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1. (WO2010077275) MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/077275 International Application No.: PCT/US2009/006408
Publication Date: 08.07.2010 International Filing Date: 07.12.2009
IPC:
C07D 237/14 (2006.01) ,C07D 401/04 (2006.01) ,C07D 403/04 (2006.01) ,C07D 409/04 (2006.01) ,C07D 253/07 (2006.01) ,A61K 31/50 (2006.01) ,A61K 31/501 (2006.01) ,A61K 31/53 (2006.01) ,A61P 11/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
237
Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
02
not condensed with other rings
06
having three 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
14
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
253
Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/166
02
not condensed with other rings
06
1,2,4-Triazines
065
having three double bonds between ring members or between ring members and non-ring members
07
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
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
50
Pyridazines; Hydrogenated pyridazines
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
50
Pyridazines; Hydrogenated pyridazines
501
not condensed and containing further heterocyclic 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
53
having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
08
Bronchodilators
Applicants:
ARENA PHARMACEUTICALS, INC. [US/US]; 6166 Nancy Ridge Drive San Diego, California 92121-3223, US (AllExceptUS)
TRAN, Thuy-Anh [US/US]; US (UsOnly)
HAYASHI, Rena [JP/US]; US (UsOnly)
IBARRA, Jason B. [US/US]; US (UsOnly)
ULLMAN, Brett [US/US]; US (UsOnly)
ZOU, Ning [CN/US]; US (UsOnly)
Inventors:
TRAN, Thuy-Anh; US
HAYASHI, Rena; US
IBARRA, Jason B.; US
ULLMAN, Brett; US
ZOU, Ning; US
Agent:
GODDARD, Christine A.; Fish & Richardson P.C. P.O: Box 1022 Minneapolis, Minnesota 55440-1022, US
Priority Data:
61/201,15008.12.2008US
61/205,72622.01.2009US
Title (EN) MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
(FR) MODULATEURS DU RÉCEPTEUR DE PROSTACYCLINE (PGI2) UTILES POUR LE TRAITEMENT DE TROUBLES ASSOCIÉS À CELUI-CI
Abstract:
(EN) Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
(FR) La présente invention concerne des dérivés de cyclohexane de formule Ia et des compositions pharmaceutiques de ceux-ci qui modulent l'activité du récepteur PGI2. Les composés de la présente invention et des compositions pharmaceutiques de ceux-ci sont associés à des procédés utiles dans le traitement de : l'hypertension artérielle pulmonaire (PAH) et des troubles associés; l'agrégation plaquettaire; une maladie coronarienne; l'infarctus du myocarde; un accident ischémique transitoire; l'angine de poitrine; un accident vasculaire cérébral; une lésion d'ischémie-reperfusion; une resténose; une fibrillation auriculaire; la formation de caillot sanguin dans une intervention chirurgicale d'angioplastie ou de pontage coronarien ou chez un individu souffrant de fibrillation auriculaire; l'athérosclérose; l'athérothrombose; l'asthme ou un symptôme de celui-ci; un trouble associé au diabète tel que la neuropathie périphérique diabétique, la néphropathie diabétique ou la rétinopathie diabétique; le glaucome ou une autre maladie des yeux avec pression intraoculaire anormale; l'hypertension; l'inflammation; le psoriasis; le rhumatisme psoriasique; la polyarthrite rhumatoïde; la maladie de Crohn; le rejet de greffe; la sclérose en plaques; le lupus érythémateux disséminé (SLE); la recto-colite hémorragique; une lésion d'ischémie-reperfusion; la resténose; l'athérosclérose; l'acné; le diabète de type 1; le diabète de type 2; la sepsie; et la bronchopneumopathie chronique obstructive (COPD).
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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: English (EN)
Filing Language: English (EN)
Also published as:
US20110245251ES2548882DK2370413