CN101128117A - Compositions comprising O-acetylsalicyl derivatives of aminocarbohydrates and amino acids - Google Patents

Compositions comprising O-acetylsalicyl derivatives of aminocarbohydrates and amino acids Download PDF

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CN101128117A
CN101128117A CNA2005800486748A CN200580048674A CN101128117A CN 101128117 A CN101128117 A CN 101128117A CN A2005800486748 A CNA2005800486748 A CN A2005800486748A CN 200580048674 A CN200580048674 A CN 200580048674A CN 101128117 A CN101128117 A CN 101128117A
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acetyl salicyl
acetyl
salicyl
amine
amino acid
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吕伊·J·于
尤金·J·范斯科特
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Abstract

The embodiments described herein include a composition and method of treatment using compositions that include at least one 0acetylsalicyl derivative. The compositions and methods are useful in preventing and treating disorders and syndromes associated with anyone of the nervous, vascular, musculoskeletal, or cutaneous systems.

Description

The composition that comprises aminosugars and amino acid whose O-acetyl acetylsalicyl derivatives
The application is incorporated herein with integral body its content according to the priority that 35U.S.C. § 119 requires the temporary patent application 60/640,225 of submission on January 3rd, 2005 by reference.
Invention field
[0001] the application relates to composition group and use composition group's method, said composition group comprises O-acetyl acetylsalicyl derivatives and acceptable excipient of pharmacy or carrier, be used for part or systematically prevention or treatment, to alleviate or to improve pain, inflammation, disorder, symptom or the syndrome relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Background
The PCT application No.PCT/US96/16534 that is entitled as " topical composition that comprises N-acetylcystein and smell shelter matter " that on October 16th, [0002] 1996 submitted to has described the topical composition group, comprise 0.01% to 50% the N-acetylcystein or the derivative of N-acetylcystein, 0.01% to 0.5% smell is sheltered material, and topical vehicle, to improve the performance of skin.
[0003] U.S.6 that is entitled as " N-acetyl aldose amine (Aldosamines), N-acetylamino acid with relevant N-acetyl compound and their topical application "; 159; 485; the U.S.6 that is entitled as " N-acetyl aldose amine with relevant N-acetyl compound and their topical application "; 524; 593B1 and the U.S.6 that is entitled as " N-acetylamino acid with relevant N-acetyl compound and their topical application "; 808; 716B2 describes and the claimed composition that comprises N-acetylamino acid and N-acetyl aldose amine, is used for topical therapeutic beauty treatment illness and disease of skin.
[0004] U.S.6 that is entitled as " composition that comprises phenyl-glycine derivative ", 824, the application of 786B2 description and claimed composition and composition, said composition comprises phenyl-glycine derivative, is used for the treatment of beauty treatment illness and disease of skin.Disclosed content all is incorporated herein by reference with integral body in above-mentioned each United States Patent (USP).
[0005] aspirin is generally used for the pain and the inflammation of respite arthritis and bursal synovitis.The modal adverse reaction of oral aspirin is a gastric irritation, and this causes 70% patient who repeats oral aspirin gastrointestinal bleeding to occur.Cortin for example metacortandracin and non-steroidal anti-inflammatory agent for example brufen, naproxen, tolmetin and sulindac also can be used for respite arthritis.But, use these medicines also can cause illeffects for a long time.Rofecoxib (Vioxx) and celecoxib (Celebrex) are non-steroid anti-inflammatory, pain relieving and antipyretic, are used for oral medication osteoarthritis, rheumatoid arthritis and analgesia and comprise dysmenorrhoea, toothache and operation pain.The mechanism of action that it is believed that these two kinds of medicines is to suppress the synthetic of prostaglandin by suppressing cyclooxygenase 2.Recent studies show that the patient who takes rofecoxib or celecoxib has more a high proportion of heart attack (heartbeat stops) than control group.
[0006] this paper pair of description with known compositions and method advantages associated and problem is not to be intended to be limited in the scope of described embodiment herein, so that they are got rid of.Really, some embodiments can comprise one or more known compositions, compound or method, and do not have noticeable shortcoming or problem.
Summary
[0007] embodiment of the present invention feature provides a kind of prevention or alleviates symptom or syndromic composition and the method relevant with nerve, blood vessel, muscle skeleton or integumentary system, by local or systematically give the composition of the patient's administering therapeutic effective dose that needs, said composition comprises at least a O-acetyl-salicylic derivate and acceptable excipient of a kind of pharmacy or carrier.By detailed description hereinafter, other features of these and various embodiments will become apparent for those skilled in the art.
Describe in detail
[0008] in order to promote understanding to embodiment described herein, can be with reference to embodiment preferred, and use special language to describe this same approach.The name of Shi Yonging only is in order to describe specific technical scheme in this article, rather than is intended to limit the scope of the invention.Unless clearly demonstrate in addition, this paper in the whole text employed singulative " a kind of (a) ", " one (an) " and " this kind (the) " comprised plural appellation.Therefore, for example, " a kind of composition " comprises multiple such composition, and single composition, and " a kind of therapeutic agent " comprises one or more treatments and/or pharmaceutical preparation and equivalent well known by persons skilled in the art or the like.
[0009] inventor has been found that, comprise O-acetyl acetylsalicyl derivatives, preferred O-acetyl salicyl aminosugars, or the amino acid whose composition of O-acetyl salicyl is useful or treats effectively with symptom or the syndrome alleviated or improvement is relevant with nerve, blood vessel, muscle skeleton or integumentary system for part or system shortsightedness or treatment.Preferred compound comprises N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-gucosamine, N-(O-acetyl salicyl)-glycine ethyl ester, N-(O-acetyl salicyl)-TEE, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-prolineamide, N-(O-acetyl salicyl)-ethyl prolinate, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamate diethyl ester, N-(O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-4-glycin ethyl ester; N, O-two (O-acetyl salicyl)-4-glycin ethyl ester, N-(O-acetyl salicyl)-3-Phenserine; N-(O-acetyl salicyl)-3-Phenserine ethyl ester; N-(O-acetyl salicyl)-lysine and N-(O-acetyl salicyl)-ornithine.These compounds are useful or treat effectively with symptom or the syndrome alleviated or improvement is relevant with nerve, blood vessel, muscle skeleton or integumentary system for part or system shortsightedness or treatment.More special and preferably, oral these compounds are useful for alleviating the arthralgia and the inflammation that are caused by arthritis or other diseases.
[0010] since aspirin (O-acetyl salicyl) part as acid amides or ester bond chemical bond on aminosugars or amino acid, can eliminate or reduce for example gastrointestinal bleeding of adverse reaction that oral aspirin causes.
[0011] by part or systemic application composition as herein described for nerve, blood vessel, muscle skeleton or integumentary system diseases associated be that treatment is effective or useful.Systemic application comprises injection, infusion and oral, and preferred approach is oral.Oral these compounds are useful especially for alleviating the arthralgia and the inflammation that are caused by arthritis or other diseases.
[0012] preferred O-acetyl acetylsalicyl derivatives of the present invention comprises by at least one O-acetyl salicyl and a dimer or the oligomer compound that aminosugar, amino acid or peptide form by acid amides and/or ester bond.The preferred O-acetyl of the present invention acetylsalicyl derivatives comprises N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-glycine ethyl ester, N-(O-acetyl salicyl)-TEE, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-prolineamide, N-(O-acetyl salicyl)-ethyl prolinate, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamate diethyl ester, N-(O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-4-glycin ethyl ester; N, O-two (O-acetyl salicyl)-4-glycin ethyl ester, N-(O-acetyl salicyl)-3-Phenserine; N-(O-acetyl salicyl)-3-Phenserine ethyl ester; N-(O-acetyl salicyl)-lysine and N-(O-acetyl salicyl)-ornithine.
[0013] the O-acetyl acetylsalicyl derivatives in the embodiment can be used for improving, treat, improve, alleviating or reduce the pain relevant with nerve, blood vessel, muscle skeleton or integumentary system, inflammation, disorder, symptom or syndromic method.
[0014] relevant with nervous system symptom and syndrome include but not limited to; (1) dementia and Alzheimer disease: carrying out property amnesia; cerebral cortex shrinks and atrophy; fiber confusion in the nerve cell; the senile plaque of amyloid; CAT reduces; (2) complication of wrist: weakness; pain; numb; numb; palm and finger are hot; (3) encephalitis: the inflammation of brain; (4) headache: antimigraine; neural or the compression occlude blood supply of blood vessel dilatation extruding; inflammation; facial; neck or scalp contraction of muscle; (5) meningitis: the infection of spinal fluid and meninx; (6) neuralgia: neuralgia; peripheral nerve disease; sciatica; herpes zoster; trigeminal neuralgia; (7) Parkinson's: trembling of limbs; myotonia; (8) amnesia: amnesia can not produce new memory, and other for example incoordination; Bell's palsy; epilepsy; multiple sclerosis; myasthenia gravis; narcolepsy; paralysis and rabies.
[0015] vascular disease, reaction and illness include but not limited to acanthosis nigricans, acrocyanosis, actinic cheilitis, actinic prurigo, dermatitis, skin disease, dermatograph, pompholyx, drug rash, eczema, erythema, migratory erythema, erythrocyanosis, acromelalgia, familial is hemorrhage, histamine response, inflammation papule and warts infringement, lichen planus, lupus erythematosus, mycosis fungoides, neurodermatitis, neuropeptide and neural blood vessel reaction, parapsoriasis, pernosis (pernio), photoallergy, wide reaction, photosensitization, pityriasis rosea, pityriasis rubra pilaris, PLE, trichophytosis, hammernose, rosacea, sclerosis, spider angioma, the T-cell disorder, telangiectasis, nettle rash and other vascular reactions.
[0016] abnormal conditions of musculoskeletal system include but not limited to, (1) osteoporosis: calcium reduces in the bone, cause the bone attenuation, easily fracture, (2) osteoarthritis: the inflammation of articular cartilage, the expansion and the pain that produce, (3) rheumatoid arthritis: the inflammation of synovial membrane and the destruction of cartilage, to heart, lung, the infringement of nerve and eyes, (4) ankylosing spondylitis: the arthritis that influences articulatio sacroiliaca and backbone, have inflammation and consistency, (5) bursal synovitis: bursal inflammation, (6) tendonitis: the inflammation of tendon, (7) gout: other for example general pain of the recidivity acute arthritis that the uric acid deposition causes and (8), toothache, operation pain, arthralgia, backache;
Figure A20058004867400201
Capsulitis and hernia.
[0017] illness of integumentary system or abnormal conditions include but not limited to, irregularity keratinization, pigmentation and immunity; Inflammation; Infect; The illness of mouth, vagina and anal mucosa; Skin trauma; Reduce with physiological function.The phenomenon of skin disorder comprises acne; Senile plaque; Contaminative skin; Spot; Celluar tissue; Skin disease; Dandruff; Dry; Pruritus, eczema; Ichthyosis; Keratosis and hyperkeratosis; Mole; Black spot; Spot shape skin; Pseudofolliculitis barbae; Light aging and photodamaged; Trichophytosis; The skin line; The tractive vestige; Skin, nail plate and hair attenuate; Wrinkle; Axersis; Oral cavity or gingival disease; Excitant, struvite, unsound damageability or abnormal mucosa, skin, hair, nail, anus or vaginal disease; Synthetic or the reparation of skin component defective; The resulting anomaly of collagen, glycosaminoglycan, proteoglycans and elastin laminin or minimizing and in corium the level of these components reduce; The unevenness of skin, nail and hair and rough surface; Skin, nail and hair screen resilience, elasticity and coiling property disappearance or reduction again; Lubricated and the gloss shortage of skin, nail and hair; Nail and hair are fragile and split; The skin yellow; Reactivity, excitant or telangiectatic skin; Dim and aging skin, nail and hair; Be used for skin bleaching and brightening and wound healing.
[0018] in children the adverse reaction relevant with oral aspirin comprise that hemorrhage of gastrointestinal tract, bleeding time prolong, hemorrhage, peptic ulcer, salicylism and reye's syndrome.Because O-acetyl salicyl aminosugar, O-acetyl salicyl amino acid or relevant compound are that wherein the adverse reaction that oral aspirin causes can be eliminated or reduce to aspirin therefore partly by acid amides or chemically combined dimer of ester bond or oligomer compound.
[0019] O-acetyl salicyl aminosugar, O-acetyl salicyl amino acid and the related compound in the embodiment can be divided into 6 groups: (1) N-(O-acetyl salicyl)-aminosugar; (2) O-(O-acetyl salicyl)-aminosugar; (3) N, O-two (O-acetyl salicyl)-aminosugar; (4) N-(O-acetyl salicyl)-amino acid; (5) N-(O-acetyl salicyl)-peptide; (6) Xiang Guan (O-acetyl salicyl)-derivative.
(1) .N-(O-acetyl salicyl)-aminosugar
[0020] aminosugar can have a plurality of amino, but embodiment preferred only has 1 amino acid for example aminoglucose and galactosamine in molecule.Usually (O-acetyl salicyl)-aminosugar is a dimer compound to N-, is formed by amido link by the amino of O-acetyl salicyl and aminosugar.For example N-(O-acetyl salicyl)-aminoglucose can be to react the dimer that forms by O-acetyl bigcatkin willow acyl chlorides and aminoglucose in the aqueous solution.N-(O-acetyl salicyl)-aminosugar also can be the oligomeric compound that is formed by O-acetyl salicyl and the amino that comprises the oligomer aminosugar of 2 to 9 sugar units.N-(O-acetyl salicyl)-aminosugar also can comprise more than 1 O-acetyl group salicyl that connects by acid amides and/or ester bond.But dimer compound preferably.Can represent N-(O-acetyl salicyl)-aminosugar by following universal architecture:
R 1(CHOH) n(CHNHR 2)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, alkyl, aralkyl or have the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace; OH can be by H, NH 2, NHCOCH 3, acetoxyl group or other acyloxy with 2 to 9 carbon atoms replace.
[0021] N-(O-acetyl salicyl)-aminosugar can be saturated or unsaturated, and is stereomeric or non-stereomeric, and straight or branched or loop type are as free acid, salt, inclined to one side salt, lactone, acid amides or ester-formin.The classical ring form of N-(O-acetyl salicyl)-aminosugar is that aminosugar partly is five-membered ring (furanose type) or hexatomic ring (pyranose type).In loop type, structure is more complicated and be difficult to represent with above-mentioned universal architecture.In this case, will represent N-(O-acetyl salicyl)-aminosugar with its chemical name.
[0022] below preferred is representational N-(O-acetyl salicyl)-aminosugar-N-(O-acetyl salicyl)-glycerine osamine (glycerosamine), N-(O-acetyl salicyl)-erythrose amine, N-(O-acetyl salicyl)-threose amine, N-(O-acetyl salicyl)-ribose amine, N-(O-acetyl salicyl)-Arabic osamine, N-(O-acetyl salicyl)-wood sugar amine, N-(O-acetyl salicyl)-lysol osamine, N-(O-acetyl salicyl)-allose amine, N-(O-acetyl salicyl)-altrose amine, N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-gulosamine, N-(O-acetyl salicyl)-idose amine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-talosamine, N-(O-acetyl salicyl)-A Luo heptose amine, N-(O-acetyl salicyl)-A Zhuo osamine in heptan, N-(O-acetyl salicyl)-glucoheptose amine, N-(O-acetyl salicyl)-mannoheptose amine, N-(O-acetyl salicyl)-Gu Luo heptose amine, N-(O-acetyl salicyl)-Ai Du osamine in heptan, N-(O-acetyl salicyl)-galactoheptose amine, N-(O-acetyl salicyl)-Ta Luo osamine in heptan, N-(O-acetyl salicyl)-glycerine amino acid, N-(O-acetyl salicyl)-erythrose amino acid, N-(O-acetyl salicyl)-threose amino acid, N-(O-acetyl salicyl)-ribose amino acid, N-(O-acetyl salicyl)-arabinose amino acid, N-(O-acetyl salicyl)-wood sugar amino acid, N-(O-acetyl salicyl)-lyxose amino acid, N-(O-acetyl salicyl)-allose amino acid, N-(O-acetyl salicyl)-altrose amino acid, N-(O-acetyl salicyl)-Glucoamino acid, N-(O-acetyl salicyl)-mannose amino acid, N-(O-acetyl salicyl)-gulose amino acid, N-(O-acetyl salicyl)-idose amino acid, N-(O-acetyl salicyl)-galactose amino acid, N-(O-acetyl salicyl)-talose amino acid, N-(O-acetyl salicyl)-A Luo heptose amino acid, N-(O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan, N-(O-acetyl salicyl)-glucoheptose amino acid, N-(O-acetyl salicyl)-mannoheptose amino acid, N-(O-acetyl salicyl)-Gu Luo heptose amino acid, N-(O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan, N-(O-acetyl salicyl)-galactoheptose amino acid, N-(O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan, N-(O-acetyl salicyl) lactose amine, N-(O-acetyl salicyl) muramic acid, N-(O-acetyl salicyl) nerve amines, N-(O-acetyl salicyl) nerve amines lactose, N-(O-acetyl salicyl)-neuraminic acid.N-(O-acetyl salicyl)-4-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-7-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-two-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-glycerine glycosyl amine; N-(O-acetyl salicyl)-erythrose base amine; N-(O-acetyl salicyl)-threose base amine; N-(O-acetyl salicyl)-ribosyl amine; N-(O-acetyl salicyl)-Arabic glycosyl amine; N-(O-acetyl salicyl)-xylosyl amine; N-(O-acetyl salicyl)-lysol glycosyl amine; N-(O-acetyl salicyl)-allose base amine; N-(O-acetyl salicyl)-altrose base amine; N-(O-acetyl salicyl)-glucosyl group amine [also making N-(O-acetyl salicyl)-gucosamine]; N-(O-acetyl salicyl)-mannose group amine; N-(O-acetyl salicyl)-gulose base amine; N-(O-acetyl salicyl)-idose base amine; N-(O-acetyl salicyl)-galactosyl amine; N-(O-acetyl salicyl)-talose base amine; N-(O-acetyl salicyl)-A Luo heptose base amine; N-(O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; N-(O-acetyl salicyl)-glucoheptose base amine; N-(O-acetyl salicyl)-mannoheptose base amine; N-(O-acetyl salicyl)-Gu Luo heptose base amine; N-(O-acetyl salicyl)-Ai Du glycosyl in heptan amine; N-(O-acetyl salicyl)-galactoheptose base amine; N-(O-acetyl salicyl)-Ta Luo glycosyl in heptan amine; wherein suffix " glycosyl amine (sylamine) " also can be with " camine " expression, and their mixture and combination.
(2) O-(O-acetyl salicyl)-aminosugar
[0023] aminosugar for example aminoglucose have 1 amino and 4 hydroxyls usually, O-acetyl salicyl is connected on any of 4 hydroxyls.O-(O-acetyl salicyl)-aminosugar can be dimer or polymer, and this depends on the number of the ester bond that forms between the hydroxyl of O-acetyl salicyl and aminosugar.For example, when 1 O-acetyl salicyl was connected on 1 hydroxyl of aminoglucose, (O-acetyl salicyl)-aminoglucose was exactly a dimer compound to the O-of Xing Chenging like this.Be connected to when 2 O-acetyl salicyls on 2 hydroxyls of aminoglucose, the two-O-of Xing Chenging (O-acetyl salicyl)-aminoglucose is the tripolymer compound like this.Can form three-O-(O-acetyl salicyl)-aminoglucose (tetramer) and four-O-(O-acetyl salicyl)-aminoglucose (pentamer) in an identical manner.(O-acetyl salicyl)-aminosugar is a dimer to preferred O-, and 1 ester bond is only arranged.This ester bond can form on any hydroxyl, although preferably on the anomeric carbon of aminosugar.For example 1-O-(O-acetyl salicyl)-aminoglucose is to be formed by the ester bond on 1 of aminoglucose, and wherein aminoglucose is pyranose or furanose type.The O-of dimer compound (O-acetyl salicyl)-aminosugar can be represented by following universal architecture:
R 1(CHOR 2) n(CHNH 2)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be H or at least one R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, have alkyl, aralkyl or the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace; OH can be by H, NH 2, NHCOCH 3, acetoxyl group or other acyloxy with 2 to 9 carbon atoms replace.
[0024] O-(O-acetyl salicyl)-aminosugar can be saturated or unsaturated, and is stereomeric or non-stereomeric, and straight or branched or loop type are as free acid, salt, inclined to one side salt, lactone, acid amides or ester-formin.The classical ring form of O-(O-acetyl salicyl)-aminosugar is that aminosugar partly is five-membered ring (furanose type) or hexatomic ring (pyranose type).In loop type, structure is more complicated and be difficult to represent with above-mentioned universal architecture.In this case, will represent O-(O-acetyl salicyl)-aminosugar with its chemical name.
[0025] below representational O-(O-acetyl salicyl)-aminosugar-O-(O-acetyl salicyl)-glycerine osamine, O-(O-acetyl salicyl)-erythrose amine, O-(O-acetyl salicyl)-threose amine, O-(O-acetyl salicyl)-ribose amine, O-(O-acetyl salicyl)-Arabic osamine, O-(O-acetyl salicyl)-wood sugar amine, O-(O-acetyl salicyl)-lysol osamine, O-(O-acetyl salicyl)-allose amine, O-(O-acetyl salicyl)-altrose amine, O-(O-acetyl salicyl)-aminoglucose, O-(O-acetyl salicyl)-mannosamine, O-(O-acetyl salicyl)-gulosamine, O-(O-acetyl salicyl)-idose amine, O-(O-acetyl salicyl)-galactosamine, O-(O-acetyl salicyl)-talosamine, O-(O-acetyl salicyl)-A Luo heptose amine, O-(O-acetyl salicyl)-A Zhuo osamine in heptan, O-(O-acetyl salicyl)-glucoheptose amine, O-(O-acetyl salicyl)-mannoheptose amine, O-(O-acetyl salicyl)-Gu Luo heptose amine, O-(O-acetyl salicyl)-Ai Du osamine in heptan, O-(O-acetyl salicyl)-galactoheptose amine, O-(O-acetyl salicyl)-Ta Luo osamine in heptan, O-(O-acetyl salicyl)-glycerine amino acid, (c)-(O-acetyl salicyl)-erythrose amino acid, O-(O-acetyl salicyl)-threose amino acid, O-(O-acetyl salicyl)-ribose amino acid, O-(O-acetyl salicyl)-arabinose amino acid, O-(O-acetyl salicyl)-wood sugar amino acid, O-(O-acetyl salicyl)-lyxose amino acid, O-(O-acetyl salicyl)-allose amino acid, O-(O-acetyl salicyl)-altrose amino acid, O-(O-acetyl salicyl)-Glucoamino acid, O-(O-acetyl salicyl)-mannose amino acid, O-(O-acetyl salicyl)-gulose amino acid, O-(O-acetyl salicyl)-idose amino acid, O-(O-acetyl salicyl)-galactose amino acid, O-(O-acetyl salicyl)-talose amino acid, O-(O-acetyl salicyl)-A Luo heptose amino acid, O-(O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan, O-(O-acetyl salicyl)-glucoheptose amino acid, O-(O-acetyl salicyl)-mannoheptose amino acid, O-(O-acetyl salicyl)-Gu Luo heptose amino acid, O-(O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan, O-(O-acetyl salicyl)-galactoheptose amino acid, O-(O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan, O-(O-acetyl salicyl) lactose amine, O-(O-acetyl salicyl) muramic acid, O-(O-acetyl salicyl) nerve amines, O-(O-acetyl salicyl) nerve amines lactose, O-(O-acetyl salicyl)-neuraminic acid.O-(O-acetyl salicyl)-4-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-7-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-two-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-glycerine glycosyl amine; O-(O-acetyl salicyl)-erythrose base amine; O-(O-acetyl salicyl)-threose base amine; O-(O-acetyl salicyl)-ribosyl amine; O-(O-acetyl salicyl)-Arabic glycosyl amine; O-(O-acetyl salicyl)-xylosyl amine; O-(O-acetyl salicyl)-lysol glycosyl amine; O-(O-acetyl salicyl)-allose base amine; O-(O-acetyl salicyl)-altrose base amine; O-(O-acetyl salicyl)-glucosyl group amine [also making O-(O-acetyl salicyl)-gucosamine]; O-(O-acetyl salicyl)-mannose group amine; O-(O-acetyl salicyl)-gulose base amine; O-(O-acetyl salicyl)-idose base amine; O-(O-acetyl salicyl)-galactosyl amine; O-(O-acetyl salicyl)-talose base amine; O-(O-acetyl salicyl)-A Luo heptose base amine; O-(O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; O-(O-acetyl salicyl)-glucoheptose base amine; O-(O-acetyl salicyl)-mannoheptose base amine; O-(O-acetyl salicyl)-Gu Luo heptose base amine; O-(O-acetyl salicyl)-Ai Du glycosyl in heptan amine; O-(O-acetyl salicyl)-galactoheptose base amine; O-(O-acetyl salicyl)-Ta Luo glycosyl in heptan amine; wherein suffix " glycosyl amine (sylamine) " also can be with " camine " expression, and their mixture and combination.
(3) N, O-two (O-acetyl salicyl)-aminosugar
[0026] aminosugar for example aminoglucose have 1 amino and 4 hydroxyls usually.1 O-acetyl salicyl can be connected on the amino, and second group can be connected in 4 hydroxyls on any.The N of Xing Chenging like this, (O-acetyl salicyl)-aminosugar is exactly a tripolymer to O-two, is formed by acid amides and ester bond by 2 O-acetyl salicyls and 1 aminosugar.N for example, O-two (O-acetyl salicyl)-aminoglucose is a tripolymer compound, is formed by 1 acid amides and 1 ester bond by 2 O-acetyl salicyls and 1 aminoglucose.When 1 O-acetyl salicyl is connected on the amino, and 2 O-acetyl salicyls are when being connected on 2 hydroxyls of aminosugar, the N of Xing Chenging like this, and O, (O-acetyl salicyl)-aminosugar is exactly the tetramer to O-three.In an identical manner, can form N, O, O, O-four (O-acetyl salicyl)-aminosugar (pentamer); N, O, O, O, O-five (O-acetyl salicyl)-aminosugar (six aggressiveness) and N, O, O, O, O, O-six (O-acetyl salicyl)-aminosugar (heptamer).Preferred N, O-two (O-acetyl salicyl)-aminosugar can be represented with following universal architecture:
R 1(CHOR 2) n(CHNHCOC 6H 4OCOCH 3)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be H or at least one R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, have alkyl, aralkyl or the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace.
[0027] N, O-two (O-acetyl salicyl)-aminosugar can be saturated or unsaturated, and is stereomeric or non-stereomeric, straight or branched or loop type are as free acid, salt, inclined to one side salt, lactone, acid amides or ester-formin.N, the classical ring form of O-two (O-acetyl salicyl)-aminosugar is that aminosugar partly is five-membered ring (furanose type) or hexatomic ring (pyranose type).In loop type, structure is more complicated and be difficult to represent with above-mentioned universal architecture.In this case, will represent N, O-two (O-acetyl salicyl)-aminosugar with its chemical name.
[0028] below representational N, O-two (O-acetyl salicyl)-aminosugar-N, O-two (O-acetyl salicyl)-glycerine osamine; N, O-two (O-acetyl salicyl)-erythrose amine; N, O-two (O-acetyl salicyl)-threose amine; N, O-two (O-acetyl salicyl)-ribose amine; N, O-two (O-acetyl salicyl)-Arabic osamine; N, O-two (O-acetyl salicyl)-wood sugar amine; N, O-two (O-acetyl salicyl)-lysol osamine; N, O-two (O-acetyl salicyl)-allose amine; N, O-two (O-acetyl salicyl)-altrose amine; N, O-two (O-acetyl salicyl)-aminoglucose; N, O-two (O-acetyl salicyl)-mannosamine; N, O-two (O-acetyl salicyl)-gulosamine; N, O-two (O-acetyl salicyl)-idose amine; N, O-two (O-acetyl salicyl)-galactosamine; N, O-two (O-acetyl salicyl)-talosamine; N, O-two (O-acetyl salicyl)-A Luo heptose amine; N, O-two (O-acetyl salicyl)-A Zhuo osamine in heptan; N, O-two (O-acetyl salicyl)-glucoheptose amine; N, O-two (O-acetyl salicyl)-mannoheptose amine; N, O-two (O-acetyl salicyl)-Gu Luo heptose amine; N, O-two (O-acetyl salicyl)-Ai Du osamine in heptan; N, O-two (O-acetyl salicyl)-galactoheptose amine; N, O-two (O-acetyl salicyl)-Ta Luo osamine in heptan; N, O-two (O-acetyl salicyl)-glycerine amino acid; N, O-two (O-acetyl salicyl)-erythrose amino acid; N, O-two (O-acetyl salicyl)-threose amino acid; N, O-two (O-acetyl salicyl)-ribose amino acid; N, O-two (O-acetyl salicyl)-arabinose amino acid; N, O-two (O-acetyl salicyl)-wood sugar amino acid; N, O-two (O-acetyl salicyl)-lyxose amino acid; N, O-two (O-acetyl salicyl)-allose amino acid; N, O-two (O-acetyl salicyl)-altrose amino acid; N, O-two (O-acetyl salicyl)-Glucoamino acid; N, O-two (O-acetyl salicyl)-mannose amino acid; N, O-two (O-acetyl salicyl)-gulose amino acid; N, O-two (O-acetyl salicyl)-idose amino acid; N, O-two (O-acetyl salicyl)-galactose amino acid; N, O-two (O-acetyl salicyl)-talose amino acid; N, O-two (O-acetyl salicyl)-A Luo heptose amino acid; N, O-two (O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl)-glucoheptose amino acid; N, O-two (O-acetyl salicyl)-mannoheptose amino acid; N, O-two (O-acetyl salicyl)-Gu Luo heptose amino acid; N, O-two (O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl)-galactoheptose amino acid; N, O-two (O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl) lactose amine; N, O-two (O-acetyl salicyl) muramic acid; N, O-two (O-acetyl salicyl) nerve amines; N, O-two (O-acetyl salicyl) nerve amines lactose; N, O-two (O-acetyl salicyl)-neuraminic acid; N, O-two (O-acetyl salicyl)-4-O-acetyl neuraminic acid; N, O-two (O-acetyl salicyl)-7-O-acetyl neuraminic acid; N, O-two (O-acetyl salicyl)-two-O-acetyl neuraminic acid, N, O-two (O-acetyl salicyl)-glycerine glycosyl amine; N, O-two (O-acetyl salicyl)-erythrose base amine; N, O-two (O-acetyl salicyl)-threose base amine; N, O-two (O-acetyl salicyl)-ribosyl amine; N, O-two (O-acetyl salicyl)-Arabic glycosyl amine; N, O-two (O-acetyl salicyl)-xylosyl amine; N, O-two (O-acetyl salicyl)-lysol glycosyl amine; N, O-two (O-acetyl salicyl)-allose base amine; N, O-two (O-acetyl salicyl)-altrose base amine; N, O-two (O-acetyl salicyl)-glucosyl group amine [also making N, O-two (O-acetyl salicyl)-gucosamine]; N, O-two (O-acetyl salicyl)-mannose group amine; N, O-two (O-acetyl salicyl)-gulose base amine; N, O-two (O-acetyl salicyl)-idose base amine; N, O-(O-acetyl salicyl)-galactosyl amine; N, O-two (O-acetyl salicyl)-talose base amine; N, O-two (O-acetyl salicyl)-A Luo heptose base amine; N, O-two (O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; N, O-two (O-acetyl salicyl)-glucoheptose base amine; N, O-two (O-acetyl salicyl)-mannoheptose base amine; N, O-two (O-acetyl salicyl)-Gu Luo heptose base amine; N, O-two (O-acetyl salicyl)-Ai Du glycosyl in heptan amine; N, O-two (O-acetyl salicyl)-galactoheptose base amine; And N, O-two (O-acetyl salicyl)-Ta Luo glycosyl in heptan amine, wherein suffix " glycosyl amine (sylamine) " also can be with " camine " expression, and their mixture and combination.
(4) N-(O-acetyl salicyl)-amino acid
[0029] dimer or other oligomer compounds of the connection of the preferably logical one or more superamide key chemistry of N-(O-acetyl salicyl)-amino acid preferably form between at least 1 O-acetyl salicyl and amino acid whose amino.N-(O-acetyl salicyl)-amino acid can be represented by following universal architecture:
R 1CHNHR 2(CH 2) nCOR 3
R wherein 1Be H, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 14 carbon atom, R 1Also can have OH, SH, SCH 3, NH 2, NHR 2, CONH 2, NHCONH 2, NHC (=NH) NH 2, NHC (=NR 2) NH 2, imidazoles, pyrrolidines or other heterocyclic radicals; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; N is 0 to 5 integer; R 3Be NH 2, OR 4R 4Be H, have alkyl, aralkyl or an aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be replaced by I, F, Cl, Br, OH or the alkoxyl with 1 to 9 carbon atom.
[0030] in the amino acid known to generally, proline can not be represented with above-mentioned universal architecture, because α amino is the part of heterocycles pyrrolidine ring.Therefore, N-(O-acetyl salicyl)-proline can only be represented with chemical name.N-(O-acetyl salicyl)-amino acid can be for example D, L or DL of stereoisomer, N-(O-acetyl salicyl)-L-tyrosine for example, or non-stereoisomer N-(O-acetyl salicyl)-glycine for example, saturated or undersaturated, the form of straight or branched or ring is as free acid, salt, inclined to one side salt, lactone, acid amides or ester-formin.Too complicated and can not be with above-mentioned universal architecture covering the time, will only describe N-(O-acetyl salicyl) amino acid as fruit structure by chemical name.
[0031] below representational N-(O-acetyl salicyl) amino acid-N-(O-acetyl salicyl)-alanine, N-(O-acetyl salicyl)-arginine; N, N '-two (O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-asparagine, N-(O-acetyl salicyl)-L-aminobutanedioic acid, N-(O-acetyl salicyl)-cysteine, N-(O-acetyl salicyl)-glycine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-histidine; N, N '-two (O-acetyl salicyl)-histidine, N-(O-acetyl salicyl)-isoleucine, N-(O-acetyl salicyl)-leucine, N-(O-acetyl salicyl)-lysine; N, N '-two (O-acetyl salicyl)-lysine, N-(O-acetyl salicyl)-methionine, N-(O-acetyl salicyl)-phenyl alanine, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-serine, N-(O-acetyl salicyl)-threonine, N-(O-acetyl salicyl)-tryptophan; N, N '-two (O-acetyl salicyl)-tryptophan, N-(O-acetyl salicyl)-tyrosine, N-(O-acetyl salicyl)-valine, N-(O-acetyl salicyl)-Beta-alanine, N-(O-acetyl salicyl)-γ-An Jidingsuan, N-(O-acetyl salicyl)-B-AIB, N-(O-acetyl salicyl)-citrulling, N-(O-acetyl salicyl)-DOPA (3, the 4-DA), N-(O-acetyl salicyl)-homocysteine, N-(O-acetyl salicyl)-homoserine, N-(O-acetyl salicyl)-ornithine; N, N '-two (O-acetyl salicyl)-ornithine, N-(O-acetyl salicyl)-phenylglycine and N-(O-acetyl salicyl)-4-glycin, and their mixture and combination.
(5) N-(O-acetyl salicyl)-peptide
[0032] N-(O-acetyl salicyl)-peptide by tripolymer or other oligomer compounds of the connection of one or more amido link chemistry, is to form between the amino of O-acetyl salicyl and dipeptides or other oligopeptides preferably.Oligopeptide comprises 2 to 10 amino acid unit usually.But preferred N-(O-acetyl salicyl)-peptide is the tripolymer compound that is formed by amido link by 1 O-acetyl salicyl and dipeptides.N-(O-acetyl salicyl)-dipeptides can be represented with following universal architecture:
R 1CHNHR 2CO?NHCHR 1COR 3
R wherein 1Be H independently, have alkyl, aralkyl or the aryl of 1 to 14 carbon atom, can have OH, SH, SCH 3, NH 2, CONH 2, NHCONH 2, NHC (=NH) NH 2, imidazoles, pyrrolidines or other heterocyclic radicals; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be NH 2, OR 4R 4Be H, have alkyl, aralkyl or an aryl of 1 to 14 carbon atom; The H that is connected with any carbon atom can be replaced by I, F, Cl, Br, OH or the alkoxyl with 1 to 9 carbon atom.
[0033] N-(O-acetyl salicyl)-peptide can be for example D, L or DL of stereoisomer, for example N-(O-acetyl salicyl)-L-Tyr-L-Tyr or non-stereoisomer N-(O-acetyl salicyl)-Gly-Gly for example.In the amino acid known to generally, proline can not be represented with above-mentioned universal architecture, because α amino is the part of heterocycles pyrrolidine ring.Therefore, N-(O-acetyl salicyl)-proline peptide can only be represented with title.N-(O-acetyl salicyl)-peptide can be saturated or undersaturated, and the form of straight or branched or ring is as free acid, salt, inclined to one side salt, lactone, acid amides or ester-formin.Many N-(O-acetyl salicyl)-oligopeptide can only be represented with their chemical name, because they can not be represented by above-mentioned universal architecture.
[0034] following is representational N-(O-acetyl salicyl)-dipeptides-N-(O-acetyl salicyl)-kyotorphin (Tyr-Arg), N-(O-acetyl salicyl)-anserine (β-Ala-1-N-Me-His), N-(O-acetyl salicyl)-β-Ala-Lys, N-(O-acetyl salicyl)-Asp-Glu, N-(O-acetyl salicyl)-carnosine (β-Ala-His), N-(O-acetyl salicyl)-Gly-Gln, N-(O-acetyl salicyl)-γ-D-Glu-Gly, N-(O-acetyl salicyl)-γ-Glu-Val, N-(O-acetyl salicyl)-γ-Glu-Ile, N-(O-acetyl salicyl)-γ-Glu-Leu, N-(O-acetyl salicyl)-γ-Glu-Met, N-(O-acetyl salicyl)-γ-Glu-Phe, N-(O-acetyl salicyl)-γ-Glu-Ala, N-(O-acetyl salicyl)-γ-Glu-Tyr, N-(O-acetyl salicyl)-γ-Glu-Phe, N-(O-acetyl salicyl)-Leu-Leu, N-(O-acetyl salicyl)-ophidine (β-Ala-2-Me-His), N-(O-acetyl salicyl)-Met-Phe, N-(O-acetyl salicyl)-Ser-Tyr-NH 2, N-(O-acetyl salicyl)-Tyr-Pro-NH 2, and their mixture and combination.
[0035] following is representational N-(O-acetyl salicyl)-tripeptides-N-(O-acetyl salicyl)-bursin (Lys-His-Gly-NH 2), N-(O-acetyl salicyl)-D-Phe-Phe-Gly; N-(O-acetyl salicyl)-diprotin A (Ile-Pro-Ile), N-(O-acetyl salicyl)-glutathione (Y-Glu-Cys-Gly), N-(O-acetyl salicyl)-pGlu-Glu-Pro-NH 2, N-(O-acetyl salicyl)-Lys-Trp-Lys, N-(O-acetyl salicyl)-Lys-Tyr-Lys, N-(O-acetyl salicyl)-ophthalmic acid, N-(O-acetyl salicyl)-norophthalmic acid (γ-Glu-Ala-Gly), N-(O-acetyl salicyl)-homoglutathion (two-γ-Glu-Cys-two-β-Ala), N-(O-acetyl salicyl)-Met-Leu-Phe, N-(O-acetyl salicyl)-Tyr-Gly-Gly, N-(O-acetyl salicyl)-Pro-Leu-Gly-NH 2, and their mixture and combination.
[0036] following is representational N-(O-acetyl salicyl)-oligopeptide-N-(O-acetyl salicyl)-Lys-Lys-Gly-Glu, N-(O-acetyl salicyl)-Arg-Pro-Lys-Pro, N-(O-acetyl salicyl)-Gly-Gly-Phe-Leu, N-(O-acetyl salicyl)-Arg-Gly-Asp-Ser, N-(O-acetyl salicyl)-Arg-Gly-Glu-Ser, N-(O-acetyl salicyl)-Met-Leu-Phe-Phe, N-(O-acetyl salicyl)-Val-Ala-Pro-Gly, N-(O-acetyl salicyl)-Val-Gly-Ser-GIu, N-(O-acetyl salicyl)-Ala-Pro-Gly-Trp-NH 2, N-(O-acetyl salicyl)-Gly-Gly-Phe-Met-NH 2, N-(O-acetyl salicyl)-endorphin 1 (Tyr-Pro-Trp-Phe-NH 2), N-(O-acetyl salicyl)-endorphin 2 (Tyr-Pro-Phe-Phe-NH 2), N-(O-acetyl salicyl)-morphiceptin (Tyr-Pro-Phe-Pro-NH 2), N-(O-acetyl salicyl)-outer deltorphin delta C (Tyr-Pro-Ile-Ser-Leu), N-(O-acetyl salicyl)-pyroGlu-Glu-Asp-Ser-Gly, N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Leu, N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Met, N-(O-acetyl salicyl)-pyroGlu-Leu-Tyr-Glu-Asn-Lys, N-(O-acetyl salicyl)-Arg-Arg-Pro-Tyr-Ile-Leu, N-(O-acetyl salicyl)-Val-Gly-Val-Ala-Pro-Gly, N-(O-acetyl salicyl)-Tyr-Pro-Ile-Ser-Leu, N-(O-acetyl salicyl)-Arg-Lys-Arg-Ala-Arg-Lys-Glu, N-(O-acetyl salicyl)-kemptide (Leu-Arg-Arg-Ala-Ser-Leu-Gly), N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Leu-Arg-Arg, N-(O-acetyl salicyl)-Met-Glu-His-Phe-Arg-Trp-Gly, N-(O-acetyl salicyl)-Arg-Val-Tyr-Ile-His-Pro-Phe, N-(O-acetyl salicyl)-β-junket deltorphin delta (Tyr-Pro-Phe-Val-Glu-Pro-Ile), N-(O-acetyl salicyl)-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, N-(O-acetyl salicyl)-Met-Gln-Met-Lys-Lys-Val-Leu-Asp-Ser, N-(O-acetyl salicyl)-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg, N-(O-acetyl salicyl)-Ile-Ala-Arg-Arg-His-Pro-Tyr-Phe-Leu, N-(O-acetyl salicyl)-Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH 2, N-(O-acetyl salicyl)-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH 2, N-(O-acetyl salicyl)-Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Arg-Gly-NH 2, and their mixture and combination.
(6) Xiang Guan (O-acetyl salicyl)-derivative
[0037] Xiang Guan derivative comprises: O-(O-acetyl salicyl)-amino acid; N, O-two (O-acetyl salicyl)-amino acid; N, O, O-three (O-acetyl salicyl)-amino acid; S-(O-acetyl salicyl)-amino acid; N, S-two (O-acetyl salicyl)-amino acid; O, S-two (O-acetyl salicyl)-amino acid is preferably from the amino acid with hydroxyl or sulfydryl.Other (O-acetyl salicyl)-derivatives comprise: N-(O-acetyl salicyl)-amino-oligosaccharide; N-(O-acetyl salicyl)-oligomeric-aminosugar; N, O-two (O-acetyl salicyl)-amino-oligosaccharide; And N, O-two (O-acetyl salicyl)-oligomeric-aminosugar.In amino-oligosaccharide and oligomeric aminosugar, O-acetyl salicyl can be connected with amino and/or hydroxyl.Above-mentioned amino acid whose example comprises serine, homoserine, 3-Phenserine, threonine, tyrosine, 4-glycin, cysteine, homocysteine and DOPA.
[0038] following is representational (O-acetyl salicyl) amino acid derivativges-S-(O-acetyl salicyl)-cysteine; N, S-two (O-acetyl salicyl)-cysteine; S-(O-acetyl salicyl)-homocysteine; N, S-two (O-acetyl salicyl)-homocysteine; O-(O-acetyl salicyl)-4-glycin; N, O-two (O-acetyl salicyl)-4-glycin; O-(O-acetyl salicyl)-serine; N, O-two (O-acetyl salicyl)-serine; O-(O-acetyl salicyl)-homoserine; N, O-two (O-acetyl salicyl)-homoserine; O-(O-acetyl salicyl)-3-Phenserine; N, O-two (O-acetyl salicyl)-3-Phenserine; O-(O-acetyl salicyl)-threonine; N, O-two (O-acetyl salicyl)-threonine, O-(O-acetyl salicyl)-tyrosine; N, O-two (O-acetyl salicyl)-tyrosine, O-(O-acetyl salicyl)-DOPA; O, O-two (O-acetyl salicyl)-DOPA; N, O-two (O-acetyl salicyl)-DOPA and N, O, O-three (O-acetyl salicyl)-DOPA; And their mixture and combination.
[0039] the O-acetyl acetylsalicyl derivatives of aminosugar, amino acid and peptide has advantage with similar pharmacy of aspirin and therapeutic action in the embodiment, but does not have for example hemorrhage of gastrointestinal tract of illeffects.This pharmacy and therapeutic action comprise analgesia, anti-inflammatory and antipyretic effect, and to the protective effect of cardiovascular system.
[0040] according to embodiment preferred, a kind of composition is provided, comprise at least aly, be used for the local illness relevant with nerve, blood vessel, muscle skeleton or integumentary system with systematic treating with the O-acetyl acetylsalicyl derivatives that is selected from aminosugar, amino acid and peptide that exists of treatment effective dose, their form and the pharmaceutically acceptable carrier of free acid, ester, acid amides, lactone or salt.
[0041] in one embodiment, said composition can comprise O-acetylsalicylic acid (aspirin) and O-acetyl acetylsalicyl derivatives, for example comprises for example O-acetyl salicyl amino sugar derivative of arginine, ornithine or lysine of aminoglucose or basic amino acid.Said composition also can comprise the mixture of O-acetyl salicyl derivative compound, has or do not exist aspirin.In a preferred embodiment, a kind of composition can comprise a kind of O-acetyl salicyl derivative compound, and does not have aspirin or other O-acetyl salicyl derivative compound.
[0042] in another embodiment, also comprise can be simultaneously or cosmetics, medicine or other reagent used in order for said composition.These reagent comprise hydroxy acid, ketone acid and relevant compound; Phenyl α acyloxy alkanoic acid and derivative thereof; N-acetyl group-aldose amine, acid of N-acetyl-amino and relevant N-acetyl compounds; Topical pain relief agent and anaesthetic; Anti-acne agents; Antibacterial agent; Anti-yeast agent, antifungal agent; Antivirotic; Dandruff removing agent; Anti-dermatitis agent; Antihistaminic; Antipruritic; Antemetic; Anti-motion sickness agent; Antiinflammatory; Anti-hyperkeratosis agent; Antiperspirant; Antipsoriatic; Antiseborrheic; Hair conditioner and hair therapy agent; Anti-aging and anti-wrinkle agent; Sun-proof and opacifier; Skin brightening agent; Depigmenting agent; Astringent; Cleaning agent; Corn, poroma and wart remover; The local cardiovascular agents of using; Vitamin; Cortin; Tanning agent; Hormone; Retinoid; Gingival disease or oral cavity nursing agent.
[0043] be incorporated into the group containing O-acetyl salicylic derivative composition produced synergistic or synergistic effects of cosmetics; drugs and other agents include: abacavir; acebutolol; paracetamol; acetaminophen sand Luo; acetazolamide; acetic acid, hydroxylamine; N-acetyl - cysteine; N-acetyl - glucosamine; N-acetyl - glutamine; N-acetyl - lysine; N-acetyl - ornithine ; N-acetyl - prolinamide; N-acetyl - proline; acetylsalicylic acid; Acitretin; alclometasone; acrivastine; actiq; acyclovir; adapalene; A Defu Wei two volts esters; cytarabine; salbutamol; alfuzosin; allopurinol; Austrian celecoxib allopurinol; almotriptan; alprazolam; Alprenolol; aluminum acetate; aluminum chloride; hydrated aluminum chloride; hydroxide; amantadine; amiloride; amino acridine; amino benzoic acid (PABA); aminocaproic acid; amino acid; amiodarone; amitriptyline; amlodipine; A Moka triazine; phenol quinoline; amorolfine; amoxapine; amphetamine; ampicillin; anagrelide; anastrozole; Anthralin; apomorphine; aprepitant; arbutin; aripiprazole yl; ascorbic acid; ascorbyl palmitate; atazanavir; atenolol; atomoxetine; atropine; azathioprine; azelaic acid; azelastine; azithromycin; bacitracin; beclomethasone dipropionate; shellfish America grid; benazepril; bendroflumethiazide; benzocaine; benzonatate; benzophenone; benzoyl peroxide; benztropine; bepridil; betamethasone dipropionate; betamethasone valerate; brimonidine; brompheniramine; bupivacaine; buprenorphine; bupropion; cloth immediately amine; butenafine; Butoconazole; cabergoline; caffeic acid ; caffeine; calcipotriene; camphor; candesartan; capsaicin; carbamazepine; carbamide peroxide; cefditoren; cefepime; cefpodoxime; celecoxib; cetirizine ; Cevimeline; chitosan; chlordiazepoxide; chlorhexidine; chloroquine; hydrochlorothiazide; chloroxylenol; chlorpheniramine; chlorpromazine; chlorpropamide; ciclopirox; cilostazol azole; cimetidine; cinacalcet; ciprofloxacin; citalopram; citric acid; cladribine; clarithromycin; clemastine; clindamycin; clioquinol; clobetasol; clomiphene ; clonidine; clopidogrel; clotrimazole; clozapine; tar; cocaine; codeine; cromolyn sodium; Crotamiton; Prosecco force triazine; cyclobenzaprine; cycloserine; Ara glycosides; dacarbazine; dalfopristin; nitrogen phenyl sulfone; daptomycin; daunorubicin; area deferoxamine; DHEA; delavirdine; desipramine; ground loratadine ; desmopressin; go hydroxyl betamethasone; dexamethasone; dexmedetomidine given; Right methylphenidate; dexrazoxane; dextroamphetamine; diazepam; dicyclomine; didanosine; hydrocodone be due; hydromorphone; diltiazem; 6; 8 - dimercapto octanoic acid (dihydro-lipoic acid); diphenhydramine; diphenoxylate; dipyridamole; disopyramide; dobutamine; many non-profit Special; dolasetron; multi-naphthalene donepezil; dopa ester; dopa amide; dopamine; dorzolamide; doxepin; doxorubicin; doxycycline; doxylamine; doxypin; degree Losey Ting; Dyclonine; econazole; according fluorine ornithine; according to Li triptans; emtricitabine; enalapril; ephedrine; adrenaline; ephedra Ning; epirubicin; eptifibatide ; ergotamine; erythromycin; according milnacipran; esmolol; esomeprazole; estazolam; estradiol; ethacrynic acid; ethinyl estradiol; according Articaine; etomidate; famciclovir; famotidine; felodipine; fentanyl; ferulic acid; fexofenadine; flecainide; fluconazole; flucytosine; fluocinolone; fluocinonide; 5 - fluorouracil; fluorine West Ting; fluphenazine; flurazepam; fluvoxamine; formoterol; furosemide; galactarolactone; galactono; galacturonic acid lactone; galantamine; gatifloxacin; gefitinib Nepal; gemcitabine; gemifloxacin; acetylglucosamine lactone; gluconic acid; gluconolactone; glucuronic acid; glucuronolactone; glycolic acid; griseofulvin; Guaifenesin; guanidine pyridine; N-guanine base histamine; haloperidol; halogen general nearly; hexyl resorcinol; homatropine; homosalate; hydralazine; hydrochlorothiazide; hydrocortisone; hydrocortisone 21 - acetate; hydrocortisone 17 - butyrate; hydrocortisone 17 - valerate; hydrogen peroxide; hydromorphone; hydroquinone; hydroquinone monomethyl ether; hydroxyzine; ranunculus henbane base; hypoxanthine ; ibuprofen; ichthyol; idarubicin; imatinib; imipramine; dense imiquimod; indinavir; indomethacin; irbesartan; irinotecan; ethyl isoproterenol Su; isoproterenol; itraconazole; kanamycin; ketamine; ketanserin; ketoconazole; ketoprofen; ketotifen; Kojic; labetalol; lactic acid; lactobionic acid; Lamy telbivudine; lamotrigine; lansoprazole; letrozole; leuprolide; levosalbutamol; levofloxacin; lidocaine; linezolid; lobeline; loperamide; losartan; Luo sand flat; lysergic acid ethyl amine; Mafenide; malic acid; maltose acid; mandelic acid; maprotiline; mebendazole; America Kala Ming; America Crowe triazine; A chlorine doxycycline; memantine; mint alcohol; pethidine; mepivacaine; mercaptopurine; mescaline; 3 - norepinephrine; between the hydroxyl isoproterenol; metaraminol; metformin; methadone; methamphetamine; methotrexate; Methoxamine; methyldopa ester; methyldopa amide; 3,4 - methylenedioxy-methamphetamine; methyl lactate; nicotinate; methylphenidate; methyl salicylate; A sulfur Mitt; metolazone; metoprolol; metronidazole; mexiletine; miconazole; midazolam; midodrine; America Groote; minocycline; minoxidil; mirtazapine; mitoxantrone; Tamoxifen enalaprilat; do indanone; monobenzone; morphine; moxifloxacin; moxonidine; mupirocin; nadolol; Naftifine; Naboo brown; nalmefene; naloxone; naproxen; nefazodone; nelfinavir; neomycin; nevirapine; nicardipine; nicotine; nifedipine; nimodipine; nisoldipine; Nizar horizon; norepinephrine; nystatin; Ao Keba amine; octreotide; methoxy octyl; octyl salicylate; ofloxacin; olanzapine; olmesartan; olopatadine; omeprazole azole; ondansetron; Oxiconazole; oxotremorine; oxybenzone; oxybutynin; oxycodone; oxymetazoline; octyl dimethyl dapsone; palonosetron; pantothenic acid; panthenol lactone; paroxetine; pemoline; penciclovir; penicillamine; penicillin; pentazocine; pentobarbital; spray statins; pentoxifylline; pergolide special forces; perindopril Cape Lee; permethrin; phencyclidine; phenelzine; non Nila Min; Fen America song triazine; phenobarbital; phenol; phenoxybenzamine; phentolamine; phenylephrine; phenylpropanolamine; phenytoin; physostigmine; pilocarpine; pimozide; pindolol; pioglitazone; horses Mary piperazine hydrochloride; piperonyl butoxide; piperazine Valenciennes level; podofilox; podophyllin; povidone-iodine; Pramipexole; pramoxine; prazosin; prednisone; PRENALTEROL; prilocaine; procainamide; procaine; procarbazine; oxaprozin; promethazine; propionate promethazine; propafenone; propoxyphene; propranolol; propylthiouracil; protriptyline; pseudoephedrine; pyrethrin; pyrilamine; pyrimethamine; quetiapine; quinapril; quinoline B cases; quinidine; quinupristin; rabeprazole; reserpine; resorcinol; retinoid; 13 - cis-retinoic acid; retinoic acid; retinol; retinol B esters; retinyl palmitate; ribavirin; ribose acid; ribose acid lactone; rifampin; rifapentine; Lifestyle Ximing; riluzole; rimantadine; risedronic acid; Lee risperidone; ritodrine; rivastigmine; rizatriptan; ropinirole; ropivacaine; salicylamide; salicylic acid; salmeterol; scopolamine; selegiline; selenium disulfide ; 5 - serotonin; sertindole; sertraline; shell rock asphalt; sibutramine; sildenafil; sotalol; streptomycin; strychnine; sulfur itraconazole; sulfonamides benzene; sulfa benzoyl; sulfa bromide dimethyl pyrimidine; sulfacetamide; Sulfachloropyridazine hydralazine; sulfa B cytosine; sulfadiazine; sulfonamides to Suoxin; sulfadoxine; sulfaguanole; sulfa forest; sulfamethoxazole; sulfamethoxazole; sulfonamides; sulfa topiramate triazine; SASP; sulfasalazine; sulfa isothiazolin; Sulfathiazole; sulfisoxazole; sulfur; tadalafil; tamsulosin; tartaric acid; tazarotene; tegaserol; telithromycin; telmisartan ; late for acetazolamide; tenofovir; terazosin; terbinafine; terbutaline; Terconazole; terfenadine; tetracaine; tetracycline; tetrahydro benzoic cefazolin; theobromine ; theophylline; thiabendazole; lipoic acid (lipoic acid); thioridazine; thiothixene; thymol; tiagabine; timolol; tinidazole; Sekondi azole; tirofiban Ban; tizanidine; tobramycin; tocainide; Torah oxazoline; tolbutamide; tolnaftate; tolterodine; tramadol; tranylcypromine; trazodone; triamcinolone acetonide Germany; triamcinolone; own triamcinolone acetonide; triamterene; triazolam; triclosan; trifluoropropionaldehyde triazine; trimethoprim; trimipramine; song topiramate Namin; triprolidine; ammonia tromethamine; tropic acid; tyramine; eleven carbonate; urea; urocanic acid; ursodeoxycholic acid; vardenafil; venlafaxine; verapamil; acetate vitamin E; voriconazole; China and France Lin; wood tar; xanthine; zafirlukast; zaleplon; topiramate lipoic; ziprasidone; zolmitriptan; Junior zolpidem....
[0044] composition that comprises O-acetyl acetylsalicyl derivatives can be mixed with solution, gel, lotion, emulsifiable paste, ointment, shampoo, spray, patch, powder, face shield, collutory or washing agent, vagina gel or preparation, perhaps other acceptable forms are used for skin, nail, hair, oral mucosa, vagina or anal mucosa, oral cavity or gum.
[0045] for the preparation liquid composite, at least a O-acetyl acetylsalicyl derivatives in the embodiment can be dissolved in the solution that water, ethanol, propane diols, butanediol and/or other local acceptable carriers make.The concentration of single O-acetyl acetylsalicyl derivatives or the total concentration that comprises all O-acetyl acetylsalicyl derivatives in the composition of more than a kind of O-acetyl acetylsalicyl derivatives can be 0.01 to 99.9% weight that accounts for total composition, preferred concentration is to account for about 0.1 of total composition to arrive about 50% weight, and preferred concentration is to account for about 0.5 of total composition to arrive about 25% weight.
[0046] for preparing the topical compositions of lotion, emulsifiable paste or ointment, can at first O-acetyl acetylsalicyl derivatives be dissolved in water, ethanol, propane diols and/or other carriers, the solution that obtains is like this mixed with the matrix or the pharmaceutically acceptable carrier that need, with preparation lotion, emulsifiable paste or ointment.The concentration of O-acetyl acetylsalicyl derivatives can be same as described above.
[0047] also topical compositions can be mixed with the form of gel or shampoo.Preparation typical gels composition comprises that for example shitosan, methylcellulose, ethyl cellulose, polyvinyl alcohol, polyquatemiums, hydroxyethylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, card pool nurse or ammonium glycyrrhetate join in the solution that comprises O-acetyl acetylsalicyl derivatives with gelling agent.The preferred concentration of gelling agent can be to account for about 0.1 of total composition to arrive about 4% weight.When the preparation shampoo, can at first O-acetyl acetylsalicyl derivatives be dissolved in water or the propane diols, the solution that obtains is like this mixed with shampoo matrix.The O-acetyl acetylsalicyl derivatives ground concentration of using in gel or shampoo form can be same as described above.
[0048] is preparation synergy or synergistic local, by with agent dissolves or be mixed in the said preparation and cosmetics, medicine or other reagent can be incorporated in above-mentioned arbitrary composition with the combination composition.The other forms of composition of sending O-acetyl acetylsalicyl derivatives is that those skilled in the art are easy to can mix, prepare or prepare.
[0049] uses for system, O-acetyl acetylsalicyl derivatives can be mixed with and be used for oral or stomach and intestine are injected outward.In oral formulations, O-acetyl acetylsalicyl derivatives can be mixed with tablet or with or not with the gelatine capsule of gelatin powder.Each tablet or capsule can comprise about 10 to about 300mg O-acetyl acetylsalicyl derivatives.For example, 1 and No. 0 Lilly gelatine capsule comprises N-(O-acetyl salicyl)-L-TEE powder of about 10Omg and 150mg respectively.In an identical manner, 1 and No. 0 Lilly gelatine capsule comprises N-(O-acetyl salicyl)-D-4-glycin ethyl ester powder of about 130mg and 200mg respectively.Inject outward for stomach and intestine, can prepare O-acetyl acetylsalicyl derivatives at aseptic condition, concentration is about 1 to about 10% in water, propane diols and/or other pharmaceutically acceptable carriers usually.
[0050] comprise in the embodiment composition of O-acetyl acetylsalicyl derivatives can the part or systemic application in the human patients of needs, be used for prevention or treatment cosmetic illness, skin disorder or with nerve, blood vessel, muscle vascular or integumentary system diseases associated.
[0051] use for the part, can every day 1 to 3 time according to the composition that comprises O-acetyl acetylsalicyl derivatives of preparation part preparation, be applied topically in the infringement or skin site relevant for 2 times preferred every day with illness or disease.Continue topical application, until eradicating or having improved illness or disease substantially.Situation or severity that the treatment phase is depended on illness or disease also depend on individual patients.Illness relevant with nerve, blood vessel, muscle skeleton or integumentary system or disease comprise pain, pruritus, inflammation, erythema, dermatitis, acne, eczema, severe Dry, ichthyosis, poroma, keratosis, hyperkeratosis illness, senile plaque, trichophytosis, wrinkle and photoaging skin.The composition that has been found that the O-of comprising acetyl acetylsalicyl derivatives of the present invention is for the part prevention or to treat the relevant illness of various nerves, blood vessel, muscle skeleton or integumentary system be useful or effective.For example, the human patients topical application of suffering from severe Dry (ichthyosis) contains the hydrophilic ointment of N-(O-acetyl salicyl)-aminoglucose (5%), every day 2 times, totally 2 weeks.When 2 weeks, treatment finished, originally thick and skin squamous became smooth, demonstrates skin by medical assessment and has improved 75%.
[0052] for systemic application, can absorb by injection, infusion or oral cavity according to the composition that comprises O-acetyl acetylsalicyl derivatives of preparation part preparation and to use, preferred approach is oral.The composition that comprises O-acetyl acetylsalicyl derivatives can every day oral 1 to 3 time, preferred 2 times, is used to prevent or treat illness or the disease relevant with nerve, blood vessel, muscle skeleton or integumentary system.Continue oral, until eradicating or having improved illness or disease substantially.
We have found that [0053] composition that systemic administration comprises O-acetyl acetylsalicyl derivatives is that treatment is useful or effective for prevention or treatment illness or the disease relevant with nerve, blood vessel, muscle skeleton or integumentary system.These illnesss or disease comprise pain, pruritus, inflammation, erythema, dermatitis, eczema, dementia, arthralgia or swelling and arthritis.For example, the two knees of a certain human patients were suffered from osteoarthritis 4 years, when walking pain symptom is arranged, and pain intensity were waited until severe in being when rest.With non-steroidal anti-inflammatory agent for example naproxen and brufen do not improve symptom, but every day, oral 10-30mg metacortandracin then had incomplete alleviation.The patient is oral several years ago aspirin, but acute gastrointestinal bleeding has taken place behind oral aspirin.The N-that this patient's oral dose is 100mg (O-acetyl salicyl)-L-TEE.Under this dosage, have only negligible discomfort or adverse reaction, be limited to the alleviation of knee pain.When oral dosage was brought up to 1g, knee pain disappeared after oral back 2 and a half hours.The patient carries out high-intensity physical exertion, but does not all feel knee pain all day.Oral dose is that N-(O-acetyl salicyl)-L-TEE of 1g has only negligible discomfort or adverse reaction.The above results shows that oral O-acetyl salicyl amino acid is that treatment is effective for the treatment illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
[0054] in compound as herein described, preferred O-acetyl acetylsalicyl derivatives comprises: N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-glycine ethyl ester, N-(O-acetyl salicyl)-TEE, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-prolineamide, N-(O-acetyl salicyl)-ethyl prolinate, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamate diethyl ester, N-(O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-4-glycin ethyl ester; N, O-two (O-acetyl salicyl)-4-glycin ethyl ester, N-(O-acetyl salicyl)-3-Phenserine; N-(O-acetyl salicyl)-3-Phenserine ethyl ester; N-(O-acetyl salicyl)-lysine, N-(O-acetyl salicyl)-ornithine, and their mixture and combination.Oral these representational compounds are effective and useful for alleviating the arthralgia or the inflammation that are caused by arthritis or other illnesss.
[0055] the following examples are illustrative, rather than limit method and composition of the present invention.That in treatment, can run into usually and it will be apparent to those skilled in the art to other appropriate changes of various conditions and parameter and adjust also in the spirit and scope of embodiment.
Embodiment 1
[0056] N-(O-acetyl salicyl)-D-aminoglucose 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 4.6 like this, and comprise 5%N-(O-acetyl salicyl)-D-aminoglucose.
[0057] 73 years old right leg suffers from above-mentioned 5%N-(O-acetyl the salicyl)-D-aminoglucose emulsifiable paste of male patient's local application of itch eczema.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 75% validity.The result shows that N-(O-acetyl salicyl)-aminosugar is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 2
[0058] N-(O-acetyl salicyl)-glycine ethyl ester 5g is dissolved in the 95ml solution, this solution is to have the propane diols of 70 parts of volume of ethanol and 30 parts of volumes to make.Zhi Bei pH value of solution is 5.3 like this, comprises 5%N-(O-acetyl salicyl)-glycine ethyl ester, is that treatment is useful or effective for topical treatment of inflammation and the illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 3
[0059] N-(O-acetyl salicyl)-glycine ethyl ester 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 4.4 like this, and comprise 5%N-(O-acetyl salicyl)-glycine ethyl ester.
[0060] 73 years old left leg suffers from above-mentioned 5%N-(O-acetyl the salicyl)-glycine ethyl ester emulsifiable paste of male patient's local application of eczema.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 75% validity.The result shows that N-(O-acetyl salicyl)-amino-acid ester is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 4
[0061] N-(O-acetyl salicyl)-L-TEE 5g is dissolved in the 95ml solution, this solution is to have the propane diols of 70 parts of volume of ethanol and 30 parts of volumes to make.Zhi Bei pH value of solution is 3.6 like this, comprises 5%N-(O-acetyl salicyl)-L-TEE, for topical therapeutic pain, inflammation and with nerve, blood vessel, muscle skeleton or integumentary system diseases associated be that treatment is useful or effective.
Embodiment 5
[0062] N-(O-acetyl salicyl)-L-TEE 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 3.0 like this, and comprise 5%N-(O-acetyl salicyl)-L-TEE.
[0063] 73 years old left thigh suffers from above-mentioned 5%N-(O-acetyl the salicyl)-L-TEE emulsifiable paste of male patient's local application of itch eczema.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 75% validity.The result shows that N-(O-acetyl salicyl)-amino-acid ester is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 6
[0064] N-(O-acetyl salicyl)-L-proline 5g is dissolved in the 95ml solution, this solution is to have the propane diols of the heat of 70 parts of volume of ethanol and 30 parts of volumes to make.Zhi Bei pH value of solution is 2.2 like this, comprises 5%N-(O-acetyl salicyl)-L-proline, for topical therapeutic itch, inflammation and with nerve, blood vessel, muscle skeleton or integumentary system diseases associated be that treatment is useful or effective.
Embodiment 7
[0065] N-(O-acetyl salicyl)-L-proline 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 2.5 like this, and comprise 5%N-(O-acetyl salicyl)-L-proline.
[0066] 73 years old the left hand back of the body suffers from above-mentioned 5%N-(O-acetyl the salicyl)-L-proline emulsifiable paste of male patient's local application of itch eczema.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 100% validity.The result shows that N-(O-acetyl salicyl)-amino acid is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 8
[0067] N-(O-acetyl salicyl)-D-4-glycin ethyl ester 5g is dissolved among the propane diols 35ml of heat, the soft paste for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 3.1 like this, and comprise 5%N-(O-acetyl salicyl)-D-4-glycin ethyl ester, for topical therapeutic severe Dry, inflammation and with nerve, blood vessel, muscle skeleton or integumentary system diseases associated be that treatment is useful or effective.
Embodiment 9
[0068] 34 years old the severe Dry illness of suffering from the X-x-linked ichthyosis and have that male patient thick and the adhesivity sauriasis is local to use as 5%N-(O-acetyl salicyl)-D-aminoglucose emulsifiable paste that embodiment 1 prepares every day 2 times, totally 2 weeks.After 2 weeks finished, reduce in treatment region adhesivity sauriasis, the skin of treatment becomes smooth.Judge that by clinical evaluation the property improved is 75%.
Embodiment 10
The male patient of [0069] 83 years old body weight 90kg has the two knee osteoarthritis histories in 4 years, and osteoarthritis confirms by X-ray and MRI, shows that the joint space reduces.Exist to walk and pain during rest always, and the symptom of touching a tender spot during palpation, intensity waits until that therefrom severe does not wait.Non-steroidal anti-inflammatory agent for example naproxen and brufen can not be alleviated this symptom, but every day oral 10-30mg metacortandracin can alleviate by halves.
[0070] this patient uses N-(O-acetyl salicyl)-L-TEE, morning oral dose 10mg, be 100mg afternoon.Under this dosage, have only negligible discomfort or adverse reaction, limited to the alleviation of knee pain.When oral dosage was brought up to 1g, knee pain disappeared after oral two and one-half-hours.Carry out the high strength physical exertion ensuing 10 hours patients, comprise the agricultural work of knocking off, be included in the pond on the bank down climbing cut the common cattail weeds from the root level, and with hand climbing pond bank to face of land level.Other manual labors comprise and mount and dismount for several times farm tractor, wherein this farm tractor in tow the trailer that the common cattail weeds are housed to sanitary fill.In a whole day with at nightfall, existing knee pain or the knee function is impaired ignores.Discomfort did not appear in morning next day again.The oral dose that the patient uses is 0.5g, has then alleviated the discomfort of knee in 12 hours by halves.When oral dosage is elevated to 0.7g, the discomfort of knee there is obvious but incomplete alleviation.
[0071] O-acetyl acetylsalicyl derivatives as herein described most preferably oral dose every day of N-(O-acetyl salicyl)-L-TEE can be about 5 to about 30mg/kg, preferred about 7 to about 20mg/kg, most preferably from about 10 arrive about 15mg/kg body weight.
[0072] The above results shows, N-(O-acetyl salicyl)-amino acid for systematic treating pain, inflammation and with nerve, blood vessel, muscle skeleton or integumentary system diseases associated be that treatment is useful or effective.
Embodiment 11
[0073] N-(O-acetyl salicyl)-glutamate diethyl ester 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste 60g.Zhi Bei emulsifiable paste or detergent composition pH are 5.2 like this, and comprise 5%N-(O-acetyl salicyl)-glutamate diethyl ester.
[0074] 73 years old right leg suffers from above-mentioned 5%N-(O-acetyl the salicyl)-glutamic acid diester emulsifiable paste of male patient's skin lesion local application of the eczema of strong itch.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 100% validity.The result shows that N-(O-acetyl salicyl)-amino-acid ester is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 12
[0075] N-(O-acetyl salicyl)-D-galactosamine 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 3.9 like this, and comprise 5%N-(O-acetyl salicyl)-D-galactosamine.
[0076] 73 years old right leg suffers from above-mentioned 5%N-(O-acetyl the salicyl)-D-galactosamine emulsifiable paste of male patient's local application of itch eczema.About 5 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 90% validity.The result shows that N-(O-acetyl salicyl)-aminosugar is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
Embodiment 13
[0077] N-(O-acetyl salicyl)-L-proline methyl ester 5g is dissolved among the propane diols 35ml of heat, the solution for preparing is like this mixed with hydrophilic ointment or oil-in-water emulsifiable paste (60g).Zhi Bei emulsifiable paste or detergent composition pH are 4.9 like this, and comprise 5%N-(O-acetyl salicyl)-L-proline methyl ester.
[0078] 73 years old left leg suffers from above-mentioned 5%N-(O-acetyl the salicyl)-L-proline methyl ester emulsifiable paste of male patient's local application of itch eczema.About 2 to 3 minutes itch disappear after local application.Judge that by the therapeutic evaluation alleviating immediately of itch had 90% validity.The result shows that N-(O-acetyl salicyl)-amino-acid ester is that treatment is useful or effective for the topical therapeutic illness relevant with nerve, blood vessel, muscle skeleton or integumentary system.
[0079] although invention has been described with reference to particularly preferred embodiment and embodiment, those skilled in the art will appreciate that to carry out various changes and not exceed its spirit and scope the present invention.

Claims (22)

1. composition, comprise at least a O-acetyl acetylsalicyl derivatives and the acceptable excipient of pharmacy or the carrier for the treatment of effective dose, wherein O-acetyl acetylsalicyl derivatives is selected from O-acetyl salicyl aminosugar, O-acetyl salicyl amino acid, O-acetyl salicyl peptide, and it is free acid, salt, inclined to one side salt, lactone, acid amides, ester, stereoisomer or non-stereoisomer form.
2. the composition of claim 1, wherein O-acetyl acetylsalicyl derivatives is selected from free acid, salt, inclined to one side salt, lactone, acid amides, ester, the N-of stereoisomer or non-stereoisomer form (O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-gucosamine, N-(O-acetyl salicyl)-glycine ethyl ester, N-(O-acetyl salicyl)-TEE, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-prolineamide, N-(O-acetyl salicyl)-ethyl prolinate, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamate diethyl ester, N-(O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-4-glycin ethyl ester; N, O-two (O-acetyl salicyl)-4-glycin ethyl ester, N-(O-acetyl salicyl)-3-Phenserine; N-(O-acetyl salicyl)-3-Phenserine ethyl ester; At least a in N-(O-acetyl salicyl)-lysine and N-(O-acetyl the salicyl)-ornithine.
3. the composition of claim 1, wherein O-acetyl salicyl aminosugar has general formula:
R 1(CHOH) n(CHNHR 2)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, have alkyl, aralkyl or the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace; OH can be by H, NH 2, NHCOCH 3, acetoxyl group or other acyloxy with 2 to 9 carbon atoms replace.
4. the composition of claim 3; wherein O-acetyl salicyl aminosugar is selected from N-(O-acetyl salicyl)-glycerine osamine; N-(O-acetyl salicyl)-erythrose amine; N-(O-acetyl salicyl)-threose amine; N-(O-acetyl salicyl)-ribose amine; N-(O-acetyl salicyl)-Arabic osamine; N-(O-acetyl salicyl)-wood sugar amine; N-(O-acetyl salicyl)-lysol osamine; N-(O-acetyl salicyl)-allose amine; N-(O-acetyl salicyl)-altrose amine; N-(O-acetyl salicyl)-aminoglucose; N-(O-acetyl salicyl)-mannosamine; N-(O-acetyl salicyl)-gulosamine; N-(O-acetyl salicyl)-idose amine; N-(O-acetyl salicyl)-galactosamine; N-(O-acetyl salicyl)-talosamine; N-(O-acetyl salicyl)-A Luo heptose amine; N-(O-acetyl salicyl)-A Zhuo osamine in heptan; N-(O-acetyl salicyl)-glucoheptose amine; N-(O-acetyl salicyl)-mannoheptose amine; N-(O-acetyl salicyl)-Gu Luo heptose amine; N-(O-acetyl salicyl)-Ai Du osamine in heptan; N-(O-acetyl salicyl)-galactoheptose amine; N-(O-acetyl salicyl)-Ta Luo osamine in heptan; N-(O-acetyl salicyl)-glycerine amino acid; N-(O-acetyl salicyl)-erythrose amino acid; N-(O-acetyl salicyl)-threose amino acid; N-(O-acetyl salicyl)-ribose amino acid; N-(O-acetyl salicyl)-arabinose amino acid; N-(O-acetyl salicyl)-wood sugar amino acid; N-(O-acetyl salicyl)-lyxose amino acid; N-(O-acetyl salicyl)-allose amino acid; N-(O-acetyl salicyl)-altrose amino acid; N-(O-acetyl salicyl)-Glucoamino acid; N-(O-acetyl salicyl)-mannose amino acid; N-(O-acetyl salicyl)-gulose amino acid; N-(O-acetyl salicyl)-idose amino acid; N-(O-acetyl salicyl)-galactose amino acid; N-(O-acetyl salicyl)-talose amino acid; N-(O-acetyl salicyl)-A Luo heptose amino acid; N-(O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan; N-(O-acetyl salicyl)-glucoheptose amino acid; N-(O-acetyl salicyl)-mannoheptose amino acid; N-(O-acetyl salicyl)-Gu Luo heptose amino acid; N-(O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan; N-(O-acetyl salicyl)-galactoheptose amino acid; N-(O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan; N-(O-acetyl salicyl) lactose amine; N-(O-acetyl salicyl) muramic acid; N-(O-acetyl salicyl) nerve amines; N-(O-acetyl salicyl) nerve amines lactose; N-(O-acetyl salicyl)-neuraminic acid .N-(O-acetyl salicyl)-4-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-7-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-two-O-acetyl neuraminic acid; N-(O-acetyl salicyl)-glycerine glycosyl amine; N-(O-acetyl salicyl)-erythrose base amine; N-(O-acetyl salicyl)-threose base amine; N-(O-acetyl salicyl)-ribosyl amine; N-(O-acetyl salicyl)-Arabic glycosyl amine; N-(O-acetyl salicyl)-xylosyl amine; N-(O-acetyl salicyl)-lysol glycosyl amine; N-(O-acetyl salicyl)-allose base amine; N-(O-acetyl salicyl)-altrose base amine; N-(O-acetyl salicyl)-glucosyl group amine [also making N-(O-acetyl salicyl)-gucosamine]; N-(O-acetyl salicyl)-mannose group amine; N-(O-acetyl salicyl)-gulose base amine; N-(O-acetyl salicyl)-idose base amine; N-(O-acetyl salicyl)-galactosyl amine; N-(O-acetyl salicyl)-talose base amine; N-(O-acetyl salicyl)-A Luo heptose base amine; N-(O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; N-(O-acetyl salicyl)-glucoheptose base amine; N-(O-acetyl salicyl)-mannoheptose base amine; N-(O-acetyl salicyl)-Gu Luo heptose base amine; N-(O-acetyl salicyl)-Ai Du glycosyl in heptan amine; N-(O-acetyl salicyl)-galactoheptose base amine, and at least a in N-(O-acetyl salicyl)-Ta Luo glycosyl in heptan amine.
5. the composition of claim 1, wherein O-acetyl salicyl aminosugar has general formula:
R 1(CHOR 2) n(CHNH 2)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be H or at least one R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, have alkyl, aralkyl or the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace; OH can be by H, NH 2, NHCOCH 3, acetoxyl group or other acyloxy with 2 to 9 carbon atoms replace.
6. the composition of claim 5; wherein O-acetyl salicyl aminosugar is selected from O-(O-acetyl salicyl)-aminosugar-O-(O-acetyl salicyl)-glycerine osamine; O-(O-acetyl salicyl)-erythrose amine; O-(O-acetyl salicyl)-threose amine; O-(O-acetyl salicyl)-ribose amine; O-(O-acetyl salicyl)-Arabic osamine; O-(O-acetyl salicyl)-wood sugar amine; O-(O-acetyl salicyl)-lysol osamine; O-(O-acetyl salicyl)-allose amine; O-(O-acetyl salicyl)-altrose amine; O-(O-acetyl salicyl)-aminoglucose; O-(O-acetyl salicyl)-mannosamine; O-(O-acetyl salicyl)-gulosamine; O-(O-acetyl salicyl)-idose amine; O-(O-acetyl salicyl)-galactosamine; O-(O-acetyl salicyl)-talosamine; O-(O-acetyl salicyl)-A Luo heptose amine; O-(O-acetyl salicyl)-A Zhuo osamine in heptan; O-(O-acetyl salicyl)-glucoheptose amine; O-(O-acetyl salicyl)-mannoheptose amine; O-(O-acetyl salicyl)-Gu Luo heptose amine; O-(O-acetyl salicyl)-Ai Du osamine in heptan; O-(O-acetyl salicyl)-galactoheptose amine; O-(O-acetyl salicyl)-Ta Luo osamine in heptan; O-(O-acetyl salicyl)-glycerine amino acid, (c)-(O-acetyl salicyl)-erythrose amino acid; O-(O-acetyl salicyl)-threose amino acid; O-(O-acetyl salicyl)-ribose amino acid; O-(O-acetyl salicyl)-arabinose amino acid; O-(O-acetyl salicyl)-wood sugar amino acid; O-(O-acetyl salicyl)-lyxose amino acid; O-(O-acetyl salicyl)-allose amino acid; O-(O-acetyl salicyl)-altrose amino acid; O-(O-acetyl salicyl)-Glucoamino acid; O-(O-acetyl salicyl)-mannose amino acid; O-(O-acetyl salicyl)-gulose amino acid; O-(O-acetyl salicyl)-idose amino acid; O-(O-acetyl salicyl)-galactose amino acid; O-(O-acetyl salicyl)-talose amino acid; O-(O-acetyl salicyl)-A Luo heptose amino acid; O-(O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan; O-(O-acetyl salicyl)-glucoheptose amino acid; O-(O-acetyl salicyl)-mannoheptose amino acid; O-(O-acetyl salicyl)-Gu Luo heptose amino acid; O-(O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan; O-(O-acetyl salicyl)-galactoheptose amino acid; O-(O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan; O-(O-acetyl salicyl) lactose amine; O-(O-acetyl salicyl) muramic acid; O-(O-acetyl salicyl) nerve amines; O-(O-acetyl salicyl) nerve amines lactose; O-(O-acetyl salicyl)-neuraminic acid; O-(O-acetyl salicyl)-4-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-7-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-two-O-acetyl neuraminic acid; O-(O-acetyl salicyl)-glycerine glycosyl amine; O-(O-acetyl salicyl)-erythrose base amine; O-(O-acetyl salicyl)-threose base amine; O-(O-acetyl salicyl)-ribosyl amine; O-(O-acetyl salicyl)-Arabic glycosyl amine; O-(O-acetyl salicyl)-xylosyl amine; O-(O-acetyl salicyl)-lysol glycosyl amine; O-(O-acetyl salicyl)-allose base amine; O-(O-acetyl salicyl)-altrose base amine; O-(O-acetyl salicyl)-glucosyl group amine [also making O-(O-acetyl salicyl)-gucosamine]; O-(O-acetyl salicyl)-mannose group amine; O-(O-acetyl salicyl)-gulose base amine; O-(O-acetyl salicyl)-idose base amine; O-(O-acetyl salicyl)-galactosyl amine; O-(O-acetyl salicyl)-talose base amine; O-(O-acetyl salicyl)-A Luo heptose base amine; O-(O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; O-(O-acetyl salicyl)-glucoheptose base amine; O-(O-acetyl salicyl)-mannoheptose base amine; O-(O-acetyl salicyl)-Gu Luo heptose base amine; O-(O-acetyl salicyl)-Ai Du glycosyl in heptan amine; O-(O-acetyl salicyl)-galactoheptose base amine; at least a in O-(O-acetyl salicyl)-Ta Luo glycosyl in heptan amine.
7. the composition of claim 1, wherein O-acetyl salicyl aminosugar has general formula:
R 1(CHOR 2) n(CHNHCOC 6H 4OCOCH 3)R 3
Wherein n is an integer, preferred 1-9; R 1Be selected from H, I, F, Cl, Br, CHO, CONH 2, COOR 4, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 19 carbon atom; R 2Be H or at least one R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be selected from H, CHO, CH 2OH, CONH 2And COOR 4And R 4Be independently selected from H, have alkyl, aralkyl or the aryl of 1 to 9 carbon atom; The H that is connected with any carbon atom can be by I, F, Cl, Br, SH, CHO, CONH 2, NH 2, alkyl, alkoxyl, aralkyl or aryl with 1 to 9 carbon atom replace.
8. the composition of claim 7, wherein O-acetyl salicyl aminosugar is selected from N, O-two (O-acetyl salicyl)-aminosugar-N, O-two (O-acetyl salicyl)-glycerine osamine; N, O-two (O-acetyl salicyl)-erythrose amine; N, O-two (O-acetyl salicyl)-threose amine; N, O-two (O-acetyl salicyl)-ribose amine; N, O-two (O-acetyl salicyl)-Arabic osamine; N, O-two (O-acetyl salicyl)-wood sugar amine; N, O-two (O-acetyl salicyl)-lysol osamine; N, O-two (O-acetyl salicyl)-allose amine; N, O-two (O-acetyl salicyl)-altrose amine; N, O-two (O-acetyl salicyl)-aminoglucose; N, O-two (O-acetyl salicyl)-mannosamine; N, O-two (O-acetyl salicyl)-gulosamine; N, O-two (O-acetyl salicyl)-idose amine; N, O-two (O-acetyl salicyl)-galactosamine; N, O-two (O-acetyl salicyl)-talosamine; N, O-two (O-acetyl salicyl)-A Luo heptose amine; N, O-two (O-acetyl salicyl)-A Zhuo osamine in heptan; N, O-two (O-acetyl salicyl)-glucoheptose amine; N, O-two (O-acetyl salicyl)-mannoheptose amine; N, O-two (O-acetyl salicyl)-Gu Luo heptose amine; N, O-two (O-acetyl salicyl)-Ai Du osamine in heptan; N, O-two (O-acetyl salicyl)-galactoheptose amine; N, O-two (O-acetyl salicyl)-Ta Luo osamine in heptan; N, O-two (O-acetyl salicyl)-glycerine amino acid; N, O-two (O-acetyl salicyl)-erythrose amino acid; N, O-two (O-acetyl salicyl)-threose amino acid; N, O-two (O-acetyl salicyl)-ribose amino acid; N, O-two (O-acetyl salicyl)-arabinose amino acid; N, O-two (O-acetyl salicyl)-wood sugar amino acid; N, O-two (O-acetyl salicyl)-lyxose amino acid; N, O-two (O-acetyl salicyl)-allose amino acid; N, O-two (O-acetyl salicyl)-altrose amino acid; N, O-two (O-acetyl salicyl)-Glucoamino acid; N, O-two (O-acetyl salicyl)-mannose amino acid; N, O-two (O-acetyl salicyl)-gulose amino acid; N, O-two (O-acetyl salicyl)-idose amino acid; N, O-two (O-acetyl salicyl)-galactose amino acid; N, O-two (O-acetyl salicyl)-talose amino acid; N, O-two (O-acetyl salicyl)-A Luo heptose amino acid; N, O-two (O-acetyl salicyl)-A Zhuo glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl)-glucoheptose amino acid; N, O-two (O-acetyl salicyl)-mannoheptose amino acid; N, O-two (O-acetyl salicyl)-Gu Luo heptose amino acid; N, O-two (O-acetyl salicyl)-Ai Du glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl)-galactoheptose amino acid; N, O-two (O-acetyl salicyl)-Ta Luo glycoprotein amino acid in heptan; N, O-two (O-acetyl salicyl) lactose amine; N, O-two (O-acetyl salicyl) muramic acid; N, O-two (O-acetyl salicyl) nerve amines; N, O-two (O-acetyl salicyl) nerve amines lactose; N, O-two (O-acetyl salicyl)-neuraminic acid; N, O-two (O-acetyl salicyl)-4-O-acetyl neuraminic acid; N, O-two (O-acetyl salicyl)-7-O-acetyl neuraminic acid; N, O-two (O-acetyl salicyl)-two-O-acetyl neuraminic acid, N, O-two (O-acetyl salicyl)-glycerine glycosyl amine; N, O-two (O-acetyl salicyl)-erythrose base amine; N, O-two (O-acetyl salicyl)-threose base amine; N, O-two (O-acetyl salicyl)-ribosyl amine; N, O-two (O-acetyl salicyl)-Arabic glycosyl amine; N, O-two (O-acetyl salicyl)-xylosyl amine; N, O-two (O-acetyl salicyl)-lysol glycosyl amine; N, O-two (O-acetyl salicyl)-allose base amine; N, O-two (O-acetyl salicyl)-altrose base amine; N, O-two (O-acetyl salicyl)-glucosyl group amine [also making N, O-two (O-acetyl salicyl)-gucosamine]; N, O-two (O-acetyl salicyl)-mannose group amine; N, O-two (O-acetyl salicyl)-gulose base amine; N, O-two (O-acetyl salicyl)-idose base amine; N, O-(O-acetyl salicyl)-galactosyl amine; N, O-two (O-acetyl salicyl)-talose base amine; N, O-two (O-acetyl salicyl)-A Luo heptose base amine; N, O-two (O-acetyl salicyl)-A Zhuo glycosyl in heptan amine; N, O-two (O-acetyl salicyl)-glucoheptose base amine; N, O-two (O-acetyl salicyl)-mannoheptose base amine; N, O-two (O-acetyl salicyl)-Gu Luo heptose base amine; N, O-two (O-acetyl salicyl)-Ai Du glycosyl in heptan amine; N, O-two (O-acetyl salicyl)-galactoheptose base amine; And N, at least a in O-two (O-acetyl salicyl)-Ta Luo glycosyl in heptan amine.
9. the composition of claim 1, wherein O-acetyl salicyl amino acid has general formula:
R 1CHNHR 2(CH 2) nCOR 3
R wherein 1Be H, have alkyl, alkoxyl, aralkyl or an aryl of 1 to 14 carbon atom, R 1Also can have OH, SH, SCH 3, NH 2, NHR 2, CONH 2, NHCONH 2, NHC (=NH) NH 2, NHC (=NR 2) NH 2, imidazoles, pyrrolidines or other heterocyclic radicals; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; N is 0 to 5 integer; R 3Be NH 2, OR 4R 4Be H, have alkyl, aralkyl or an aryl of 1 to 14 carbon atom; The H that is connected with any carbon atom can be replaced by I, F, Cl, Br, OH or the alkoxyl with 1 to 9 carbon atom.
10. the composition of claim 9, wherein O-acetyl salicyl amino acid is selected from N-(O-acetyl salicyl) amino acid: N-(O-acetyl salicyl)-alanine, N-(O-acetyl salicyl)-arginine; N, N '-two (O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-asparagine, N-(O-acetyl salicyl)-L-aminobutanedioic acid, N-(O-acetyl salicyl)-cysteine, N-(O-acetyl salicyl)-glycine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-histidine; N, N '-two (O-acetyl salicyl)-histidine, N-(O-acetyl salicyl)-isoleucine, N-(O-acetyl salicyl)-leucine, N-(O-acetyl salicyl)-lysine; N, N '-two (O-acetyl salicyl)-lysine, N-(O-acetyl salicyl)-methionine, N-(O-acetyl salicyl)-phenyl alanine, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-serine, N-(O-acetyl salicyl)-threonine, N-(O-acetyl salicyl)-tryptophan; N, N '-two (O-acetyl salicyl)-tryptophan, N-(O-acetyl salicyl)-tyrosine, N-(O-acetyl salicyl)-valine, N-(O-acetyl salicyl)-Beta-alanine, N-(O-acetyl salicyl)-γ-An Jidingsuan, N-(O-acetyl salicyl)-B-AIB, N-(O-acetyl salicyl)-citrulling, N-(O-acetyl salicyl)-DOPA (3, the 4-DA), N-(O-acetyl salicyl)-homocysteine, N-(O-acetyl salicyl)-homoserine, N-(O-acetyl salicyl)-ornithine; At least a in N, N '-two (O-acetyl salicyl)-ornithine, N-(O-acetyl salicyl)-phenylglycine and N-(O-acetyl the salicyl)-4-glycin.
11. the composition of claim 1, wherein O-acetyl salicyl peptide has general formula:
R 1CHNHR 2CO?NHCHR 1COR 3
R wherein 1Be H independently, have alkyl, aralkyl or the aryl of 1 to 14 carbon atom, can have OH, SH, SCH 3, NH 2, CONH 2, NHCONH 2, NHC (=NH) NH 2, imidazoles, pyrrolidines or other heterocyclic radicals; R 2Be O-acetyl salicyl, use CH 3COOC 6H 4CO represents; R 3Be NH 2, OR 4R 4Be H, have alkyl, aralkyl or an aryl of 1 to 14 carbon atom; The H that is connected with any carbon atom can be replaced by I, F, Cl, Br, OH or the alkoxyl with 1 to 9 carbon atom.
12. the composition of claim 11, wherein O-acetyl salicyl peptide is to be selected from N-(O-acetyl salicyl)-kyotorphin (Tyr-Arg), N-(O-acetyl salicyl)-anserine (β-Ala-1-N-Me-His), N-(O-acetyl salicyl)-β-Ala-Lys, N-(O-acetyl salicyl)-Asp-Glu, N-(O-acetyl salicyl)-carnosine (β-Ala-His), N-(O-acetyl salicyl)-Gly-Gln, N-(O-acetyl salicyl)-γ-D-Glu-Gly, N-(O-acetyl salicyl)-γ-Glu-Val, N-(O-acetyl salicyl)-γ-Glu-Ile, N-(O-acetyl salicyl)-γ-Glu-Leu, N-(O-acetyl salicyl)-γ-Glu-Met, N-(O-acetyl salicyl)-γ-Glu-Phe, N-(O-acetyl salicyl)-γ-Glu-Ala, N-(O-acetyl salicyl)-γ-Glu-Tyr, N-(O-acetyl salicyl)-γ-Glu-Phe, N-(O-acetyl salicyl)-Leu-Leu, N-(O-acetyl salicyl)-ophidine (β-Ala-2-Me-His), N-(O-acetyl salicyl)-Met-Phe, N-(O-acetyl salicyl)-Ser-Tyr-NH 2, N-(O-acetyl salicyl)-Tyr-Pro-NH 2In at least a dipeptides.
13. the composition of claim 11, wherein O-acetyl salicyl peptide is a tripeptides, is selected from N-(O-acetyl salicyl)-bursin (Lys-His-Gly-NH 2), N-(O-acetyl salicyl)-D-Phe-Phe-Gly; N-(O-acetyl salicyl)-diprotin A (Ile-Pro-Ile), N-(O-acetyl salicyl)-glutathione (Y-Glu-Cys-Gly), N-(O-acetyl salicyl)-pGlu-Glu-Pro-NH 2, N-(O-acetyl salicyl)-Lys-Trp-Lys, N-(O-acetyl salicyl)-Lys-Tyr-Lys, N-(O-acetyl salicyl)-ophthalmic acid, N-(O-acetyl salicyl)-norophthalmic acid (γ-Glu-Ala-Gly), N-(O-acetyl salicyl)-homoglutathion (two-γ-Glu-Cys-two-β-Ala), N-(O-acetyl salicyl)-Met-Leu-Phe, N-(O-acetyl salicyl)-Tyr-Gly-Gly, N-(O-acetyl salicyl)-Pro-Leu-Gly-NH 2In at least a.
14. the composition of claim 11, wherein O-acetyl salicyl peptide is an oligopeptide, is selected from N-(O-acetyl salicyl)-Lys-Lys-Gly-Glu, N-(O-acetyl salicyl)-Arg-Pro-Lys-Pro, N-(O-acetyl salicyl)-Gly-Gly-Phe-Leu, N-(O-acetyl salicyl)-Arg-Gly-Asp-Ser, N-(O-acetyl salicyl)-Arg-Gly-Glu-Ser, N-(O-acetyl salicyl)-Met-Leu-Phe-Phe, N-(O-acetyl salicyl)-Val-Ala-Pro-Gly, N-(O-acetyl salicyl)-Val-Gly-Ser-GIu, N-(O-acetyl salicyl)-Ala-Pro-Gly-Trp-NH 2, N-(O-acetyl salicyl)-Gly-Gly-Phe-Met-NH 2, N-(O-acetyl salicyl)-endorphin 1 (Tyr-Pro-Trp-Phe-NH 2), N-(O-acetyl salicyl)-endorphin 2 (Tyr-Pro-Phe-Phe-NH 2), N-(O-acetyl salicyl)-morphiceptin (Tyr-Pro-Phe-Pro-NH 2), N-(O-acetyl salicyl)-outer deltorphin delta C (Tyr-Pro-Ile-Ser-Leu), N-(O-acetyl salicyl)-pyroGlu-Glu-Asp-Ser-Gly, N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Leu, N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Met, N-(O-acetyl salicyl)-pyroGlu-Leu-Tyr-Glu-Asn-Lys, N-(O-acetyl salicyl)-Arg-Arg-Pro-Tyr-Ile-Leu, N-(O-acetyl salicyl)-Val-Gly-Val-Ala-Pro-Gly, N-(O-acetyl salicyl)-Tyr-Pro-Ile-Ser-Leu, N-(O-acetyl salicyl)-Arg-Lys-Arg-Ala-Arg-Lys-Glu, N-(O-acetyl salicyl)-kemptide (Leu-Arg-Arg-Ala-Ser-Leu-Gly), N-(O-acetyl salicyl)-Tyr-Gly-Gly-Phe-Leu-Arg-Arg, N-(O-acetyl salicyl)-Met-Glu-His-Phe-Arg-Trp-Gly, N-(O-acetyl salicyl)-Arg-Val-Tyr-Ile-His-Pro-Phe, N-(O-acetyl salicyl)-β-junket deltorphin delta (Tyr-Pro-Phe-Val-Glu-Pro-Ile), N-(O-acetyl salicyl)-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, N-(O-acetyl salicyl)-Met-Gln-Met-Lys-Lys-Val-Leu-Asp-Ser, N-(O-acetyl salicyl)-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg, N-(O-acetyl salicyl)-Ile-Ala-Arg-Arg-His-Pro-Tyr-Phe-Leu, N-(O-acetyl salicyl)-Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH 2, N-(O-acetyl salicyl)-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH 2, N-(O-acetyl salicyl)-Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Arg-Gly-NH 2In at least a.
15. the composition of claim 1, wherein O-acetyl acetylsalicyl derivatives is selected from O-(O-acetyl salicyl)-amino acid; N, O-two (O-acetyl salicyl)-amino acid; N, O, O-three (O-acetyl salicyl)-amino acid; S-(O-acetyl salicyl)-amino acid; N, S-two (O-acetyl salicyl)-amino acid; O, S-two (O-acetyl salicyl)-amino acid is preferably from the amino acid with hydroxyl or sulfydryl.Other (O-acetyl salicyl)-derivatives comprise: N-(O-acetyl salicyl)-amino-oligosaccharide; N-(O-acetyl salicyl)-oligomeric-aminosugar; N, O-two (O-acetyl salicyl)-amino-oligosaccharide; And N, in O-two (O-acetyl salicyl)-oligomeric-aminosugar at least-kind.
16. the composition of claim 1, wherein O-acetyl acetylsalicyl derivatives is selected from S-(O-acetyl salicyl)-cysteine; N, S-two (O-acetyl salicyl)-cysteine; S-(O-acetyl salicyl)-homocysteine; N, S-two (O-acetyl salicyl)-homocysteine; O-(O-acetyl salicyl)-4-glycin; N, O-two (O-acetyl salicyl)-4-glycin; O-(O-acetyl salicyl)-serine; N, O-two (O-acetyl salicyl)-serine; O-(O-acetyl salicyl)-homoserine; N, O-two (O-acetyl salicyl)-homoserine; O-(O-acetyl salicyl)-3-Phenserine; N, O-two (O-acetyl salicyl)-3-Phenserine; O-(O-acetyl salicyl)-threonine; N, O-two (O-acetyl salicyl)-threonine, O-(O-acetyl salicyl)-tyrosine; N, O-two (O-acetyl salicyl)-tyrosine, O-(O-acetyl salicyl)-DOPA; O, O-two (O-acetyl salicyl)-DOPA; N, O-two (O-acetyl salicyl)-DOPA and N, O, at least a in O-three (O-acetyl salicyl)-DOPA.
17. the composition of claim 1, wherein O-acetyl acetylsalicyl derivatives is N-(O-acetyl salicyl)-L-TEE.
18. one kind is prevented or treatment illness or syndromic method, comprises the composition of system or local application claim 1, wherein this illness or syndrome are arbitrary relevant with nerve, blood vessel, muscle skeleton or integumentary system.
19. the method for claim 18, wherein O-acetyl acetylsalicyl derivatives is selected from N-(O-acetyl salicyl)-aminoglucose, N-(O-acetyl salicyl)-mannosamine, N-(O-acetyl salicyl)-galactosamine, N-(O-acetyl salicyl)-gucosamine N-(O-acetyl salicyl)-glycine ethyl ester, N-(O-acetyl salicyl)-TEE, N-(O-acetyl salicyl)-proline, N-(O-acetyl salicyl)-prolineamide, N-(O-acetyl salicyl)-ethyl prolinate, N-(O-acetyl salicyl)-glutamine, N-(O-acetyl salicyl)-glutamic acid, N-(O-acetyl salicyl)-glutamate diethyl ester, N-(O-acetyl salicyl)-arginine, N-(O-acetyl salicyl)-4-glycin ethyl ester; N, O-two (O-acetyl salicyl)-4-glycin ethyl ester, N-(O-acetyl salicyl)-3-Phenserine; N-(O-acetyl salicyl)-3-Phenserine ethyl ester; At least a in N-(O-acetyl salicyl)-lysine and N-(O-acetyl the salicyl)-ornithine.
20. the method for claim 18, wherein oral N-(O-acetyl salicyl)-TEE is used to prevent or treat the illness of musculoskeletal system, is selected from osteoporosis, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, bursal synovitis and tendonitis.
21. the composition of claim 1 also comprises other reagent, is selected from hydroxy acid, ketone acid; Phenyl α acyloxy alkanoic acid and derivative thereof; N-acetyl group-aldose amine, acid of N-acetyl-amino and relevant N-acetyl compounds; Topical pain relief agent and anaesthetic; Anti-acne agents; Antibacterial agent; Anti-yeast agent, antifungal agent; Antivirotic; Dandruff removing agent; Anti-dermatitis agent; Antihistaminic; Antipruritic; Antemetic; Anti-motion sickness agent; Antiinflammatory; Anti-hyperkeratosis agent; Antiperspirant; Antipsoriatic; Antiseborrheic; Hair conditioner and hair therapy agent; Anti-aging and anti-wrinkle agent; Sun-proof and opacifier; Skin brightening agent; Depigmenting agent; Astringent; Cleaning agent; Corn, poroma and wart remover; The local cardiovascular agents of using; Vitamin; Cortin; Tanning agent; Hormone; Retinoid; At least a in gingival disease or the oral cavity nursing agent.
22 The composition of claim 21; wherein said additional agent is selected from abacavir; acebutolol; paracetamol; acetaminophen Shalom; acetazolamide; acetic acid, hydroxylamine; N-acetyl - cysteine ; N-acetyl - glucosamine; N-acetyl - glutamine; N-acetyl - lysine; N-acetyl - ornithine; N-acetyl - prolinamide; N-acetyl - proline; acetyl salicylic acid; Acitretin; alclometasone; acrivastine; actiq; acyclovir; adapalene; adefovir two volts esters; cytarabine; salbutamol; alfuzosin; allopurinol; Austrian celecoxib allopurinol; almotriptan; alprazolam; Alprenolol; aluminum acetate; aluminum chloride; hydrated aluminum chloride; hydroxide; amantadine; amiloride; amino acridine; amino benzoic acid (PABA); aminocaproic acid; amino acid; amiodarone; amitriptyline; amlodipine; A Moka triazine; phenol quinoline; amorolfine; amoxapine; amphetamine; ampicillin; anagrelide; anastrozole; Anthralin; apomorphine; aprepitant; arbutin; aripiprazole; ascorbic acid; ascorbyl palmitate; atazanavir; atenolol; Alto Paxil; atropine; azathioprine; azelaic acid; azelastine; azithromycin; bacitracin; beclomethasone dipropionate; shellfish MAG; benazepril; bendroflumethiazide; benzocaine; benzene Zona ester; benzophenone; benzoyl peroxide; benztropine; bepridil; betamethasone dipropionate; betamethasone valerate; brimonidine; brompheniramine; cloth ratio Cain; buprenorphine; bupropion; cloth immediately amine; butenafine; Butoconazole; cabergoline; caffeic acid; caffeine; calcipotriene; camphor; candesartan; capsaicin Su; carbamazepine; carbamide peroxide; cefditoren; cefepime; cefpodoxime; celecoxib; cetirizine; Cevimeline; chitosan; chlordiazepoxide; chlorhexidine; Chloroquine; hydrochlorothiazide; chloroxylenol; chlorpheniramine; chlorpromazine; chlorpropamide; ciclopirox; cilostazol; cimetidine; cinacalcet; ciprofloxacin; citalopram; citric acid; cladribine; clarithromycin; clemastine; clindamycin; clioquinol; clobetasol; clomiphene; clonidine; clopidogrel; clotrimazole; clozapine; tar ; cocaine; codeine; cromolyn sodium; Crotamiton; Prosecco force triazine; cyclobenzaprine; cycloserine; cytarabine; dacarbazine; dalfopristin; nitrogen phenyl sulfone; Dato mildew Su; daunorubicin; area deferoxamine; DHEA; delavirdine; desipramine; ground loratadine; desmopressin; go hydroxyl betamethasone; dexamethasone; dextromethorphan care microphone fixed; Right methylphenidate; dexrazoxane; dextroamphetamine; diazepam; dicyclomine; didanosine; hydrocodone; hydromorphone; diltiazem; 6; 8 - dimercapto octanoic acid (dihydro- lipoic acid); diphenhydramine; diphenoxylate; dipyridamole; disopyramide; dobutamine; dofetilide; dolasetron; multi-naphthalene donepezil; dopa ester; dopa amide; dopamine; dorzolamide; doxepin; doxorubicin; doxycycline; doxylamine; doxypin; duloxetine; Dyclonine; econazole; eflornithine; By Li triptans; emtricitabine; enalapril; ephedrine; adrenaline; ephedra Ning; epirubicin; eptifibatide; ergotamine; erythromycin; according milnacipran; esmolol; esomeprazole; estazolam; estradiol; ethacrynic acid; ethinyl estradiol; according Articaine; etomidate; famciclovir; famotidine; felodipine; fentanyl; ferulic acid ; fexofenadine; flecainide; fluconazole; flucytosine; fluocinolone; fluocinonide; 5 - fluorouracil; fluoxetine; fluphenazine; flurazepam; fluvoxamine; formoterol Castro; furosemide; galactarolactone; galactono; galacturonic acid lactone; galantamine; gatifloxacin; gefitinib; gemcitabine; gemifloxacin; acetylglucosamine lactone; gluconic acid; Portugal sugar acid lactone; glucuronic acid; glucuronolactone; glycolic acid; griseofulvin; Guaifenesin; guanethidine; N-guanine base histamine; haloperidol; halogen general nearly ; have resorcin; homatropine; homosalate; hydralazine; hydrochlorothiazide; hydrocortisone; hydrocortisone 21 - acetate; hydrocortisone 17 - butyrate; hydrocortisone 17 - valerate; hydrogen peroxide; hydromorphone; hydroquinone; hydroquinone monomethyl ether; hydroxyzine; hyoscyamine; hypoxanthine; ibuprofen; ichthyol; idarubicin; imatinib; C m triazine; dense imiquimod; indinavir; indomethacin; irbesartan; irinotecan; ethyl isoproterenol; isoproterenol; itraconazole; kanamycin; ketamine; ketanserin; ketoconazole; ketoprofen; ketotifen; kojic acid; labetalol; lactic acid; lactose acid; lamivudine; lamotrigine; lansoprazole; letrozole; acetate bright leuprolide; levosalbutamol; levofloxacin; lidocaine; linezolid; lobeline; loperamide; losartan; loxapine; lysergic acid ethyl amine; Mafenide; malic acid; maltose acid ; mandelic acid; maprotiline; mebendazole; America Kala Ming; America Crowe triazine; A chlorine doxycycline; memantine; menthol; pethidine; mepivacaine; mercaptopurine; mescaline; 3 - norepinephrine; between the hydroxyl isoproterenol; metaraminol; metformin; methadone; methamphetamine; methotrexate; Methoxamine; methyldopa ester; methyldopa amide; 3,4 - methylenedioxy-methamphetamine; methyl lactate; nicotinate; methylphenidate; methyl salicylate; methylthio Mitt; metolazone; metoprolol; metronidazole; America mexiletine; miconazole; midazolam; midodrine; America Groote; minocycline; minoxidil; mirtazapine; mitoxantrone; Tamoxifen enalaprilat; do indanone; monobenzone; morphine; moxifloxacin; moxonidine; mupirocin; nadolol; Naftifine; nalbuphine; nalmefene; naloxone; naproxen; nefazodone; nelfinavir; neomycin; nevirapine; nicardipine; nicotine; nifedipine; nimodipine; nisoldipine; Nizar horizon; norepinephrine; nystatin; Ao Keba amine; octreotide; A Oxygen octyl; octyl salicylate; ofloxacin; olanzapine; olmesartan; olopatadine; omeprazole; ondansetron; Oxiconazole; oxotremorine; hydroxy benzoic ketone; oxybutynin; oxycodone; oxymetazoline; octyl dimethyl dapsone; palonosetron; pantothenic acid; panthenol lactone; paroxetine; pemoline; penciclovir; Penicillium amine; penicillin; pentazocine; pentobarbital; spray statins; pentoxifylline; pergolide special forces; perindopril; permethrin; phencyclidine; phenelzine; non Nila Min ; Fen America song triazine; phenobarbital; phenol; phenoxybenzamine; phentolamine; phenylephrine; phenylpropanolamine; phenytoin; physostigmine; pilocarpine; pimozide; pindolol; pyrrole rosiglitazone; horses Mary piperazine hydrochloride; piperonyl butoxide; piperazine Valenciennes level; podofilox; podophyllin; povidone-iodine; pramipexole; pramoxine; prazosin; prednisone; Puri Castro; prilocaine; procainamide; procaine; procarbazine; oxaprozin; promethazine; propionic promethazine; propafenone; propoxyphene; propranolol; C thiouracil; protriptyline; pseudoephedrine; pyrethrin; pyrilamine; pyrimethamine; quetiapine; quinapril; Kui Yi Zong; quinidine; quinupristin; rabeprazole; reserpine Ping; resorcinol; retinoid; 13 - cis-retinoic acid; retinoic acid; retinol; retinol acetate; retinyl palmitate; ribavirin; ribose acid; ribose acid lactone; rifampin; rifapentine; Lifestyle Ximing; riluzole; rimantadine; risedronic acid; risperidone; ritodrine; rivastigmine; rizatriptan; Luo Requip; ropivacaine; salicylamide; salicylic acid; salmeterol; scopolamine; selegiline; selenium sulfide; 5 - serotonin; sertindole; sertraline; shell rock asphalt; Sibu Sibutramine; sildenafil; sotalol; streptomycin; strychnine; sulfur itraconazole; sulfonamides benzene; sulfa benzoyl; sulfa bromide dimethyl pyrimidine; sulfacetamide; Sulfachloropyridazine hydralazine; sulfa B cytosine; sulfonamides pyrimidine; sulfonamides to Suoxin; sulfadoxine; sulfaguanole; sulfa forest; sulfamethoxazole; sulfamethoxazole; sulfonamides; sulfonamides pyrazine; sulfasalazine; sulfasalazine; sulfa isothiazolin; Sulfathiazole; sulfa exclusive oxazole; sulfur; tadalafil; tamsulosin; tartaric acid; tazarotene; tegaserol; telithromycin; telmisartan; late for acetazolamide; tenofovir; terazosin; terbinafine Fen; terbutaline; Terconazole; terfenadine; tetracaine; tetracycline; tetrahydro benzoic cefazolin; theobromine; theophylline; thiabendazole; lipoic acid (lipoic acid); thioridazine triazine; thiothixene; thymol; tiagabine; timolol; tinidazole; Sekondi azole; tirofiban; tizanidine; tobramycin; tocainide; tolazoline morpholine; tolbutamide; tolnaftate; tolterodine; tramadol; tranylcypromine; trazodone; triamcinolone acetonide; triamcinolone; own triamcinolone acetonide; triamterene; triazolam ; triclosan; trifluoropropionaldehyde triazine; trimethoprim; trimipramine; song topiramate Namin; triprolidine; tromethamine; tropic acid; tyramine; eleven carbonate; urea; Urocanic acid; ursodeoxycholic acid; vardenafil; venlafaxine; verapamil; acetate vitamin E; voriconazole; warfarin; wood tar; xanthine; zafirlukast; zaleplon; topiramate lipoic; ziprasidone; zolmitriptan; Junior zolpidem at least one....
CNA2005800486748A 2005-01-03 2006-01-03 Compositions comprising O-acetylsalicyl derivatives of aminocarbohydrates and amino acids Pending CN101128117A (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101544579B (en) * 2009-05-07 2013-05-22 兰州大学 Use and preparation method of 4-(-2-acetoxybenzoyl)aminobutyric acid and ester derivative thereof
CN102215812B (en) * 2008-11-19 2014-09-10 宝丽化成工业有限公司 Anti-wrinkle agents
CN106924272A (en) * 2015-12-31 2017-07-07 中国医学科学院药物研究所 Purposes of the salicylic acid glucosides methyl in prevention and/or systemic lupus erythematosus and its complication medicine is prepared
CN115869294A (en) * 2022-10-25 2023-03-31 广东药科大学 Application of tropine acid and derivatives thereof in preparation of medicine for treating psoriasis

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102215812B (en) * 2008-11-19 2014-09-10 宝丽化成工业有限公司 Anti-wrinkle agents
CN101544579B (en) * 2009-05-07 2013-05-22 兰州大学 Use and preparation method of 4-(-2-acetoxybenzoyl)aminobutyric acid and ester derivative thereof
CN106924272A (en) * 2015-12-31 2017-07-07 中国医学科学院药物研究所 Purposes of the salicylic acid glucosides methyl in prevention and/or systemic lupus erythematosus and its complication medicine is prepared
CN106924272B (en) * 2015-12-31 2021-04-13 中国医学科学院药物研究所 Application of methyl salicylate glucoside in preparation of medicines for preventing and/or treating systemic lupus erythematosus and complications thereof
CN115869294A (en) * 2022-10-25 2023-03-31 广东药科大学 Application of tropine acid and derivatives thereof in preparation of medicine for treating psoriasis
CN115869294B (en) * 2022-10-25 2023-10-20 广东药科大学 Application of tolypic acid and derivative thereof in preparation of psoriasis treatment drugs

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