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1. (EP3078658) C5AR ANTAGONISTS

Office : European Patent Office
Application Number: 16167779 Application Date: 21.12.2009
Publication Number: 3078658 Publication Date: 12.10.2016
Publication Kind : B1
Designated States: AL, AT, BA, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LI, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR
Prior PCT appl.: Application Number:US2009068941 ; Publication Number: Click to see the data
IPC:
C07D 211/60
A61K 31/445
A61K 31/451
A61K 31/4545
A61K 31/5377
A61P 37/06
C07D 401/06
C07D 401/10
C07D 401/14
C07D 405/10
C07D 413/12
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
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
60
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
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
451
having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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
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
5377
not condensed and containing further heterocyclic rings, e.g. timolol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
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
06
linked by a carbon chain containing only aliphatic carbon 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
10
linked by a carbon chain containing aromatic rings
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
14
containing three or more hetero rings
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
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
CPC:
A61K 31/445
A61K 31/451
A61K 31/454
A61K 31/4545
A61K 31/5377
C07D 211/60
C07D 401/06
C07D 401/10
C07D 401/12
C07D 401/14
C07D 405/10
C07D 413/12
C07D 413/14
C07D 211/14
C07D 211/22
Applicants: CHEMOCENTRYX INC
Inventors: FAN PINGCHEN
GREENMAN KEVIN LLOYD
LELETI MANMOHAN REDDY
LI YANDONG
POWERS JAY
TANAKA HIROKO
YANG JU
ZENG YIBIN
Priority Data: 09835688 21.12.2009 EP
13991908 22.12.2008 US
2009068941 21.12.2009 US
Title: (DE) C5AR-ANTAGONISTEN
(EN) C5AR ANTAGONISTS
(FR) ANTAGONISTES DE C5AR
Abstract: front page image
(EN) A process for preparing a compound of formula (ii), comprising (a) treating a compound of formula (i) with H 2 and a platinum oxide catalyst under reducing conditions; and (b) subjecting the product of step (a) to resolution with di-toluoyl-L-tartaric acid to provide compound (ii) in about 97% enantiomeric excess.
(FR) L'invention porte sur des composés qui sont des modulateurs du récepteur de C5a. Les composés sont des pipéridines substituées, et sont utiles dans des compositions pharmaceutiques. L'invention porte également sur des méthodes de traitement de maladies et de troubles mettant en jeu l'activation pathologique de récepteurs de C5a.
Also published as:
DZDZP2011000468RSP-2016/0606UAa201109018AR077162IL213676MXMX/a/2011/006550
SG172338MA32975JP2012513402CN102264227CA2747522EA201101009
MX2011006550CO6400172KR1020110100661BRPI0923384NZ594140DK2381778
AU2009330194CA2965223VN28786ID051.4755TH128002IN3071/KOLNP/2011
PT2381778WO/2010/075257