US2011009448A1PendingUtilityA1
Compound
Est. expiryOct 24, 2022(expired)· nominal 20-yr term from priority
Inventors:Nigel VickerSu XiangdongDharshini GaneshapillaiAtul PurohitMichael John ReedBarry Victor Lloyd Potter
A61P 37/00A61P 9/00A61P 3/10A61P 3/00A61P 29/00A61P 3/04A61P 35/00C07D 209/08C07D 277/14A61P 11/06C07D 263/56C07D 235/08A61P 19/00C07D 277/64A61P 19/02C07D 417/12
50
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Claims
Abstract
A compound having Formula I wherein one of R 1 and R 2 is a group of the formula wherein R 4 is selected from H and hydrocarbyl, R 5 is a hydrocarbyl group and L is an optional linker group, or R 1 and R 2 together form a ring substituted with the group wherein R 3 is H or a substituent, and wherein X is selected from S, O, NR 6 and C(R 7 )(R 8 ), wherein R 6 is selected from H and hydrocarbyl groups, wherein each of R 7 and R 8 are independently selected from H and hydrocarbyl groups.
Claims
exact text as granted — not AI-modified1 - 38 . (canceled)
39 . A compound having Formula I
wherein one of R 1 and R 1 is a group of the formula
wherein R 4 is selected from H and hydrocarbyl, R 5 is a hydrocarbyl group and L is an optional linker group,
or R 1 and R 2 together form a ring substituted with the group
wherein R 3 is H or a substituent
and wherein X is selected from S, O, NR 6 and C(R 7 )(R 8 ), wherein R 6 is selected from H and hydrocarbyl groups, wherein each of R 7 and R 8 are independently selected from H and hydrocarbyl groups.
40 . A compound according to claim 39 having Formula II
41 . A compound according to claim 39 , wherein L is not present.
42 . A compound according to claim 39 , wherein R 1 and R 2 together form a ring substituted with the group
43 . A compound according to claim 39 , wherein R 1 and R 2 together form a carbocyclic ring.
44 . A compound according to claim 39 , wherein R 1 and R 2 together form a six-membered ring.
45 . A compound according to claim 39 , wherein R 1 and R 2 together form an aryl ring.
46 . A compound according to claim 39 , having Formula III.
47 . A compound according to claim 39 , having Formula IV.
48 . A compound according to claim 39 , having Formula V.
49 . A compound according to claim 39 , having Formula VI.
50 . A compound according to claim 39 , having Formula VII.
51 . A compound according to claim 39 , wherein R 3 is selected from H, hydrocarbyl, —S-hydrocarbyl, —S—H, halogen and N(R 9 )(R 10 ), wherein each of R 9 and R 10 are independently selected from H and hydrocarbyl groups.
52 . A compound according to claim 39 , wherein R 3 is selected from H and C 1 -C 10 alkyl groups.
53 . A compound according to claim 39 , wherein R 3 is —CH 3 .
54 . A compound according to claim 39 , having Formula VIII.
55 . A compound according to claim 39 , having Formula IX.
56 . A compound according to claim 39 , having Formula X.
57 . A compound according to claim 39 , having Formula XI.
58 . A compound according to claim 39 , wherein R 3 is selected from O, hydrocarbyl, and N(R 9 ) wherein R 9 is selected from H and hydrocarbyl groups.
59 . A compound according to claim 39 , wherein R 3 is selected from O, C 1 -C 10 alkenyl groups, such as C 1 -C 6 alkenyl group, and C 1 -C 3 alkenyl group, NH and N—C 1 -C 10 alkyl groups, such as N—C 1 -C 6 alkyl group, and N—C 1 -C 3 alkyl group.
60 . A compound according to claim 39 , wherein R 4 is selected from H and C 1 -C 10 alkyl groups, such as C 1 -C 6 alkyl group, and C 1 -C 3 alkyl group.
61 . A compound according to claim 39 , wherein R 4 is H.
62 . A compound according to claim 39 , wherein R 4 is a group of the formula
63 . A compound according to claim 39 , wherein R 5 is a substituted ring.
64 . A compound according to claim 39 , wherein R 5 is a carbocyclic ring.
65 . A compound according to claim 39 , wherein R 5 is a six-membered ring.
66 . A compound according to claim 39 , wherein R 5 is an aryl ring.
67 . A compound according to claim 39 , wherein R 5 is a group having the formula
wherein each of R 11 , R 12 , R 13 , R 14 and R 15 are independently selected from H, halogen, and hydrocarbyl groups.
68 . A compound according to claim 67 wherein each of R 11 , R 12 , R 13 , R 14 and R 15 are independently selected from H, halogen, alkyl, phenyl, O-alkyl, O-phenyl, nitrile, haloalkyl, carboxyalkyl, —CO 2 H, CO 2 alkyl, and NH-acetyl groups.
69 . A pharmaceutical composition comprising a compound according to claim 39 , optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant.
70 . A compound according to claim 39 , for use in medicine.
71 . A method of providing therapy for a condition or disease associated with 11β-HSD, comprising administering a compound of claim 39 to a mammal.
72 . A method according to claim 71 , wherein the condition or disease is selected from the group consisting of metabolic disorders such as diabetes and obesity; cardiovascular disorders such as hypertension; glaucoma; inflammatory disorders such as arthritis or asthma; immune disorders; bone disorders such as osteoporosis; cancer, intra-uterine growth retardation; apparent mineralocorticoid excess syndrome (AME); polycystic ovary syndrome (PCOS); hirsutism; acne; oligo- or amenorrhea; adrenal cortical adenoma and carcinoma; Cushing's syndrome; pituitary tumours; invasive carcinomas; breast cancer; and endometrial cancer.
73 . A method according to claim 71 , further comprising manufacturing a medicament for use in the therapy of a condition or disease associated with adverse 11β-HSD levels, comprising administering a compound of claim 39 to a mammal.
74 . A method according to claim 71 , further comprising manufacturing a pharmaceutical capable of modulating 11β-HSD activity, comprising administering a compound of claim 39 to a mammal.
75 . A method according to claim 71 , further comprising manufacturing a pharmaceutical capable of inhibiting 11β-HSD activity, comprising administering a compound of claim 39 to a mammal.
76 . A method comprising:
(a) performing a 11β-HSD assay with one or more candidate compounds having the formula as defined in claim 39 ; (b) determining whether one or more of said candidate compounds is/are capable of inhibiting 11β-HSD activity, and (c) selecting one or more of said candidate compounds that is/are capable of modulating 11β-HSD activity.
77 . A method comprising:
(a) performing a 11β-HSD assay with one or more candidate compounds having the formula as defined in claim 39 ; (b) determining whether one or more of said candidate compounds is/are capable of inhibiting 11β-HSD activity, and (c) selecting one or more of said candidate compounds that is/are capable of inhibiting 11β-HSD activity.
78 . A compound identified by the method according to claim 76 .
79 . A compound identified by the method according to claim 77 .
80 . A compound according to claim 78 for use in medicine.
81 . A compound according to claim 79 for use in medicine.
82 . A pharmaceutical composition comprising a compound according to claim 80 optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant.
83 . A pharmaceutical composition comprising a compound according to claim 81 optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant.
84 . A method comprising manufacturing a compound of claim 78 for use in the therapy of a condition or disease associated with 11β-HSD activity.
85 . A method comprising manufacturing a compound of claim 79 for use in the therapy of a condition or disease associated with 11β-HSD activity.
86 . A method according to claim 82 , wherein the condition or disease is selected from the group consisting of metabolic disorders such as diabetes and obesity; cardiovascular disorders such as hypertension; glaucoma; inflammatory disorders such as arthritis or asthma; immune disorders; bone disorders such as osteoporosis; cancer, intra-uterine growth retardation; apparent mineralocorticoid excess syndrome (AME); polycystic ovary syndrome (PCOS); hirsutism; acne; oligo- or amenorrhea; adrenal cortical adenoma and carcinoma; Cushing's syndrome; pituitary tumours; invasive carcinomas; breast cancer; and endometrial cancer.
87 . A method according to claim 84 , further comprising manufacturing a medicament for use in the therapy of a condition or disease associated with adverse 11β-HSD levels.
88 . A method according to claim 84 , wherein 11β-HSD is 11β-HSD Type 1.
89 . A method according to claim 84 , wherein 11β-HSD is 11β-HSD Type 2.
90 . A method according to claim 85 , further comprising manufacturing a medicament for use in the therapy of a condition or disease associated with adverse 11β-HSD levels.
91 . A method according to claim 85 , wherein 11β-HSD is 11β-HSD Type 1.
92 . A method according to claim 85 , wherein 11β-HSD is 11β-HSD Type 2.Cited by (0)
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