Nova Patents
TWI242560B

Prostaglandin agonists useful for the treatment of bone disorders and pharmaceutical compositions containing them

Abstract

The present invention relates to a prostaglandin motivator, a method of using the prostaglandin motivator, a pharmaceutical composition containing the prostaglandin motivator, and a tool set containing the prostaglandin motivator. This prostaglandin agonist is used to treat bone disorders including osteoporosis.

TWI242560B, drawing sheet 1
Sheet 1 of 52

Term

No projected expiry on record.

  1. Priority
  2. Filed
  3. Granted
  4. Today

10 claims: 10 independent, 0 dependent

  1. 1
    A compound represented by formula IOr a pharmaceutically acceptable salt thereof, wherein B is N;A is (C1-C6) Alkyl, or (C3-C7)Cycloalkyl (C1-C6) Alkyl, the A part can be optionally substituted with a hydroxyl group or a halogen group on the carbon to form a mono-, di- or tri-substituent;Q is -(C4-C8)Alkylene-or-(C1-C5) Alkylene-X-;X is thienyl or furyl;Z is carboxy;K is (C1-C8) Alkylene;M is -Ar where Ar is phenylbenzo[b]furanyl or 2,3-dihydrobenzo[1,4]diooctyl;the Ar part can be optionally on the carbon Is selected from R1Is substituted by the substituents, where R1Is halo or (C1-C6) Alkyl, the (C1-C6) The alkyl group can be optionally substituted with a hydroxyl group. 一種由式I代表之化合物 或其藥學可接受的鹽類，其中B是N;A是(C1-C6)烷醯基，或(C3-C7)環烷基(C1-C6)烷醯基，該A部份可選擇性的在碳上分別以羥基或鹵基取代成單-，二-或三-取代基;Q是-(C4-C8)伸烷基-或-(C1-C5)伸烷基-X-;X是噻吩基或呋喃基；Z是羧基；K是(C1-C8)伸烷基；M是-Ar其中Ar為苯基苯並[b]呋喃基、或2,3-二氫苯並[1,4]戴奧辛基；該Ar部份可選擇性的在碳上為選自R1之取代基所取代，其中R1為鹵基或(C1-C6)烷基，該(C1-C6)烷基可選擇性地為羥基所取代。
  2. 2
    For example, the compound of item 1 in the scope of patent application, where A is (C1-C6) Alkyl, the (C1-C6) Alkyl groups can be selectively substituted with halogen groups on carbon to mono-, di- or tri-substituents;Q is -(C4-C8)Alkylene-or-(C1-C5) Alkylene-X-;K is methylene or ethylene;R1Is a chloro group, a fluoro group, or (C1-C4) Alkyl, the (C1-C4) Alkyl groups can be optionally substituted by hydroxyl groups 如申請專利範圍第1項之化合物，其中A是(C1-C6)烷醯基，該(C1-C6)烷醯基可在碳上各自以鹵基選擇性的取代成單-、二-或三-取代基；Q是-(C4-C8)伸烷基-或-(C1-C5)伸烷基-X-；K是亞甲基或亞乙基；R1為氯基、氟基、或(C1-C4)烷基，該(C1-C4)烷基可選擇性地為羥基所取代
  3. 3
    For example, the compound of item 1 in the scope of patent application, where A is (C1-C6) Alkyl, the (C1-C6) Alkyl groups can optionally be substituted with hydroxyl or halo groups to form mono-, di- or tri-substituents on carbon;K is methylene;Q is -(C4-C8)Alkylene-or-(C1-C5) Alkylene -X-;M is -Ar, and -Ar is phenyl, where -Ar is R1Replaced;R1As (C1-C6) An alkyl group, which can be optionally substituted by a hydroxyl group. 如申請專利範圍第1項之化合物，其中A是(C1-C6)烷醯基，該(C1-C6)烷醯基可選擇性的在碳上各自以羥基或鹵基取代成單-、二-或三-取代基；K是亞甲基；Q是-(C4-C8)伸烷基-或-(C1-C5)伸烷基-X-；M是-Ar，且-Ar為苯基，其中-Ar為R1所取代；R1為(C1-C6)烷基，其可選擇性地為羥基所取代。
  4. 4
    For example, the compound of item 1 in the scope of patent application, where A is (C1-C6) Alkyl, the (C1-C6) Alkyl groups can be optionally substituted with halogen groups on carbon to mono-, di- or tri-substituents;K is (C1-C8) Alkylene;Q is -(C4-C8)Alkylene-or-(C1-C5) Alkylene -X-;M is -Ar, and -AT is phenyl, benzofuranyl, or 2,3-dihydrobenzo[1,4]dioctyl;and R1Is halo or (C1-C6)alkyl. 如申請專利範圍第1項之化合物，其中A是(C1-C6)烷醯基，該(C1-C6)烷醯基可選擇性的在碳上各自以鹵基取代成單-、二-或三-取代基；K是(C1-C8)伸烷基；Q是 -(C4-C8)伸烷基-或 -(C1-C5)伸烷基-X-;M是-Ar，且-AT為苯基、苯並呋喃基、或2,3-二氫苯並[1,4]戴奧辛基；及R1為鹵基或(C1-C6)烷基。
  5. 5
    For example, the compound of item 1 in the scope of patent application, where A is (C3-C6) Alkyl, the (C3-C6) Alkyl can be optionally substituted with halo on carbon to become mono-, di- or tri-substituent;K is (C3-C8) Alkylene,;Q is -(C4-C8) Alkylene-, or-(C1-C5) Alkylene -X-;M is -Ar, and -Ar is phenyl;and R1Is halo or (C1-C6)alkyl. 如申請專利範圍第1項之化合物，其中A是(C3-C6)烷醯基，該(C3-C6)烷醯基可在碳上選擇性的以鹵基取代成為單-,雙-或三-取代基；K是(C3-C8)伸烷基，；Q是 -(C4-C8)伸烷基-，或-(C1-C5)伸烷基-X-;M是-Ar，且-Ar為苯基；而R1為鹵基或(C1-C6)烷基。
  6. 6
    Such as the compound of item 2 in the scope of the patent application, wherein A is propionyl;Q is n-hexylene;Z is carboxy;K is methylene;and M is 4-(n-1-hydroxyhexyl)phenyl. 如申請專利範圍第2項之化合物，其中A是丙醯基；Q是n-伸己基；Z是羧基；K是亞甲基；及M是4-(n-1-羥基己基)苯基。
  7. 7
    A medicinal composition for treating osteoporosis, fractures or low-bone disorders or for increasing bone mass, which comprises an effective amount of the compound of the first item in the scope of the patent application, or a pharmaceutically acceptable salt thereof, and a pharmacologically acceptable Accepted carrier. 一種用於治療骨質疏鬆症、骨折或低骨質病症或用於增加骨質之醫藥組成物，其包含有效量的申請專利範圍第1項之化合物、或其藥學可接受的鹽類，及一種藥學可接受的載體。
  8. 8
    For example, the pharmaceutical composition of item 7 of the scope of patent application is used for treating osteoporosis, wherein the effective amount is the amount for treating osteoporosis. 如申請專利範圍第7項之醫藥組成物，其係用於治療骨質疏鬆症，其中該有效量為治療骨質疏鬆症之量。
  9. 9
    For example, the pharmaceutical composition of item 7 of the scope of patent application is used to increase bone mass, wherein the effective amount is an amount that can increase bone mass. 如申請專利範圍第7項之醫藥組成物，其係用於增加骨質，其中該有效量為可增加骨質之量。
  10. 10
    For example, the pharmaceutical composition of item 7 of the scope of patent application is used for treating fractures, wherein the effective amount is the amount for treating fractures. 如申請專利範圍第7項之醫藥組成物，其係用於治療骨折，其中該有效量為治療骨折之量。
Independent claims10