HRP20050334A2 - Halogenated selective androgen receptor modulators and methods of use thereof - Google Patents

Halogenated selective androgen receptor modulators and methods of use thereof

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Publication number
HRP20050334A2
HRP20050334A2 HR20050334A HRP20050334A HRP20050334A2 HR P20050334 A2 HRP20050334 A2 HR P20050334A2 HR 20050334 A HR20050334 A HR 20050334A HR P20050334 A HRP20050334 A HR P20050334A HR P20050334 A2 HRP20050334 A2 HR P20050334A2
Authority
HR
Croatia
Prior art keywords
androgen receptor
subject
selective androgen
methods
receptor modulators
Prior art date
Application number
HR20050334A
Inventor
T. Dalton James
Duane
Yin Donghua
He Yali
Mitchell
A. Veverka Karen
Original Assignee
University Of Tennessee Research Foundation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US10/270,732 external-priority patent/US6998500B2/en
Application filed by University Of Tennessee Research Foundation filed Critical University Of Tennessee Research Foundation
Publication of HRP20050334A2 publication Critical patent/HRP20050334A2/en

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
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    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/04—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C233/07—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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    • C07C335/16—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C335/18—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems

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  • Health & Medical Sciences (AREA)
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  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Reproductive Health (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
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  • Obesity (AREA)
  • Urology & Nephrology (AREA)
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  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

Selective androgen receptor modulator (SARM) compounds having the formula Ia: wherein X is O; T is OH, OR, -NHCOCH 3 , or NHCOR; Z is CN; Y is CF 3 , I, Br, Cl, CN, C(R) 3 or Sn(R) 3 ; or Z and Y together with the benzene ring to which they are attached form a fused bicyclic carbocyclic or heterocyclic ring system; Q is F, Cl, Br or I; R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, CH 2 F, CHF 2 , CF 3 , CF 2 CF 3 , aryl, phenyl, F, Cl, Br, I, alkenyl or OH; and R 1 is CH 3 , CH 2 F, CHF 2 , CF 3 , CH 2 CH 3 , or CF 2 CF 3 ; can be used in the treatment of osteoporosis, osteopenia, low bone mass, bone fragility, osteomalacia, or any combination thereof, a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, or a female subject having an Androgen Decline in Female (ADIF)-associated condition, in a subject.
HR20050334A 2002-10-16 2005-04-14 Halogenated selective androgen receptor modulators and methods of use thereof HRP20050334A2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10/270,732 US6998500B2 (en) 2000-08-24 2002-10-16 Selective androgen receptor modulators and methods of use thereof
US10/371,213 US7026500B2 (en) 2000-08-24 2003-02-24 Halogenated selective androgen receptor modulators and methods of use thereof
PCT/US2003/032507 WO2004035736A2 (en) 2002-10-16 2003-10-14 Halogenated selective androgen receptor modulators and methods of use thereof

Publications (1)

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HRP20050334A2 true HRP20050334A2 (en) 2005-12-31

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HR20050334A HRP20050334A2 (en) 2002-10-16 2005-04-14 Halogenated selective androgen receptor modulators and methods of use thereof
HR20070457A HRP20070457A2 (en) 2002-10-16 2007-10-01 Halogenated selective androgen receptor modulators and methods of use thereof

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US (1) US7026500B2 (en)
EP (3) EP2305636A1 (en)
JP (4) JP4764719B2 (en)
KR (3) KR101107031B1 (en)
CN (3) CN100999481A (en)
AT (1) ATE430125T1 (en)
AU (1) AU2003287074B2 (en)
BR (1) BR0314891A (en)
CA (3) CA2588083A1 (en)
CY (1) CY1109858T1 (en)
DE (1) DE60327456D1 (en)
DK (1) DK1558565T3 (en)
EA (2) EA011744B1 (en)
ES (1) ES2324606T3 (en)
GE (2) GEP20094820B (en)
HK (1) HK1080070A1 (en)
HR (2) HRP20050334A2 (en)
IL (2) IL182880A0 (en)
MX (1) MXPA05004076A (en)
PT (1) PT1558565E (en)
SI (1) SI1558565T1 (en)
TW (1) TWI332955B (en)
WO (1) WO2004035736A2 (en)

Families Citing this family (82)

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US7759520B2 (en) * 1996-11-27 2010-07-20 University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
US7622503B2 (en) 2000-08-24 2009-11-24 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
US20070173546A1 (en) * 2000-08-24 2007-07-26 Dalton James T Selective androgen receptor modulators and method of use thereof
US7855229B2 (en) * 2000-08-24 2010-12-21 University Of Tennessee Research Foundation Treating wasting disorders with selective androgen receptor modulators
US20030232792A1 (en) * 2000-08-24 2003-12-18 Dalton James T. Selective androgen receptor modulators and methods of use thereof
US8445534B2 (en) 2000-08-24 2013-05-21 University Of Tennessee Research Foundation Treating androgen decline in aging male (ADAM)-associated conditions with SARMs
US7919647B2 (en) 2000-08-24 2011-04-05 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
US7645898B2 (en) * 2000-08-24 2010-01-12 University Of Tennessee Research Foundation Selective androgen receptor modulators and method of use thereof
US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US8853266B2 (en) * 2001-12-06 2014-10-07 University Of Tennessee Research Foundation Selective androgen receptor modulators for treating diabetes
US20070161608A1 (en) * 2001-12-06 2007-07-12 Dalton James T Selective androgen receptor modulators for treating muscle wasting
PT1463497E (en) * 2001-12-06 2011-12-20 Gtx Inc Treating muscle wasting with selective androgen receptor modulators
US7772433B2 (en) * 2002-02-28 2010-08-10 University Of Tennessee Research Foundation SARMS and method of use thereof
US20040197928A1 (en) * 2002-10-15 2004-10-07 Dalton James T. Method for detecting selective androgen receptor modulators
AU2003287077B2 (en) * 2002-10-15 2007-09-20 University Of Tennessee Research Foundation Methylene-bridged selective androgen receptor modulators and methods of use thereof
EP1558233A2 (en) * 2002-10-16 2005-08-03 GTX, Inc. Treating androgen decline in aging male (adam)-associated conditions with sarms
US20060276539A1 (en) * 2002-10-16 2006-12-07 Dalton James T Treating Androgen Decline in Aging Male (ADAM)- associated conditions with SARMS
US8309603B2 (en) 2004-06-07 2012-11-13 University Of Tennessee Research Foundation SARMs and method of use thereof
EP1592658B1 (en) * 2003-01-13 2013-04-24 University of Tennessee Research Foundation Large-scale synthesis of selective androgen receptor modulators
EP1594490A4 (en) * 2003-01-22 2006-03-22 Gtx Inc Treating androgen deficiency in female (adif)-associated conditions with sarms
FI20030958A0 (en) * 2003-06-27 2003-06-27 Orion Corp New compounds
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