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(12) Patent Application Publication (10) Pub. No.: US 2010/0267821 A1 Terauchi Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2010/0267821 A1 Terauchi Et Al US 2010O267821A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0267821 A1 Terauchi et al. (43) Pub. Date: Oct. 21, 2010 (54) PROPHYLACTIC OR THERAPEUTICAGENT Publication Classification FOR RRTABLE BOWEL, SYNDROME (51) Int. Cl. A6II 3/343 (2006.01) (75) Inventors: Jun Terauchi, Osaka-Shi (JP); C07D 307/77 (2006.01) Fumihiko Sato, Osaka-shi (JP); A6IPI/00 (2006.01) Nobuhiro Inatomi, Osaka-shi (JP) (52) U.S. Cl. ......................................... 514/468; 549/458 (57) ABSTRACT Correspondence Address: The present invention provides a prophylactic or therapeutic EDWARDS ANGELL PALMER & DODGE LLP agent for irritable bowel syndrome, which comprises a com P.O. BOX SS874 pound represented by formula (I): BOSTON, MA 02205 (US) R2 (73) Assignee: Takeda Pharmaceutical Company Limited, Osaka-Shi (JP) A cí6. (21) Appl. No.: 12/826,473 O Y. O (22) Filed: Jun. 29, 2010 X wherein, R' represents an optionally substituted hydrocarbon group, etc., R represents a hydrogen atom or an optionally Related U.S. Application Data substituted hydrocarbon group, R represents a hydrogen (63) Continuation of application No. 12/225,269, filed on atom, an optionally substituted hydrocarbon group, etc., X Sep. 17, 2008, now abandoned, filed as application No. represents CHR, NR, CO, O or S (wherein, R represents a PCT/JP2007/055526 on Mar. 19, 2007. hydrogenatom, an optionally Substituted hydrocarbon group, etc.), Y represents C, CH or N. -------- represents a single bond or double bond, ring A rep resents an optionally substituted 5- to 7-membered oxygen (30) Foreign Application Priority Data containing heterocyclic ring, ring B represents an optionally Substituted benzene ring, and m represents an integer of 1 to Mar. 20, 2006 (JP) ............................ JP 2006-076532 4, or a salt thereof. Patent Application Publication Oct. 21, 2010 Sheet 1 of 4 US 2010/0267821A1 Fig. 1) 60 • wa -w---osmo-we-a-w or a raw wrim reme won h &M terrata sorrisov rea are - a r -- am Me wawa (n=4-5) 50 ck > 4. O 30 O O 0.3 3 30 Control Compound A (mg/kg, p.o.) Patent Application Publication Oct. 21, 2010 Sheet 2 of 4 US 2010/0267821A1 Fig. 2 2 1 O seoa,joJequinN 0.3 Normal Control Compound A (mg/kg, p.o.) group Patent Application Publication Oct. 21, 2010 Sheet 3 of 4 US 2010/0267821A1 (Fig. 3) ??JZ/S30???oJequunN Patent Application Publication Oct. 21, 2010 Sheet 4 of 4 US 2010/0267821A1 Fig. 4) 12 10 68 4. Normal Control 10 30 group 9 Melatonin (mg/kg, p.o.) US 2010/0267821 A1 Oct. 21, 2010 PROPHYLACTIC OR THERAPEUTICAGENT DISCLOSURE OF INVENTION FOR RRTABLE BOWEL, SYNDROME Problems to be Solved by the Invention RELATED APPLICATIONS 0014. The object of the present invention is to provide a 0001. This application is a continuation of U.S. patent prophylactic or therapeutic agent for irritable bowel syn application Ser. No. 12/225,269 filed on Sep. 17, 2008, which drome. claims priority to PCT/JP2007/055526, filed on Mar. 19, 2007, which claims the benefit of JP 2006-076532, filed Mar. Means of Solving the Problems 20, 2006. The contents of each of these applications is incor 0015 The present inventors found out that certain mela porated herein by reference in their entirety. tonin agonists are effective for a prevention or treatment of irritable bowel syndrome, and resulted in the completion of TECHNICAL FIELD the present invention. 0002 The present invention relates to a prophylactic or 0016 That is, the present invention provides: therapeutic agent for irritable bowel syndrome. 00.17 1 A pharmaceutical composition for a prevention or treatment of irritable bowel syndrome, which comprises BACKGROUND ART a compound represented by formula (I): 0003 Irritable bowel syndrome (IBS) is a disorder that shows dysfunction of lower bowel such as abnormal defeca R2 tion (diarrhea or constipation) and concomitant abdominal R1 symptoms of abdominal pain and discomfort lasting for sev 1. eral months. (CH2) 0004. The pathophysiology of irritable bowel syndrome is Y. O still unclear, but it is now that mental stress is closely involved in the development of symptom, and a high coincidence rate of mental disorder Such as depression and hysteria has been X made known. Sleep disorder is often observed in patients with irritable bowel syndrome, and it is reported recently that sleep wherein, R' represents an optionally substituted hydrocarbon disorder in patients with irritable bowel syndrome correlates group, an optionally Substituted amino group or an optionally with the degree of abdominal symptoms (see non-patent substituted heterocyclic group, R represents a hydrogen documents 1. atom oran optionally substituted hydrocarbon group, R rep 0005. In addition, there is a report that, compared to resents a hydrogen atom, an optionally Substituted hydrocar healthy individuals and patients with irritable bowel syn bon group or an optionally substituted heterocyclic group, X drome having no depressive symptoms, patients with irritable represents CHR, NR, CO, O or S (wherein, R represents a bowel syndrome having depressive symptoms show more hydrogenatom, an optionally Substituted hydrocarbon group severe abdominal symptoms and sleep disorders (see non or hydroxyl group), Y represents C, CH or N. patent document 2). represents a single bond or double bond, ring A repre 0006 Further, there is a report that melatonin, known as a sents an optionally substituted 5- to 7-membered heterocyclic hormone regulating sleep-wake cycle, improves significantly ring containing, an oxygen atom, the abdominal symptoms Such as abdominal pain, abdominal ring B represents an optionally Substituted benzene ring, and bloating and sense of urgency for defecation in female m represents an integer of 1 to 4, or a salt thereof; patients suffering from irritable bowel syndrome (see non 0018 (2 The pharmaceutical composition for a preven patent document 3). tion or treatment of irritable bowel syndrome according to 0007 Furthermore, there is a report that melatonin shows the above-mentioned 1, wherein the compound repre an inhibitory action on partial restraint stress-induced defeca sented by formula (I) or a salt thereof is (S) N-2-(1,6,7, tion which is an experimental model based on defecation 8-tetrahydro-2H-indeno5,4-bfuran-8-yl)ethylpropiona abnormality for irritable bowel syndrome (see non-patent document 4). mide; 0008. In addition, patent document 1 discloses that (S)- 0019. 3. A method for a prevention or treatment of irri N-2-(1,6,7,8-tetrahydro-2H-indeno5,4-bfuran-8-yl)ethyl table bowel syndrome, which comprises administering an propionamide (general name: Ramelteon) has a melatonin effective amount of a compound represented by formula receptor MT1/MT2 agonistic action. (I): 0009 patent document 1 U.S. Pat. No. 6,034,239 0010 non-patent document 1 Monica Jarrett et al., Digestive Diseases and Sciences, Vol. 45, No. 5 (May 2000), pp. 952-959 00.11 non-patent document 2 Jennifer J.T. Robert et. al., Digestive Diseases and Sciences, Vol. 49, Nos. 7/8 (August 2004), pp. 1250-1258 0012 non-patent document 3 W. Z. Luet. al., Aliment Pharmacol Ther 2005; 22: pp. 927-934 0013 non-patent document 4 G. S. Song et. al., Neuro gastroenterol Motil 2005; 17: pp. 744–750 US 2010/0267821 A1 Oct. 21, 2010 wherein, R' represents an optionally substituted hydrocarbon BEST MODE FOR CARRYING OUT THE group, an optionally Substituted amino group or an optionally INVENTION substituted heterocyclic group, R represents a hydrogen atom or an optionally substituted hydrocarbon group, R rep 0027. Examples of melatonin agonists to be used for a resents a hydrogen atom, an optionally Substituted hydrocar preventive or therapeutic agent for irritable bowel syndrome bon group or an optionally Substituted heterocyclic group, X in the present invention include a compound represented by the above formula (I) or a salt thereof. VEC-162 (Vanda), represents CHR, NR, CO, O or S (wherein, R represents a LY-156735 (Lilly), Agomelatine (Servier), and the like. hydrogenatom, an optionally substituted hydrocarbon group Among them, the compound represented by the above for or hydroxyl group), Y represents C, CH or N. mula (I) or a salt thereof is preferred. represents a single bond or double bond, 0028. Hereinafter, the compound represented by formula ring A represents an optionally substituted 5- to 7-membered (I) or a salt thereof will be illustrated. heterocyclic ring containing an oxygen atom, (0029. In the above formula (I), R' represents an optionally ring B represents an optionally Substituted benzene ring, and Substituted hydrocarbon group, an optionally Substituted m represents an integer of 1 to 4, or a salt thereof; amino group or an optionally substituted heterocyclic group, 0020 4. The method for a prevention or treatment R represents a hydrogen atom or an optionally substituted according to the above-mentioned 3, wherein the com hydrocarbon group, R represents a hydrogen atom, an pound represented by formula (I) or a salt thereof is (S)— optionally Substituted hydrocarbon group or an optionally N-2-(1,6,7,8-tetrahydro-2H-indeno5,4-bfuran-8-yl) substituted heterocyclic group, X represents CHRNR, CO, ethylpropionamide; Oor S (wherein, R represents a hydrogenatom, an optionally 0021 5. Use of a compound represented by formula (I): Substituted hydrocarbon group or hydroxyl group), Y repre sents C, CH or N, represents a single bond or double bond, R2 ring A represents an optionally substituted 5- to 7-membered heterocyclic ring containing an oxygen atom, R1 1. ring B represents an optionally Substituted benzene ring, and (CH2) m represents an integer of 1 to 4. 0030 Preferably, in case that X represents CHY is C or Y. O CH. 0031. In this specification, examples of the “hydrocarbon X group' in the “optionally substituted hydrocarbon group' include an aliphatic hydrocarbon group, a monocyclic Satu rated hydrocarbon group and an aromatic hydrocarbon group, wherein, R' represents an optionally substituted hydrocarbon and preferred is a group having 1 to 16 carbons.
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