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1. (WO1998048804) ANTITHROMBOTIC AGENTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/048804 International Application No.: PCT/US1998/008717
Publication Date: 05.11.1998 International Filing Date: 30.04.1998
Chapter 2 Demand Filed: 20.11.1998
IPC:
A61K 31/4025 (2006.01) ,A61K 31/4155 (2006.01) ,A61K 31/4178 (2006.01) ,A61K 31/422 (2006.01) ,A61K 31/427 (2006.01) ,A61K 31/4439 (2006.01) ,A61K 31/454 (2006.01) ,A61K 31/5377 (2006.01) ,C07D 333/56 (2006.01) ,C07D 333/58 (2006.01) ,C07D 409/12 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (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
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
4025
not condensed and containing further heterocyclic rings, e.g. cromakalim
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
415
1,2-Diazoles
4155
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
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
4178
not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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
42
Oxazoles
422
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
427
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
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
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
50
condensed with carbocyclic rings or ring systems
52
Benzo [b] thiophenes; Hydrogenated benzo [b] thiophenes
54
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
56
Radicals substituted by oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
50
condensed with carbocyclic rings or ring systems
52
Benzo [b] thiophenes; Hydrogenated benzo [b] thiophenes
54
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
58
Radicals substituted by nitrogen atoms
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
12
linked by a chain containing hetero atoms as chain links
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
ELI LILLY AND COMPANY [US/US]; Lilly Corporate Center Indianapolis, IN 46285, US (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
CHIRGADZE, Nickolay Y. [RU/US]; US (UsOnly)
DENNEY, Michael, L. [US/US]; US (UsOnly)
FISHER, Matthew, J. [US/US]; US (UsOnly)
FOGLESONG, Robert, J. [US/US]; US (UsOnly)
HARPER, Richard, W. [US/US]; US (UsOnly)
JOHNSON, Mary, G. [US/US]; US (UsOnly)
LIN, Ho-Shen [US/US]; US (UsOnly)
LYNCH, Michael, P. [US/US]; US (UsOnly)
MCCOWAN, Jefferson, R. [US/US]; US (UsOnly)
MILLER, Shawn, C. [US/US]; US (UsOnly)
PALKOWITZ, Alan, D. [US/US]; US (UsOnly)
RICHETT, Michael, E. [US/US]; US (UsOnly)
SALL, Daniel, Jon [US/US]; US (UsOnly)
SMITH, Gerald, Floyd [US/US]; US (UsOnly)
TAKEUCHI, Kumiko [US/US]; US (UsOnly)
ZHANG, Minsheng [CN/US]; US (UsOnly)
Inventors:
CHIRGADZE, Nickolay Y.; US
DENNEY, Michael, L.; US
FISHER, Matthew, J.; US
FOGLESONG, Robert, J.; US
HARPER, Richard, W.; US
JOHNSON, Mary, G.; US
LIN, Ho-Shen; US
LYNCH, Michael, P.; US
MCCOWAN, Jefferson, R.; US
MILLER, Shawn, C.; US
PALKOWITZ, Alan, D.; US
RICHETT, Michael, E.; US
SALL, Daniel, Jon; US
SMITH, Gerald, Floyd; US
TAKEUCHI, Kumiko; US
ZHANG, Minsheng; US
Agent:
JACKSON, Thomas, E. ; Eli Lilly and Company Lilly Corporate Center Indianapolis, IN 46285, US
Priority Data:
60/045,18830.04.1997US
Title (EN) ANTITHROMBOTIC AGENTS
(FR) AGENTS ANTITHROMBOTIQUES
Abstract:
(EN) This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of defined compounds of formula (I) as thrombin inhibitors.
(FR) La présente invention concerne de nouveaux composés représentés par la formule (I) (et leurs sels pharmaceutiquement acceptables ), tels que définis dans la description, des procédés et des intermédiaires pour leur préparation. La présente invention concerne également des formulations pharmaceutiques comprenant ces nouveaux composés, et leur utilisation comme inhibiteurs de thrombine.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP1027051US6391901JP2002501503 CA2288224AU1998074700