2-alkylidene-19-nor-vitamin d compounds
Abstract
The invention provides a new class of compounds related to vitamin D, that is, derivatives of 2-alkylidene-19-norvitamin D, as well as a general procedure for their chemical synthesis. The compounds have the formula (I) * formula * in which Y {sub, 1} and Y {sub, 2}, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy protecting group , R {sub, 6} and R {sub, 8}, which can represent the group - {(} CH {sub, 2} {{sub, x} -, where x is an integer from 2 to 5, and representing the R groups any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and high bone calcium mobilization activity, resulting in new therapeutic agents for the treatment of diseases in which bone formation is desired, particularly in osteoporosis of low bone turnover. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and in inducing their differentiation to monocytes, thus evidencing their use as anticancer agents and for the treatment of diseases such as psoriasis.

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Projected expiry passed 11 February 2018, 8.6 years ago.
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2 sheets
Sheet 1 Sheet 2
54 members in 16 offices
Priority claims5
| Document | Office | Kind | Date |
|---|---|---|---|
| 19970819693 | United States of America | – | |
| 81969397 | United States of America | A | |
| 81969397 | United States of America | A | |
| 819693 | – | – | – |
| US19970819693 | – | – | – |
Members54
| Document | Office | Kind | |
|---|---|---|---|
| CA2283829A1 | Canada | A1 | |
| WO9841501A1 | World Intellectual Property Organization (WIPO) | A1 | |
| AU6280198A | Australia | A | |
| US5843928A | United States of America | A | |
| US5936133A | United States of America | A | |
| NO994398D0 | Norway | D0 | |
| NO994398L | Norway | L | |
| AU714253B2 | Australia | B2 | |
| EP0970047A1 | European Patent Office (EPO) | A1 | |
| NZ337503A | New Zealand | A | |
| KR20000076306A | Republic of Korea | A | |
| JP2001504135A | Japan | A | |
| CA2404548A1 | Canada | A1 | |
| WO0174766A1 | World Intellectual Property Organization (WIPO) | A1 | |
| AU4790501A | Australia | A | |
| US6392071B1 | United States of America | B1 | |
| US2002087015A1 | United States of America | A1 | |
| EP0970047B1 | European Patent Office (EPO) | B1 | |
| AT223890T | Austria | T | |
| ATE223890T1 | Austria | T1 | |
| DE69807852D1 | Germany | D1 | |
| DK0970047T3 | Denmark | T3 | |
| KR20020091167A | Republic of Korea | A | |
| EP1268416A1 | European Patent Office (EPO) | A1 | |
| ES2179451T3This record | Spain | T3 | |
| PT970047E | Portugal | E | |
| US6537981B2 | United States of America | B2 | |
| IL152020D0 | Israel | D0 | |
| KR100380914B1 | Republic of Korea | B1 | |
| US2003181427A1 | United States of America | A1 | |
| JP2003529581A | Japan | A | |
| US6696431B2 | United States of America | B2 | |
| MXPA02009590A | Mexico | A | |
| US2004167104A1 | United States of America | A1 | |
| NZ522160A | New Zealand | A | |
| AU2001247905B2 | Australia | B2 | |
| JP2006117680A | Japan | A | |
| JP3786713B2 | Japan | B2 | |
| CA2283829C | Canada | C | |
| US7094774B2 | United States of America | B2 | |
| NO322535B1 | Norway | B1 | |
| EP1268416B1 | European Patent Office (EPO) | B1 | |
| AT374178T | Austria | T | |
| ATE374178T1 | Austria | T1 | |
| DE60130640D1 | Germany | D1 | |
| JP4022071B2 | Japan | B2 | |
| JP4035144B2 | Japan | B2 | |
| DK1268416T3 | Denmark | T3 | |
| ES2291305T3 | Spain | T3 | |
| IL152020A | Israel | A | |
| DE60130640T2 | Germany | T2 | |
| US2009143342A1 | United States of America | A1 | |
| CA2404548C | Canada | C | |
| DE69807852T2 | Germany | T2 |
Numbers
- Publication
- 2179451
- Publication, DOCDB
- 2179451
- Publication, EPODOC
- ES2179451T
- Application
- 98905102
- Application, DOCDB
- 98905102
- Application, EPODOC
- ES19980905102T
Titles2
- Spanish
- COMPUESTOS DE 2-ALQUILIDEN-19-NOR-VITAMINA D.
- English
- COMPOUNDS OF 2-ALQUILIDEN-19-NOR-VITAMINA D.
Classification
- CPC, 20
- C07C401/00
- Y02P20/55
- C07F7/1804
- A61P11/06
- A61P17/00
- A61P17/06
- A61P17/10
- A61P17/14
- A61P17/16
- A61P19/02
- A61P19/08
- A61P19/10
- A61P29/00
- A61P3/02
- A61P35/00
- A61P37/02
- A61P37/04
- A61P37/06
- A61P9/12
- A61P3/10
- IPC, 11
- A61K31 593
- A61P19 08
- A61P19 10
- C07C35 17
- C07C49 743
- C07C69 732
- C07C69 757
- C07C401 00
- C07F7 18
- C07F9 53
- C07F19 00