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1. (WO2005048916) TETRAHYDROSPIRO-BETA-CARBOLINE-1,3 '-PYRROLIDINE DERIVATIVES AND THEIR USE IN GHSR-RELATED DISORDERS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2005/048916 International Application No.: PCT/SE2004/001688
Publication Date: 02.06.2005 International Filing Date: 18.11.2004
Chapter 2 Demand Filed: 02.06.2005
IPC:
C07D 471/14 (2006.01) ,C07D 471/18 (2006.01) ,C07D 471/22 (2006.01) ,C07D 491/14 (2006.01) ,C07D 491/20 (2006.01) ,C07D 491/22 (2006.01) ,A61K 31/438 (2006.01) ,A61K 31/407 (2006.01) ,A61P 3/04 (2006.01) ,A61P 3/10 (2006.01) ,A61P 5/08 (2006.01) ,A61P 9/04 (2006.01) ,A61P 9/10 (2006.01) ,A61P 35/00 (2006.01) ,C07D 471/00 (2006.01) ,C07D 491/00 (2006.01) ,C07D 209/00 (2006.01) ,C07D 221/00 (2006.01) ,C07D 317/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12
in which the condensed system contains three hetero rings
18
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
22
in which the condensed systems contains four or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12
in which the condensed system contains three hetero rings
20
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
22
in which the condensed system contains four or more hetero rings
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
438
the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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
407
condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
06
of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
08
for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
04
Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
221
Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/-C07D219/187
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
317
Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
Applicants:
BRANDT, Peter [SE/SE]; SE (UsOnly)
BREMBERG, Ulf [SE/SE]; SE (UsOnly)
CROSSLEY, Roger [GB/GB]; GB (UsOnly)
GRAFFNER NORDBERG, Malin [SE/SE]; SE (UsOnly)
JENMALM JENSEN, Annika [SE/SE]; SE (UsOnly)
RINGBERG, Erik [SE/SE]; SE (UsOnly)
WARD, Terry [GB/GB]; GB (UsOnly)
BIOVITRUM AB [SE/SE]; S-112 76 Stockholm, SE (AllExceptUS)
Inventors:
BRANDT, Peter; SE
BREMBERG, Ulf; SE
CROSSLEY, Roger; GB
GRAFFNER NORDBERG, Malin; SE
JENMALM JENSEN, Annika; SE
RINGBERG, Erik; SE
WARD, Terry; GB
Agent:
HÖGLUND, Lars; BIOVITRUM AB S-112 76 Stockholm, SE
Priority Data:
0303078-020.11.2003SE
60/560,69008.04.2004US
Title (EN) TETRAHYDROSPIRO-BETA-CARBOLINE-1,3 '-PYRROLIDINE DERIVATIVES AND THEIR USE IN GHSR-RELATED DISORDERS
(FR) NOUVELLES CARBOLINES-BETA EN TANT QU'ANTAGONISTES DE RECEPTEUR DE SECRETAGOGUE D'HORMONE DE CROISSANCE
Abstract:
(EN) The present invention relates to compounds of Formula (I): Formula (I) wherein R3-R8, X, and Y are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.
(FR) La présente invention a trait à des composés de formule (I), dans laquelle : R3-R8, X et Y sont tels que définis dans la description, à des procédés pour la préparation des composés, à des compositions pharmaceutiques comportant les composés, et à l'utilisation des composés et des compositions dans la prophylaxie ou le traitement de trouble lié au récepteur de sécrétagogue d'hormone de croissance. Des exemples de tels troubles sont l'obésité et des troubles associés tels que le diabète de type II, la dyslipidémie et le syndrome métabolique du syndrome Prader-Willi, des maladies cardio-vasculaires telles que la maladie vasculaire athérosclérotique, l'angine de poitrine, l'infarctus du myocarde et l'accident cérébrovasculaire, l'acromégalie et le cancer, notamment les carcinomes mammaire, pulmonaire, prostatique, thyroïdien et endocrinien hypophysaire.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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 Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LU, MC, NL, PL, PT, RO, SE, SI, SK, 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)