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Quisapride Hydrochloride



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Quisapride Hydrochloride

(R) – quinuclidine-3-5 – ((S) -2 – (( 4 – amino-5-chloro-2-ethoxy benzoylamino) methyl) morpholino) hexanoate

IND Filed china

A 5-HT4 agonist potentially for the treatment of gastrointestinal motility disorders.

SHR-116 958, SHR 116958

CAS 1132682-83-7 (Free)

Shanghai Hengrui Pharmaceutical Co., Ltd.

CAS 1274633-87-2 (dihcl)

  • (3R)-1-Azabicyclo[2.2.2]oct-3-yl (2S)-2-[[(4-amino-5-chloro-2-ethoxybenzoyl)amino]methyl]-4-morpholinehexanoate hydrochloride (1:2)
  • SHR 116958
  • C27 H41 Cl N4 O5 . 2 Cl H,
    4-Morpholinehexanoic acid, 2-[[(4-amino-5-chloro-2-ethoxybenzoyl)amino]methyl]-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, hydrochloride (1:2), (2S)-


5-HT is a neurotransmitter Chong, widely distributed in the central nervous system and peripheral tissues, 5-HT receptor subtypes at least seven, and a wide variety of physiological functions of 5-HT receptor with different interactions related. Thus, the 5-HT receptor subtypes research is very necessary.

The study found that the HT-5 4 receptor agonists useful for treating a variety of diseases, such as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome, constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, postoperative intestinal infarction, central nervous system disorders, Alzheimer’s disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disease, heart failure , arrhythmias, intestinal pseudo-obstruction, gastroparesis, diabetes and apnea syndrome.

The HT-5 4 receptor agonists into benzamides, benzimidazole class and indole alkylamines three kinds, which benzamides derivatives act on the neurotransmitter serotonin in the central nervous system by modulation, It showed significant pharmacological effect. The role of serotonin and benzamides derivatives and pharmacologically related to many diseases. Therefore, more and more people will focus on the human body produce serotonin, a storage position and the position of serotonin receptors, and to explore the relationship between these positions with a variety of diseases.

Commonly used in clinical cisapride (cisapride) and Mosapride (Tony network satisfied) is one of the novel benzamides drugs.

These drugs mainly through the intestinal muscle between the excited 5-HT neurofilament preganglionic and postganglionic neurons 4 receptor to promote the release of acetylcholine and enhancing cholinergic role in strengthening the peristalsis and contraction of gastrointestinal smooth muscle. In large doses, it can antagonize the HT-53 receptors play a central antiemetic effect, when typical doses, through the promotion of gastrointestinal motility and antiemetic effect. These drugs can increase the lower esophageal smooth muscle tension and promote esophageal peristalsis, improving the antrum and duodenum coordinated motion, and promote gastric emptying, but also promote the intestinal movement and enhanced features, increase the role of the proximal colon emptying, It is seen as the whole digestive tract smooth muscle prokinetic effect of the whole gastrointestinal drugs.

Mainly used for reflux esophagitis, functional dyspepsia, gastroparesis, postoperative gastrointestinal paralysis, functional constipation and intestinal pseudo-obstruction patients. Since there is slight antagonism cisapride the HT-5 3 and anti-D2 receptor, can cause cardiac adverse reactions, prolonged QT occurs, and therefore, patients with severe heart disease, ECG QT prolonged, low potassium, and low blood magnesium prohibited drug. Liver and kidney dysfunction, lactating women and children is not recommended. Due to increase between drug diazepam, ethanol, acenocoumarol, cimetidine and ranitidine the absorption of anticholinergic drugs may also antagonize the effect of this product to promote peristalsis of the stomach, should be aware of when using these, such as when diarrhea should reduce, anticoagulant therapy should pay attention to monitoring the clotting time. Mosapride selective gastrointestinal tract the HT-5 4 receptor agonists, there is no antagonism of D2 receptors, does not cause QT prolonged, reduce adverse reactions, mainly fatigue, dizziness, loose stools, mild abdominal pain , the efficacy of cisapride equivalent clinical effect broader Puka cisapride (prucalopride, Pru) of benzimidazole drugs, with high selectivity and specificity of the HT-5 4 receptor, increasing cholinergic neurotransmitters quality release, stimulate peristalsis reflex, enhance colon contraction, and accelerate gastric emptying, gastrointestinal motility to promote good effect, can effectively relieve the patient’s symptoms of constipation, constipation and for treatment of various gastrointestinal surgery peristalsis slow and weak, and intestinal pseudo-obstruction.

WO2005068461 discloses as the HT-5 4 receptor agonists benzamides compounds, particularly discloses compounds represented by the formula:


ATI-7505 is stereoisomeric esterified. Cisapride analogs, safe and effective treatment of various gastrointestinal disorders, including gastroparesis, gastroesophageal reflux disease and related disorders. The drug can also be used to treat a variety of central nervous system disorders. ATI-7505 for the treatment or prevention of gastroesophageal reflux disease, also taking cisapride significantly reduced side effects. These side effects include diarrhea, abdominal cramps and blood pressure and heart rate rise.

Further, the compounds and compositions of this patent disclosure also useful in treating emesis and other diseases. Such as indigestion, gastroesophageal reflux, constipation, postoperative ileus, and intestinal pseudo-obstruction. In the course of treatment, but also taking cisapride reduce the side effects.

ΑΉ-7505 as the HT-5 4 receptor ligands may be mediated by receptors to treat the disease. These receptors are located in several parts of the central nervous system, modulate the receptor can be used to affect the CNS desired modulation.

ATI-7505 contained in the ester moiety does not detract from the ability of the compounds to provide treatment, but to make the compound easier to serum and / or cytosolic esterases degraded, so you can avoid the drug cytochrome P450 detoxification system, and this system with cisapride cause side effects related, thus reducing side effects.

The HT-Good 5 4 receptor agonists and should the HT-5 4 receptor binding powerful, while the other hardly shows affinity for the receptor, and show functional activity as agonists. They should be well absorbed from the gastrointestinal tract, metabolically stable and possess desirable pharmacokinetic properties. When targeting the receptor in the central nervous system, they should cross the blood-free, selectively targeting peripheral nervous system receptors, they should not pass through the blood-brain barrier. They should be non-toxic, and there is little proof of side effects. Furthermore, the ideal drug candidate will be a stable, non-hygroscopic and easily formulated in the form of physical presence.

Based on the HT-5 4 receptor agonists current developments, the present invention relates to a series of efficacy better, safer, less side effects of the benzamide derivatives.




WO 2009033360

Example 3

(R) – quinuclidine-3-5 – ((S) -2 – (( 4 – amino-5-chloro-2-ethoxy benzoylamino) methyl) morpholino) hexanoate



China Pharmaceuticals: Asia Insight: China Has R&D…/cd837477-44e9-4f98-a2b9-97620cd64576.pdf

Nov 6, 2012 – levofolinate, sevoflurane inhalation, ambroxol hydrochloride, ioversol, etc ….. dextromethorphan hydrochloride 复方沙芬那敏. 3.2 …… quisapride.

Pharmazie (2011), 66(11), 826-830

//////SHR-116 958, SHR 116958, Quisapride Hydrochloride, preclinical


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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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