1. A support worn on the face having a built-in drug carrier formed to surround the face around the eyes and comprising: a housing with a predetermined installation space defined therein and a plurality of vent holes formed in one side in the proximity of the globe of the eye when the support worn on the face is worn, the vent holes serving to communicate the installation space with the outside; a main body having a fixing member for fixing the housing to the face of a user; and a drug carrier installed inside the main body and containing medicinal ingredients useful for protecting the eyes from diseases and relieving eye fatigue; and a power supply supplying power to the drug carrier, wherein the drug carrier comprises a medicinal herb layer containing the medicinal ingredients to enable transdermal delivery of the medicinal ingredients and a substrate supporting the medicinal herb layer and equipped with a light-emitting lamp irradiating IR or UV light to the medicinal herb layer so as to activate the transdermal delivery of the medicinal ingredients contained in the medicinal herb layer.
2. (canceled)
3. The support worn on the face having a built-in drug carrier of claim 1, wherein the medicinal herb layer comprises a magnet generating a magnetic field or a low frequency generator so as to enhance the transdermal delivery of the medicinal ingredients.
4. The support worn on the face having a built-in drug carrier of claim 1, wherein the housing is equipped with an auxiliary LED light-emitting module irradiating light with wavelength of 430-670 nm toward the face of the user in order to reduce wrinkles around the eyes.
5. The support worn on the face having a built-in drug carrier of claim 1, wherein a light guide plate contacting with the skin around the eyes is formed inside the housing and a light-emitting diode is installed at one side of the light guide plate so as to irradiate light with wavelength of 430-670 nm through the light guide plate.
6. The support worn on the face having a built-in drug carrier of claim 1, wherein the medicinal herb layer comprises a pad formed by pulverizing or extracting at least one medicinal herb selected from duckweed, semiaquilegia, grape, yellow bean, hibisci cortex, citri pericarpium, grape root, lettuce, lettuce seed, pea flower, ginko nut, rugosa rose, sunflower, sunflower root, rose of Sharon, equiseti herba, ginkgonis germen, glycinis testa, ginseng nodus, spinaciae herba, mori cortex, mori fructus, mori folium, persicae fructus immaturus, pruni lignum, pruni resina, pruni radix, pruni folium, pruni ramulus, pruni semen, pruni flos, mori favilla, motherwort, lonicerae folium, lonicerae flos, porpyrae siccus, pruni caulis, persicae calyx, petasiteae rhizoma, colocasiae rhizoma, Colocasia esculenta tuber, Colocasia esculenta folium, armeniacae semen, ricini semen, glycinis semen ptisanari, whole plant of Trichosanthes cucumeroides, pini pollen, fici fructus, brassicae herba, eriobotryae fructus, pini cortex, pini polium, terebinthinae oleum, brassicae herba, hirundinis nidus, fucus cum caesalpiniae, fucus cum carthami, Trichosanthes cucumeroides semen, melo pediculus, raphani radix, glycine semen nigrae, tuberous root of Trichosanthes cucumeroides, Trichosanthes cucumeroides radix, juniperi favilla, ricini folium, carthami flos, carthami novella, trigonellae semen, verbenae herba, carthami semen, curcumae radix, Curcuma longa rhizoma, apis nidus, mali fructus, Angelica sinensis radix, honey, ginseng, acanthopanacis cortex, hordei fructus germinatus, wild honey, auriculariae polyporus, phragmitis folium, toonae folium, toonae radicis cortex, massa medicata fermentata, phragmitis rhizoma, phragmitis favilla, Allium fistulosum, capsellae semen, capsellae herba, coprini herba, Citrus unshiu immature peel, Colocasia esculenta rhizoma, amaranthi semen, lycii radicis cortex, cyperi rhizoma, perillae folium, allii bulbus, sanguisorbae radix, cnidii rhizoma, Acorus calamus rhizoma, papaveris fructus pericarpium, portulacea herba, foeniculi fructus, raphani semen, cnidii surculus, cassiae folium, ixertis herba, lasiosphaera seu calvatia, sacchari tuber, lycii fructus, asparagi radix, liriopes radix, rehmanniae radix, rehmanniae radix preparata, white ginseng, mint, tangerine, sweet potato, poria, dioscoreae rhizoma, achyranthis radix, dendrobii herba, cassiae semen, chrysanthemum, cuscutae semen, aurantii fructus pericarpium, gazellae cornu, saposhnikovia radix, celosiae semen, schizandrae fructus, glycyrrhizae radix, coptidis rhizoma, tribuli fructus, ligustici rhizoma, chrysanthemum, equiseti herba, osterici radix, viticis fructus, glycyrrhizae radix preparata, gypsum, scutellariae radix, forsythiae fructus, moutan cortex, alismatis rhizoma, corni fructus, marigold, tribuli fructus, angelicae gigantis radix, hirudonis caro, cicadae periostracum, bupleuri radix, cimicifugae rhizoma, ginseng, clematidis radix, anemarrhenae rhizoma, citri pericarpium, atractylodis rhizoma, scrophulariae radix, Angelica pubescens radix, carthami semen, acanthopanacis cortex, sophorae radix, thujae resina, Polygonum multiflorum radix, astragali radix, schizonepetae spica, fingered citron, banana, mushroom, blueberry, green coffee berry, green tea, kale, carrot, spinach, lettuce, pumpkin and broccoli.
7. The support worn on the face having a built-in drug carrier of claim 1, wherein the medicinal herb layer comprises at least one medicinal herb selected from chrysanthemum, lemon, orange, cherry, pomegranate, grape, strawberry, rose, lilac, acacia, freesia, lily, lavender, mint, jasmine, mugwort, rosemary, pine, flavonoid, fir, coffee, ginseng, fingered citron, chamomile, cypress, geranium, juniper, roseclary, sage, lime, neroli, sandalwood bergamot, eucalyptus, lime neroli, peppermint, ylang-ylang, patchouli, myrrh, frankincense, cedarwood, sandalwood, which is extracted and encapsulated to form the medicinal herb layer.
8. The support worn on the face having a built-in drug carrier of claim 1, wherein the fixing member is formed such that it extends backwards from the housing and its rear ends are placed over the ears of the user, and the housing or the fixing member is equipped with a magnet member capable of stimulating at least one part selected from the Taiyang acupoints corresponding to the temples of the user, the Qiuhou and Chengqi acupoints below the eyes, the Wangu and Fengchi acupoints at the back of the head, and the ridge of the nose.
9. The support worn on the face having a built-in drug carrier of claim 1, wherein view holes are formed in the housing so that the user can see ahead while wearing the support worn on the face.
10. The support worn on the face having a built-in drug carrier of claim 9, wherein a pair of the view holes are formed in the housing, in front of the right and left eyes, and the housing is further equipped with two polarizing lenses of different polarizing directions, each of which is installed to cover each of the view holes.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A compound of the formula
wherein
Ar1 is selected from the group consisting of: phenylene and 6-membered heteroarylene containing 1, 2 or 3 nitrogen atoms,
R1 is selected from the group consisting of:
halogen, CN, OH, \u2014NO2, C1-6-alkyl, C2-4-alkenyl, C3-7-cycloalkyl, \u2014(C1-3-alkyl)-(C3-7-cycloalkyl), \u2014O\u2014(C1-6-alkyl), \u2014O\u2014(C3-7-cycloalkyl), \u2014O\u2014(C1-3-alkyl)-(C3-7-cycloalkyl), \u2014NH2, heterocyclyl, \u2014(C1-3-alkyl)-heterocyclyl, \u2014O-(heterocyclyl), \u2014O\u2014(C1-3-alkyl)-(heterocyclyl), \u2014O-phenyl and \u2014O\u2014(C1-3-alkyl)-phenyl,
wherein each alkyl, cycloalkyl and heterocyclyl is optionally substituted with one or more substituents selected from F and OH;
wherein in the NH2-group, one or both hydrogen atoms may independently of each other be replaced by a group selected from C1-6-alkyl, C3-7-cycloalkyl and \u2014(C1-3-alkyl)-(C3-7-cycloalkyl),
wherein said C1-6-alkyl, C3-7-cycloalkyl and \u2014(C1-3-alkyl)-(C3-7-cycloalkyl) groups may each be substituted by one or more F or OH, wherein said substituents are the same or different; and
wherein each heterocyclyl group is selected from a 4- to 7-membered monocyclic heterocyclic ring that contains 1, 2 or 3 hetereoatoms independently selected from N, O and S and may be substituted with one or more substituents independently of each other selected from methyl, \u2014CF3, F and OH, wherein, if two methyl groups are attached to the same carbon atom of the heterocyclyl group, they may be connected to each other to form a spiro-cyclopropyl group;
or, if two R1-groups are attached to adjacent C-atoms of Ar1, they may be linked with each other and together form a C3-5-alkylene bridging group in which 1, 2 or 3 \u2014CH2-groups may independently of each be replaced by \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, \u2014S(\u2550O)\u2014, \u2014S(\u2550O)2\u2014, \u2014NH\u2014 or \u2014N(C1-4-alkyl)-, wherein the alkylene bridge may optionally be substituted by one or two C1-3-alkyl groups;
n is 1, 2 or 3;
Ar2 is phenylene,
which is optionally substituted with F;
R2 is selected from the group consisting of: H and C1-4-alkyl optionally substituted with 1-3 F;
R3 is selected from the group consisting of: H and C1-4-alkyl;
R4 is selected from the group consisting of:
C1-6-alkyl, C3-7-cycloalkyl, (C3-7-cycloalkyl)-(C1-3-alkyl)-, C3-6-alkenyl, C3-6-alkynyl, heterocyclyl, heterocyclyl-(C1-3-alkyl)-, aryl, aryl-(C1-3-alkyl)-, 5- or 6-membered heteroaryl containing 1, 2 or 3 heteroatoms independently selected from N, O and S and (5-membered heteroaryl)-(C1-3-alkyl)-, wherein the heteroaryl moiety has 5 ring atoms and contains 1, 2 or 3 heteroatoms independently selected from N, O and S,
wherein each cycloalkyl and heterocyclyl may be optionally substituted with one or more C1-4-alkyl, and
wherein in each cycloalkyl and heterocyclyl a \u2014CH2-group may optionally be replaced by \u2014C(\u2550O)\u2014, and
wherein each alkyl, cycloalkyl and heterocyclyl may be optionally substituted with one or more groups independently selected from the group consisting of: F, Cl, Br, CN, OH and optionally mono- or polyfluorated \u2014O\u2014(C1-4-alkyl), wherein the alkyl moiety of said \u2014O\u2014(C1-3-alkyl) group may be substituted by one or more F, and
wherein each aryl and heteroaryl group may be optionally substituted with one or more substituents independently of each other selected from F, Cl, \u2014O\u2014CH3, \u2014O\u2014CF3, \u2014O\u2014CHF2, CH3 and \u2014NH\u2014C(\u2550O)\u2014(C1-3-alkyl);
or R3 and R4 are connected with each other and together with the N-atom to which they are attached form a group selected from the group consisting of:
azetidinyl, pyrrolidinyl, piperidinyl and azepanyl,
wherein in each of these cyclic groups one or two CH2-groups may independently of each other be replaced by N, O, S, C(\u2550O) or SO2, andor
wherein each of these groups may be substituted by one or more F or C1-4-alkyl; and
R5 is selected from the group consisting of H, F, Cl, CN and \u2014O\u2014(C1-3-alkyl), wherein the alkyl moiety of the \u2014O\u2014(C1-3-alkyl) group may be substituted by one or more F; and
wherein each of the above-mentioned alkyl and \u2014O-alkyl groups may be substituted by one or more F;
or a tautomer or a salt thereof.
2. A compound of formula (I) according to claim 1, wherein
Ar2 is
R2 is \u2014CH3;
R3 is H or \u2014CH3;
R5 is H; and
n is 1 or 2.
3. A compound of formula (I) according to claim 1, wherein Arl is selected from the group consisting of: phenylene, pyridinylene and pyrimidinylene.
4. A compound of formula (I) according to claim 1, wherein R1 is selected from the group consisting of:
F, Cl, Br, CN, OH, C1-4-alkyl, C3-7-cycloalkyl, \u2014O\u2014(C1-6-alkyl), \u2014O\u2014(C3-7-cycloalkyl), \u2014O\u2014(C1-3-alkyl)-(C3-7-cycloalkyl), \u2014NH2, heterocyclyl, \u2014O\u2014(C1-3-alkyl)-(heterocyclyl), \u2014O-phenyl and \u2014O\u2014(CH2)1-2-phenyl,
wherein each alkyl, cycloalkyl and heterocyclyl is optionally substituted with one or more substituents selected from F and OH;
wherein in the NH2-group, one or both hydrogen atoms may independently of each other be replaced by a group selected from C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl and C3-7-cycloalkyl groups may each be substituted by one or more F or OH, wherein said substituents are the same or different; and
wherein each heterocyclyl group is selected from tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl and may be substituted with one or more F or OH;
or, if two R1-groups are attached to adjacent C-atoms of Ar1, they may be linked with each other and together form a C3-5-alkylene bridging group in which 1, 2 or 3 \u2014CH2-groups may independently of each be replaced by \u2014O\u2014, \u2014C(\u2550O)\u2014, \u2014S\u2014, \u2014NH\u2014 or \u2014N(C1-4-alkyl)-, wherein the alkylene bridge may optionally be substituted by one or two C1-3-alkyl groups.
5. A compound of formula (I) according to claim 1, wherein R1 is selected from the group consisting of:
F, Cl, Br, CN, OH, C1-3-alkyl, C3-5-cycloalkyl, \u2014O\u2014(C1-6-alkyl), \u2014O\u2014(C3-7-cycloalkyl), \u2014O\u2014(C1-3-alkyl)-(C3-5-cycloalkyl), \u2014NH2, heterocyclyl, \u2014O-phenyl and \u2014O\u2014(CH2)1-2-phenyl,
wherein each alkyl, cycloalkyl and heterocyclyl is optionally substituted with one or more substituents selected from F and OH;
wherein in the NH2-group, one or both hydrogen atoms may independently of each other be replaced by a group selected from C1-4-alkyl and C3-5-cycloalkyl; and
wherein each heterocyclyl group is selected from pyrrolidinyl and morpholinyl and may be substituted with one or two F or OH;
or, if two R1-groups are attached to adjacent C-atoms of Ar1, they may be linked with each other and together form a \u2014O\u2014CH2\u2014CH2\u2014CH2\u2014O\u2014 group;
or, if n is 2, the second R1 group is selected from the group consisting of F, Cl, CN, and CH3.
6. A compound of formula (I) according to claim 1, wherein R4 is selected from the group consisting of:
C1-5-alkyl, C3-5-cycloalkyl, (C3-5-cycloalkyl)-CH2\u2014, C3-5-alkenyl, C3-5-alkynyl, heterocyclyl, heterocyclyl-(C1-3-alkyl)-, phenyl, 6-membered heteroaryl containing 1 or 2 N atoms and thiazolyl-CH2\u2014,
wherein the heterocyclyl group is selected from the group consisting of oxetanyl, tetrahydrofuranyl and tetrahydropyranyl, and
wherein each cycloalkyl may be optionally substituted with one or two CH3, and
wherein each alkyl and cycloalkyl may be optionally substituted with one or more groups independently selected from the group consisting of: F, Cl, CN, OH, \u2014O\u2014CHF2, \u2014O\u2014CF3 and \u2014O\u2014CH3, and
wherein the phenyl, thiazolyl and 6-membered heteroaryl groups may each be optionally substituted with one or two substituents inde-pendently of each other selected from F, Cl and \u2014NH\u2014C(\u2550O)\u2014CH3.
7. A compound of formula (I) according to claim 1, wherein R3 is H and R4 is selected from the group consisting of:
C1-5-alkyl optionally substituted with one to three F andor one CN or OH;
C3-5-cycloalkyl optionally substituted with one CH3, wherein said CH3-group may be substituted with one to three F;
(C3-5-cycloalkyl)-CH2\u2014 optionally substituted in the cycloalkyl moiety with one or two F;
C3-5-alkenyl;
C3-5-alkynyl;
oxetanyl, tetrahydrofuranyl, tetrahydropyranyl;
oxetanyl-CH2\u2014;
phenyl optionally substituted with F;
pyridinyl, pyrimidinyl and
thiazolyl-CH2\u2014 optionally substituted with \u2014NH\u2014C(\u2550O)\u2014CH3;
or the groups R3 and R4 may be connected with each other and together with the N-atom to which they are attached form the group
8. A compound according to claim 1 having the formula
wherein
n is 1 or 2;
Ar1 is selected from the group consisting of:
R1 is selected from the group consisting of F, Cl, Br, CN, OH, C1-3-alkyl, C3-5-cycloalkyl, \u2014O\u2014(C1-6-alkyl), \u2014O\u2014(C3-7-cycloalkyl), \u2014O\u2014(C1-3-alkyl)-(C3-5-cycloalkyl), \u2014NH2, heterocyclyl, \u2014O-phenyl and \u2014O\u2014(CH2)1-2-phenyl,
wherein each alkyl, cycloalkyl and heterocyclyl is optionally substituted with one or more substituents selected from F and OH;
wherein in the NH2-group, one or both hydrogen atoms may independently of each other be replaced by a group selected from C1-4-alkyl and C3-5-cycloalkyl; and
wherein each heterocyclyl group is selected from pyrrolidinyl and morpholinyl and may be substituted with one or two F or OH;
or, if two R1-groups are attached to adjacent C-atoms of Ar1, they may be linked with each other and together form a \u2014O\u2014CH2\u2014CH2\u2014CH2\u2014O\u2014 group;
or, if n is 2, the second R1 group is selected from the group consisting of F, Cl, CN, and CH3;
R3 is H or CH3; and
R4 is selected from the group consisting of:
C1-5-alkyl optionally substituted with one to three F andor one CN or OH;
C3-5-cycloalkyl optionally substituted with one CH3, wherein said CH3-group may be substituted with one to three F;
(C3-5-cycloalkyl)\u2014CH2\u2014 optionally substituted in the cycloalkyl moiety with one or two F;
C3-5-alkenyl;
C3-5-alkynyl;
oxetanyl, tetrahydrofuranyl, tetrahydropyranyl;
oxetanyl-CH2\u2014;
phenyl optionally substituted with F;
pyridinyl, pyrimidinyl and
thiazolyl-CH2\u2014 optionally substituted with \u2014NH\u2014C(\u2550O)\u2014CH3;
or R3 and R4 are connected with each other and together with the N-atom to which they are attached form the group
or a salt thereof.
9. A compound according to claim 1 having the formula
wherein
the (R1)n\u2014Ar1\u2014 moiety is selected from a group consisint of:
and
R4 is selected from the group consisting of:
ethyl, \u2014CH2\u2014CHF2, cyclopropyl and
or a pharmaceutically acceptable salt thereof.
10. A compound according to claim 1 selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.
11. A pharmaceutically acceptable salt of a compound according to claim 1.
12. A method of therapeutically treating obesity or type 2 diabetes which comprises administering to a host suffering from one of the said conditions a therapeutically effective amount of a compound according to claim 1.
13. A pharmaceutical composition comprising a compound according to claim 1 together with one or more inert carriers andor diluents.