Abstract

The aim of the present invention is to provide a compound containing a diheterocyclic ribavirin analog, a stereoisomer, a prodrug, a pharmaceutically acceptable salt, a compound salt and/or a solvated compound with structural general formula (I) as follows, and/or a stereoisomer, a tautomer, a prodrug, a pharmaceutically acceptable salt, a compound salt and/or a solvate thereof, which have an anti-tumor effect and use.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• C07H 1/00 - Processes for the preparation of sugar derivatives
• A61K 31/706 - 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
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 35/00 - Antineoplastic agents

Abstract

An object of the present invention is to provide: as an invention of an antibacterial and antifungal activity, 3-(2,4-difluorophenyl)-5-substituted-2-methylpyrazolo[1,5-a] pyrimidin-7-phenolate derivatives and analogues having the following general formula or prodrug, a preparation method and pharmacological activity test procedure therefor, and the pharmacological activity thereof; and a pharmaceutical chemical research and preparation method, and uses of the compounds as antibacterial and antifungal drugs. The definitions of R and M + in the general formula I are set forth in the description. The 3-(2,4-difluorophenyl)-5-substituted-2-methylpyrazolo[1,5-a] pyrimidin-7-phenolate derivatives and analogues of the formula I of the present application can be compatible with the other known antibacterial and antifungal drugs and drugs for treating bacterial infections with various complications, such as inflammation, viruses and immune system diseases.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 31/10 - Antimycotics
• A61P 31/04 - Antibacterial agents

Abstract

Disclosed are a novel andrographolide derivative and analogue as well as a preparation method of the novel andrographolide derivative and analogue and an application to the treatment, the prevention and the relief on human viruses and neoplastic diseases. The present invention also relates to a medicine composition of the compound and an application as antivirus and anticancer disease medicine. Through chemical synthesis and preparation, semi-synthesis multi-series andrographolide analogues can be obtained. The analogues have the following general formula I.

IPC Classes  ?

• C07D 307/58 - One oxygen atom, e.g. butenolide
• C07D 307/60 - Two oxygen atoms, e.g. succinic anhydride
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 471/04 - Ortho-condensed systems
• C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
• C07D 487/04 - Ortho-condensed systems
• C07D 487/18 - Bridged systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• C07F 9/655 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
• C07F 9/6568 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane ringsBicyclic carbocyclic ring systems
• C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
• C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
• C07H 17/04 - Heterocyclic radicals containing only oxygen as ring hetero atoms
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/365 - Lactones
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/437 - 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/665 - Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents

Abstract

Chain compounds containing Adamantane or adamantane-like group, its stereoisomers, prodrugs, pharmaceutical salts, complex salt and solvate are provided. It comprises formula (I), where in S is a optionally substituted cyclic group, P is a optionally substituted functional group linkable S or T, T is a optionally substituted Adamantane or adamantane-like group, the structures of S, P, T can be combined all together or two kinds of them independently. The compounds have antitumor, antiviral, treating nervous system disease and inflammatory disease activities, and they can be used as drugs. Further, the present invention provides the preparation method for the compounds and use of the compounds.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
• C07D 491/18 - Bridged systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• C07D 471/18 - Bridged systems
• C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
• C07D 309/10 - Oxygen atoms
• C07D 493/08 - Bridged systems
• C07D 471/08 - Bridged systems
• C07D 213/65 - One oxygen atom attached in position 3 or 5
• C07D 495/10 - Spiro-condensed systems
• C07D 221/22 - Bridged ring systems
• C07D 207/404 - 2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
• C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/439 - 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 the ring forming part of a bridged ring system, e.g. quinuclidine
• A61K 31/4164 - 1,3-Diazoles
• A61K 31/4168 - 1,3-Diazoles having a nitrogen atom attached in position 2, e.g. clonidine
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/351 - 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 not condensed with another ring
• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/047 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
• A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
• A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
• A61K 31/35 - 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
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/385 - Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
• A61P 35/00 - Antineoplastic agents
• A61P 31/12 - Antivirals
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention discloses a pharmaceutical composition comprising a compound of formula (I) or stereoisomer, prodrug, pharmaceutically acceptable salt, double salt and/or solvate thereof as an active ingredient, as well as pharmaceutically acceptable carriers. The dosage form of said pharmaceutical composition is one of the pharmaceutically acceptable dosage forms. The present invention also discloses use of the pharmaceutical composition for treatment of bacterial infections, wherein said bacteria are Gram positive bacteria, including Staphylococcus, Micrococcus pneumoniae, Enterococcus faecalis, Streptococcus, Streptococcus bovis, Streptococcus pneumoniae, Peptostreptococcus, suppurative Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus riridans, Streptococcus agalactiae B and Bacillus diphtheriae, etc.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 9/12 - AerosolsFoams
• A61K 9/10 - DispersionsEmulsions
• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/70 - Web, sheet or filament bases
• A61K 9/06 - OintmentsBases therefor
• A61K 9/107 - Emulsions
• A61K 9/08 - Solutions
• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61K 9/02 - SuppositoriesBougiesBases for suppositories or bougies
• A61P 31/04 - Antibacterial agents

Abstract

Disclosed are pharmaceutical compound tromantadine of the following formula (I), derivatives and analogs thereof, and their uses as anti-tumor pharmaceuticals. The present compounds can be used solely or in combination with other known anti-tumor pharmaceuticals for the treatment of tumor-relating diseases, or in combination with other known pharmaceuticals for the treatment of other diseases associated with concomitant tumor diseases, such as viral, mycotic and bacterial caused diseases, neurological diseases, emdorcine system diseases, immune system diseases, etc.

IPC Classes  ?

• C07C 235/14 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 31/12 - Antivirals
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics

Abstract

Memantine with an adamantane structure, derivatives and analogues thereof can be used as medicine for treating some diseases such as tumor. The medicines are the compound having the following structure (I), its derivatives and analogues deriving from the structure (I), the compounds with a new structure produced by taking the said structure as a fundamental structure or a structure fragment, as well as inorganic acid salts, organic acid salts, inorganic alkali salts, organic alkali salts or complex salts of the derivatives and analogues of the said structure and prodrugs thereof. In combination with other therapeutic agents, these compounds can be used as anti-tumor medicine for treating tumor-related or other diseases accompanied by tumor, including diseases caused by virus, bacteria, and fungus, nervous system diseases, endocrine system diseases, immune system diseases and the like.

IPC Classes  ?

• C07C 13/615 - Adamantanes
• A61K 31/13 - Amines, e.g. amantadine
• A61P 35/00 - Antineoplastic agents

Abstract

Pyrimidine derivatives and analogs, their pharmaceutically acceptable salts, processes for preparing them, pharmaceutical compositions comprising them, and their use in manufacture of medicaments for treating inflammatory and infectious diseases induced by bacteria and/or fungi are disclosed.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 265/22 - Oxygen atoms
• C07D 239/91 - Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
• C07D 487/14 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• C07D 233/88 - Nitrogen atoms, e.g. allantoin
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
• C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 311/92 - NaphthopyransHydrogenated naphthopyrans
• C07D 231/38 - Nitrogen atoms
• C07D 239/95 - QuinazolinesHydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
• C07D 239/70 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
• C07H 15/203 - Monocyclic carbocyclic rings other than cyclohexane ringsBicyclic carbocyclic ring systems
• C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
• A61K 31/59 - Compounds containing 9,10-seco-cyclopenta[a]hydro- phenanthrene ring systems
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/539 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more oxygen atoms in the same ring, e.g dioxazines
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/437 - 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61P 31/04 - Antibacterial agents

Abstract

Gambogic acid cyclization analogues with formula I, II and III are disclosed, wherein cycles A, B and C are saturated or unsaturated alicyclic, alicyclic heterocyclic, aromatic ring or aromatic heterocyclic groups containing 4-10 members, and R1-R12 groups contain one or more of glycosyl, poly-hydroxy, amino acid group, acyloxy, phosphoric acid oxygen, sulfonic acid oxygen, alkoxy, aryloxy, heterocyclic oxygen, mercapto, substituted mercapto, chain alkyl, and/or cycle group. The gambogic acid cyclization analogues of the invention are synthesized from extracted and purified gambogic acid. Said gambogic acid cyclization analogues have antitumor, antiviral, antibacterial and antifungal activities and can be used as antitumor, antiviral, immune, antibacterial and antifungal medical agents. The medical agents may also contain other known antitumor, antiviral, immune, antibacterial and antifungal medicines.

IPC Classes  ?

• C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
• C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 513/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings
• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• C07H 17/04 - Heterocyclic radicals containing only oxygen as ring hetero atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
• A61K 31/706 - 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
• A61K 31/529 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/4196 - 1,2,4-Triazoles
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 35/00 - Antineoplastic agents
• A61P 31/12 - Antivirals
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 37/02 - Immunomodulators

Abstract

Medicines with adamantane structure and their derivatives and analogues having new activity and indications such as antitumor, and their uses as medicine for treating some diseases such as tumor. The medicines are the compounds having the following structures, the derivatives and analogues deriving from the structures, the new structural compounds deriving from the parent or fragment structures, the compounds having the same or different structures and the similar or relative bioactivities by predigesting, expanding the said structure or/and by replacing the said structure on the basis of isosterism, their salts, double salts and the prodrugs thereof. These compounds can be in combination with other therapeutic agents to use as antitumor medicine for treating tumor-related or tumor-accompanying diseases, including viral diseases, bacterial diseases, fungal diseases, nervous system diseases, endocrine system diseases, immune system diseases and so on.

IPC Classes  ?

• C07C 211/38 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
• C07C 211/19 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings containing condensed ring systems
• C07C 237/14 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated and containing rings
• C07C 65/26 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic containing rings other than six-membered aromatic rings
• C07C 49/513 - Saturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system
• A61K 31/13 - Amines, e.g. amantadine
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61P 35/00 - Antineoplastic agents
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 31/12 - Antivirals
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The invention discloses gambogic glycoside derivatives and analogs represented by formula I, the preparation and the application thereof, wherein the substituents R1-R12 are defined as in the description. The gambogic glycoside derivatives and analogs of the invention were synthesized from extracted and purified gambogic acid. The obtained gambogic glycoside derivatives and analogs have antitumor, antivirus, antibacterial and antifungal activities and can be used as antitumor, antivirus, immune, antibacterial and antifungal medicines. The gambogic glycoside derivatives and analogs of the invention can be used together with other known antitumor, antivirus, immune, antibacterial and antifungal medicines.

IPC Classes  ?

• C07H 17/04 - Heterocyclic radicals containing only oxygen as ring hetero atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61P 35/00 - Antineoplastic agents