SK6842000A3 - A mixture of inhibitors, a combined pharmaceutical composition comprising the same and use thereof - Google Patents

A mixture of inhibitors, a combined pharmaceutical composition comprising the same and use thereof Download PDF

Info

Publication number: SK6842000A3
Authority: SK; Slovakia
Prior art keywords: compound; indinavir; pharmaceutically acceptable; acceptable salt; ester
Prior art date: 1997-11-13

Application number

SK684-2000A

Other languages

English (en)

Slovak (sk)

Inventor

Joseph P Vacca

Jiunn H Lin

Kuang C Yeh

Jeffrey A Chodakewitz

Paul J Deutsch

William D Ju

Original Assignee

Merck & Co Inc

Priority date (The priority date 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 date listed.)

1997-11-13

Filing date

1998-11-12

Publication date

2000-12-11

1998-04-15 Priority claimed from GBGB9807938.7A external-priority patent/GB9807938D0/en

1998-09-08 Priority claimed from GBGB9819590.2A external-priority patent/GB9819590D0/en

1998-11-12 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

2000-12-11 Publication of SK6842000A3 publication Critical patent/SK6842000A3/sk

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 15
239000000203 mixture Substances 0.000 title claims description 68
239000003112 inhibitor Substances 0.000 title claims description 6
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NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims abstract description 237
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CBVCZFGXHXORBI-PXQQMZJSSA-N indinavir Chemical compound C([C@H](N(CC1)C[C@@H](O)C[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H]2C3=CC=CC=C3C[C@H]2O)C(=O)NC(C)(C)C)N1CC1=CC=CN=C1 CBVCZFGXHXORBI-PXQQMZJSSA-N 0.000 claims description 144
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WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 claims description 42
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229910000033 sodium borohydride Inorganic materials 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
235000009518 sodium iodide Nutrition 0.000 description 1
239000012321 sodium triacetoxyborohydride Substances 0.000 description 1
HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
230000003381 solubilizing effect Effects 0.000 description 1
239000007921 spray Substances 0.000 description 1
238000003756 stirring Methods 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
238000010254 subcutaneous injection Methods 0.000 description 1
239000000126 substance Substances 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000000829 suppository Substances 0.000 description 1
238000001356 surgical procedure Methods 0.000 description 1
229940054565 sustiva Drugs 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
230000002195 synergetic effect Effects 0.000 description 1
230000001839 systemic circulation Effects 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
229940095064 tartrate Drugs 0.000 description 1
JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
238000011285 therapeutic regimen Methods 0.000 description 1
238000000003 thermogravimetry coupled to Fourier transform infrared spectroscopy Methods 0.000 description 1
239000004408 titanium dioxide Substances 0.000 description 1
235000010215 titanium dioxide Nutrition 0.000 description 1
238000004448 titration Methods 0.000 description 1
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
230000001988 toxicity Effects 0.000 description 1
231100000419 toxicity Toxicity 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
229940023080 viracept Drugs 0.000 description 1
230000003612 virological effect Effects 0.000 description 1
239000001993 wax Substances 0.000 description 1
238000009736 wetting Methods 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1
235000008939 whole milk Nutrition 0.000 description 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
- 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
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
- 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
- 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
- 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
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants

Landscapes

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)
Immunology (AREA)
Molecular Biology (AREA)
Bioinformatics & Cheminformatics (AREA)
Virology (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Tropical Medicine & Parasitology (AREA)
AIDS & HIV (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Gastroenterology & Hepatology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

SK684-2000A 1997-11-13 1998-11-12 A mixture of inhibitors, a combined pharmaceutical composition comprising the same and use thereof SK6842000A3 (en)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US6542197P	1997-11-13	1997-11-13
GBGB9807938.7A GB9807938D0 (en)	1998-04-15	1998-04-15	Combination therapy for the treatment of AIDS
US9094098P	1998-06-26	1998-06-26
GBGB9819590.2A GB9819590D0 (en)	1998-09-08	1998-09-08	Combination therapy for the treatment of aids
PCT/US1998/024097 WO1999025352A1 (en)	1997-11-13	1998-11-12	Combination therapy for the treatment of aids

Publications (1)

Publication Number	Publication Date
SK6842000A3 true SK6842000A3 (en)	2000-12-11

Family

ID=27451773

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK684-2000A SK6842000A3 (en)	1997-11-13	1998-11-12	A mixture of inhibitors, a combined pharmaceutical composition comprising the same and use thereof

Country Status (24)

Country	Link
EP (1)	EP1044000B1 (es)
JP (1)	JP2001522889A (es)
KR (1)	KR20010032055A (es)
CN (1)	CN1285747A (es)
AR (1)	AR013758A1 (es)
AT (1)	ATE218866T1 (es)
AU (1)	AU749795B2 (es)
BG (1)	BG104507A (es)
BR (1)	BR9814146A (es)
CA (1)	CA2309164A1 (es)
CO (1)	CO4970782A1 (es)
DE (1)	DE69806062T2 (es)
EA (1)	EA200000513A1 (es)
ES (1)	ES2177103T3 (es)
HU (1)	HUP0100365A3 (es)
ID (1)	ID24922A (es)
IL (1)	IL135994A0 (es)
IS (1)	IS5481A (es)
NO (1)	NO20002481L (es)
PE (1)	PE20000020A1 (es)
PL (1)	PL340430A1 (es)
SK (1)	SK6842000A3 (es)
TR (1)	TR200001938T2 (es)
WO (1)	WO1999025352A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB9820417D0 (en) *	1998-09-18	1998-11-11	Glaxo Group Ltd	Antiviral combinations
WO2003011221A2 (en)	2001-07-30	2003-02-13	University Of Southern California	PREPARATION AND USE OF α-KETO PHOSPHONATES
AU2004206821C1 (en)	2003-01-14	2009-10-01	Gilead Sciences, Inc.	Compositions and methods for combination antiviral therapy
GB2400553A (en) *	2003-04-14	2004-10-20	Cipla Ltd	Antiviral pharmaceutical combination of lamivudine, stavudine and efavirenz, or derivatives thereof
TWI471145B (zh)	2005-06-13	2015-02-01	Bristol Myers Squibb & Gilead Sciences Llc	單一式藥學劑量型
TWI375560B (en)	2005-06-13	2012-11-01	Gilead Sciences Inc	Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
KR100234863B1 (ko) *	1993-12-15	1999-12-15	폴락 돈나 엘	사람 면역결핍 바이러스 프로테아제 억제제

1998
- 1998-11-11 CO CO98066470A patent/CO4970782A1/es unknown
- 1998-11-12 TR TR2000/01938T patent/TR200001938T2/xx unknown
- 1998-11-12 ES ES98959424T patent/ES2177103T3/es not_active Expired - Lifetime
- 1998-11-12 AU AU15225/99A patent/AU749795B2/en not_active Ceased
- 1998-11-12 ID IDW20000895A patent/ID24922A/id unknown
- 1998-11-12 EP EP98959424A patent/EP1044000B1/en not_active Expired - Lifetime
- 1998-11-12 AT AT98959424T patent/ATE218866T1/de not_active IP Right Cessation
- 1998-11-12 PL PL98340430A patent/PL340430A1/xx unknown
- 1998-11-12 BR BR9814146-5A patent/BR9814146A/pt not_active Application Discontinuation
- 1998-11-12 EA EA200000513A patent/EA200000513A1/ru unknown
- 1998-11-12 AR ARP980105720A patent/AR013758A1/es unknown
- 1998-11-12 HU HU0100365A patent/HUP0100365A3/hu unknown
- 1998-11-12 CN CN98813077A patent/CN1285747A/zh active Pending
- 1998-11-12 SK SK684-2000A patent/SK6842000A3/sk unknown
- 1998-11-12 IL IL13599498A patent/IL135994A0/xx unknown
- 1998-11-12 DE DE69806062T patent/DE69806062T2/de not_active Expired - Fee Related
- 1998-11-12 PE PE1998001094A patent/PE20000020A1/es not_active Application Discontinuation
- 1998-11-12 JP JP2000520785A patent/JP2001522889A/ja not_active Withdrawn
- 1998-11-12 KR KR1020007005176A patent/KR20010032055A/ko not_active Withdrawn
- 1998-11-12 CA CA002309164A patent/CA2309164A1/en not_active Abandoned
- 1998-11-12 WO PCT/US1998/024097 patent/WO1999025352A1/en not_active Ceased
2000
- 2000-05-09 IS IS5481A patent/IS5481A/is unknown
- 2000-05-12 NO NO20002481A patent/NO20002481L/no not_active Application Discontinuation
- 2000-06-05 BG BG104507A patent/BG104507A/bg unknown

Also Published As

Publication number	Publication date
HUP0100365A2 (hu)	2002-05-29
AR013758A1 (es)	2001-01-10
KR20010032055A (ko)	2001-04-16
EP1044000B1 (en)	2002-06-12
NO20002481L (no)	2000-07-12
EA200000513A1 (ru)	2000-10-30
CA2309164A1 (en)	1999-05-27
DE69806062D1 (de)	2002-07-18
CN1285747A (zh)	2001-02-28
IS5481A (is)	2000-05-09
ES2177103T3 (es)	2002-12-01
ATE218866T1 (de)	2002-06-15
EP1044000A1 (en)	2000-10-18
CO4970782A1 (es)	2000-11-07
TR200001938T2 (tr)	2001-07-23
AU749795B2 (en)	2002-07-04
PE20000020A1 (es)	2000-01-27
BG104507A (bg)	2001-03-30
DE69806062T2 (de)	2003-03-20
ID24922A (id)	2000-08-31
JP2001522889A (ja)	2001-11-20
HUP0100365A3 (en)	2002-06-28
AU1522599A (en)	1999-06-07
WO1999025352A1 (en)	1999-05-27
IL135994A0 (en)	2001-05-20
PL340430A1 (en)	2001-02-12
NO20002481D0 (no)	2000-05-12
BR9814146A (pt)	2000-10-03

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US6180634B1 (en)	2001-01-30	Combination therapy for the treatment of AIDS
US6689761B1 (en)	2004-02-10	Combination therapy for HIV infection
WO2001082919A2 (en)	2001-11-08	Methods of and compounds for inhibiting calpains
SK6842000A3 (en)	2000-12-11	A mixture of inhibitors, a combined pharmaceutical composition comprising the same and use thereof
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