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1. (WO2010074052) MELANIN PRODUCTION INHIBITOR
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/074052 International Application No.: PCT/JP2009/071279
Publication Date: 01.07.2010 International Filing Date: 22.12.2009
IPC:
A61K 31/045 (2006.01) ,A61K 8/34 (2006.01) ,A61K 31/065 (2006.01) ,A61K 31/075 (2006.01) ,A61K 31/085 (2006.01) ,A61K 31/135 (2006.01) ,A61K 31/137 (2006.01) ,A61K 31/198 (2006.01) ,A61K 31/40 (2006.01) ,A61K 31/4015 (2006.01) ,A61K 31/4164 (2006.01) ,A61K 31/4409 (2006.01) ,A61K 31/444 (2006.01) ,A61K 31/4453 (2006.01) ,A61K 31/4545 (2006.01) ,A61K 31/495 (2006.01) ,A61K 31/5375 (2006.01) ,A61P 17/16 (2006.01) ,A61Q 19/02 (2006.01) ,A61K 8/40 (2006.01) ,C07D 207/12 (2006.01) ,C07D 207/404 (2006.01) ,C07D 213/30 (2006.01) ,C07D 213/38 (2006.01) ,C07D 233/58 (2006.01) ,C07D 295/02 (2006.01) ,C07D 295/08 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
045
Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
8
Cosmetics or similar toilet preparations
18
characterised by the composition
30
containing organic compounds
33
containing oxygen
34
Alcohols
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
045
Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
065
Diphenyl-substituted acyclic alcohols
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
075
Ethers or acetals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
075
Ethers or acetals
085
having an ether linkage to aromatic ring nuclear carbon
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
135
having aromatic rings, e.g. methadone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
13
Amines, e.g. amantadine
135
having aromatic rings, e.g. methadone
137
Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
197
the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198
Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4015
having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4409
only substituted in position 4, e.g. isoniazid, iproniazid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
444
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4453
only substituted in position 1, e.g. propipocaine, diperodon
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4545
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
16
Emollients or protectives, e.g. against radiation
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
Q
SPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
19
Preparations for care of the skin
02
for chemically bleaching or whitening the skin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
8
Cosmetics or similar toilet preparations
18
characterised by the composition
30
containing organic compounds
40
containing nitrogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
12
Oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30
having two double bonds between ring members or between ring members and non-ring members
34
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
36
Oxygen or sulfur atoms
40
2,5-Pyrrolidine-diones
404
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
28
Radicals substituted by singly-bound oxygen or sulfur atoms
30
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
36
Radicals substituted by singly-bound nitrogen atoms
38
having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
56
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
58
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
02
containing only hydrogen and carbon atoms in addition to the ring hetero elements
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04
with substituted hydrocarbon radicals attached to ring nitrogen atoms
08
substituted by singly bound oxygen or sulfur atoms
Applicants:
ポーラ化成工業株式会社 POLA CHEMICAL INDUSTRIES INC. [JP/JP]; 静岡県静岡市駿河区弥生町6番48号 6-48, Yayoi-cho, Suruga-ku, Shizuoka-shi, Shizuoka 4228009, JP (AllExceptUS)
横山 浩治 YOKOYAMA, Kouji [JP/JP]; JP (UsOnly)
木村 誠 KIMURA, Makoto [JP/JP]; JP (UsOnly)
玉井 将志 TAMAI, Masashi [JP/JP]; JP (UsOnly)
斉藤 優子 SAITOH, Yuko [JP/JP]; JP (UsOnly)
加藤 朋美 KATO, Tomomi [JP/JP]; JP (UsOnly)
池田 優 IKEDA, Yu [JP/JP]; JP (UsOnly)
Inventors:
横山 浩治 YOKOYAMA, Kouji; JP
木村 誠 KIMURA, Makoto; JP
玉井 将志 TAMAI, Masashi; JP
斉藤 優子 SAITOH, Yuko; JP
加藤 朋美 KATO, Tomomi; JP
池田 優 IKEDA, Yu; JP
Agent:
川口 嘉之 KAWAGUCHI, Yoshiyuki; 東京都中央区東日本橋3丁目4番10号 アクロポリス21ビル6階 Acropolis 21 Building 6th floor, 4-10, Higashi Nihonbashi 3-chome, Chuo-ku, Tokyo 1030004, JP
Priority Data:
2008-32596922.12.2008JP
Title (EN) MELANIN PRODUCTION INHIBITOR
(FR) INHIBITEUR DE LA PRODUCTION DE MÉLANINE
(JA) メラニン産生抑制剤
Abstract:
(EN) Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3’s present in the compound corresponds to the number of X’s and, when two or more R3’s are present, the R3’s are independently present and the adjacent two R3’s may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.
(FR) La présente invention porte sur un inhibiteur de la production de mélanine démontrant une excellente activité d'inhibition de la mélanine et une sécurité élevée. Ledit inhibiteur de la production de mélanine comprend un composé représenté par la formule générale (1) (à l'exception du clotrimazole) et/ou un sel pharmaceutiquement acceptable dudit composé. Dans la formule, A1, A2 et A3 sont sélectionnés indépendamment parmi un atome d'hydrogène, un groupe aryle pouvant comporter un substituant, et un groupe hétérocyclique aromatique pouvant comporter un substituant, au moins un desdits A1, A2 et A3 étant sélectionné parmi le groupe aryle et le groupe hétérocyclique aromatique, le nombre total des atomes de carbone contenus dans A1, A2 et A3 étant compris entre 6 et 50 et, lorsque au moins deux desdits A1, A2 et A3 représentent les groupes aryle ou les groupes hétérocycliques aromatiques, les deux groupes aryle ou hétérocyclique aromatique adjacents pouvant être liés entre eux via une chaîne alkyle ou une chaîne alcényle pour former un cycle; m représente un nombre entier de 0 à 2; X représente un hétéroatome, un atome d'hydrogène ou un atome de carbone; R1 et R2 sont sélectionnés indépendamment parmi un atome d'hydrogène et un groupe oxo, et lorsqu'un desdits R1 ou R2 est un groupe oxo, l'autre n'est pas présent; et R3 est sélectionné parmi un atome d'hydrogène et un groupe hydrocarbure C1-C8 dans lequel un ou plusieurs atomes d'hydrogène ou atomes de carbone peuvent être remplacés par un hétéroatome ou des hétéroatomes, le nombre de R3 présents dans le composé correspondant au nombre de X et, lorsque deux R3 ou plus sont présents, lesdits R3 sont présents de manière indépendante et deux R3 adjacents peuvent être liés entre eux pour former, avec X, un cycle, les terminaisons des R3 pouvant être liées à un atome de carbone auquel sont liés A1, A2 et A3, et ainsi former un cycle.
(JA)  メラニン産生抑制作用に優れ、安全性の高いメラニン産生抑制剤を提供する。 下記一般式(1)で表される化合物(クロトリマゾールを除く。)及び/又はそれらの薬理学的に許容される塩を、メラニン産生抑制剤とする。 式中、A1、A2及びA3は、独立して、水素原子、置換基を有していてもよいアリール、及び置換基を有していてもよい芳香族複素環基から選ばれる、但し、A1、A2及びA3の少なくとも一つは、前記アリール又は前記芳香族複素環基から選ばれ、A1、A2及びA3の合計炭素数は6~50である、また、A1、A2及びA3の2つ以上が、前記アリール又は前記芳香族複素環基であるとき、隣り合う2つの前記アリール又は前記芳香族複素環基が、アルキル鎖又はアルケニル鎖を介して結合して、さらに環を形成していてもよい、mは、0~2の整数である、Xは、複素原子、水素原子又は炭素原子である、R1及びR2は、独立して、水素原子及びオキソから選ばれる、但し、R1及びR2の一方がオキソのとき、もう一方は存在しない、R3は、水素原子、又は一部の水素原子若しくは炭素原子が複素原子で置換されていてもよい、炭素数1~8の炭化水素基から選ばれ、R3は、Xに応じた数で存在する、但し、R3が2つ以上のとき、R3は独立である、また、R3が2つ以上のとき、隣り合う2つのR3は互いに結合して、Xと共に環を形成していてもよい、また、R3の末端が、A1、A2及びA3が結合している炭素原子に結合して、環を形成していてもよい。
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)
Also published as:
UAa201109121IL213694MXMX/a/2011/005218SG171722EP2380567JPWO2010074052
US20110243865CN102264357RU2011130514CA2747770US20140363389MX2011005218
EP2845587KR1020110098839BRPI0922548EP3009123CA2934300AU2009331298
VN27838ID051.4374MYPI 2011002868TH110598US20150328107IN5127/CHENP/2011
ES2706379