US2003162690A1PendingUtilityA1
Benzamides and related inhibitors of factor Xa
Est. expiryFeb 29, 2020(expired)· nominal 20-yr term from priority
Inventors:Bing-Yan ZhuPenglie ZhangLingyan WangWenrong HuangErick GoldmanWenhao LiJingmei ZuckettYonghong SongRobert M. Scarborough
C07D 217/22C07D 233/56C07D 213/75C07D 249/08C07C 259/18C07D 401/12C07D 333/38A61K 31/44C07D 409/14A61K 31/616C07D 295/125C07D 213/81C07D 409/12C07C 311/46C07C 311/16C07C 237/42A61K 9/2054C07D 213/82C07C 317/44C07C 257/18A61P 7/00C07D 231/12C07D 233/64A61K 45/06A61P 7/02A61K 9/20C07C 255/60A61K 9/4858C07C 317/40A61K 9/2013A61K 9/48A61K 9/4866
54
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Claims
Abstract
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described Compositions containing such compounds are also described The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders
Claims
exact text as granted — not AI-modifiedWhat is claimed:
1 . A compound of formula VI
wherein:
Z′ and Z″ are each independently a C 1 -C 6 alkyl which is optionally substituted with a hydroxyl, carboxylic acid or carboxylic acid ester group;
R 1a is a member selected from the group of H, —F, —Cl and Br;
R 1d2 and R 1d4 are each H;
R 1d1 and R 1d3 are each independently a member selected from the group of H, —Cl, —F, —Br, —OH and —OMe,
R 1e is a member selected from the group of —F, —Cl, —Br, —OH, -Me and —OMe,
and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof
2 . A compound of claim 1 wherein Z′ is -Me and Z″ is —CH 2 OH, —CH 2 CO 2 H, or —CH 2 CO 2 CH 3
3 . A compound of claim 1 having the following structure:
4 . A compound of claim 1 having the following structure:
5 . A compound of claim 1 having the following structure
6 A compound of claim 1 having the following structure:
7 A compound of claim 1 having the following structure:
8 A compound of claim 1 having the following structure:
9 . A compound of claim 1 having the following structure
10 . A compound of claim 1 having the following structure.
11 . A compound of claim 1 having the following structure.
12 A compound of claim 1 having the following structure
13 A compound of claim 1 having the following structure:
14 . A compound of claim 1 having the following structure
15 . A compound of claim 1 having the following structure
16 . A compound of claim 1 having the following structure.
17 A compound of claim 1 having the following structure:
18 . A compound of claim 1 having the following structure:
19 . A pharmaceutical composition for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of one of claims 1 - 18 .
20 . A method for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of one of claims 1 - 18 .
21 . The method of claim 20 , wherein the condition is selected from the group consisting of:
acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, occlusive coronary thrombus occurring post-thrombolytic therapy or post-coronary angioplasty, a thrombotically mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, transient ischemic attacks, venous thrombosis, deep venous thrombosis, pulmonary embolus, coagulopathy, disseminated intravascular coagulation, thrombotic thrombocytopenic purpura, thromboangiitis obliterans, thrombotic disease associated with heparin-induced thrombocytopenia, thrombotic complications associated with extracorporeal circulation, thrombotic complications associated with instrumentation, and thrombotic complications associated with the fitting of prosthetic devices
22 . A method for inhibiting the coagulation of a biological sample comprising the step of administering a compound of one of claims 1 - 18 .
23 A compound formula VII
wherein
A-Q is a member selected from the group of.
where Z′ is a C 1 -C 6 alkyl which is optionally substituted with a hydroxyl, carboxylic acid or carboxylic acid ester group,
R 1a is a member selected from the group of H, —F, —Cl and Br;
R 1d2 and R 1d4 are each H;
R 1d1 and R 1d3 are each independently a member selected from the group of H, —Cl, —F, —Br, —OH and —OMe;
R 1e is a member selected from the group of —F, —Cl, —Br, —OH, -Me and —OMe,
and all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof
24 . A compound of claim 23 , wherein A-Q is.
and Z′ is -Me, —CH 2 OH, —CH 2 CO 2 H, or —CH 2 CO 2 CH 3
25 A compound of claim 24 having the following structure
26 A compound of claim 24 having the following structure:
27 . A compound of claim 24 having the following structure.
28 . A compound of claim 24 having the following structure
29 . A compound of claim 24 having the following structure:
30 . A compound of claim 24 having the following structure:
31 A compound of claim 24 having the following structure:
32 A compound of claim 24 having the following structure
33 A compound of claim 24 having the following structure.
34 . A compound of claim 24 having the following structure:
35 . A compound of claim 24 having the following structure
36 . A compound of claim 24 having the following structure
37 . A compound of claim 24 having the following structure:
38 . A compound of claim 24 having the following structure
39 A compound of claim 24 having the following structure
40 . A compound of claim 24 having the following formula:
41 . A compound of claim 23 having the following formula
42 . A compound of claim 23 having the following formula
43 . A compound of claim 23 having the following structure:
44 A compound of claim 23 having the following structure
45 . A compound of claim 23 having the following structure:
46 A compound of claim 23 having the following structure:
47 . A compound of claim 23 having the following structure.
48 . A compound of claim 23 having the following structure:
49 A compound of claim 23 having the following structure:
50 . A compound of claim 23 having the following stricture.
51 . A compound of claim 23 having the following structure
52 . A compound of claim 23 having the following structure
53 . A compound of claim 23 having the following structure
54 A compound of claim 23 having the following structure:
55 . A compound of claim 23 having the following structure:
56 . A compound of claim 23 having the following structure:
57 . A compound of claim 23 having the following structure:
58 . A compound of claim 23 having the following structure.
59 A compound of claim 23 having the following structure
60 . A compound of claim 23 having the following structure.
61 A compound of claim 23 having the following structure:
62 . A compound of claim 23 having the following structure.
63 . A compound of claim 23 having the following structure:
64 . A compound of claim 23 having the following structure:
65 . A compound of claim 23 having the following structure:
66 . A compound of claim 23 having the following structure:
67 A compound of claim 23 having the following structure
68 . A compound of claim 23 having the following structure:
69 A pharmaceutical composition for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of one of claims 23 - 68
70 . A method for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of one of claims 23 - 68 .
71 The method of claim 70 , wherein the condition is selected from the group consisting of acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, occlusive coronary thrombus occurring post-thrombolytic therapy or post-coronary angioplasty, a thrombotically mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, transient ischemic attacks, venous thrombosis, deep venous thrombosis, pulmonary embolus, coagulopathy, disseminated intravascular coagulation, thrombotic thrombocytopenic purpura, thromboangiitis obliterans, thrombotic disease associated with heparin-induced thrombocytopenia, thrombotic complications associated with extracorporeal circulation, thrombotic complications associated with instrumentation, and thrombotic complications associated with the fitting of prosthetic devices.
72 . A method for inhibiting the coagulation of a biological sample comprising the step of administering a compound of one of claims 23 - 68Join the waitlist — get patent alerts
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