Back to results
US 2006/0235002 A1Published application
Novel physiologically active substance
AssigneesMercian Corporation, Eisai R&D Management Co., Ltd.
InventorsMitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
Life of this patent
Estimating the term…
Abstract
A compound represented by the following general formula (I): (I) wherein R7 and R21 are the same or different and each represents optionally substituted C2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.
Claims45
A compound represented by the formula (I):
- wherein R7 and R2, the same or different, represent
- 1) a C2 to C22 alkoxy group which may have a substituent,
- 2) an unsaturated C2 to C22 alkoxy group which may have a substituent,
- 3) a C7 to C22 aralkyloxy group which may have a substituent,
- 4) a 5-membered to 14-membered heteroaralkyloxy group which may have a substituent,
- 5) RC(═Y)—O—, wherein Y represents an oxygen atom or sulfur atom, and R represents
- a) a hydrogen atom,
- b) a C2 to C22 alkyl group which may have a substituent,
- c) an unsaturated C2 to C22 alkyl group which may have a substituent,
- d) a C6 to C14 aryl group which may have a substituent,
- e) a 5-membered to 14-membered heteroaryl group which may have a substituent,
- f) a C7 to C22 aralkyl group which may have a substituent,
- g) a 5-membered to 14-membered heteroaralkyl group which may have a substituent,
- h) a C1 to C22 alkoxy group which may have a substituent,
- i) an unsaturated C2 to C22 alkoxy group which may have a substituent,
- j) a C6 to C14 aryloxy group which may have a substituent,
- k) a C3 to C14 cycloalkyl group which may have a substituent,
- l) a 3-membered to 14-membered non-aromatic heterocyclic group which may have a substituent or
- m) a 5-membered to 14-membered heteroaryloxy group which may have a substituent,
- 6) RS1RS2RS3SiO—, wherein RS1, RS2 and RS3, the same or different, represent
- a) a C1 to C6 alkyl group or
- b) a C6 to C14 aryl group,
- 7) a halogen atom,
- 8) RN1RN2N—RM—, wherein RM represents
- a) a single bond,
- b) —CO—O—,
- c) —SO2—O—,
- d) —CS—O— or
- e) —CO—NRN3—, wherein RN3 represents a hydrogen atom or a C1 to C6 alkyl group which may have a substituent, provided that, the leftmost bond in b) to e) is bonded to the nitrogen atom, and
- RN1 and RN2, the same or different, represent
- a) a hydrogen atom,
- b) a C1 to C22 alkyl group which may have a substituent,
- c) an unsaturated C2 to C22 alkyl group which may have a substituent,
- d) an aliphatic C2 to C22 acyl group which may have a substituent,
- e) an aromatic C7 to C15 acyl group which may have a substituent,
- f) a C6 to C14 aryl group which may have a substituent,
- g) a 5-membered to 14-membered heteroaryl group which may have a substituent,
- h) a C7 to C22 aralkyl group which may have a substituent,
- i) a C1 to C22 alkylsulfonyl group which may have a substituent,
- j) a C6 to C14 arylsulfonyl group which may have a substituent,
- k) a 3-membered to 14-membered non-aromatic heterocyclic group formed by RN1 and RN2 together in combination with the nitrogen atom to which RN1 and RN2 are bonded, wherein the 3-membered to 14-membered non-aromatic heterocyclic group may have a substituent,
- l) a 5-membered to 14-membered heteroaralkyl group which may have a substituent,
- m) a C3 to C14 cycloalkyl group which may have a substituent or
- n) a 3-membered to 14-membered non-aromatic heterocyclic group which may have a substituent,
- 9) RN4SO2—O—, wherein RN4 represents
- a) a C1 to C22 alkyl group which may have a substituent,
- b) a C6 to C14 aryl group which may have a substituent,
- c) a C1 to C22 alkoxy group which may have a substituent,
- d) an unsaturated C2 to C22 alkoxy group which may have a substituent,
- e) a C6 to C14 aryloxy group which may have a substituent,
- f) a 5-membered to 14-membered heteroaryloxy group which may have a substituent,
- g) a C7 to C22 aralkyloxy group which may have a substituent or
- h) a 5-membered to 14-membered heteroaralkyloxy group which may have a substituent,
- 10) (RN5O)2PO—O—, wherein RN5 represents
- a) a C1 to C22 alkyl group which may have a substituent,
- b) an unsaturated C2 to C22 alkyl group which may have a substituent,
- c) a C6 to C14 aryl group which may have a substituent,
- d) a 5-membered to 14-membered heteroaryl group which may have a substituent,
- e) a C7 to C22 aralkyl group which may have a substituent or
- f) a 5-membered to 14-membered heteroaralkyl group which may have a substituent,
- 11) (RN1RN2N)2PO—O—, wherein RN1 and RN2 are the same as defined above or
- 12) (RN1RN2N)(RN5O)PO—O—, wherein RN1, RN2 and RN5 are the same as defined above;
- or a pharmacologically acceptable salt thereof, or a hydrate of those.
60 more elements
Dependencies are inferred from the claim text.