Naphtholactams and lactones as bone morphogenetic protein active agents
First Claim
Patent Images
1. A compound of the formula:
- ##STR265## wherein Q is an optionally substituted carbon atom;
Y is an optionally substituted imino group;
Z1 ##STR266## Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo;
Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;
R1 and R2 taken together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; and
ring A is a benzene ring which may be substituted in addition to R1 and R2 ;
or a salt thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
A compound of the formula: wherein
Q is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;
Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;
Z1 is a C1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;
Z2 is an optionally substituted C1-3 alkylene group;
Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;
one of R1 and R2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;
the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; or
R1 and R2 taken together with adjacent --c═c-- form a ring; and
ring A is a benzene ring which may be substituted in addition to R1 and R2 ; or a salt thereof.
136 Citations
19 Claims
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1. A compound of the formula:
- ##STR265## wherein Q is an optionally substituted carbon atom;
Y is an optionally substituted imino group; Z1 ##STR266## Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 and R2 taken together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; andring A is a benzene ring which may be substituted in addition to R1 and R2 ; or a salt thereof. - View Dependent Claims (2, 13, 14)
- ##STR265## wherein Q is an optionally substituted carbon atom;
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3. A compound of the formula:
- ##STR267## wherein Q is CR4 wherein R4 is (i) a hydrogen atom, (ii) a halogen atom, (iii) an optionally substituted hydrocarbon group or (iv) an optionally substituted hydroxyl group;
X is C═
O;Y is NR5 wherein R5 is (i) a hydrogen atom, (ii) an optionally substituted hydrocarbon group or (iii) an acyl group; Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo; m and n each represent 0; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 and R2 together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; andring A is a benzene ring which may be substituted in addition to R1 and R2. - View Dependent Claims (4, 5, 6, 7, 8, 9, 10, 11, 12)
- ##STR267## wherein Q is CR4 wherein R4 is (i) a hydrogen atom, (ii) a halogen atom, (iii) an optionally substituted hydrocarbon group or (iv) an optionally substituted hydroxyl group;
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15. A process of enhancing cell differentiation inducing factor comprising administering to a patient in need thereof a compound of the formula:
- ##STR271## wherein Q is an optionally substituted carbon atom;
Y is an optionally substituted imino group; Z1 is ##STR272## Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; one of R1a and R2a is a hydrogen atom, an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group; the other of R1a and R2 is an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group;
orR1a and R2a together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; andring A is a benzene ring which may be substituted in addition to R1a and R2a ; or a salt thereof.
- ##STR271## wherein Q is an optionally substituted carbon atom;
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16. A method of treating or preventing neuropathy or bone-and-joint disease which comprises administering to a mammal in need thereof an effective amount of compound of the formula:
- ##STR273## wherein Q is an optionally substituted carbon atom;
Y is an optionally substituted imino group; Z1 ##STR274## Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; one of R1a and R2a is a hydrogen atom, an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group; the other of R1a and R2a is an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group;
orR1a and R2a together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; andring A is a benzene ring which may be which may be substituted in addition to R1a and R2a ; or a salt thereof.
- ##STR273## wherein Q is an optionally substituted carbon atom;
-
17. A process of treating or preventing neuropathy or bone-and-joint disease which comprises administering to a patient in need thereof a compound of the formula:
- ##STR275## wherein Q is an optionally substituted carbon atom;
Y is an optionally substituted imino group; Z1 ##STR276## Z2 is a C1-3 alkylene group optionally substituted by hydroxy or oxo; Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; one of R1a and R2a is a hydrogen atom, an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group; the other of R1a and R2a is an optionally substituted C1-6 alkyl group or an optionally substituted C1-6 alkoxy group;
orR1a and R2a together with adjacent --C═
C-- form a C1-6 alkyleneoxy or C1-6 alkylenedioxy group; andring A is a benzene ring which may be substituted in addition to R1a and R2a ; or a salt thereof. - View Dependent Claims (18, 19)
- ##STR275## wherein Q is an optionally substituted carbon atom;
Specification
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Current AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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Original AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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InventorsHazama, Masatoshi, Ogino, Masaki, Notoya, Kohei, Marui, Shogo
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Primary Examiner(s)Raymond, Richard L.
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Application NumberUS08/945,631Time in Patent Office852 DaysField of Search540/521, 540/522, 544/125, 544/126, 546/65, 546/110, 548/421, 548/423, 548/450, 548/451, 514/215, 514/217, 514/237.8, 514/287, 514/290, 514/410, 514/411US Class Current514/215CPC Class CodesA61K 31/4035 Isoindoles, e.g. phthalimideA61K 31/4741 condensed with ring systems...A61K 31/4745 condensed with ring systems...C07D 209/64 with an oxygen atom in posi...C07D 209/66 with oxygen atoms in positi...C07D 317/70 condensed with ring systems...C07D 401/04 directly linked by a ring-m...C07D 405/04 directly linked by a ring-m...C07D 471/04 Ortho-condensed systemsC07D 491/04 Ortho-condensed systems
