibitor compound KR100293299B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9303518.6 1993-02-22
GB939303518A GB9303518D0 (en) 1993-02-22 1993-02-22 Combinations of retroviral inhibitors
PCT/US1994/000710 WO1994019008A1 (en) 1993-02-22 1994-01-18 Combinations of retroviral inhibitors

Publications (2)

Publication Number Publication Date
KR960700743A true KR960700743A (en) 1996-02-24
KR100293299B1 KR100293299B1 (en) 2001-09-17

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ID=10730826

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KR1019950703531A KR100293299B1 (en) 1993-02-22 1994-01-18 Retrovirus inhibitor compound

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EP (1) EP0684836A1 (en)
JP (1) JPH08509469A (en)
KR (1) KR100293299B1 (en)
CN (1) CN1118142A (en)
AU (1) AU679497B2 (en)
CA (1) CA2155129C (en)
GB (1) GB9303518D0 (en)
HU (1) HUT72493A (en)
IL (1) IL108696A (en)
MX (1) MXPA94001311A (en)
NO (1) NO307738B1 (en)
NZ (1) NZ261740A (en)
WO (1) WO1994019008A1 (en)
ZA (1) ZA941036B (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2889014A1 (en) 2005-07-22 2007-01-26 Nextamp Sa METHOD AND DEVICE FOR TATOOTING HORODATES, METHOD AND DEVICE FOR DECODING HORODATES, APPLICATIONS AND CORRESPONDING COMPUTER PROGRAM PRODUCTS

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3526015A1 (en) * 1985-07-20 1987-01-22 Philips Patentverwaltung METHOD FOR DETERMINING THE SPATIAL DISTRIBUTION OF THE SPREAD CROSS SECTIONS FOR ELASTICALLY SCREENED X-RAY RADIATION AND ARRANGEMENT FOR IMPLEMENTING THE METHOD
US5004746A (en) * 1987-09-29 1991-04-02 Merrell Dow Pharmaceuticals Inc. Anti-retroviral castanospermine esters
US4999146A (en) * 1990-02-12 1991-03-12 Thermax Wire Corp. Process for manufacture of low density polytetrofluoroethylene insulated cable
HU210647B (en) * 1991-01-02 1995-06-28 Merrell Dow Pharma Process for producing antiviral difluoro-statone derivatives and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
ZA941036B (en) 1994-08-25
HUT72493A (en) 1996-05-28
HU9502451D0 (en) 1995-10-30
CA2155129C (en) 1999-04-13
NZ261740A (en) 1996-10-28
NO953272D0 (en) 1995-08-21
NO307738B1 (en) 2000-05-22
EP0684836A1 (en) 1995-12-06
NO953272L (en) 1995-08-21
CN1118142A (en) 1996-03-06
MXPA94001311A (en) 2003-11-13
IL108696A (en) 1999-06-20
AU679497B2 (en) 1997-07-03
IL108696A0 (en) 1994-05-30
CA2155129A1 (en) 1994-09-01
AU6091894A (en) 1994-09-14
GB9303518D0 (en) 1993-04-07
JPH08509469A (en) 1996-10-08
KR100293299B1 (en) 2001-09-17
WO1994019008A1 (en) 1994-09-01

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