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 Title: |
US5817689:
Indole derivatives having a 2-phenyl-ethanolamino-substituted lower alkyl group at the 2-or 3-position thereof
[ Derwent Title ]
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| Country: |
US United States of America
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| Inventor: |
Kato, Shiro; Sakai, Japan
Harada, Hiroshi; Suita, Japan
Hirokawa, Yoshimi; Ikoma, Japan
Yoshida, Naoyuki; Sakai, Japan
Kawashima, Hitoshi; Osaka, Japan
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| Assignee: |
Dainippon Pharmaceutical Co., Ltd., Osaka, Japan
other patents from DAINIPPON PHARMACEUTICAL CO. LTD. (133415) (approx. 145)
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| Published / Filed: |
1998-10-06
/ 1997-05-29
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| Application Number: |
US1997000836983
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| IPC Code: |
Advanced:
A61K 31/40;
A61K 31/404;
C07D 209/14;
C07D 209/24;
C07D 209/30;
Core:
A61K 31/403;
C07D 209/00;
more...
IPC-7:
A61K 31/40;
C07D 209/14;
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| ECLA Code: |
C07D209/14; M07D209/14;
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| U.S. Class: |
Current:
514/415;
514/411;
514/866;
514/909;
548/431;
548/506;
Original:
514/415;
514/411;
514/866;
514/909;
548/431;
548/506;
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| Field of Search: |
548/506,431
514/411,415
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| Priority Number: |
| 1994-11-29 |
JP1994000321402 |
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| Abstract: |
PCT No. PCT/JP95/02400 Sec. 371 Date May 29, 1997 Sec. 102(e) Date May 29, 1997 PCT Filed Nov. 27, 1995 PCT Pub. No. WO96/16938 PCT Pub. Date Jun. 6, 1996An indole derivative of the formula: <IMAGE>l-lower alkoxy, carboxy-lower alkoxy, lower alkoxycarbonyl, phenyl-lower alkoxy, lower alkyl being optionally substituted by hydroxy, di-lower alkylaminosulfonyl, etc., R2 is hydrogen, halogen, lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, etc., R3 is hydrogen or lower alkyl, R4 is halogen or trifluoromethyl, R5 is lower alkyl, or a salt thereof, these compounds being potent beta 3-adrenergic receptor-stimulating agent with excellent adrenoceptor selectivity, and being useful in the prophylaxis or treatment of obesity or diabetes mellitus.
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| Attorney, Agent or Firm: |
Foley & Lardner ;
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| Primary / Asst. Examiners: |
McKane, Joseph; Stockton, Laura L.
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| INPADOC Legal Status: |
Show legal status actions
Family Legal Status Report
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| Designated Country: |
AL AM AP BB BG BY EE GE IS KG KR KZ LK LR LT LV AT BE CH DE DK ES FR GB GR IE IT LI LU MC
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| Family: |
Show 43 known family members
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First Claim:
Show all 25 claims |
We claim:
1. An indole derivative of the formula [I]: [Figure] wherein R1 is a lower alkyl group being optionally substituted by a hydroxy group, a phenylsulfonylamino group, a lower alkylsulfonylamino group, a mono- or di-lower alkylaminosulfonyl group, or a group selected from the following (a) to (d), or combines with R2 to form a methylenedioxy group, said methylenedioxy group being optionally substituted by a carboxyl group or a lower alkoxycarbonyl group,
- (a) a group of the formula:--X--Ra (wherein X is O, S or NH, Ra is a hydrogen atom or a lower alkyl group, provided that when X is S, then Ra is a lower alkyl group);
- (b) a group of the formula: [Figure] Rb (wherein Rb is a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group or a carboxyl group, Rbb is a lower alkoxycarbonyl group or a carboxyl group, m is an integer of 0 to 3, and n is 0 or 1);
- (c) a group of the formula:--O(CH2)p --Rc (wherein Rc is a lower alkanoyl group, a hydroxy group, a cyano group, a phenyl group, a mono- or di-lower alkylaminocarbonyl group, or a group of the formula: [Figure] (wherein RA is a hydrogen atom or a lower alkyl group), and p is an integer of 1 to 4); and
- (d) a group of the formula:--Y--(CH2)q --Rd (wherein Y is NH or S, Rd is a carboxyl group or a lower alkoxycarbonyl group, and q is an integer of 1 to 4);
- R2 is a hydrogen atom, a halogen atom, a lower alkyl group being optionally substituted by a hydroxy group, a hydroxy group, a lower alkoxy group, or a group of the above (b) or (c), or combines with R1 to form a methylenedioxy group, said methylenedioxy group being optionally substituted by a carboxyl group or a lower alkoxycarbonyl group;
- R3 is a hydrogen atom or a lower alkyl group;
- W is a group of the formula [II] which bonds to the 2- or 3-position of the indole nucleus: [Figure] wherein R4 is a halogen atom or a trifluoromethyl group, and R5 is a lower alkyl group, or a salt thereof.
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| Background / Summary: |
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| Drawing Descriptions: |
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| Description: |
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| PCT Number: |
PCT/JP95/02400
WO9616938
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| PCT Pub./Filed Dates: |
1996-06-06 / 1995-11-27
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| § 371 / 102(e) Dates: |
1997-05-29 / 1997-05-29
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| Forward References: |
Show 4 U.S. patent(s) that reference this one
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| Foreign References: |
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| Other Abstract Info: |
CHEMABS 125(11)142550C
DERABS C96-277685
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| Other References: |
Bobzin et al., "Aromatic Alkaloids from the Marine Sponge Chelonaplysilla", J. Org. Chem., 56, 4403-4407 (1991).
(5 pages)
Cited by 5 patents
[ISI abstract]
Chemical Abstract, 78, 431, 71665s (1973).
Clifton et al., "Arylethanolamines Derived from Salicylamide with α-and β-Adrenoceptor Blocking Activities. Preparation of Lebetalol, Its Enantiomers, and Related Salicylamides", 25, 670-679 (1982).
(10 pages)
Cited by 19 patents
Jackman et al., "Some tryptamine derivatives: 1-aryloxy-3-[(2-indol-3'-ylethyl)amino]propan-2-ols", J. Pharm. Pharmacol., 17, 742-746 (1965).
Chemical Abstract, 96, 726, 142543k (1982).
Chemical Abstract, 109, 666, 128763n (1988).
Kato et al., CA 122:239540, May 8, 1995.
Patent Abstracts of Japan for JP 06345731, 1994.
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