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1. (WO2013064681) N-(PYRID-4-YL)AMIDES AND N-(PYRIMIDIN-4-YL)AMIDES AND THEIR PHARMACEUTICAL AND COSMETIC USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2013/064681 International Application No.: PCT/EP2012/071811
Publication Date: 10.05.2013 International Filing Date: 05.11.2012
IPC:
C07D 213/75 (2006.01) ,C07D 239/52 (2006.01) ,C07D 405/12 (2006.01) ,A61K 31/44 (2006.01) ,A61K 31/4433 (2006.01) ,A61K 31/506 (2006.01) ,A61Q 5/02 (2006.01) ,A61Q 7/00 (2006.01) ,A61Q 9/00 (2006.01) ,A61Q 19/10 (2006.01) ,A61P 17/00 (2006.01)
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
60
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
72
Nitrogen atoms
75
Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
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
4433
containing a six-membered ring with oxygen as a ring hetero atom
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
Q
SPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
5
Preparations for care of the hair
02
Preparations for cleaning the hair
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
Q
SPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
7
Preparations for affecting hair growth
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
Q
SPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
9
Preparations for removing hair or for aiding hair removal
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
10
Washing or bathing preparations
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
Applicants:
GALDERMA RESEARCH & DEVELOPMENT [FR/FR]; 2400 Route des Colles Les Templiers F-06410 Biot, FR
Inventors:
POINSARD, Cédric; FR
Agent:
CASALONGA, Axel; CASALONGA & ASSOCIES 8 avenue Percier F-75008 PARIS, FR
Priority Data:
115999704.11.2011FR
61/555,58304.11.2011US
Title (EN) N-(PYRID-4-YL)AMIDES AND N-(PYRIMIDIN-4-YL)AMIDES AND THEIR PHARMACEUTICAL AND COSMETIC USE
(FR) N-(PYRID-4-YL)AMIDES ET N-(PYRIMIDIN-4-YL)AMIDES ET LEUR UTILISATION PHARMACEUTIQUE ET COSMÉTIQUE
Abstract:
(EN) The present invention relates generally to the field of pharmaceuticals and cosmetics. More specifically, the present invention pertains to certain N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) which are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in therapy, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin; seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. The present invention also relates to compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) an androgen receptor using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
(FR) De manière générale, cette invention concerne le domaine des produits pharmaceutiques et cosmétiques. Plus spécifiquement, cette invention concerne certains N-(pyrid-4-yl)amides et N-(pyrimidin-4-yl)amides de formule (1) qui sont de puissants modulateurs (par ex., inhibiteurs) du récepteur des androgènes, et qui sont utiles, par exemple, en thérapie, pour traiter, par exemple, une maladie ou une affection dermatologique ; une maladie ou un dérèglement des glandes sébacées ; l'acné ; l'hyperséborrhée ; la peau grasse ; la dermatite séborrhéique ; l'hyperpilosité ou hirsutisme ; l'eczéma constitutionnel ; ou l'alopécie androgène ; notamment, l'acné. Cette invention concerne également des compositions (par ex., compositions pharmaceutiques, compositions cosmétiques) contenant les composés ; des procédés de préparation desdites compositions ; des procédés de modulation (par ex., inhibition) du récepteur des androgènes faisant appel aux composés et/ou aux compositions selon l'invention ; et l'utilisation médicale et/ou cosmétique desdits composés et compositions.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, 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, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, 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, RS, 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: English (EN)
Filing Language: English (EN)
Also published as:
CA2853723US20140234245CN104039767EP2788326JP2014532686IL232333
KR1020140088204RU2014122543FR2982261BR112014010458RU0002625789