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(12) Patent Application Publication (10) Pub. No.: US 2004/0152713 A1 Petrie (43) Pub

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(12) Patent Application Publication (10) Pub. No.: US 2004/0152713 A1 Petrie (43) Pub US 2004O152713A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0152713 A1 Petrie (43) Pub. Date: Aug. 5, 2004 (54) METHODS FORTREATING JOINT PAIN OR (52) U.S. Cl. ...................... 514/266.2, 514/310; 514/314; IMPROVING SLEEP USING AN ESTROGEN 514/256 AGONISTIANTAGONIST (57) ABSTRACT (75) Inventor: Charles D. Petrie, Cranston, RI (US) The present invention provides methods, pharmaceutical Correspondence Address: compositions and kits for treating joint pain and/or improv PFIZER INC. ing sleep using a SERM of formula (I): PATENT DEPARTMENT, MS8260-1611 EASTERN POINT ROAD GROTON, CT 06340 (US) (I) (73) Assignee: Pfizer Inc. (21) Appl. No.: 10/761,672 (22) Filed: Jan. 21, 2004 Related U.S. Application Data (60) Provisional application No. 60/441,830, filed on Jan. 22, 2003. Publication Classification wherein the variables A, B, D, E, e, G, Y and Z are as (51) Int. Cl.' .................... A61K 31/517; A61K 31/4709 defined in the Specification. US 2004/0152713 A1 Aug. 5, 2004 METHODS FOR TREATING JOINT PAIN OR ceSS is associated with changes to an individual's circadian IMPROVING SLEEP USING AN ESTROGEN and diurnal rhythms. With increasing age the total amount of AGONISTIANTAGONIST Sleep tends to shorten and the amount of deep sleep can decrease or disappear. Sleep may become more fragmented FIELD OF THE INVENTION and interrupted for the elderly and these changes with timing 0001. This invention relates to methods for treating joint and Structure of Sleep are often associated with Significant pain and/or improving sleep using an estrogen agonist/ morbidity. Similarly, non-elderly individuals may also antagonist also known as Selective estrogen receptor modu exhibit disturbances in the normal Sleep process. These lators (hereinafter referred to as SERMs). The invention also disturbances in the normal Sleep process have been corre relates to pharmaceutical compositions useful for improving lated with more frequent napping, decreased daytime alert Sleep. neSS and declining intellectual function and cognitive ability. 0006 For individuals suffering from a sleep disorder the BACKGROUND OF THE INVENTION normal Sleep cycle is also disrupted. The Sleep disorder 0002 Almost all persons by age forty have some patho generally affects the afflicted individual’s ability to fall logical change in weight bearing joints. Men and women are and/or stay asleep, and involve Sleeping too little, Sleeping equally affected, but onset is earlier in men. Joint cartilage, too much or resulting in abnormal behavior associated with also called hyaline cartilage, is made up of 95% water and Sleep. There are numerous types of Sleep disorders with the extracellular matrix and 5% chondrocytes. The extracellular International Classification of Sleep Disorders having over matrix comprises proteoglycans and Type II collagen. Joint Seventy Sleep disorders listed. Sleep disorders, Such as pain can result from various progressive diseases as well as various types of dySSomnias and parasomnias, can lead to a various acute conditions related to the joints. Typical Symp lowered quality of life and reduced personal health for those tomatic treatment of joint pain includes the management of afflicted with them. Sleep disorders can also endanger public pain by administration of medicaments and changes in Safety by contributing to traffic and industrial accidents. In lifestyle Such as diet and exercise. certain instances the sleep disorder can be life threatening. 0.003 Examples of compounds that have been used to 0007 Examples of current drugs used to improve sleep treat joint pain include nonsteroidal anti-inflammatory drugs include those that act as hypnotic Sedatives and that may also (NSAIDs), Such as aspirin, acetominophen, ibuprofen, act as anxiolytics. BenZodiazepines, which act as anxiolytics naproxen, ketoprofen, nabumetone, etodolac, Salsalate, and are also useful for inducing Sleep, enhance the effect of Sulindac, diclofenac, tolmetin, flurbiprofen, piroXicam, the inhibitory neurotransmitter gamma-aminobutyric acid fenoprofen, indomethacin, meclofenamate, Oxaprozin, (GABA). Benzodiazepines, Such as diazepam (Valium(E)) diflunisal and ketorolac, and Selective cyclooxygenase-2 and temazepam (RestorilE), are used as sleeping pills. (COX-2) inhibitors such as 4-5-(4-methylphenyl)-3-(trif Triazolam and estazolam are also used to induce Sleep. luoromethyl)-1H-pyrazol-1-ylbenzenesulfonamide (cele Zolpidem, including its tartrate Salt, is used to induce Sleep coxib), 4-4-(methylsulfonyl)phenyl)-3-phenyl-2(5H)-fura and acts by a mechanism similar to the benzodiazepines. none (rofecoxib), Valdecoxib and etoricoxib. NSAIDs can Over the counter remedies used to induce Sleep include have unwanted side effects Such as ulcers, therefore NSAIDs preparations containing antihistamines, Such as diphenhy are Sometimes administered with other compounds that dramine. Sedative antidepressants Such as amitryptyline and ameliorate the side effects of the NSAIDs. Typical com traZodone have also been used as Sleep inducing agents. pounds that are used in combination with NSAIDs include Dopaminergic agents Such as levodopa/carbidopa, bro proton pump inhibitorS Such as omeprazole; antacids Such as mocriptine meSylate and pergolide, and opiods Such as Sucralfate; and H2 blockerS Such as ranitidine, cimetidine, codeine, propoxyphene, oxycodone, pentazocrine, hydroc famotidine, and nizatidine. In addition, products derived odone and methadone have also been used as Sleep inducing from natural Substances have been used to treat various agents. The known therapeutic regimens Suffer from numer types of joint pain. Examples of natural Substances include ous problems, including residual effects in daytime function, hyaluronic acid, glucosamine, chondroitin Sulfate and cap impairment of memory, potential for addiction or rebound Saicin. Intraarticular corticosteriods have also been used to insomnia which may be associated with increased dream treat joint pain. intensity and the occurrence of nightmares and the like. There is a continuing need for new methods of improving 0004) The use of SERMs, such as those of formula I, for Sleep in patients in need thereof. the treatment of osteoarthritis has been disclosed in U.S. patent application Publication No. 2001-0041718A1. The 0008. It has been found that the SERMs of Formula (I), use of SERMs, such as those of formula I, for the treatment described hereinafter, are useful in the treatment of joint pain of rheumatoid arthritis has been disclosed in U.S. patent and/or in improving Sleep. The present invention provides application Publication No. 2002-0049198A1. There is a methods of treating or preventing joint pain and/or improv continuing need for new methods of treating joint pain in ing sleep using a SERM of Formula (I). patients Suffering from or at risk of Suffering from joint pain. SUMMARY OF THE INVENTION 0005 Sleep is a complex process with many parts of the nervous System being involved in controlling it and influ 0009. The present invention provides methods of treating encing its different Stages. The Stages or levels of Sleep joint pain and/or improving sleep, the methods comprising include drowsiness, light sleep, deep sleep and dream Sleep. administering to a patient in need thereof, a therapeutically Individuals vary widely in their requirements for Sleep, effective amount of a SERM. A first embodiment of the which is influenced by a variety of factors including the present invention is the method of treating joint pain and/or individual's current emotional State. The natural aging pro improving Sleep, the method comprising administering to a US 2004/0152713 A1 Aug. 5, 2004 patient in need thereof, a therapeutically effective amount of 0027) G is a SERM of formula (I): 0028) (a)-NR'R'; (I) (b)b y CH2)m- \ -N 72 V 0029 wherein n is 0, 1 or 2; m is 1, 2 or 3; Z is -NH-, -O-, -S-, or -CH2-, optionally fused on adjacent carbon atoms with one or two phenyl rings and, optionally independently substituted on carbon with one to three sub Stituents and, optionally, independently on nitrogen with a chemically suitable substituent selected from R"; or 0030) (c) a bicyclic amine containing five to 0010) wherein: twelve carbon atoms, either bridged or fused and 0.011) A is selected from CH and NR; optionally substituted with 1-3 substituents inde 0012 B, D and E are independently selected from pendently selected from R"; or CH and N: 0031 Z' and G in combination may be 0013 Y is 0014 (a) phenyl, optionally substituted with 1-3 R2 Substituents independently selected from R"; 0015 (b) naphthyl, optionally substituted with 1-3 substituents independently selected from R"; 0016 (c) C-C cycloalkyl, optionally substituted with 1-2 substituents independently selected from R; 0032) W is 0017 (d) C-C cycloalkenyl, optionally substi 0033) (a) -CH-; tuted with 1-2 substituents independently selected 0034 (b) -CH=CH-; from R"; 0035) (c) -O-; 0018 (e) a five membered heterocycle containing up to two heteroatoms Selected from the group 0036) (d) -NR-; consisting of -O-, -NR- and -SO), , 0037 (e) -S(O) ; optionally substituted with 1-3 substituents inde pendently selected from R"; 0019 (f) a six membered heterocycle containing (f) O| up to two heteroatoms Selected from the group consisting of -O-, -NR- and -SO), optionally substituted with 1-3 substituents inde pendently selected from R"; or 0038 (g) –CR(OH)–: 0020 (g) a bicyclic ring system consisting of a 0039) (h)-CONR-; five or six membered heterocyclic ring fused to a
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