# US 2015/0104485 A1 · Compounds for the treatment and/or care of the skin and/or mucous membranes and their use in cosmetic or pharmaceutical compositions

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- Number: US 2015/0104485 A1
- Document ID: US20150104485A1
- Status: Published application
- Kind: A1
- Application number: 14/391,472
- Filed: 2013-04-16
- Published: 2015-04-16
- Earliest claimed: 2012-04-16
- Assignees: Lubrizol Advanced Materials, Inc.
- Applicants: Lubrizol Advanced Materials, Inc.
- Inventors: Jose Maria Garcia Anton; Antonio Vicente Ferrer Montiel; Cristina Carreño Serraïma; Raquel Delgado González; Juan Cebrián Puche
- Web page: https://patentgrep.com/patent/US20150104485A1

## CPC

- C07K 7/06: having 5 to 11 amino acids
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 38/005: {Enzyme inhibitors (protease inhibitors A61K38/55)}
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 5/18: of the parathyroid hormones
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61P 17/14: for baldness or alopecia
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/22: Anxiolytics
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 31/18: for HIV
- A61P 33/00: Antiparasitic agents
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/02: Immunomodulators
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/02: for chemically bleaching or whitening the skin
- A61Q 19/08: Anti-ageing preparations
- C07K 1/02: in solution {(C07K1/003, C07K1/006 take precedence)}
- C07K 5/0804: {and aliphatic}
- C07K 5/1005: {and aliphatic}
- C07K 5/1008: {the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala}
- A61Q 1/04: for lips
- A61Q 1/06: Lipsticks
- A61Q 1/10: for eyes, e.g. eyeliner, mascara
- A61Q 1/14: Preparations for removing make-up
- A61Q 15/00: Anti-perspirants or body deodorants (deodorisation of air A61L9/00)
- A61Q 17/04: Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
- A61Q 19/001: {Preparations for care of the lips}
- A61Q 19/10: Washing or bathing preparations
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Compounds of general formula (I): Ri—Wn—Xm-AAi-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 (I) their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, preparation processes, cosmetic and/or pharmaceutical compositions which contain them and their use in medicine, particularly in the treatment and/or prevention of pain, inflammation, itching, pigmentation disorders and angiogenic skin disorders, and in processes of treatment and/or care of the skin and/or mucous membranes.

## Claims

### Claim 1

A compound of general formula (I),
R1—Wn—Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 (I)
its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, wherein:
AA1 is selected from the group consisting of -Ser- and a bond;
AA2 is selected from the group consisting of -Val- and -Ala -;
AA3 is selected from the group consisting of -Arg- and -Thr-;
AA4 is selected from the group consisting of -Val- and -Asn-;
AA5 is selected from the group consisting of -Ala- and -Thr-;
AA6 is selected from the group consisting of -Val- and a bond;
W, X, Y, Z are amino acids and are independently selected from amongst themselves;
n, m, p and q are independently selected from amongst themselves and have a value of 0 or 1;
n+m+p+q is smaller than or equal to 2;
with the condition that if AA1 is a bond, AA2 is -Ala-, AA4 is -Val- and AA6 is a bond, then AA5 is -Thr-;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Val- and AA6 is a bond, then AA5 is -Ala-;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Asn-, and AA6 is -Val-, then AA5 is -Ala-;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Arg-, AA4 is -Val-, and AA6 is -Val-, then AA5 is -Thr-;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Asn-, AA5 is -Ala- and AA6 is a bond, then n+m+p+q is equal to 0;
with the condition that if AA1 is a bond, AA2 is -Ala-, AA3 is -Thr-, AA4 is -Val-, AA6 is a bond and p+q is greater or equal to 1, then AA5 is -Ala-;
with the condition that if AA1 is a bond, AA2 is -Ala-, AA3 is -Thr-, AA4 is -Asn-, AA5 is -Thr- and AA6 is a bond, then n+m+p+q is smaller than or equal to 1;
with the condition that if AA1 is a bond, AA2 is -Ala-, AA3 is -Thr-, AA4 is -Asn-, AA6 is a bond, X is -Gly- and W is -Leu-, then AA5 is -Thr-;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Val-, AA5 is -Ala-, and AA6 is a bond, then p and q are 0;
with the condition that if AA1 is a bond, AA2 is -Ala-, AA3 is -Arg-, AA4 is -Val-, AA6 is a bond, Y is Ala, and Z is -Leu-, then AA5 is -Ala-;
R1 is selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and R5—CO—, wherein R5 is selected from the group consisting of H, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heterocyclyl, and substituted or unsubstituted heteroarylalkyl;
R2 is selected from the group consisting of —NR3R4, —OR3, and —SR3, wherein R3 and R4 are independently selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl; and
R1 or R2 are not α-amino acids

### Claim 2 (depends on 1)

The compound according to claim 1, wherein R1 is selected from the group consisting of H, a polymer derived from polyethylene glycol, and R5—CO—, wherein R5 is selected from the group consisting of substituted or unsubstituted C1-C24 alkyl radicals, substituted or unsubstituted C2-C24 alkenyls, substituted or unsubstituted C2-C24 alkynyls, substituted or unsubstituted C3-C24cycloalkyls, substituted or unsubstituted C5-C24 cycloalkenyls, substituted or unsubstituted C8-C24 cycloalkynyls, substituted or unsubstituted C6-C30 aryls, substituted or unsubstituted C7-C24 aralkyl, substituted or unsubstituted heterocyclyl rings of 3-10 members, and substituted or unsubstituted heteroarylalkyls of 2 to 24 carbon atoms and 1 to 3 atoms other than carbon and an alkyl chain of 1 to 6 carbon atoms, and R5—CO— is not an α-amino acid.

### Claim 3 (depends on 2)

The compound according to claim 2, wherein R1 is selected from the group consisting of H, acetyl, tert-butanoyl, hexanoyl, 2-methylhexanoyl, cyclohexanecarboxyl, octanoyl, decanoyl, lauroyl, myristoyl, palmitoyl, stearoyl, oleoyl, and linoleoyl.

### Claim 4 (depends on 1)

The compound according to claim 1, wherein R2 is selected from the group consisting of —NR3R4, —OR3, —SR3, wherein R3 and R4 are independently selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted C1-C24 alkyls, substituted or unsubstituted C2-C24 alkenyls, substituted or unsubstituted C2-C24 alkynyls, substituted or unsubstituted C3-C24 cycloalkyls, substituted or unsubstituted C5-C24 cycloalkenyls, substituted or unsubstituted C8-C24 cycloalkynyls, substituted or unsubstituted C6-C30aryls, substituted or unsubstituted C7-C24 aralkyls, substituted or unsubstituted heterocyclyl rings of 3-10 members, and substituted or unsubstituted heteroarylalkyl of 2 to 24 carbon atoms and 1 to 3 atoms other than carbon where the alkyl chain is of 1 to 6 carbon atoms and where —NR3R4 is not an α-amino acid.

### Claim 5 (depends on 4)

The compound according to claim 4, wherein R3 and R4 are independently selected from the group consisting of H, methyl, ethyl, hexyl, dodecyl and hexadecyl.

### Claim 6 (depends on 1)

The compound according to claim 1, wherein R1 is selected from the group consisting of H, acetyl, lauroyl, myristoyl or palmitoyl, AA1 is -L-Ser-, AA2 is -L-Val-, AA3 is -L-Arg-, AA4 is -L-Val-, AA5 is -L-Ala-, AA6 is -L-Val- and R2 is selected from the group consisting of —NR3R4 and —OR3 wherein R3 and R4 are independently selected from H, methyl, ethyl, hexyl, dodecyl and hexadecyl.

### Claim 7 (depends on 1)

The compound according to claim 1, wherein R1 is selected from the group consisting of H, acetyl, lauroyl, myristoyl and palmitoyl, AA1 is a bond, AA2 is -L-Ala-, AA3 is -L-Thr-, AA4 is -L-Asn-, AA5 is -L-Thr-, AA6 is a bond, and R2 is selected from the group consisting of —NR3R4 and —OR3, wherein R3 and R4 are independently selected from H, methyl, ethyl, hexyl, dodecyl and hexadecyl.

### Claim 8

(canceled)

### Claim 9

(canceled)

### Claim 10 (depends on 1)

A process of preparing a compound of general formula (I), its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, according to claim 1, wherein the process is carried out in solid phase or in solution.

### Claim 11

(canceled)

### Claim 12 (depends on 1)

A cosmetic or pharmaceutical composition which comprises a cosmetically or pharmaceutically effective amount of at least one compound of general formula (I), its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, according to claim 1, and at least one cosmetically or pharmaceutically acceptable excipient or adjuvant.

### Claim 13

(canceled)

### Claim 14

(canceled)

### Claim 15 (depends on 12)

The composition according to claim 12, wherein the compound of general formula (I), its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, is incorporated into a cosmetic or pharmaceutical delivery system or sustained release system selected from the group consisting of liposomes, mixed liposomes, oleosomes, niosomes, ethosomes, millicapsules, microcapsules, nanocapsules, nanostructured lipid carriers, sponges, cyclodextrins, vesicles, micelles, mixed micelles of surfactants, surfactant-phospholipid mixed micelles, millispheres, microspheres, nanospheres, lipospheres, microemulsions, nanoemulsions, miniparticles, milliparticles, microparticles, nanoparticles and solid lipid nanoparticles or is adsorbed on a cosmetically or pharmaceutically acceptable solid organic polymer or solid mineral support selected from the group consisting of talc, bentonite, silica, starch and maltodextrin.

### Claim 16

(canceled)

### Claim 17

(canceled)

### Claim 18 (depends on 12)

The composition according to claim 12, wherein the composition is present in a formulation selected from the group consisting of creams, multiple emulsions, anhydrous compositions, aqueous dispersions, oils, milks, balsams, foams, lotions, gels, cream gels, hydroalcoholic solutions, hydroglycolic solutions, hydrogels, liniments, sera, soaps, shampoos, conditioners, serums, ointments, mousses, pomades, powders, bars, pencils, sprays, aerosols, capsules, gelatin capsules, soft capsules, hard capsules, tablets, sugar coated tablets, granules, chewing gum, solutions, suspensions, emulsions, syrups, elixirs, polysaccharide films, jellies and gelatin or is incorporated into a product selected from the group consisting of under-eye concealers, make-up foundation, make-up removing lotions, make-up removing milks, eye shadows, lipsticks, lip gloss, lip protectors and powders.

### Claim 19

(canceled)

### Claim 20 (depends on 12)

The composition according to claim 12, wherein the compound of general formula (I), its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, is incorporated into a fabric, a non-woven fabric or a medical device.

### Claim 21

(canceled)

### Claim 22 (depends on 12)

The composition according to claim 12, comprising a cosmetically or pharmaceutically effective amount of at least one adjuvant selected from the group consisting of agents which inhibit the release of cytokines, agents inhibiting matrix metalloproteinases, whitening or depigmenting agents, melanin synthesis inhibiting agents, anti-inflammatory and/or analgesic agents, anti-itching agents, antiangiogenic agents, anti-reddening agents, agents that inhibit vascular permeability, venotonic agents, agents acting on capillary circulation and/or microcirculation, calming agents, sunscreens and organic or mineral photoprotective agents active against ultraviolet A and/or B rays and/or infrared A rays, agents that inhibit serine proteases, agents stimulating melanocyte proliferation, agents for the treatment and/or care of sensitive skin, agents modulating PPARγ, agents inhibiting neuronal exocytosis, agents inhibiting muscular contraction, antiaging agents, anti-wrinkle agents, antiperspirant agents, anesthetic agents, inhibitors of acetylcholine-receptor aggregation, anti-cholinergic agents, melanin synthesis stimulating agents, propigmenting agents, self-tanning agents, NO-synthase inhibiting agents, 5α-reductase inhibiting agents, lysyl- and/or prolyl hydroxylase inhibiting agents, antioxidants, free radical scavengers and/or agents against atmospheric pollution, reactive carbonyl species scavengers, anti-glycation agents, antihistamine agents, antiviral agents, antiparasitic agents, emulsifiers, emollients, organic solvents, liquid propellants, skin conditioners, humectants, substances which retain moisture, alpha hydroxy acids, beta hydroxy acids, moisturizers, hydrolytic epidermal enzymes, vitamins, amino acids, proteins, pigments or colorants, dyes, biopolymers, gelling polymers, thickeners, surfactants, softening agents, emulsifiers, binding agents, preservatives, agents able to reduce or treat the bags under the eyes, exfoliating agents, keratolytic agents, desquamating agents, antimicrobial agents, antifungal agents, fungistatic agents, bactericidal agents, bacteriostatic agents, agents stimulating the synthesis of dermal or epidermal macromolecules and/or capable of inhibiting or preventing their degradation, collagen synthesis-stimulating agents, elastin synthesis-stimulating agents, decorin synthesis-stimulating agents, laminin synthesis-stimulating agents, defensin synthesis-stimulating agents, chaperone synthesis-stimulating agents, cAMP synthesis-stimulating agents, AQP-3 modulating agents, aquaporin synthesis-modulating agents, proteins from the aquaporin family, hyaluronic acid synthesis-stimulating agents, glycosaminoglycan synthesis-stimulating agents, fibronectin synthesis-stimulating agents, sirtuin synthesis-stimulating agents, heat shock proteins, heat shock protein synthesis-stimulating agents, agents stimulating the synthesis of lipids and components of the stratum corneum, ceramides, fatty acids, agents that inhibit collagen degradation, agents that inhibit elastin degradation, agents stimulating fibroblast proliferation, agents stimulating keratinocyte proliferation, agents stimulating adipocyte proliferation, agents stimulating keratinocyte differentiation, agents stimulating or delaying adipocyte differentiation, agents inhibiting acetylcholinesterase, skin relaxant agents, antihyperkeratosis agents, comedolytic agents, anti-psoriatic agents, DNA repair agents, DNA protecting agents, stabilizers, firming agents, anti-stretch mark agents, binding agents, agents regulating sebum production, lipolytic agents or agents stimulating lipolysis, adipogenic agents, agents modulating PGC-1α synthesis, agents which increase or reduce the triglyceride content of adipocytes, anti-cellulite agents, agents which inhibit PAR-2 activity, agents stimulating healing, coadjuvant healing agents, agents stimulating reepithelialization, coadjuvant reepithelialization agents, cytokine growth factors, agents stimulating angiogenesis, agents acting on cell metabolism, agents to improve dermal-epidermal junction, agents inducing hair growth, hair growth inhibiting or retardant agents, agents delaying hair loss, preservatives, perfumes, cosmetic and/or absorbent and/or body odor masking deodorants, chelating agents, plant extracts, essential oils, marine extracts, agents obtained from a biotechnological process, mineral salts, cell extracts, or mixtures thereof.

### Claim at position 23

23-37. (canceled)

### Claim 38

A method of treatment of the skin and/or mucous membranes which comprises the administration to the skin and/or mucous membranes of a cosmetically or pharmaceutically effective quantity of at least one compound of general formula (I),
R1—Wn—Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 (I)
its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, wherein:
AA1 is selected from the group consisting of -Ser- and a bond;
AA2 is selected from the group consisting of -Val- and -Ala -;
AA3 is selected from the group consisting of -Arg- and -Thr-;
AA4 is selected from the group consisting of -Val- and -Asn-;
AA5 is selected from the group consisting of -Ala- and -Thr-;
AA6 is selected from the group consisting of -Val- and a bond;
W, X, Y, Z are amino acids and are independently selected from amongst themselves;
n, m, p and q are independently selected from amongst themselves and have a value of 0 or 1;
n+m+p+q is smaller than or equal to 2;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Val-, AA5 is -Ala-, and AA6 is a bond, then p and q are 0;
R1 is selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and R5—CO—, wherein R5 is selected from the group consisting of H, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted heteroarylalkyl;
R2 is selected from the group consisting of —NR3R4, —OR3 and —SR3, wherein R3 and R4 are independently selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl; and
R1 or R2 are not α-amino acids.

### Claim 39 (depends on 38)

The method according to claim 38, wherein the treatment of the skin and/or mucous membranes is the treatment of aging and/or photoaging, treatment of wrinkles and/or expression wrinkles and/or treatment of the spots due to aging and/or photoaging.

### Claim 40

A method of treatment of pain, inflammation, itching, angiogenic disorders and/or diseases of the skin and/or pigmentation disorders and/or diseases, inhibition of cytokine release, inhibition of matrix metalloproteinase activity or inhibition of melanogenesis, which comprises the administration to a mammal's body of a cosmetically or pharmaceutically effective quantity of at least one compound of general formula (I),
R1—Wn—Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 (I)
its stereoisomers, mixtures thereof and/or its cosmetically or pharmaceutically acceptable salts, wherein
AA1 is selected from the group consisting of -Ser- and a bond;
AA2 is selected from the group consisting of -Val- and -Ala -;
AA3 is selected from the group consisting of -Arg- and -Thr-;
AA4 is selected from the group consisting of -Val- and -Asn-;
AA5 is selected from the group consisting of -Ala- and -Thr-;
AA6 is selected from the group consisting of -Val- and a bond;
W, X, Y, Z are amino acids and are independently selected from amongst themselves;
n, m, p and q are independently selected from amongst themselves and have a value of 0 or 1;
n+m+p+q is smaller than or equal to 2;
with the condition that if AA1 is a bond, AA2 is -Val-, AA3 is -Thr-, AA4 is -Val-, AA5 is -Ala-, and AA6 is a bond, then p and q are 0;
R1 is selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and R5—CO—, wherein R5 is selected from the group consisting of H, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted heteroarylalkyl;
R2 is selected from the group consisting of —NR3R4, —OR3 and —SR3, wherein R3 and R4 are independently selected from the group consisting of H, a polymer derived from polyethylene glycol, substituted or unsubstituted non-cyclic aliphatic groups, substituted or unsubstituted alicyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted aralkyl; and
R1 or R2 are not α-amino acids.

### Claim 41 (depends on 40)

The method according to claim 40, wherein the inflammation is selected from the group consisting of neurogenic inflammation, joint inflammation, tendon inflammation, muscular inflammation, sepsis, vascular inflammation, respiratory inflammation, chronic obstructive pulmonary disease, rhinitis, allergic rhinitis, asthma, otitis, intestinal inflammation, Crohn's disease, pancreatitis, hepatitis, conditions related to chronic inflammation, acute inflammation, nephritis, systemic lupus erythematosus, arthritis, rheumatoid arthritis, adult and juvenile rheumatoid arthritis, Still's disease, psoriatic arthritis, osteoarthritis, arthritis caused by gout, rheumatoid spondylitis, glomerulonephritis, neuritis, nerve tissue inflammation, multiple sclerosis, immune system disorders, Sjögren's syndrome, atherosclerosis, myocarditis, pericarditis, vasculitis, inflammatory skin conditions, acne, rosacea, papules, pustules, telangiectasias, psoriasis, sensitive skin, redness, erythema, dermatitis, atopic dermatitis, contact dermatitis, diaper dermatitis, seborrheic dermatitis, eczema, hyperproliferative skin disease, burns, sunburn, inflammation of the vaginal mucus, vulvodynia, vaginitis, inflammation of the oral mucosa, gingivitis, periodontitis, inflammatory eye diseases, uveitis, ocular and vernal conjunctivitis, sarcoidosis, peptic ulcers, urticaria, bullous pemphigoid, scleroderma, fibrosis, angioedema, anaphylaxis, alopecia, cirrhosis of the liver, restenosis, polymyalgia rheumatica, seronegative spondyloarthropathy, ankylosing spondylitis, Reiter's syndrome, dermatomyositis, inclusion body myositis, polymyositis, and lymphangioleiomyomatosis.

### Claim 42 (depends on 40)

The method according to claim 40, wherein the cytokine is an interleukin.

### Claim 43 (depends on 40)

The method according to claim 40, wherein the matrix metalloproteinase is collagenase.

### Claim 44 (depends on 40)

The method according to claim 40, wherein the inhibition of melanogenesis is obtained by inhibition of tyrosinase.